# US 2010/0168093 A1 · Substituted 3-amino-4 -hydroxy pyrrolidines compounds, their preparation and use as medicaments

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2010/0168093 A1
- Document ID: US20100168093A1
- Status: Published application
- Kind: A1
- Application number: 12/226,560
- Filed: 2007-04-30
- Published: 2010-07-01
- Earliest claimed: 2006-04-28
- Inventors: Miguel Angel Pericas-Brondo; Antoni Torrens-Jover; Susana Yenes-Minguez; Félix Cuevas Cordobés; Carmen Garcia Granda
- Web page: https://patentgrep.com/patent/US20100168093A1

## CPC

- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- C07D 207/14: Nitrogen atoms not forming part of a nitro radical
- C07D 207/48: Sulfur atoms
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 413/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to substituted pyrrolidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.

## Claims

### Claim 1

Substituted pyrrolidine compounds of general formula (I),
wherein
R1 represents a hydrogen atom, an unbranched or branched, saturated, optionally at least mono-substituted C1-6-aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; an optionally at least mono-substituted benzhydryl group; a (C═O)—R5 group; a group; a (SO2)—R6 group; or a (C═O)—NR7R7a group;
R2 represents a hydrogen atom; a substituted or unsubstituted aliphatic group; a (C═O)—R8 group; a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH;
R3 and R4, equal or different, represent a hydrogen atom; an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; with the condition (proviso) that R3 and R4 may not at the same time represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N1 S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
R5 and R6 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R7 and R7a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R8 represents a hydrogen atom; a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R12 and R12a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
with the provisos that
if R2 represents a hydrogen atom;
and R1 represents a hydrogen atom or a condensed aryl group;
R3 and R4 may not form together with their bridging nitrogen atom a triazole group;
if R2 represents a hydrogen atom;
and R1 represents a hydrogen atom; a substituted C1-2 alkyl group; a condensed aryl group; a benzyl group;
R3 and R4 may not form together with their bridging nitrogen atom a substituted, unsaturated, condensed ring system containing at least 4 nitrogen atoms as ring members; an unsaturated, (C═O)-substituted, uncondensed, 6-membered ring system in which one additional carbon atom is replaced by nitrogen.
if R2 represents a hydrogen atom;
and R3 and R4 form together with their bridging nitrogen atom a pyrrolidine ring, a piperidine ring, a piperazine ring or a morpholine ring;
R1 may not represent a hydrogen atom; a methyl group; an unsaturated tert-butyl group; a (C═O)-substituted alkyl-heteroaryl group;
if R2 represents a hydrogen atom;
and R1 does not represent a benzyl group;
and either R3 or R4 represents a hydrogen atom;
either R3 or R4 may not represent a substituted alkyl-heteroaryl group; an alkyl-aryl group; a substituted heteroaryl group; an unsubstituted methyl group; a substituted alkyl group; an aryl group; a cyclohexyl group; an alkyl-cycloalkyl group wherein the cycloalkyl group contains at least one heteroatom;
if R2 represents a hydrogen atom;
and R1 represents an alkyl group;
and either R3 or R4 represents a hydrogen atom; the other of R3 or R4 may not represent a substituted or unsubstituted C1-2 alkyl group; a branched C1-4 alkyl group; a substituted or unsubstituted C3-6 cycloalkyl group in which optionally at least one carbon atom is optionally replaced by N, S or O; a cycloheptyl group;
if R2 represents a hydrogen atom;
and R1 represents an alkyl group;
either R3 or R4 may not represent a cyclohexyl group while the other represents at the same time an alkyl-aryl group; or either R3 or R4 may not represent an alkyl group while the other represents at the same time an alkyl-aryl group;
if R2 represents a hydrogen atom;
and R1 represents a benzhydryl group;
and either R3 or R4 represents a hydrogen atom;
either R3 or R4 may not represent a (C═O)-substituted alkyl-aryl group; a (C═O)-substituted aryl group;
if R2 represents a hydrogen atom;
and R1 represents benzyl;
and either R3 or R4 represents a hydrogen atom;
the other of R3 or R4 may not represent a substituted or unsubstituted C1-2 alkyl group; an unsubstituted benzyl group; a C3-8 substituted alkyl group; a substituted alkyl-aryl group;
or
R3 or R4, together with their bridging nitrogen atom may not form a tetrahydropyrimidine ring; a triazolo pyrimidine ring;
if R2 represents a benzyl group;
and either R3 or R4 represents a hydrogen atom either R3 or R4 may not represent a (C═O)-substituted alkyl-aryl group;
if R2 represents a C1-3 alkyl group;
and either R3 or R4 represents a hydrogen atom either R3 or R4 may not represent an unsubstituted C1-2 alkyl group;
a substituted alkyl group; a substituted or unsubstituted aryl group; a substituted heteroaryl group; a (C═O)-substituted alkyl-aryl group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 2 (depends on 1)

Compound according to claim 1, characterized in that R1 represents a hydrogen atom, an unbranched or branched, optionally at least mono-substituted C1-6-alkyl radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; an optionally at least mono-substituted benzhydryl group; a (C═O)—R5 group; a group; a (SO2)—R8 group; or a (C═O)—NR7R7a group;
R2 represents a (C═O)—R8 group, with R8 representing a hydrogen atom; a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;
R3 and R4, equal or different, represent a hydrogen atom; an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted C1-8-aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; with the condition (proviso) that R3 and R4 may not at the same time represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF2, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N1 S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—N R12R12a group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR11 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
R5, R6, R7a, R9, R10, R11, R12 and R12a have the meaning according to claim 1; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 3 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a hydrogen atom, an unbranched or branched, saturated, optionally at least mono-substituted C1-6-alkyl radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; an optionally at least mono-substituted benzhydryl group; a (C═O)—R5 group; a group; a (SO2)—R6 group; or a (C═O)—NR7R7a group;
R2 represents a linear, substituted or unsubstituted C C1-6 alkyl group; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH;
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a — (C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
R5, R6, R7, R7a, R9, R10, R11, R12 and R12a have the meaning according to claim 1;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 4 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted heteroaryl group; a branched or unbranched, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; an optionally at least mono-substituted benzhydryl group; a (C═O)—R5 group; a group; a (SO2)—R6 group; or a (C═O)—NR7R7a group;
R2 represents a linear, substituted or unsubstituted C1-6 alkyl group; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH;
R3 and R4, identical or different, represent a hydrogen atom; a saturated or unsaturated, unsubstituted C3-8 aliphatic group; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group; an unsubstituted heteroaryl group; a saturated or unsaturated, optionally at least mono-substituted alkyl-cycloalkyl group; an unsubstituted alkyl-aryl group; a saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group; with the condition that R3 and R4 may not at the same time represent a hydrogen atom;
R5, R6, R7 and R7a have the meaning according to claim 1;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 5 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents an unbranched or branched, optionally at least mono-substituted C2-6-alkyl radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated unsubstituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; an optionally at least mono-substituted benzhydryl group; a (C═O)—R5 group; a (SO2)—R6 group; a (C═O)—NR7R7a group;
R2 represents a hydrogen atom;
R3 and R4 together with their bridging nitrogen atom form
1) a ring system A in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
2) an A-X—B group,
wherein
A represents a ring system in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF2, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF2, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
3) an A-X—B—Y—C group,
wherein
A represents a ring system in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF2, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
R5, R6, R7, R7a, R9, R10, R11, R12 and R12a have the meaning according to claim 1;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 6 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; an optionally at least mono-substituted benzhydryl group; a (C═O)—R5 group; a (SO2)—R6 group; or a (C═O)—NR7R7a group;
R2 represents a hydrogen atom;
R3 represents a hydrogen atom;
R4 represents a saturated or unsaturated, unsubstituted, linear C3-8 aliphatic group; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing 4 or 5-membered cycloalkyl group; an unsubstituted heteroaryl group; a saturated or unsaturated, unsubstituted alkyl-cycloalkyl group; an unsubstituted C1-6alkyl-heteroaryl group;
R5, R6, R7 and R7a have the meaning according to claim 1;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 7 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a hydrogen atom, an unbranched or branched, saturated C1-6 alkyl radical which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group wherein the C1-6-alkyl and/or the cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an aryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C3-6-alkyl-aryl group wherein the C3-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C3-6-alkyl-heteroaryl group wherein the C3-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (C═O)—R5 group; a (SO2)—R6 group; or a (C═O)— NR7R7a group;
R2 represents a (C═O)—R8 group, with R8 representing a hydrogen atom; a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;
R3 and R4, equal or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted C1-8-aliphatic radical; a saturated or unsaturated, optionally at least mono- substituted, optionally at least one heteroatom as ring member containing cycloalkyl group; a branched or unbranched, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group; an optionally at least mono-substituted aryl group; an optionally at least mono-substituted heteroaryl group; a branched or unbranched, optionally at least mono-substituted C1-6-alkyl-aryl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted C1-6-alkyl-heteroaryl group; with the condition that R3 and R4 may at the same time not represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF2, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF2, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
R5, R6, R7, R7a, R9, R10, R11, R12 and R12a have the meaning according to claim 1;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 8 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a hydrogen atom, an unbranched or branched, saturated C1-6 alkyl radical which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, carboxy, amido, cyano, carbamyl, nitro, —SO2NH2 or C1-6-alkoxy; an optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group wherein the C1-6-alkyl and/or the cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an aryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF2, CN, nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF2, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated, C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the heteroaryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH1 OH, SO2, CF2, CN, nitro, —SO2NH2 or C1-6-alkoxy; an optionally at least mono-substituted benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF2, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (C═O)—R5 group; a group; a (SO2)—R6 group; or a (C═O)—NR7R7a group;
R2 represents a C1-6 alkyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF2; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF2;
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12 group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12 group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
R5, R6, R7, R7a, R9, R10, R11, R12 and R12a have the meaning according to claim 1;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 9 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents an optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group wherein the C1-6-alkyl and/or the cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (C═O)—R5 group; a (SO2)—R6 group; or a (C═O)—NR7R7a group;
R2 represents a C1-6 alkyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH1 CF3;
R3 and R4, identical or different, represent a hydrogen atom; a saturated or unsaturated, unsubstituted C3-8 aliphatic group; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group with substituents independently selected from the group consisting of F1 Cl, Br, I, NH2, SH, OH, CF3, CN1 nitro; an unsubstituted heteroaryl group; an optionally at least mono-substituted C1-6 alkyl-cycloalkyl group; an unsubstituted C1-6 alkyl-aryl group; an unsubstituted C1-6 alkyl-heteroaryl group; with the condition that R3 and R4 may not at the same time represent a hydrogen atom;
R5, R6, R7 and R7a have the meaning according to claim 1;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 10 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents an unbranched or branched, optionally at least mono-substituted C1-6-alkyl radical which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group wherein the C1-6-alkyl and/or the cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an aryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C3-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (C═O)—R5 group; a (SO2)—R6 group; or a (C═O)—NR7R7a group;
R2 represents a hydrogen atom;
R3 and R4 together with their bridging nitrogen atom form
1) a 4 to 18 membered ring system A in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
2) an A-X—B group,
wherein
A represents 4 to 18 membered ring system in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12 group;
3) an A-X—B—Y—C group,
wherein
A represents 4 to 18 membered ring system in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF2, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a —O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
R5, R5, R7, R7a, R9, R10, R11, R12 and R12a have the meaning according to claim 1;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 11 (depends on 1)

Compounds according to any of claims 1, characterized in that R1 represents an optionally at least one heteroatom as ring member containing cycloalkyl group wherein the C1-6-alkyl and/or the cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optional: substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optional: substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN1 nitro, —SO2NH2 or C1-6-alkoxy; a (C═O)—R5 group; a (SO2)—R6 group; or a (C═O)—NR7R7a group;
R2 represents a hydrogen atom;
R3 represents a hydrogen atom;
R4 represents a saturated or unsaturated, unsubstituted, linear C3-8 aliphatic group; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing 4 or 5-membered cycloalkyl group; an unsubstituted heteroaryl group; a saturated or unsaturated, unsubstituted alkyl-cycloalkyl group; an unsubstituted C1-6 alkyl-heteroaryl group;
R5, R6, R7 and R7a have the meaning according to claim 1;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 12 (depends on 1)

Compound according to claim 1, characterized in that R1 represents a hydrogen atom, an unbranched or branched C1-6 alkyl radical which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH; OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group wherein the C1-6-alkyl and/or the cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an aryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN1 nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN1 nitro, —SO2NH2 or C1-6-alkoxy; a (SO2)—R6 group;
R2 represents a (C═O)—R8 group, with R8 representing a hydrogen atom; a methyl group; an ethyl group; a propyl group; a butyl group; a pentyl group; a hexyl group;
R3 and R4, equal or different, represent a hydrogen atom, an unbranched or branched C1-8-alkyl group, which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a saturated or unsaturated, optionally at least one heteroatom as ring member containing cycloalkyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an aryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, CO—OH, CO—O—CH3, O—CH3, nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, CO—OH, CO—O—CH3, O—CH3, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-aryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, CO—OH, CO—O—CH3, O—CH3, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; with the condition that R3 and R4 may at the same time not represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated 4 to 18 membered ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a OH2—(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated 4 to 18 membered ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted 01-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11 group;
a NH—R11 group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated 4 to 18 membered ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11n group; a NH—R11 group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH1 OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
R6 represents a hydrogen atom; a C1-6 alkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, or CN; an alkyl-cycloalkyl group which is optionally at least mono- substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a branched or unbranched alkyl-aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched C1-6 alkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-cycloalkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a branched or unbranched alkyl-aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 13 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a hydrogen atom, an unbranched or branched C1-6 alkyl radical which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, carboxy, amido, cyano, carbamyl, nitro, —SO2NH2 or C1-6-alkoxy; an optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group wherein the C1-6-alkyl and/or the cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an aryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated, C16-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the heteroaryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an optionally at least mono-substituted benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a group; a (SO2)—R6 group;
R2 represents a methyl , ethyl, propyl or butyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated 4 to 18 membered ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C3-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated 4 to 18 membered ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated 4 to 18 membered ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
R6 represents a hydrogen atom; a C1-6 alkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, or CN; an alkyl-cycloalkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a branched or unbranched alkyl-aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched C1-6 alkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-cycloalkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a branched or unbranched alkyl-aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 14 (depends on 1)

Compounds according to claim 1, characterized in that re represents an optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group wherein the C1-6-alkyl and/or the cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I1 NH2, SH1 OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (SO2)—R6 group;
R2 represents a methyl, ethyl, propyl or butyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R3 and R4, identical or different, represent a hydrogen atom; a saturated or unsaturated, unsubstituted C3-6 aliphatic group; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group with substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, CN, nitro;
an unsubstituted heteroaryl group; a C1-6 alkyl-cycloalkyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an unsubstituted C1-6 alkyl-aryl group; an unsubstituted C1-6 alkyl-heteroaryl group; with the condition that R3 and R4 may not at the same time represent a hydrogen atom;
R6 represents a hydrogen atom; a C1-6 alkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, or CN; an alkyl-cycloalkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a branched or unbranched alkyl-aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 15 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents an unbranched or branched, saturated, optionally at least mono-substituted C1-6-alkyl radical which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group wherein the C1-6-alkyl and/or the cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; an aryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (SO2)—R6 group;
R2 represents a hydrogen atom;
R3 and R4 together with their bridging nitrogen atom form
1) a 4 to 18 membered ring system A in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
2) an A-X—B group,
wherein
A represents a 4 to 18 membered ring system in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
X group; a —NH— group; a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
3) an A-X—B—Y—C group,
wherein
A represents a 4 to 18 membered ring system in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2—(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated 4 to β membered ring system, in which at least 1 carbon atom is optionally replaced by N or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, or CF3;
R6 represents a hydrogen atom; a C1-6 alkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, or CN; an alkyl-cycloalkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a branched or unbranched alkyl-aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched alkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-cycloalkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a branched or unbranched alkyl-aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 16 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents an optionally at least one heteroatom as ring member containing C1-6-alkyl-cycloalkyl group wherein the C1-6-alkyl and/or the cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN1 nitro, —SO2NH2 or C1-6-alkoxy; a heteroaryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched, saturated C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (SO2)—R6 group;
R2 represents a hydrogen atom;
R3 represents a hydrogen atom;
R4 represents a saturated or unsaturated, unsubstituted, linear C3-13 aliphatic group; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing 4 or 5-membered cycloalkyl group; an unsubstituted heteroaryl group; a saturated or unsaturated, unsubstituted alkyl-cycloalkyl group; an unsubstituted C1-6 alkyl-heteroaryl group;
R6 represents a hydrogen atom; a C1-6 alkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a cycloalkyl group selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, adamantyl, pyrroline, pyrrolidine, pyrrolidineone, pyrazoline, pyrazolinone, oxopyrazolinone, aziridine, acetidine, tetrahydropyrrole, oxirane, oxetane, dioxetane, tetrahydrofurane, dioxane, dioxolane, oxathiolane, oxazolidine, thiirane, thietane, thiolane, thiane, thiazolidine, piperidine, piperazine or morpholine which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, or CN; an alkyl-cycloalkyl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a branched or unbranched alkyl-aryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; an alkyl-heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 17 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a branched or unbranched C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (SO2)—R6 group with R6 being an aryl group, preferably a phenyl or a naphtyl group, which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R2 represents a (C═O)—R8 group, with R8 representing a hydrogen atom; a methyl group; an ethyl group; a propyl group; a butyl group; a pentyl group; a hexyl group;
R3 and R4, identical or different, represent a hydrogen atom; a C3-8 alkyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, CN; an optionally at least mono-substituted quinoline group; a phenyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, CN; a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, CN; with the condition that R3 and R4 may not at the same time represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated 4 to 18 membered ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated 4 to 18 membered ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with Rn being a linear or branched C1-6 alkyl group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated 4 to 18 membered ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF2, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 18 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a branched or unbranched C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (SO2)—R6 group with R6 being an aryl group, preferably a phenyl or a naphtyl group, which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R2 represents a methyl, ethyl, propyl or butyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated 4 to 18 membered ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR16 group with R10 being a linear or branched C1-6 alkyl group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated 4 to 18 membered ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated 4 to 18 membered ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 19 (depends on 1)

Compounds according to any of claim 1, characterized in that R1 represents a branched or unbranched C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (SO2)—R6 group with R6 being an aryl group, preferably a phenyl or a naphtyl group, which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R2 represents a methyl, ethyl, propyl or butyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R3 and R4, identical or different, represent a hydrogen atom; a saturated or unsaturated, optionally at least mono-substituted C3-8 aliphatic group with substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, CN, nitro; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group with substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, CN, nitro; an unsubstituted heteroaryl group; a saturated or unsaturated, optionally at least mono-substituted C1-6 alkyl-cycloalkyl group; a saturated or unsaturated, unsubstituted C1-6 alkyl-aryl group; a saturated or unsaturated, unsubstituted C1-6 alkyl-heteroaryl group; with the condition that R3 and R4 may not at the same time represent a hydrogen atom;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 20 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a branched or unbranched C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (SO2)—R6 group with R6 being an aryl group, preferably a phenyl or a naphtyl group, which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R2 represents a hydrogen atom;
R3 and R4 together with their bridging nitrogen atom form
1) a 4 to 18 membered ring system A in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
2) an A-X—B group,
wherein
A represents a 4 to 18 membered ring system in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
3) an A-X—B—Y—C group,
wherein
A represents a 4 to 18 membered ring system in which the ring containing the nitrogen atom is saturated, but may be condensed with an unsaturated ring, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated 4 to 12 membered ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 21 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a branched or unbranched C1-6-alkyl-aryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a branched or unbranched C1-6-alkyl-heteroaryl group wherein the C1-6-alkyl and/or the aryl group is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a benzhydryl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, SO2, CF3, CN, nitro, —SO2NH2 or C1-6-alkoxy; a (SO2)—R6 group with R6 being an aryl group, preferably a phenyl or a naphtyl group, which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a heteroaryl group which is optionally at least mono-substituted by substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R2 represents a hydrogen atom;
R3 represents a hydrogen atom;
R4 represents a saturated or unsaturated, unsubstituted, linear C3-6 aliphatic group; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing 4 or 5-membered cycloalkyl group; an unsubstituted heteroaryl group; a saturated or unsaturated, unsubstituted alkyl-cycloalkyl group; an unsubstituted C1-6 alkyl-heteroaryl group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 22 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a benzyl group or a (SO2)—R6 group with R6 being an aryl group;
R2 represents a (C═O)—R8 group, with R8 representing a hydrogen atom; a methyl group; an ethyl group; a propyl group; a butyl group; a pentyl group; a hexyl group;
R3 and R4, identical or different, represent a C3-8 alkyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, CN; an optionally at least mono-substituted quinoline group; a phenyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, CN; a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, CN;
or
R3 and R4 together with their bridging nitrogen atom form
1) a ring system A, comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
2) an A-X—B group,
wherein
A represents a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a linear optionally substituted C1-2 alkyl chain, —O—, or a —SO2— group;
B represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
3) an A-X—B—Y—C group,
wherein
A represents a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a linear C1-2 alkyl chain, —O—, or a —SO2— group;
B represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
Y represents a bond, a —NH— group, a linear C1-2-aliphatic group;
C represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 23 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a benzyl group or a (SO2)—R6 group with R6 being an aryl group;
R2 represents a methyl, ethyl, propyl or butyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3;
R3 and R4 together with their bridging nitrogen atom form
1) a ring system A, comprising:
and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
2) an A-X—B group,
wherein
A represents a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a linear C1-2 alkyl chain, —O—, or a —SO2— group;
B represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
3) an A-X—B—Y—C group,
wherein
A represents a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a linear C1-2 alkyl chain, —O—, or a —SO2— group;
B represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
Y represents a bond, a —NH— group, a linear C1-2 alkyl group;
C represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 24 (depends on 1)

Compounds according to claim 1, characterized in that R1 represents a benzyl group or a (SO2)—R6 group with R6 being an aryl group;
R2 represents a hydrogen atom;
R3 and R4 together with their bridging nitrogen atom form
1) a ring system A, comprising:
and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
2) an A-X—B group,
wherein
A represents a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a linear C1-2 alkyl chain, —O—, or a —SO2— group;
B represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
3) an A-X—B—Y—C group,
wherein
A represents a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a linear C1-2 alkyl chain, —O—, or a —SO2— group;
B represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6 alkoxy group;
Y represents a bond, a —NH— group, a linear C1-2-alkyl group;
C represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 25 (depends on 1)

Compounds according to claim 1 selected from the group consisting of
[1] (3,4-trans)-1-benzyl-4-(3,4-dihydroisoquinolin-2(1H)-yl)pyrrolidine-3-ol,
[2] (3,4-trans)-1-benzyl-4-morpholinopyrrolidine-3-ol,
[3] (3,4-trans)-1-benzyl-4-(4-(2-methyl-3H-imidazo[4,5-b]pyridin-3-yl)piperidin-1-yl)pyrrolidine-3-ol,
[4] (3,4-trans)-1-benzyl-4-(3-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)propyl amino)pyrrolidine-3-ol,
[5] (3,4-trans)-1-benzyl-4-(4-((3,4-dihydroisoquinolin-2(1H)-yl)methyl)piperidin-1-yl)pyrrolidine-3-ol,
[6] 1-(4-(6-((3,4-trans)-1-benzyl-4-hydroxypyrrolidine-3-yl)-5,6,7,8-tetrahydropyrido [4,3-d]pyrimidin-2-ylamino)phenyl)ethanone,
[7] 1-(1-((3,4-trans)-1-benzyl-4-hydroxypyrrolidine-3-yl)piperidin-4-yl)-1H-benzo[d] [1,3] oxazin-2(4H)-one,
[8] (3,4-trans)-1-benzyl-4-(2-(4-phenoxyphenylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)pyrrolidine-3-ol,
[9] (3,4-trans)-1-benzyl-4-(3-(3,4-dihydroisoquinolin-2(1H)-yl)propylamino)pyrrolidine -3-ol,
[10] (3,4-trans)-1-benzyl-4-(4-(4-methoxypyrimidin-2-yl)piperazin-1-yl)pyrrolidine-3-ol,
[11] (3,4-trans)-1-benzyl-4-(2,3,8,8a-tetrahydrocyclopenta[ij]isoquinolin-1(7H)-yl)pyrrolidine-3-ol,
[12] tert-butyl-4-((3,4-trans)-1-benzyl-4-hydroxypyrrolidine-3-yl)piperazine-1-carboxylate,
[13] tert-butyl 4-((3,4-trans)-4-hydroxy-1-(phenylsulfonyl)pyrrolidine-3-yl)piperazine-1-carboxylate,
[14] (3,4-trans)-4-morpholino-1-(phenylsulfonyl)pyrrolidine-3-ol,
[15] (3,4-trans)-4-(3,4-dihydroisoquinolin-2(1H)-yl)-1-(phenylsulfonyl)pyrrolidine-3-ol,
[16] (3,4-trans)-4-(3,4-dihydroisoquinolin-2(1H)-yl)-1((S)-I-phenylethyl)pyrrolidine-3-ol,
[17] (3,4-trans)-1-benzyl-4-(4-benzylpiperazin-1-yl)pyrrolidine-3-ol,
[18] (3,4-trans)-1-benzyl-4-(4-phenylpiperazin-1-yl)pyrrolidine-3-ol,
[19] Ethyl 2-(4-((3,4-trans)-1-benzyl-4-hydroxypyrrolidine-3-yl)piperazin-1-yl)acetate,
[20] (4-((3,4-trans)-1-benzyl-4-hydroxypyrrolidine-3-yl)piperazin-1-yl)(phenyl)methanone,
[21] Ethyl 4-((3,4-trans)-1-benzyl-4-hydroxypyrrolidine-3-yl)piperazine-1-carboxilate,
[22] tert-butyl 4-((3,4-trans)-1-(4-fluorobenzyl)-4-hydroxypyrrolidine-3-yl)piperazine-1-carboxylate,
[23] (3,4-trans)-1-benzyl-4-(4-methylpiperazin-1-yl)pyrrolidine-3-ol,
[24] tert-butyl-4-(3,4-trans)-4-acetoxy-1-benzylpyrrolidine-3-yl)piperazine-1-carboxylate,
[25] (3,4-trans)-1-benzyl-4-(piperazin-1-yl)pyrrolidine-3-yl acetate,
[26] tert-butyl 4-((3,4-trans)-4-acetoxypyrrolidine-3-yl)piperazine-1-carboxylate,
[27] trans 1-Benzyl-4-(4-(2-phenyl-phenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate,
[28] trans 1-Benzyl-4-(4-(2-phenyl-phenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[29] (3,4-trans)-1-benzyl-4-(phenylamino)pyrrolidin-3-ol,
[30] (3,4-trans)-1-benzyl-4-(benzylamino)pyrrolidin-3-ol,
[31] (3R,4R)-1-benzyl-4-(octylamino)pyrrolidin-3-ol,
[32] (3,4-trans)-1-benzyl-4-(4-methoxybenzylamino)pyrrolidin-3-ol,
[33] (3,4-trans)-1-benzyl-4-(butylamino)pyrrolidin-3-ol,
[34] (3R,4R)-1-benzyl-4-(4-(4-chloro-2,5-dimethylphenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate,
[35] (3R,4R)-1-benzyl-4-(4-tosylpiperazin-1-yl)pyrrolidin-3-yl acetate,
[36] (3,4-trans)-1-benzyl-4-(butylamino)pyrrolidin-3-ol,
[37] (3R,4R)-1-benzyl-4-(4-methoxyphenylamino)pyrrolidin-3-ol,
[38] Methyl 4-((3,4-trans)-1-benzyl-4-hydroxypyrrolidin-3-ylamino)benzoate,
[39] (3R,4R)-1-benzyl-4-(4-(naphthalen-1-ylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate,
[40] (3R,4R)-1-benzyl-4-(4-(2-chlorophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol,
[41] (3R,4R)-1-benzyl-4-(4-(2-bromophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate,
[42] (3R,4R)-1-benzyl-4-(4-(2-bromophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol,
[43] (3R,4R)-1-benzyl-4-(4-(5-fluoro-2-methylphenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate,
[44] (3R,4R)-1-benzyl-4-(4-(5-fluoro-2-methylphenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol,
[45] (3R,4R)-1-benzyl-4-(4-(phenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate,
[46] (3R,4R)-1-benzyl-4-(4-(phenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol,
[47] (3R,4R)-1-benzyl-4-(4-(2-fluorophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate,
[48] (3R,4R)-1-benzyl-4-(4-(2-fluorophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol,
[49] (3R,4R)-1-benzyl-4-(4-(naphthalen-1-ylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol,
[50] (3R,4R)-1-benzyl-4-(4-(4-chloro-2,5-dimethylphenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol,
[51] (3R,4R)-1-benzyl-4-(4-tosylpiperazin-1-yl)pyrrolidin-3-ol,
[52] (3R,4R)-1-benzyl-4-(4-(2-chlorophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate,
[53] (3,4-trans)-1-benzyl-4-(4-(4-chloro-2,5-dimethylphenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate dihydrochloride,
[54] (3,4-trans)-1-benzyl-4-(4-(4-chloro-2,5-dimethylphenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[55] (3S,4S)-1-benzyl-4-(4-(4-chloro-2,5-dimethylphenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[56] (3,4-trans)-1-benzyl-4-(4-tosylpiperazin-1-yl)pyrrolidin-3-yl acetate dihydrochloride,
[57] (3,4-trans)-1-benzyl-4-(4-tosylpiperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[58] (3R,4R)-1-benzyl-4-(4-tosylpiperazin-1-yl)pyrrolidin-3-ol dihydorchloride,
[59] (3S,4S)-1-benzyl-4-(4-tosylpiperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[60] (3,4-trans)-1-benzyl-4-(4-(naphthalen-1-ylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate dihydrochloride,
[61] (3,4-trans)-1-benzyl-4-(4-(naphthalen-1-ylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[62] (3S-4S)-1-benzyl-4-(4-(naphthalen-1-ylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[63] (3,4-trans)-1-benzyl-4-(4-(2-chlorophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate dihydrochloride,
[64] (3,4-trans)-1-benzyl-4-(4-(2-chlorophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[65] (3S,4S)-1-benzyl-4-(4-(2-chlorophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[66] (3,4-trans)-1-benzyl-4-(4-(2-bromophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate dihydrochloride,
[67] (3,4-trans)-1-benzyl-4-(4-(2-bromophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[68] (3S,4S)-1-benzyl-4-(4-(2-bromophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[69] (3,4-trans)-1-benzyl-4-(4-(5-fluoro-2-methylphenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate dihydrochloride,
[70] (3,4-trans)-1-benzyl-4-(4-(5-fluoro-2-methylphenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[71] (3S,4S)-1-benzyl-4-(4-(5-fluoro-2-methylphenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[72] (3,4-trans)-1-benzyl-4-(4-(phenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate,
[73] (3,4-trans)-1-benzyl-4-(4-(phenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol,
[74] (3S,4S)-1-benzyl-4-(4-(phenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol,
[75] (3,4-trans)-1-benzyl-4-(4-(2-fluorophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-yl acetate dihydrochloride,
[76] (3,4-trans)-1-benzyl-4-(4-(2-fluorophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[77] (3S,4S)-1-benzyl-4-(4-(2-fluorophenylsulfonyl)piperazin-1-yl)pyrrolidin-3-ol dihydrochloride,
[78] (3,4-trans)-1-benzyl-4-(4-(2-chloro-6-fluorobenzyl)piperazin-1-yl)pyrrolidine-3-ol
[79] (3,4-trans)-1-benzyl-4-(4-(3,4-dichlorobenzyl)piperazin-1-yl)pyrrolidine-3-ol
[80] (3,4-trans)-1-benzyl-4-hydroxypyrrolidin-3-yl)piperazin-1-yl)(furan-2-yl)methanone
[81] (3,4-trans)-1-benzyl-4-(4-ethylpiperazin-1-yl)pyrrolidin-3-ol,
[82] (3,4-trans)-1-benzyl-4-(4-(2-methoxyphenyl)piperazin-1-yl)pyrrolidin-3-ol,
[83] (3,4-trans)-1-benzyl-4-(4-(4-fluorophenyl)piperazin-1-yl)pyrrolidin-3-ol,
[84] (3,4-trans)-1-benzyl-4-(4-(2-chlorophenyl)piperazin-1-yl)pyrrolidin-3-ol,
[85] (3R,4R)-1-benzyl-4-(4-(2-chlorophenyl)piperazin-1-yl)pyrrolidin-3-ol,
[86] (35,45)-1-benzyl-4-(4-(2-chlorophenyl)piperazin-1-yl)pyrrolidin-3-ol,
[87] 1-(4-((3,4-trans)-1-benzyl-4-hydroxypyrrolidin-3-yl)piperazin-1-yl)ethanone,
[88] (3,4-trans)-1-benzyl-4-(4-(3,4-dichlorophenyl)piperazin-1-yl)pyrrolidin-3-ol,
[89] (3,4-trans)-1-benzyl-4-(4-(3,4-dichlorophenyl)piperazin-1-yl)pyrrolidin-3-ol,
or
[90] (3,4-trans)-cert-butyl 3-(3,4-dihydroisoquinolin-2(1H)-yl)-4-hydroxypyrrolidine-1-carboxylate;
optionally in form of a corresponding salt, or a corresponding solvate.

### Claim 26 (depends on 1)

Substituted pyrrolidine compounds according to claim 1 of general formula (IA),
wherein
Z represents H or CH3;
R2 represents a hydrogen atom; a substituted or unsubstituted aliphatic group; a (C═O)—R8 group; a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH;
R3 and R4, equal or different, represent a hydrogen atom; an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; with the condition (proviso) that R3 and R4 may not at the same time represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, N112, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R10 group; or a (C═O)—NR12R12a group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)— O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
R8 represents a hydrogen atom; a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R12 and R12a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
W represents F, Cl, Br, I, NH2, SH, OH, SO2, CF2, carboxy, amido, cyano, carbamyl, nitro, phenyl, benzyl, —SO2NH2, C1-6 alkyl and/or C1-6-alkoxy;
r represents either 0, 1, 2 or 3;
with the provisos that
if R2 represents a hydrogen atom;
R3 and R4 may not form together with their bridging nitrogen atom a triazole group;
if R2 represents a hydrogen atom;
R3 and R4 may not form together with their bridging nitrogen atom a substituted, unsaturated, condensed ring system containing at least 4 nitrogen atoms as ring members; an unsaturated, (C═O)-substituted, uncondensed, 6-membered ring system in which one additional carbon atom is replaced by nitrogen.
if R2 represents a hydrogen atom;
and either R3 or R4 represents a hydrogen atom;
the other of R3 or R4 may not represent a substituted or unsubstituted C1-2alkyl group; an unsubstituted benzyl group; a C3-8 substituted alkyl group; a substituted alkyl-aryl group;
or
R3 or R4, together with their bridging nitrogen atom may not form a a tetrahydropyrimidine ring; a triazolo pyrimidine ring;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 27 (depends on 26)

Substituted pyrrolidine compounds according to claim 26
wherein
Z represents H or CH3; preferably Z represents H;
R2 represents a hydrogen atom; a methyl, ethyl, propyl or butyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a (C═O)—R8 group, with R8 representing a hydrogen atom; a methyl group; an ethyl group; a propyl group; a butyl group; a pentyl group; a hexyl group; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; preferably R2 represents a hydrogen atom; a (C═O)—R8 group, with R8 representing a hydrogen atom; a methyl group; an ethyl group; a propyl group; a butyl group; a pentyl group; a hexyl group
R3 and R4, identical or different, represent a hydrogen atom; a saturated or unsaturated, unsubstituted C3-8 aliphatic group; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group; an unsubstituted heteroaryl group; a saturated or unsaturated, optionally at least mono-substituted alkyl-cycloalkyl group; an unsubstituted alkyl-aryl group; a saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group; with the condition that R3 and R4 may not at the same time represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a ring system A, comprising:
and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
2) an A-X—B group,
wherein
A represents a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a linear C1-2 alkyl chain, —O—, or a —SO2— group;
B represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
3) an A-X—B—Y—C group,
wherein
A represents a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a linear C1-2 alkyl chain, —O—, or a —SO2— group;
B represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6 alkoxy group;
Y represents a bond, a —NH— group, a linear C1-2-alkyl group;
C represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
R8 represents a hydrogen atom; a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R12 and R12a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
W represents substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, OCF3, unsubstituted C1-6alkyl and/or unsubstituted C1-6-alkoxy;
r represents either 0, 1, 2 or 3;
with the provisos that
if R2 represents a hydrogen atom;
R3 and R4 may not form together with their bridging nitrogen atom a triazole group; a substituted, unsaturated, condensed ring system containing at least 4 nitrogen atoms as ring members; an unsaturated, (C═O)— substituted, uncondensed, 6-membered ring system in which one additional carbon atom is replaced by nitrogen; or may not form a tetrahydropyrimidine ring; a triazolo pyrimidine ring
if R2 represents a hydrogen atom;
and either R3 or R4 represents a hydrogen atom;
the other of R3 or R4 may not represent a substituted or unsubstituted C1-2 alkyl group; an unsubstituted benzyl group; a C3-8 substituted alkyl group; a substituted alkyl-aryl group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 28 (depends on 27)

Substituted pyrrolidine compounds according to claim 27, according to either formula (IAa) or (IAb)
wherein
R2 represents a hydrogen atom; a methyl, ethyl, propyl or butyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a (C═O)—R8 group, with R8 representing a hydrogen atom; a methyl group; an ethyl group; a propyl group; a butyl group; a pentyl group; a hexyl group; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; preferably R2 represents hydrogen or (C═O)—CH3;
R4,—if present as in case of general formula (IAb)—represents a saturated or unsaturated, unsubstituted C3-8 aliphatic group; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group; an unsubstituted heteroaryl group; a saturated or unsaturated, optionally at least mono-substituted alkyl-cycloalkyl group; an unsubstituted alkyl-aryl group; a saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group;
or
Q—if present as in case of general formula (IAa)—represents N or CH, preferably Q represents N; and
Rx—if present as in case of general formula (IAa)—represents
hydrogen; a —(C═O)R8 group with R8 being either hydrogen or an optionally substituted C1-6 aliphatic group; or a —(C═O)OR10 group with R10 being either hydrogen or an optionally substituted C1-6 aliphatic group;
or X—B with
X representing a bond, an —NH— group, a —(C═O)— group, a linear C1-2 alkyl chain, —O—, —S— or an —SO2— group; preferably X represents a bond or SO2; and
B representing a phenyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system selected from a heterocyclyl, preferably from:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
W represents substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3, OCF3, unsubstituted C1-6alkyl and/or unsubstituted C1-6-alkoxy; preferably represents H;
r represents either 0, 1, 2 or 3; preferably is 0;
with the proviso that
if in a compound according to general formula (IAb) R2 represents a hydrogen atom;
R4 may not represent a substituted or unsubstituted C1-2alkyl group; an unsubstituted benzyl group; a C3-8 substituted alkyl group; a substituted alkyl-aryl group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 29 (depends on 1)

Substituted pyrrolidine compounds according to claim 1 of general formula (IB),
wherein
R2 represents a hydrogen atom; a substituted or unsubstituted aliphatic group; a (C═O)—R8 group; a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH;
R3 and R4, equal or different, represent a hydrogen atom; an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; with the condition (proviso) that
R3 and R4 may not at the same time represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R10 group; a NH—R11 group; or a (C═O)—NR12R12a group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
R6 represents a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R8 represents a hydrogen atom; a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R12 and R12a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, Optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 30 (depends on 29)

Substituted pyrrolidine compounds according to claim 29,
wherein
R2 represents a hydrogen atom; a methyl, ethyl, propyl or butyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; a (C═O)—R8 group, with R8 representing a hydrogen atom; a methyl group; an ethyl group; a propyl group; a butyl group; a pentyl group; a hexyl group; or a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH, CF3; preferably R2 represents a hydrogen atom; a (C═O)—R8 group, with R8 representing a hydrogen atom; a methyl group; an ethyl group; a propyl group; a butyl group; a pentyl group; a hexyl group
R3 and R4, identical or different, represent a hydrogen atom; a saturated or unsaturated, unsubstituted C3-8 aliphatic group; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group; an unsubstituted heteroaryl group; a saturated or unsaturated, optionally at least mono-substituted alkyl-cycloalkyl group; an unsubstituted alkyl-aryl group; a saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group; with the condition that R3 and R4 may not at the same time represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a ring system A, comprising:
and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
2) an A-X—B group,
wherein
A represents a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a linear C1-2 alkyl chain, —O—, or a —SO2— group;
B represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
3) an A-X—B—Y—C group,
wherein
A represents a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3; a C1-6-aliphatic group; a C1-6-alkoxy group; a (C═O)—OR10 group with R10 being a linear or branched C1-6 alkyl group;
X represents a bond, a —NH— group, a —(C═O)— group, a linear C1-2 alkyl chain, —O—, or a —SO2— group;
B represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; or a ring system comprising:
which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6 alkoxy group;
Y represents a bond, a —NH— group, a linear C1-2-alkyl group;
C represents an aryl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group; a naphtyl group which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkoxy group;
R6 represent an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; preferably represents an optionally at least mono-substituted aryl group;
R8 represents a hydrogen atom; a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R12 and R12a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

### Claim 31 (depends on 1)

Substituted pyrrolidine compounds according to claim 1 according to general formula (I),
wherein
R1 represents H or C(O)OCH3;
R2 represents a hydrogen atom; a substituted or unsubstituted aliphatic group; a (C═O)—R8 group; a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH;
R3 and R4, equal or different, represent a hydrogen atom;
an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; with the condition (proviso) that R3 and R4 may not at the same time represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R10 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
R8 represents a hydrogen atom; a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R12 and R12a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;

### Claim 32 (depends on 1)

A process for the manufacture of substituted pyrrolidine compounds of general formula (I) according to claim 1, characterized in that at least one pyrroline compound of general formula (II),
wherein R1 has the meaning given above, is reacted with a per-acid, preferably MCPBA to form a compound of general formula (III),
wherein R1 has the meaning given above, followed by reacting the epoxyo-pyrroline compound of formula III with a compound of formula (IV)
together with LiClO4, ACN at preferably 90° C. to give a compound of formula I, in which R2 is H; alternatively followed by reacting the pyrrolidine compound of formula I with a base to give a compound of formula I, in which R2 has the meaning according to claim 1.

### Claim 33 (depends on 1)

A medicament comprising at least one substituted pyrrolidine compound of general formula (I) according to claim 1,
wherein
R1 represents a hydrogen atom, an unbranched or branched, saturated, optionally at least mono-substituted C1-6-aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; an optionally at least mono-substituted benzhydryl group; a (C═O)—R5 group; a group; a (SO2)—R6 group; or a (C═O)—NR7R7a group;
R2 represents a hydrogen atom; a substituted or unsubstituted aliphatic group; a (C═O)—R8 group; a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH;
R3 and R4, equal or different, represent a hydrogen atom; an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system; with the condition (proviso) that R3 and R4 may not at the same time represent a hydrogen atom;
or
R3 and R4 together with their bridging nitrogen atom form
1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Br, I, NH2, SH, OH1 CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
2) an A-X—B group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF2, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
3) an A-X—B—Y—C group,
wherein
A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
X represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11 group; a NH—R11 group; or a (C═O)—NR12R12a group;
Y represents a bond, a —NH— group, a —(C═O)— group, a branched or linear, optionally substituted C1-6-aliphatic chain, —O—, or a —SO2— group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group; a C1-6-alkyl-aryl group; a C1-6-alkyl-heteroaryl group; a C1-6-alkoxy group; a (C═O)—R9 group; a (C═O)—OR10 group; a CH2-(C═O)—O—R11 group; a (SO2)—R11group; a NH—R11 group; or a (C═O)—NR12R12a group;
R5 and R6 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R7 and R7a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R8 represents a hydrogen atom; a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono- substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R12 and R12a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system; a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
with the provisos that
if R2 represents a hydrogen atom;
and R1 represents a hydrogen atom or a condensed aryl group;
R3 and R4 may not form together with their bridging nitrogen atom a triazole group;
if R2 represents a hydrogen atom;
and R1 represents a hydrogen atom; a substituted C1-2 alkyl group; a condensed aryl group; a benzyl group;
R3 and R4 may not form together with their bridging nitrogen atom a substituted, unsaturated, condensed ring system containing at least 4 nitrogen atoms as ring members; an unsaturated, (C═O)-substituted, uncondensed, 6-membered ring system in which two carbon atoms are replaced by nitrogen.
if R2 represents a hydrogen atom;
and R3 and R4 form together with their bridging nitrogen atom a pyrrolidine ring, a piperidine ring, a piperazine ring or a morpholine ring;
R1 may not represent a hydrogen atom; a methyl group; an unsaturated tert-butyl group; a (C═O)-substituted alkyl-heteroaryl group;
if R2 represents a hydrogen atom;
and R1 does not represent a benzyl group;
and either R3 or R4 represents a hydrogen atom;
either R3 or R4 may not represent a substituted alkyl-heteroaryl group; an alkyl-aryl group; a substituted heteroaryl group; an unsubstituted methyl group; a substituted alkyl group; an aryl group; a cyclohexyl group; an alkyl-cycloalkyl group wherein the cycloalkyl group contain at least one heteroatom;
if R2 represents a hydrogen atom;
and R1 represents an alkyl group;
and either R3 or R4 represents a hydrogen atom;
either R3 or R4 may not represent a substituted or unsubstituted C1-2 alkyl group; a branched C1-1 alkyl group; a substituted or unsubstituted C3-6 cycloalkyl group in which optionally at least one carbon atom is optionally replaced by N, S or O; a cycloheptyl group;
if R2 represents a hydrogen atom;
and R1 represents an alkyl group;
either R3 or R4 may not represent a cyclohexyl group while the other represents at the same time an alkyl-aryl group; or either R3 or R4 may not represent an alkyl group while the other represents at the same time an alkyl-aryl group;
if R2 represents a hydrogen atom;
and R1 represents a benzhydryl group;
and either R3 or R4 represents a hydrogen atom;
either R3 or R4 may not represent a (C═O)-substituted alkyl-aryl group; a (C═O)-substituted aryl group;
if R2 represents a hydrogen atom;
and R1 represents benzyl;
and either R3 or R4 represents a hydrogen atom;
either R3 or R4 may not represent a substituted or unsubstituted C1-2 alkyl group; a substituted C3-8 alkyl group; a substituted aryl group; a substituted alkyl-aryl group;
or
R3 or R4, together with their bridging nitrogen atom may not form a tetrahydropyrimidine ring; a triazolo pyrimidine ring;
if R2 represents a benzyl group;
and either R3 or R4 represents a hydrogen atom;
either R3 or R4 may not represent a (C═O)-substituted alkyl-aryl group;
if R2 represents a C1-3 alkyl group;
and either R3 or R4 represents a hydrogen atom either R3 or R4 may not represent an unsubstituted C1-2 alkyl group; a substituted alkyl group; a substituted or unsubstituted aryl group; a substituted heteroaryl group; a (C═O)-substituted alkyl-aryl group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof, or a prodrug thereof,
and one or more pharmaceutically acceptable excipients and/or carriers.

### Claim at position 34

34-57. (canceled)

### Claim 58 (depends on 1)

A method for the prophylaxis and/or treatment of a sigma receptor-mediated disease or condition, which comprises administering to a subject in need thereof at least one substituted pyrrolidine compound according to claim 1.

### Claim at position 36

59-63. (canceled)