# US 10,246,413 B2 · Selective FKBP51 ligands for treatment of psychiatric disorders

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- Number: US 10,246,413 B2
- Document ID: US10246413B2
- Status: Granted
- Kind: B2
- Application number: 15/703,056
- Filed: 2017-09-13
- Published: 2018-03-15
- Granted: 2019-04-02
- Earliest claimed: 2013-09-19
- Assignees: Max-Planck-Gesellschaft zur Forderung der Wissenschaften e.V.
- Applicants: Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
- Inventors: Steffen Gaali; Felix Hausch; Alexander Kirschner; Xixi Feng; Andreas Bracher; Gerd Ruehter
- Web page: https://patentgrep.com/patent/US10246413B2

## CPC

- C07D 207/16: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- C07D 211/60: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D 211/78: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D 279/12: not condensed with other rings
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 401/14: containing three or more hetero rings
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07K 5/06139: {with the first amino acid being heterocyclic}
- C12N 9/90: Isomerases (5.)
- C12Y 502/01008: Peptidylprolyl isomerase (5.2.1.8), i.e. cyclophilin
- G16B 15/00: ICT specially adapted for analysing two-dimensional [2D] or three-dimensional [3D] molecular structures, e.g. structural or functional relations or structure alignment
- G16B 15/30: Drug targeting using structural data; Docking or binding prediction
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- C12Y: ENZYMES
- G16B: BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

The present invention relates to compounds having a selective FKBP51 ligand scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said selective FKBP51 ligand compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

## Claims

### Claim 1

A compound of the general formula (I):
wherein:
X represents —CH2CH2;
Y represents —O—;
Z represents a covalent bond;
R* represents —R**, —CH2—R**, —CH2—CH═CH2, -cyclo-C6H11, or -cyclo-C5H9;
R** represents
R′ and R″ represent independently of each other —CH3, —C2H5, —CH(CH3)2, —CH2CH═CH2, -cyclo-C3H5, or —C(CH3)3;
RA represents:
RB represents: —R26,
RC represents: —R27,
RD represents: —R28,
R1-R22, R18′-R22′, R26-R39 represent independently of each other —H, —OH, —OCH3, —OC2H5, —OC3H7, —O-cyclo-C3H5, —OCH(CH3)2, —OC(CH3)3, —OC4H9, —OCH2—COOH, —OPh, —OCH2-Ph, —OCPh3, —CH2—OH, —C2H4—OH, —C3H6—OH, —CH(OH)—CH2—OH, —CH2—OCH3, —C2H4—OCH3, —C4H8—OCH3, —C3H6—OCH3, —CH2—OC2H5, —C2H4—OC2H5, —C3H6—OC2H5, —C4H8—OC2H5, —CH2—OC3H7, —C2H4—OC3H7, —C3H6—OC3H7, —CH2—O-cyclo-C3H5, —C2H4—O-cyclo-C3H5, —C3H6—O-cyclo-C3H5, —C4H8—O-cyclo-C3H5, —CH2—OCH(CH3)2, —C2H4—OCH(CH3)2, —C3H6—OCH(CH3)2, —C4H8—OCH(CH3)2, —CH2—OC(CH3)3, —C2H4—OC(CH3)3, —C3H6—OC(CH3)3, —C4H8—OC(CH3)3, —CH2—OC4H9, —C2H4—OC4H9, —C3H6—OC4H9, —C4H8—OC4H9, —CH2—OPh, —C2H4—OPh, —C3H6—OPh, —C4H8—OPh, —CH2—OCH2-Ph, —C2H4—OCH2-Ph, —C3H6—OCH2-Ph, —C4H8—OCH2-Ph, —SH, —SCH3, —SC2H5, —SC3H7, —S-cyclo-C3H5, —SCH(CH3)2, —SC(CH3)3, —NO2, —F, —Cl, —Br, —I, —P(O)(OH)2, —P(O)(OCH3)2, —P(O)(OC2H5)2, —P(O)(OCH(CH3)2)2, —C(OH)[P(O)(OH)2]2, —Si(CH3)2(C(CH3)3), —Si(C2H5)3, —Si(CH3)3, —N3, —CN, —OCN, —NCO, —SCN, —NCS, —CHO, —COCH3, —COC2H5, —COC3H7, —CO-cyclo-C3H5, —COCH(CH3)2, —COC(CH3)3, —COOH, —COCN, —COOCH3, —COOC2H5, —COOC3H7, —COO-cyclo-C3H5, —COOCH(CH3)2, —COOC(CH3)3, —OOC—CH3, —OOC—C2H5, —OOC—C3H7, —OOC-cyclo-C3H5, —OOC—CH(CH3)2, —OOC—C(CH3)3, —CONH2, —CH2—CONH2, —CONHCH3, —CONHC2H5, —CONHC3H7, —CONH-cyclo-C3H5, —CONH[CH(CH3)2], —CONH[C(CH3)3], —CON(CH3)2, —CON(C2H5)2, —CON(C3H7)2, —CON(cyclo-C3H5)2, —CON[CH(CH3)2]2, —CON[C(CH3)3]2, —NHCOCH3, —NHCOC2H5, —NHCOC3H7, —NHCO-cyclo-C3H5, —NHCO—CH(CH3)2, —NHCO—C(CH3)3, —NHCO—OCH3, —NHCO—OC2H5, —NHCO—OC3H7, —NHCO—O-cyclo-C3H5, —NHCO—OCH(CH3)2, —NHCO—OC(CH3)3, —NH2, —NHCH3, —NHC2H5, —NHC3H7, —NH-cyclo-C3H5, —NHCH(CH3)2, —NHC(CH3)3, —N(CH3)2, —N(C2H5)2, —N(C3H7)2, —N(cyclo-C3H5)2, —N[CH(CH3)2]2, —N[C(CH3)3]2, —SOCH3, —SOC2H5, —SOC3H7, —SO-cyclo-C3H5, —SOCH(CH3)2, —SOC(CH3)3, —SO2CH3, —SO2C2H5, —SO2C3H7, —SO2-cyclo-C3H5, —SO2CH(CH3)2, —SO2C(CH3)3, —SO3H, —SO3CH3, —SO3C2H5, —SO3C3H7, —SO3-cyclo-C3H5, —SO3CH(CH3)2, —SO3C(CH3)3, —SO2NH2, —SO2NHCH3, —SO2NHC2H5, —SO2NHC3H7, —SO2NH-cyclo-C3H5, —SO2NHCH(CH3)2, —SO2NHC(CH3)3, —SO2N(CH3)2, —SO2N(C2H5)2, —SO2N(C3H7)2, —SO2N(cyclo-C3H5)2, —SO2N[CH(CH3)2]2, —SO2N[C(CH3)3]2, —O—S(═O)CH3, —O—S(═O)C2H5, —O—S(═O)C3H7, —O—S(═O)-cyclo-C3H5, —O—S(═O)CH(CH3)2, —O—S(═O)C(CH3)3, —S(═O)(═NH)CH3, —S(═O)(═NH)C2H5, —S(═O)(═NH)C3H7, —S(═O)(═NH)-cyclo-C3H5, —S(═O)(═NH)CH(CH3)2, —S(═O)(═NH)C(CH3)3, —NH—SO2—CH3, —NH—SO2—C2H5, —NH—SO2—C3H7, —NH—SO2-cyclo-C3H5, —NH—SO2—CH(CH3)2, —NH—SO2—C(CH3)3, —O—SO2—CH3, —O—SO2—C2H5, —O—SO2—C3H7, —O—SO2-cyclo-C3H5, —O—SO2—CH(CH3)2, —O—SO2—C(CH3)3, —OCF3, —CH2—OCF3, —C2H4—OCF3, —C3H6—OCF3, —OC2F5, —CH2—OC2F5, —C2H4—OC2F5, —C3H6—OC2F5, —O—COOCH3, —O—COOC2H5, —O—COOC3H7, —O—COO-cyclo-C3H5, —O—COOCH(CH3)2, —O—COOC(CH3)3, —NH—CO—NH2, —NH—CO—NHCH3, —NH—CO—NHC2H5, —NH—CS—N(C3H7)2, —NH—CO—NHC3H7, —NH—CO—N(C3H7)2, —NH—CO—NH[CH(CH3)2], —NH—CO—NH[C(CH3)3], —NH—CO—N(CH3)2, —NH—CO—N(C2H5)2, —NH—CO—NH-cyclo-C3H5, —NH—CO—N(cyclo-C3H5)2, —NH—CO—N[CH(CH3)2]2, —NH—CS—N(C2H5)2, —NH—CO—N[C(CH3)3]2, —NH—CS—NH2, —NH—CS—NHCH3, —NH—CS—N(CH3)2, —NH—CS—NHC2H5, —NH—CS—NHC3H7, —NH—CS—NH-cyclo-C3H5, —NH—CS—NH[CH(CH3)2], —NH—CS—NH[C(CH3)3], —NH—CS—N(cyclo-C3H5)2, —NH—CS—N[CH(CH3)2]2, —NH—CS—N[C(CH3)3]2, —NH—C(═NH)—NH2, —NH—C(═NH)—NHCH3, —NH—C(═NH)—NHC2H5, —NH—C(═NH)—NHC3H7, —O—CO—NH-cyclo-C3H5, —NH—C(═NH)—NH-cyclo-C3H5, —NH—C(═NH)—NH[CH(CH3)2]—O—CO—NH[CH(CH3)2], —NH—C(═NH)—NH[C(CH3)3], —NH—C(═NH)—N(CH3)2, —NH—C(═NH)—N(C2H5)2, —NH—C(═NH)—N(C3H7)2, —NH—C(═NH)—N(cyclo-C3H5)2, —O—CO—NHC3H7, —NH—C(═NH)—N[CH(CH3)2]2, —NH—C(═NH)—N[C(CH3)3]2, —O—CO—NH2, —O—CO—NHCH3, —O—CO—NHC2H5, —O—CO—NH[C(CH3)3], —O—CO—N(CH3)2, —O—CO—N(C2H5)2, —O—CO—N(C3H7)2, —O—CO—N(cyclo-C3H5)2, —O—CO—N[CH(CH3)2]2, —O—CO—N[C(CH3)3]2, —O—CO—OCH3, —O—CO—OC2H5, —O—CO—OC3H7, —O—CO—O-cyclo-C3H5, —O—CO—OCH(CH3)2, —O—CO—OC(CH3)3, —CH2F, —CHF2, —CF3, —CH2C1, —CH2Br, —CH2I, —CH2—CH2F, —CH2—CHF2, —CH2—CF3, —CH2—CH2C1, —CH2—CH2Br, —CH2—CH2I, -cyclo-C5H9, -cyclo-C6H11, —CH2-cyclo-C6H11, —CH2—CH2-cyclo-C6H11, -cyclo-C7H13, -cyclo-C8H15, -Ph, —CH2-Ph, —CH2—CH2-Ph, —CH═CH-Ph, —CPh3, —CH3, —C2H5, —C3H7, —CH(CH3)2, —C4H9, —CH2—CH(CH3)2, —CH(CH3)—C2H5, —C(CH3)3, —C5H11, —CH(CH3)—C3H7, —CH2—CH(CH3)—C2H5, —CH(CH3)—CH(CH3)2, —C(CH3)2—C2H5, —CH2—C(CH3)3, —CH(C2H5)2, —C2H4—CH(CH3)2, —C6H13, —C7H15, —C8H17, —C3H6—CH(CH3)2, —C2H4—CH(CH3)—C2H5, —CH(CH3)—C4H9, —CH2—CH(CH3)—C3H7, —CH(CH3)—CH2—CH(CH3)2, —CH(CH3)—CH(CH3)—C2H5, —CH2—CH(CH3)—CH(CH3)2, —CH2—C(CH3)2—C2H5, —C(CH3)2—C3H7, —C(CH3)2—CH(CH3)2, —C2H4—C(CH3)3, —CH(CH3)—C(CH3)3, —CH═CH2, —CH2—CH═CH2, —C(CH3)═CH2, —CH═CH—CH3, —C2H4—CH═CH2, —CH2—CH═CH—CH3, —CH═CH—C2H5, —CH2—C(CH3)═CH2, —CH(CH3)—CH═CH, —CH═C(CH3)2, —C(CH3)═CH—CH3, —CH═CH—CH═CH2, —C3H6—CH═CH2, —C2H4—CH═CH—CH3, —CH2—CH═CH—C2H5, —CH═CH—C3H7, —CH2—CH═CH—CH═CH2, —CH═CH—CH═CH—CH3, —CH═CH—CH2—CH═CH2, —C(CH3)═CH—CH═CH2, —CH═C(CH3)—CH═CH2, —CH═CH—C(CH3)═CH2, —C2H4—C(CH3)═CH2, —CH2—CH(CH3)—CH═CH2, —CH(CH3)—CH2—CH═CH2, —CH2—CH═C(CH3)2, —CH2—C(CH3)═CH—CH3, —CH(CH3)—CH═CH—CH3, —C(CH3)═C(CH3)2, —C(CH3)2—CH═CH2, —CH(CH3)—C(CH3)═CH2, —C(CH3)═CH—CH═CH2, —CH═C(CH3)—CH═CH2, —CH═CH—C(CH3)═CH2, —C4H8—CH═CH2, —C3H6—CH═CH—CH3, —C2H4—CH═CH—C2H5, —CH2—CH═CH—C3H7, —CH═CH—C4H9, —C3H6—C(CH3)═CH2, —C2H4—CH(CH3)—CH═CH2, —CH2—CH(CH3)—CH2—CH═CH2, —C2H4—CH═C(CH3)2, —CH(CH3)—C2H4—CH═CH2, —C2H4—C(CH3)═CH—CH3, —CH2—CH(CH3)—CH═CH—CH3, —CH(CH3)—CH2—CH═CH—CH3, —CH2—CH═CH—CH(CH3)2, —CH2—CH═C(CH3)—C2H5, —CH2—C(CH3)═CH—C2H5, —CH(CH3)—CH═CH—C2H5, —CH═CH—CH2—CH(CH3)2, —CH═CH—CH(CH3)—C2H5, —CH═C(CH3)—C3H7, —C(CH3)═CH—C3H7, —CH2—CH(CH3)—C(CH3)═CH2, —C[C(CH3)3]═CH2, —CH(CH3)—CH2—C(CH3)═CH2, —CH(CH3)—CH(CH3)—CH═CH2, —CH═CH—C2H4—CH═CH2, —CH2—C(CH3)2—CH═CH2, —C(CH3)2—CH2—CH═CH2, —CH2—C(CH3)═C(CH3)2, —CH(CH3)—CH═C(CH3)2, —C(CH3)2—CH═CH—CH3, —CH═CH—CH2—CH═CH—CH3, —CH(CH3)—C(CH3)═CH—CH3, —CH═C(CH3)—CH(CH3)2, —C(CH3)═CH—CH(CH3)2, —C(CH3)═C(CH3)—C2H5, —CH═CH—C(CH3)3, —C(CH3)2—C(CH3)═CH2, —CH(C2H5)—C(CH3)═CH2, —C(CH3)(C2H5)—CH═CH2, —CH(CH3)—C(C2H5)═CH2, —CH2—C(C3H7)═CH2, —CH2—C(C2H5)═CH—CH3, —CH(C2H5)—CH═CH—CH3, —C(C4H9)═CH2, —C(C3H7)═CH—CH3, —C(C2H5)═CH—C2H5, —C(C2H5)═C(CH3)2, —C[CH(CH3)(C2H5)]═CH2, —C[CH2—CH(CH3)2]═CH2, —C2H4—CH═CH—CH═CH2, —CH2—CH═CH—CH2—CH═CH2, —C3H6—C═C—CH3, —CH2—CH═CH—CH═CH—CH3, —CH═CH—CH═CH—C2H5, —CH2—CH═CH—C(CH3)═CH2, —CH2—CH═C(CH3)—CH═CH2, —CH2—C(CH3)═CH—CH═CH2, —CH(CH3)—CH2—C≡CH, —CH(CH3)—CH═CH—CH═CH2, —CH═CH—CH2—C(CH3)═CH2, —CH(CH3)—C≡C—CH3, —CH═CH—CH(CH3)—CH═CH2, —CH═C(CH3)—CH2—CH═CH2, —C2H4—CH(CH3)—C≡CH, —C(CH3)═CH—CH2—CH═CH2, —CH═CH—CH═C(CH3)2, —CH2—CH(CH3)—CH2—C≡CH, —CH═CH—C(CH3)═CH—CH3, —CH═C(CH3)—CH═CH—CH3, —CH2—CH(CH3)—C≡CH, —C(CH3)═CH—CH═CH—CH3, —CH═C(CH3)—C(CH3)═CH2, —C(CH3)═CH—C(CH3)═CH2, —C(CH3)═C(CH3)—CH═CH2, —CH═CH—CH═CH—CH═CH2, —C≡CH, —C≡C—CH3, —CH2—C≡CH, —C2H4—C≡CH, —CH2—C═C—CH3, —C═C—C2H5, —C3H6—C═CH, —C2H4—C═C—CH3, —CH2—C═C—C2H5, —C≡C—C3H7, —CH(CH3)—C≡CH, —C4H8—C≡CH, —C2H4—C≡C—C2H5, —CH2—C≡C—C3H7, —C≡C—C4H9, —C≡C—C(CH3)3, —CH(CH3)—C2H4—C≡CH, —CH2—CH(CH3)—C≡C—CH3, —CH(CH3)—CH2—C≡C—CH3, —CH(CH3)—C≡C—C2H5, —CH2—C≡C—CH(CH3)2, —C≡C—CH(CH3)—C2H5, —C≡C—CH2—CH(CH3)2, —CH(C2H5)—C≡C—CH3, —C(CH3)2—C≡C—CH3, —CH(C2H5)—CH2—C≡CH, —CH2—CH(C2H5)—C≡CH, —C(CH3)2—CH2—C≡CH, —CH2—C(CH3)2—C≡CH, —CH(CH3)—CH(CH3)—C≡CH, —CH(C3H7)—C≡CH, —C(CH3)(C2H5)—C≡CH, —CH2—CH(C≡CH)2, —C≡C—C≡CH, —CH2—C≡C—C≡CH, —C≡C—C≡C—CH3, —CH(C≡CH)2, —C2H4—C≡C—C≡CH, —CH2—C≡C—CH2—C≡CH, —C≡C—C2H4—C≡CH, —CH2—C≡C—C≡C—CH3, —C≡C—CH2—C≡C—CH3, —C≡C—C≡C—C2H5, —C(C═CH)2—CH3, —C≡C—CH(CH3)—C≡CH, —CH(CH3)—C≡C—C≡CH, —CH(C≡CH)—CH2—C≡CH, —CH(C≡CH)—C≡C—CH3,
R18 and R18′ or R19 and R19′ or R20 and R20′ or R21 and R21′ or R22 and R22′ form together ═O,
or ═CR23′R24′, wherein R23′ and R24′ represent independently of each other —H, —CH3, —C2H5, —CF3, —CH2CF3, or —C2F5;
R23-R25 represent independently of each other —H, —CH2—OCH3, —C2H4—OCH3, —C3H6—OCH3, —CH2—OC2H5, —C2H4—OC2H5, —C3H6—OC2H5, —CH2—OC3H7, —C2H4—OC3H7, —C3H6—OC3H7, —CH2—O-cyclo-C3H5, —C2H4—O-cyclo-C3H5, —C3H6—O-cyclo-C3H5, —CH2—OCH(CH3)2, —C2H4—OCH(CH3)2, —C3H6—OCH(CH3)2, —CH2—OC(CH3)3, —C2H4—OC(CH3)3, —C3H6—OC(CH3)3, —CH2—OC4H9, —C2H4—OC4H9, —C3H6—OC4H9, —CH2—OPh, —C2H4—OPh, —C3H6—OPh, —CH2—OCH2-Ph, —C2H4—OCH2-Ph, —C3H6—OCH2-Ph, —CH2F, —CHF2, —CF3, —CH2Cl, —CH2Br, —CH2I, —CH2—CH2F, —CH2—CHF2, —CH2—CF3, —CH2—CH2Cl, —CH2—CH2Br, —CH2—CH2I, -cyclo-C8H15, -Ph, —CH2-Ph, —CH2—CH2-Ph, —CH═CH-Ph, —CPh3, —CH3, —C2H5, —C3H7, —CH(CH3)2, —C4H9, —CH2—CH(CH3)2, —CH(CH3)—C2H5, —C(CH3)3, —C5H11, —CH(CH3)—C3H7, —CH2—CH(CH3)—C2H5, —CH(CH3)—CH(CH3)2, —C(CH3)2—C2H5, —CH2—C(CH3)3, —CH(C2H5)2, —C2H4—CH(CH3)2, —C6H13, —C7H15, —C8H17, —C3H6—CH(CH3)2, —C2H4—CH(CH3)—C2H5, —CH(CH3)—C4H9, —CH2—CH(CH3)—C3H7, —CH(CH3)—CH2—CH(CH3)2, —CH(CH3)—CH(CH3)—C2H5, —CH2—CH(CH3)—CH(CH3)2, —CH2—C(CH3)2—C2H5, —C(CH3)2—C3H7, —C(CH3)2—CH(CH3)2, —C2H4—C(CH3)3, —CH(CH3)—C(CH3)3, —CH═CH2, —CH2—CH═CH2, —C(CH3)═CH2, —CH═CH—CH3, —C2H4—CH═CH2, —CH2—CH═CH—CH3, —CH═CH—C2H5, —CH2—C(CH3)═CH2, —CH(CH3)—CH═CH, —CH═C(CH3)2, —C(CH3)═CH—CH3, —CH═CH—CH═CH2, —C3H6—CH═CH2, —C2H4—CH═CH—CH3, —CH2—CH═CH—C2H5, —CH═CH—C3H7, —CH2—CH═CH—CH═CH2, —CH═CH—CH═CH—CH3, —CH═CH—CH2—CH═CH2, —C(CH3)═CH—CH═CH2, —CH═C(CH3)—CH═CH2, —CH═CH—C(CH3)═CH2, —C2H4—C(CH3)═CH2, —CH2—CH(CH3)—CH═CH2, —CH(CH3)—CH2—CH═CH2, —CH2—CH═C(CH3)2, —CH2—C(CH3)═CH—CH3, —CH(CH3)—CH═CH—CH3, —CH═CH—CH(CH3)2, —CH═C(CH3)—C2H5, —C(CH3)═CH—C2H5, —C(CH3)═C(CH3)2, —C(CH3)2—CH═CH2, —CH(CH3)—C(CH3)═CH2, —C(CH3)═CH—CH═CH2, —CH═C(CH3)—CH═CH2, —CH═CH—C(CH3)═CH2, —C4H8—CH═CH2, —C3H6—CH═CH—CH3, —C2H4—CH═CH—C2H5, —CH2—CH═CH—C3H7, —CH═CH—C4H9, —C3H6—C(CH3)═CH2, —C2H4—CH(CH3)—CH═CH2, —CH2—CH(CH3)—CH2—CH═CH2, —C2H4—CH═C(CH3)2, —CH(CH3)—C2H4—CH═CH2, —C2H4—C(CH3)═CH—CH3, —CH2—CH(CH3)—CH═CH—CH3, —CH(CH3)—CH2—CH═CH—CH3, —CH2—CH═CH—CH(CH3)2, —CH2—CH═C(CH3)—C2H5, —CH2—C(CH3)═CH—C2H5, —CH(CH3)—CH═CH—C2H5, —CH═CH—CH2—CH(CH3)2, —CH═CH—CH(CH3)—C2H5, —CH═C(CH3)—C3H7, —C(CH3)═CH—C3H7, —CH2—CH(CH3)—C(CH3)═CH2, —C[C(CH3)3]═CH2, —CH(CH3)—CH2—C(CH3)═CH2, —CH(CH3)—CH(CH3)—CH═CH2, —CH═CH—C2H4—CH═CH2, —CH2—C(CH3)2—CH═CH2, —C(CH3)2—CH2—CH═CH2, —CH2—C(CH3)═C(CH3)2, —CH(CH3)—CH═C(CH3)2, —C(CH3)2—CH═CH—CH3, —CH═CH—CH2—CH═CH—CH3, —CH(CH3)—C(CH3)═CH—CH3, —CH═C(CH3)—CH(CH3)2, —C(CH3)═CH—CH(CH3)2, —C(CH3)═C(CH3)—C2H5, —CH═CH—C(CH3)3, —C(CH3)2—C(CH3)═CH2, —CH(C2H5)—C(CH3)═CH2, —C(CH3)(C2H5)—CH═CH2, —CH(CH3)—C(C2H5)═CH2, —CH2—C(C3H7)═CH2, —CH2—C(C2H5)═CH—CH3, —CH(C2H5)—CH═CH—CH3, —C(C4H9)═CH2, —C(C3H7)═CH—CH3, —C(C2H5)═CH—C2H5, —C(C2H5)═C(CH3)2, —C[CH(CH3)(C2H5)]═CH2, —C[CH2—CH(CH3)2]═CH2, —CH2—CH═CH—CH═CH—CH3, —CH═CH—CH═CH—C2H5, —CH2—CH═CH—C(CH3)═CH2, —CH2—CH═C(CH3)—CH═CH2, —CH2—C(CH3)═CH—CH═CH2, —CH(CH3)—CH2—C≡CH, —CH(CH3)—CH═CH—CH═CH2, —CH═CH—CH2—C(CH3)═CH2, —CH(CH3)—C≡C—CH3, —CH═CH—CH(CH3)—CH═CH2, —CH═C(CH3)—CH2—CH═CH2, —C2H4—CH(CH3)—C≡CH, —C(CH3)═CH—CH2—CH═CH2, —CH═CH—CH═C(CH3)2, —CH2—CH(CH3)—CH2—C≡CH, —CH═CH—C(CH3)═CH—CH3, —CH═C(CH3)—CH═CH—CH3, —CH2—CH(CH3)—C≡CH, —C(CH3)═CH—CH═CH—CH3, —CH═C(CH3)—C(CH3)═CH2, —C(CH3)═CH—C(CH3)═CH2, —C(CH3)═C(CH3)—CH═CH2, —CH═CH—CH═CH—CH═CH2, —C≡CH, —C≡C—CH3, —CH2—C≡CH, —C2H4—C═CH, —CH2—C≡C—CH3, —C═C—C2H5, —C3H6—C═CH, —C2H4—C═C—CH3, —CH2—C═C—C2H5, —C═C—C3H7, —CH(CH3)—C≡CH, —C4H8—C═CH, —C2H4—C═C—C2H5, —CH2—C═C—C3H7, —C═C—C4H9, —C═C—C(CH3)3, —CH(CH3)—C2H4—C═CH, —CH2—CH(CH3)—C≡C—CH3, —CH(CH3)—CH2—C≡C—CH3, —CH(CH3)—C═C—C2H5, —CH2—C═C—CH(CH3)2, —C═C—CH(CH3)—C2H5, —C═C—CH2—CH(CH3)2, —CH(C2H5)—C═C—CH3, —C(CH3)2—C═C—CH3, —CH(C2H5)—CH2—C≡CH, —CH2—CH(C2H5)—C≡CH, —C(CH3)2—CH2—C≡CH, —CH2—C(CH3)2—C≡CH, —CH(CH3)—CH(CH3)—C≡CH, —CH(C3H7)—C≡CH, —C(CH3)(C2H5)—C═CH, —CH2—CH(C≡CH)2, —C≡C—C≡CH, —CH2—C≡C—C≡CH, —C≡C—C≡C—CH3, —CH(C≡CH)2, —C2H4—C═C—C═CH, —CH2—C≡C—CH2—C≡CH, —C═C—C2H4—C═CH, —CH2—C═C—C═C—CH3, —C═C—CH2—C═C—CH3, —C≡C—C≡C—C2H5, —C(C═CH)2—CH3, —C≡C—CH(CH3)—C≡CH, —CH(CH3)—C≡C—C≡CH, —CH(C≡CH)—CH2—C≡CH, or —CH(C≡CH)—C≡C—CH3;
RN represents —H, —CH2—OCH3, —C2H4—OCH3, —C3H6—OCH3, —CH2—OC2H5, —C2H4—OC2H5, —C3H6—OC2H5, —CH2—OC3H7, —C2H4—OC3H7, —C3H6—OC3H7, —CH2—O-cyclo-C3H5, —C2H4—O-cyclo-C3H5, —C3H6—O-cyclo-C3H5, —CH2—OCH(CH3)2, —C2H4—OCH(CH3)2, —C3H6—OCH(CH3)2, —CH2—OC(CH3)3, —C2H4—OC(CH3)3, —C3H6—OC(CH3)3, —CH2—OC4H9, —C2H4—OC4H9, —C3H6—OC4H9, —CH2—OPh, —C2H4—OPh, —C3H6—OPh, —CH2—OCH2-Ph, —C2H4—OCH2-Ph, —C3H6—OCH2-Ph, —CHO, —COCH3, —COC2H5, —COC3H7, —CO-cyclo-C3H5, —COCH(CH3)2, —COC(CH3)3, —COCN, —COOCH3, —COOC2H5, —COOC3H7, —COO-cyclo-C3H5, —COOCH(CH3)2, —COOC(CH3)3, —CONH2, —CONHCH3, —CONHC2H5, —CONHC3H7, —CONH-cyclo-C3H5, —CONH[CH(CH3)2], —CONH[C(CH3)3], —CON(CH3)2, —CON(C2H5)2, —CON(C3H7)2, —CON(cyclo-C3H5)2, —CON[CH(CH3)2]2, —CON[C(CH3)3]2, —SO2CH3, —SO2C2H5, —SO2C3H7, —SO2-cyclo-C3H5, —SO2CH(CH3)2, —SO2C(CH3)3, —CH2—OCF3, —C2H4—OCF3, —C3H6—OCF3, —OC2F5, —CH2—OC2F5, —C2H4—OC2F5, —C3H6—OC2F5, —CH2F, —CHF2, —CF3, —CH2Cl, —CH2Br, —CH2I, —CH2—CH2F, —CH2—CHF2, —CH2—CF3, —CH2—CH2Cl, —CH2—CH2Br, —CH2—CH2I, -cyclo-C8H15, -Ph, —CH2-Ph, —CH2—CH2-Ph, —CH═CH-Ph, —CPh3, —CH3, —C2H5, —C3H7, —CH(CH3)2, —C4H9, —CH2—CH(CH3)2, —CH(CH3)—C2H5, —C(CH3)3, —C5H11, —CH(CH3)—C3H7, —CH2—CH(CH3)—C2H5, —CH(CH3)—CH(CH3)2, —C(CH3)2—C2H5, —CH2—C(CH3)3, —CH(C2H5)2, —C2H4—CH(CH3)2, —C6H13, —C7H15, —C8H17, —C3H6—CH(CH3)2, —C2H4—CH(CH3)—C2H5, —CH(CH3)—C4H9, —CH2—CH(CH3)—C3H7, —CH(CH3)—CH2—CH(CH3)2, —CH(CH3)—CH(CH3)—C2H5, —CH2—CH(CH3)—CH(CH3)2, —CH2—C(CH3)2—C2H5, —C(CH3)2—C3H7, —C(CH3)2—CH(CH3)2, —C2H4—C(CH3)3, —CH(CH3)—C(CH3)3, —CH═CH2, —CH2—CH═CH2, —C(CH3)═CH2, —CH═CH—CH3, —C2H4—CH═CH2, —CH2—CH═CH—CH3, —CH═CH—C2H5, —CH2—C(CH3)═CH2, —CH(CH3)—CH═CH, —CH═C(CH3)2, —C(CH3)═CH—CH3, —CH═CH—CH═CH2, —C3H6—CH═CH2, —C2H4—CH═CH—CH3, —CH2—CH═CH—C2H5, —CH═CH—C3H7, —CH2—CH═CH—CH═CH2, —CH═CH—CH═CH—CH3, —CH═CH—CH2—CH═CH2, —C(CH3)═CH—CH═CH2, —CH═C(CH3)—CH═CH2, —CH═CH—C(CH3)═CH2, —C2H4—C(CH3)═CH2, —CH2—CH(CH3)—CH═CH2, —CH(CH3)—CH2—CH═CH2, —CH2—CH═C(CH3)2, —CH2—C(CH3)═CH—CH3, —CH(CH3)—CH═CH—CH3, —CH═CH—CH(CH3)2, —CH═C(CH3)—C2H5, —C(CH3)═CH—C2H5, —C(CH3)═C(CH3)2, —C(CH3)2—CH═CH2, —CH(CH3)—C(CH3)═CH2, —C(CH3)═CH—CH═CH2, —CH═C(CH3)—CH═CH2, —CH═CH—C(CH3)═CH2, —C4H8—CH═CH2, —C3H6—CH═CH—CH3, —C2H4—CH═CH—C2H5, —CH2—CH═CH—C3H7, —CH═CH—C4H9, —C3H6—C(CH3)═CH2, —C2H4—CH(CH3)—CH═CH2, —CH2—CH(CH3)—CH2—CH═CH2, —C2H4—CH═C(CH3)2, —CH(CH3)—C2H4—CH═CH2, —C2H4—C(CH3)═CH—CH3, —CH2—CH(CH3)—CH═CH—CH3, —CH(CH3)—CH2—CH═CH—CH3, —CH2—CH═CH—CH(CH3)2, —CH2—CH═C(CH3)—C2H5, —CH2—C(CH3)═CH—C2H5, —CH(CH3)—CH═CH—C2H5, —CH═CH—CH2—CH(CH3)2, —CH═CH—CH(CH3)—C2H5, —CH═C(CH3)—C3H7, —C(CH3)═CH—C3H7, —CH2—CH(CH3)—C(CH3)═CH2, —C[C(CH3)3]═CH2, —CH(CH3)—CH2—C(CH3)═CH2, —CH(CH3)—CH(CH3)—CH═CH2, —CH═CH—C2H4—CH═CH2, —CH2—C(CH3)2—CH═CH2, —C(CH3)2—CH2—CH═CH2, —CH2—C(CH3)═C(CH3)2, —CH(CH3)—CH═C(CH3)2, —C(CH3)2—CH═CH—CH3, —CH═CH—CH2—CH═CH—CH3, —CH(CH3)—C(CH3)═CH—CH3, —CH═C(CH3)—CH(CH3)2, —C(CH3)═CH—CH(CH3)2, —C(CH3)═C(CH3)—C2H5, —CH═CH—C(CH3)3, —C(CH3)2—C(CH3)═CH2, —CH(C2H5)—C(CH3)═CH2, —C(CH3)(C2H5)—CH═CH2, —CH(CH3)—C(C2H5)═CH2, —CH2—C(C3H7)═CH2, —CH2—C(C2H5)═CH—CH3, —CH(C2H5)—CH═CH—CH3, —C(C4H9)═CH2, —C(C3H7)═CH—CH3, —C(C2H5)═CH—C2H5, —C(C2H5)═C(CH3)2, —C[CH(CH3)(C2H5)]═CH2, —C[CH2—CH(CH3)2]═CH2, —C2H4—CH═CH—CH═CH2, —CH2—CH═CH—CH2—CH═CH2, —C3H6—C═C—CH3, —CH2—CH═CH—CH═CH—CH3, —CH═CH—CH═CH—C2H5, —CH2—CH═CH—C(CH3)═CH2, —CH2—CH═C(CH3)—CH═CH2, —CH2—C(CH3)═CH—CH═CH2, —CH(CH3)—CH2—C≡CH, —CH(CH3)—CH═CH—CH═CH2, —CH═CH—CH2—C(CH3)═CH2, —CH(CH3)—C≡C—CH3, —CH═CH—CH(CH3)—CH═CH2, —CH═C(CH3)—CH2—CH═CH2, —C2H4—CH(CH3)—C≡CH, —C(CH3)═CH—CH2—CH═CH2, —CH═CH—CH═C(CH3)2, —CH2—CH(CH3)—CH2—C≡CH, —CH═CH—C(CH3)═CH—CH3, —CH═C(CH3)—CH═CH—CH3, —CH2—CH(CH3)—C≡CH, —C(CH3)═CH—CH═CH—CH3, —CH═C(CH3)—C(CH3)═CH2, —C(CH3)═CH—C(CH3)═CH2, —C(CH3)═C(CH3)—CH═CH2, —CH═CH—CH═CH—CH═CH2, —C≡CH, —C≡C—CH3, —CH2—C≡CH, —C2H4—C≡CH, —CH2—C≡C—CH3, —C≡C—C2H5, —C3H6—C≡CH, —C2H4—C≡C—H3, —CH2—C≡C—C2H5, —C≡C—C3H7, —CH(CH3)—C≡CH, —C4H8—C≡CH, —C2H4—C═C≡—C2H5, —CH2—C═C—C3H7, —C═C—C4H9, —C≡C—C(CH3)3, —CH(CH3)—C2H4—C≡CH, —CH2—CH(CH3)—C≡C—CH3, —CH(CH3)—CH2—C≡C—CH3, —CH(CH3)—C═C—C2H5, —CH2—C═C—CH(CH3)2, —C≡C—CH(CH3)—C2H5, —C═C—CH2—CH(CH3)2, —CH(C2H5)—C≡C—CH3, —C(CH3)2—C≡C—CH3, —CH(C2H5)—CH2—C≡CH, —CH2—CH(C2H5)—C≡CH, —C(CH3)2—CH2—C≡CH, —CH2—C(CH3)2—C≡CH, —CH(CH3)—CH(CH3)—C≡CH, —CH(C3H7)—C≡CH, —C(CH3)(C2H5)—C═CH, —CH2—CH(C≡CH)2, —C≡C—C≡CH, —CH2—C≡C—C≡CH, —C≡C—C≡C—CH3, —CH(C≡CH)2, —C2H4—C≡C—C≡CH, —CH2—C≡C—CH2—C≡CH, —C═C—C2H4—C═CH, —CH2—C═C—C═C—CH3, —C≡C—CH2—C≡C—CH3, —C≡C—C≡C—C2H5, —C(C≡CH)2—CH3, —C≡C—CH(CH3)—C≡CH, —CH(CH3)—C≡C—C≡CH, —CH(C≡CH)—CH2—C≡CH, or —CH(C≡CH)—C≡C—CH3;
L1, represents: —CH2—, —C2H4—, —C3H6—, —C4H8—, —C5H10—, —C6H12—C7H14—, —C8H16—, —C9H18—, —C10H20—, —CH2CH2O—, —CH(CH3)—, —C[(CH3)2]—, —CH(C3H7)—, —CH2—CH(CH3)—, —CH(CH3)—CH2—, —CH(CH3)—C2H4—, —CH2—CH(CH3)—CH2—, —C2H4—CH(CH3)—, —CH2—C[(CH3)2]—, —C[(CH3)2]—CH2—, —CH(CH3)—CH(CH3)—, —C[(C2H5)(CH3)]—, —(CH2—CH2—O)n—CH2—CH2—, —C(CH3)═CH—C(CH3)═CH—, —C2H4—CH═CH—CH═CH—, —CH2—CH═CH—CH2—CH═CH—, —C3H6—C═C—CH2—, —CH2—CH═CH—CH═CH—CH2—, —CH(CH3)—C≡C—CH2—, —CH═CH—CH═CH—C2H4—, —CH2—CH═CH—C(CH3)═CH—, —CH2—CH═C(CH3)—CH═CH—, —CH2—C(CH3)═CH—CH═CH—, —CH(CH3)—CH═CH—CH═CH—, —CH═CH—CH2—C(CH3)═CH—, —CONH—, —NHCO—, —CH2—CONH—, —CONH—CH2—, —NHCO—CH2—, or —CH2—NHCO—;
L2 and L3 represent independently of each other:
a bond, —CH2—, —C2H4—, —C3H6—, —C4H8—, —C5H10—, —C6H12—, —C7H14—, —C8H16—, —C9H18—, —C10H20—, —CH2CH2O—, —CH(CH3)—, —C[(CH3)2]—, —CH(C3H7)—, —CH2—CH(CH3)—, —CH(CH3)—CH2—, —CH(CH3)—C2H4—, —CH2—CH(CH3)—CH2—, —C2H4—CH(CH3)—, —CH2—C[(CH3)2]—, —C[(CH3)2]—CH2—, —CH(CH3)—CH(CH3)—, —C[(C2H5)(CH3)]—, —(CH2—CH2—O)n—CH2—CH2—, —C(CH3)═CH—C(CH3)═CH—, —C2H4—CH═CH—CH═CH—, —CH2—CH═CH—CH2—CH═CH—, —C3H6—C═C—CH2—, —CH2—CH═CH—CH═CH—CH2—, —CH(CH3)—C≡C—CH2—, —CH═CH—CH═CH—C2H4—, —CH2—CH═CH—C(CH3)═CH—, —CH2—CH═C(CH3)—CH═CH—, —CH2—C(CH3)═CH—CH═CH—, —CH(CH3)—CH═CH—CH═CH—, —CH═CH—CH2—C(CH3)═CH—, —CONH—, —NHCO—, —CH2—CONH—, —CONH—CH2—, —NHCO—CH2—, or —CH2—NHCO—; and
wherein each n is an integer from 1 to 10; or
L1-RB and L2-RC or L1-RB and L3-RD or L2-RC and L3-RD form together a cyclic ring selected from the group consisting of:
or enantiomers, stereoisomeric forms, mixtures of enantiomers, anomers, deoxy-forms, diastereomers, mixtures of diastereomers, prodrugs, tautomers, hydrates, solvates or racemates thereof or pharmaceutically acceptable salts thereof.

### Claim 2 (depends on 1)

The compound according to claim 1 of the general formula (Ia):
wherein
X, Y, Z, R*, RA and RB are defined according to claim 1;
RC represents —R38;
RD represents —H, —CH3, —CH2F, —CHF2, —CF3, —C2H5, —CH2OH, —CH2OMe, —CH2NH2, —CH2NHCH3, —CH2N(CH3)2, —CH2NHCOH, or —CH2NHCOCH3; or
RC and RD form together a carbocyclic ring selected from the group consisting of:
R38 and R39 are defined according to claim 1; and
L1 represents —CH2—, —C2H4—, —C3H6—, —C4H8—, —C5H10—, —C6H12—, —C7H14—, —C8H16—, —C9H18—, —C10H20—, —CH(CH3)—, —C[(CH3)2]—, —CH2—CH(CH3)—, —CH(CH3)—CH2—, —CH(CH3)—C2H4—, —CH2—CH(CH3)—CH2—, —C2H4—CH(CH3)—, —CH2—C[(CH3)2]—, —C[(CH3)2]—CH2—, —CH(CH3)—CH(CH3)—, —C[(C2H5)(CH3)]—, —CH(C3H7)—, —CH2CH2O—, —(CH2—CH2—O)n—CH2—CH2—, —C(CH3)═CH—C(CH3)═CH—, —CH(CH3)—C≡C—CH2—, —C2H4—CH═CH—CH═CH—, —CH2—CH═CH—CH2—CH═CH—, —C3H6—C≡C—CH2—, —CH2—CH═CH—CH═CH—CH2—, —CH═CH—CH═CH—C2H4—, —CH2—CH═CH—C(CH3)═CH—, —CH2—CH═C(CH3)—CH═CH—, —CH2—C(CH3)═CH—CH═CH—, —CH(CH3)—CH═CH—CH═CH—, —CH═CH—CH2—C(CH3)═CH—, —(C═O)NH—, —NH(C═O)—, —CH2(C═O)NH—, —(C═O)NHCH2—, —NH(C═O)CH2—, or —CH2NH(C═O)—,
wherein n is an integer from 1 to 10.

### Claim 3 (depends on 1)

The compound according to claim 1 of the general formula (VI):
wherein
XA represents —CH2—;
p is an integer of 0 or 1;
R11, R12, R13, RB, RC, RD, L1, L2 and L3 are defined according to claim 1,
wherein at least one of R11, R12, and R13 is not —H; and
“” represents a C═C bond or a C—C bond.

### Claim 4 (depends on 1)

The compound according to claim 1 selected from the group consisting of:
2-(3-((R)-3-(3,4-dimethoxyphenyl)-1-(((S)-1-((S)-2-(3,4,5-
trimethoxyphenyl)pent-4-enoyl)pyrrolidine-2-
carbonyl)oxy)propyl)phenoxy)acetic acid,
A09
(S)-(R)-3-(3,4-dimethoxyphenyl)-1-(3-(2-
morpholinoethoxy)phenyl)propyl-1-((S)-
3-cyclopropyl-2-(3,4,5-
trimethoxyphenyl)propanoyl)pyrrolidine-2-carboxylate,
A15
(S)-(R)-3 -(3,4-dimethoxyphenyl)-1-(3-(2-
morpholinoethoxy)phenyl)propyl-1-((S)-
2-((R)-cyclohex-2-en-1-yl)-2-(3,4,5-
trimethoxyphenyl)acetyl)pyrrolidine-2-carboxylate, and
A21
(S)-(R)-3-(3,4-dimethoxyphenyl)-1-(3-(2-
morpholinoethoxy)phenyl)propyl-1-
((S)-2-cyclohexyl-2-(3,4,5-
trimethoxyphenyl) acetyl)pyrrol-idine -2-carboxylate,

### Claim 5 (depends on 1)

A method for inhibiting a FK506-binding protein comprising contacting a cell with an effective amount of a compound according to claim 1.

### Claim 6 (depends on 1)

A method for treating a disease comprising administering a therapeutically effective amount of a compound according to claim 1 to a subject in need thereof, wherein the disease is selected from a psychiatric disorder, a neurological disorder, a metabolic disease, cancer, a glucocorticoid hyposensitivity syndrome, peripheral glucocorticoid resistance, an infectious disease, alopecia, abnormally elevated intraocular pressure, macular degeneration, oxidative damage to eye tissues, vision disorder, a sleeping disorder, asthma, diabetes, traumatic brain injury, nerve injury, Alzheimer's disease, Huntington's disease, Parkinson's disease, ischemia, and memory impairment.

### Claim 7 (depends on 6)

The method according to claim 6, wherein the psychiatric disease is an affective disorder or an anxiety disorder; wherein the metabolic disease is a localized adiposity, metabolic syndrome or obesity; wherein the cancer is prostate cancer, acute lymphoblastic leukaemia or melanoma; and wherein the infectious disease is selected from the group consisting of malaria and Legionnaires' disease.

### Claim 8 (depends on 1)

A pharmaceutical composition comprising at least one compound according to claim 1 together with at least one pharmaceutically acceptable carrier, solvent or excipient.

### Claim 9 (depends on 7)

The method according to claim 7, wherein the affective disorder is selected from the group consisting of: depression, bipolar disorder, mania, substance induced mood disorder and seasonal affective disorder (SAD); and wherein the anxiety disorder is selected from the group comprising or consisting of generalized anxiety disorder, panic disorder, panic disorder with agoraphobia, phobias, obsessive-compulsive disorder, post-traumatic stress disorder, separation anxiety and childhood anxiety disorders.

### Claim 10 (depends on 9)

The method according to claim 9, wherein the depression is selected from major depression or major depressive disorder.

### Claim 11 (depends on 1)

The compound according to claim 1, wherein L1 represents —C2H4—.

### Claim 12 (depends on 11)

The compound according to claim 11, wherein L2 and L3 represents a bond.

### Claim 13 (depends on 1)

The compound according to claim 1, wherein RA represents

### Claim 14 (depends on 1)

The compound according to claim 1, wherein RB represents
RC represents
and RD represents H.

### Claim 15 (depends on 1)

The compound according to claim 1, having the structure of Formula (IV):

### Claim 16 (depends on 15)

The compound according to claim 15, wherein R1, R2, R11, R12 and R13 each represents —OCH3.

### Claim 17 (depends on 16)

The compound according to claim 16, wherein R6 represents —OCH2—COOH or