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US 2009/0275628 A1Published application
Substituted Spiro-Compounds And The Use Thereof For Producing Medicaments
AssigneeGruenenthal GmbH
InventorsRobert Frank, Ruth Jostock, Melanie Reich, Gregor Bahrenberg, Hans Schick, Helmut Sonnenschein
Life of this patent
Estimating the term…
Abstract
The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.
Claims26
1-25. (canceled)
A substituted spiro compound corresponding to formula I
- wherein
- n is 0, 1 or 2;
- and
- I.)
- R1 denotes:
- a linear or branched, saturated or unsaturated, unsubstituted or mono- or polysubstituted aliphatic group optionally containing one or more heteroatoms as chain members;
- or
- an unsubstituted or mono- or polysubstituted, unsaturated or saturated cycloaliphatic group which optionally contains one or more heteroatoms as ring members, and which optionally may be bound via a linear or branched, unsubstituted or mono- or polysubstituted alkylene, alkenylene or alkinylene group optionally containing one or more heteroatoms as chain members, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- or
- an unsubstituted or mono- or polysubstituted aryl or heteroaryl group which optionally may be bound via a linear or branched, unsubstituted or mono- or polysubstituted alkylene, alkenylene or alkinylene group optionally containing one or more heteroatoms as chain members, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- or
- a —C(═O)—NR11R12 group;
- and
- R2, R3, R4, R5, R6, R7 and R8 each independently denote hydrogen, or
- a linear or branched, saturated or unsaturated, unsubstituted or mono- or polysubstituted aliphatic group optionally containing one or more heteroatoms as chain members;
- or
- II.)
- R1 and R3 together denote a —(CH2)p— group, wherein p is 3, 4, 5 or 6;
- and
- R2, R4, R5, R6, R7 and R8 each independently denote hydrogen, or
- a linear or branched, saturated or unsaturated, unsubstituted or mono- or polysubstituted aliphatic group optionally containing one or more heteroatoms as chain members;
- or
- III.)
- R1, R2, R7 and R8 each denote hydrogen, and
- R3, R4, R5 and R6 each independently denote a linear or branched, saturated or unsaturated, unsubstituted or mono- or polysubstituted aliphatic group optionally containing one or more heteroatoms as chain members;
- and
- R9 denotes hydrogen, or
- a linear or branched, saturated or unsaturated, unsubstituted or mono- or polysubstituted aliphatic group optionally containing one or more heteroatoms as chain members;
- or
- an unsubstituted or mono- or polysubstituted, unsaturated or saturated cycloaliphatic group which optionally contains one or more heteroatoms as ring members, and which optionally may be bound via a linear or branched, unsubstituted or mono- or polysubstituted alkylene, alkenylene or alkinylene group optionally containing one or more heteroatoms as chain members, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- or
- an unsubstituted or mono- or polysubstituted aryl or heteroaryl group which optionally may be bound via a linear or branched, unsubstituted or mono- or polysubstituted alkylene, alkenylene or alkinylene group optionally containing one or more heteroatoms as chain members, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- R10 denotes:
- a linear or branched, saturated or unsaturated, unsubstituted or mono- or polysubstituted aliphatic group optionally containing one or more heteroatoms as chain members;
- or
- an unsubstituted or mono- or polysubstituted, unsaturated or saturated cycloaliphatic group which optionally contains at least one heteroatom as a ring member, and which optionally may be bound via a linear or branched, unsubstituted alkylene, alkenylene or alkinylene group, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- or
- an unsubstituted or mono- or polysubstituted phenyl group, with the proviso that either of the two meta positions and the para position of said phenyl group are not both substituted with substituents which are bound to the phenyl group via identical atoms selected from the group consisting of oxygen, sulfur and nitrogen;
- or
- an unsubstituted or mono- or polysubstituted group selected from the group consisting of naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyranyl, pyridinyl, imidazolyl, indolyl, isoindolyl, benzo[b]furanyl, benzo[b]thiophenyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, quinazolinyl, quinoxalinyl, quinolinyl, isoquinolinyl, benzimidazolyl, benzoxazolyl, benzotriazolyl, benzisoxazolyl, [1,2,3,4]-tetrahydronaphthyl, [1,2,3,4]-tetrahydroquinolinyl, [1,2,3,4]-tetrahydroisoquinolinyl, [1,2,3,4]-tetrahydroquinazolinyl;
- 2H-benzo[1.4]oxazin-3(4H)-onyl, (3,4)-dihydroquinolin-2(1H)-onyl, [3,4]-dihydro-2H-1,4-benzoxazinyl and benzothiazolyl;
- or
- an unsubstituted or mono- or polysubstituted aryl or heteroaryl group which is bound via a —(CH2)—, —(CH2)2— or —(CH2)3 group, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- or
- a —C(═O)—NR13R14 group;
- R11 and R13 each independently denote:
- a linear or branched, saturated or unsaturated, unsubstituted or mono- or polysubstituted aliphatic group;
- or
- an unsubstituted or mono- or polysubstituted, unsaturated or saturated cycloaliphatic group which optionally contains one or more heteroatoms as ring members, and which optionally may be bound via a —(CH2)w— group, wherein w is 1, 2, 3, 4 or 5, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- or
- an unsubstituted or mono- or polysubstituted aryl or heteroaryl group which optionally may be bound via a —(CH2)—, —(CH2)2— or —(CH2)3 group, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- R12 and R14 each independently denote hydrogen, or
- a linear or branched, saturated or unsaturated, unsubstituted or mono- or polysubstituted aliphatic group;
- an unsubstituted or mono- or polysubstituted, unsaturated or saturated cycloaliphatic group which optionally contains one or more heteroatoms as ring members, and which optionally may be bound via a linear or branched, unsubstituted or mono- or polysubstituted alkylene, alkenylene or alkinylene group optionally containing one or more heteroatoms as chain members, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- or
- or an unsubstituted or mono- or polysubstituted aryl or heteroaryl group which optionally may be bound via a —(CH2)— group, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- or
- R11 and R12, or R13 and R14, respectively, together with the nitrogen atom to which they are bound form an unsubstituted or mono- or polysubstituted, unsaturated or saturated heterocycloaliphatic ring which optionally contains one or more further heteroatoms as rign members, and which optionally may be condensed with an unsubstituted or mono- or polysubstituted mono- or polycyclic ring system;
- wherein
- substituents of the above-mentioned heterocycloaliphatic group formed by R11 and R12, or by R13 and R14, are independently selected from the group consisting of oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF3, —SF5, —OH, —O—C1-5 alkyl, —NH2, —NO2, —O—CF3, —S—CF3, —SH, —S—C1-5 alkyl, —C1-5 alkyl, —O—C(═O)—C1-5 alkyl, —NH—C1-5 alkyl, —N(C1-5 alkyl)2, —NH—C(═O)—O—C1-5 alkyl, —C(═O)—NH2, —C(═O)—NH—C1-5 alkyl, —C(═O)—N—(C1-5 alkyl)2, cyclohexyl, cyclopentyl, pyridinyl, pyridazinyl, pyrimidinyl, [1,2,5]-thiadiazolyl, thiazolyl, —(CH2)-benzo[b]furanyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein the cyclic portion of a pyrimidinyl, [1,2,5]-thiadiazolyl, thiazolyl, pyridinyl, cyclopentyl, cyclohexyl, pyridazinyl, —O-phenyl, —O-benzyl, phenyl, —(CH2)-benzo[b]furanyl and benzyl group optionally may be substituted with substituents independently selected from the group consisting of F, Cl, Br, —OH, —CF3, —SF5, —CN, —NO2, —C1-5 alkyl, —O—C1-5 alkyl, —O—CF3, —S—CF3, phenyl and —O-benzyl;
- and
- substituents of the above-mentioned aliphatic groups are independently selected from the group consisting of F, Cl, Br, I, —CN, —NO2, —OH, —SH and —NH2;
- or a salt or solvate thereof.
60 more elements
A method of treating or inhibiting a disorder or disease state selected from the group consisting of pain, arthralgia;
- migraine;
- depression;
- neuropathy;
- nerve injuries;
- neurodegenerative diseases;
- cognitive dysfunctions;
- epilepsy;
- respiratory diseases;
- coughing;
- urinary incontinence;
- overactive bladder;
- stomach ulcers;
- irritable bowel syndrome;
- strokes;
- irritations of the eyes;
- irritations of the skin;
- neurotic skin diseases;
- inflammatory diseases;
- diarrhea;
- pruritus;
- eating disorders;
- medication drug or alcohol dependency or addiction;
- medication, drug or alcohol abuse;
- withdrawal symptoms in medication, drug or alcohol dependency;
- development of tolerance to medication;
- or for diuresis;
- antinatriuresis;
- influencing the cardiovascular system;
- increasing vigilance;
- increasing libido;
- modulating motor activity;
- anxiolysis;
- local anaesthesia;
- or inhibiting undesirable side effects triggered by administration of vanilloid receptor 1 agonists in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a compound corresponding to formula I according to claim 1.
31 more elements
Dependencies are inferred from the claim text.