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EP0229444A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Medicaments for the treatment of anxiety

Assignee: Glaxo Group Ltd
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Filing: 1986-07-23
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Granted: —
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Expires: 2006-07-23
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Abstract

Abstract The invention relates to the use of compounds which act as 5-hydroxytryptamine (5-HT) antagonists at 5-HT "M" receptors in the treatment of anxiety.

Inventors

  • 👤 Michael Brian Tyers

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-09 21:30
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/46; A61K31/40; A61K31/44; A61K31/445; A61K31/55; A61P; A61P25/00; A61P25/20; A61P43/00

Claims Analysis

Total Claims: 13
Claim 1
Independent Claim 131 words
Use of compounds which act as antagonists of 5-hydroxytryptamine (5-HT) at 5-HT "M" receptors for the manufacture of a medicament for the treatment of anxiety, excluding tetrahydrocarbazolone derivatives of the general formula (I) wherein R a represents a hydrogen atom or a C 1-10 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl-(C 1-4 )alkyl, C 3-6 alkenyl, C 3-10 alkynyl, phenyl or phenyl-(C 1-3 )alkyl group, and one of the groups represented by R b , R c and R d is a hydrogen atom or a C 1-6 alkyl, C 3-7 cycloalkyl, C 2-6 alkenyl or phenyl-(C 1-3 )alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C 1-6 alkyl group; and physiologically acceptable salts and solvates thereof.
Claim 2
Dependent Claim 131 words
Use of compounds which act as antagonists of 5-hydroxytryptamine (5-HT) at 5-HT "M" receptors for the manufacture of a medicament for the treatment of anxiety, excluding tetrahydrocarbazolone derivatives of the general formula (I) wherein R a represents a hydrogen atom or a C 1-10 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl-(C 1-4 )alkyl, C 3-6 alkenyl, C 3-10 alkynyl, phenyl or phenyl-(C 1-3 )alkyl group, and one of the groups represented by R b , R c and R d is a hydrogen atom or a C 1-6 alkyl, C 3-7 cycloalkyl, C 2-6 alkenyl or phenyl-(C 1-3 )alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C 1-6 alkyl group; and physiologically acceptable salts and solvates thereof.
Claim 3
Dependent Claim 28 words
Use according to claim 1 wherein the compound which acts as an antagonist of 5-HT at 5-HT "M" receptors is an azabicyclo derivative or a benzoic acid derivative.
Claim 4
Dependent Claim 23 words
Use according to claim 2 wherein the azabicyclo derivative contains a bridged piperidyl group such as a tropyl, pseudotropyl, homotropyl or quinuclidinyl group.
Claim 5
Dependent Claim 16 words
Use according to claim 2 wherein the benzoic acid derivative is a benzoate or benzamide derivative.
Claim 6
Dependent Claim 114 words
Use according to claim 1 wherein the compound which acts as an antagonist of 5-HT at 5-HT "M" receptors is a compound of formula (II) wherein R 1 and R 2 independently represent hydrogen, halogen, C 1-4 alkoxy, hydroxy, amino, C 1-4 alkylamino, di(C 1-4 ) alkylamino, mercapto or C 1-4 alkylthio; R 3 represents hydrogen, C 1-4 alkyl, C 3-5 alkenyl, aryl or aralkyl; , R 4 represents hydrogen, C 1-7 alkyl, C 3-5 alkenyl or aralkyl; n is 2 or 3; the free valence is attached to either fused ring and the azabicyclic ring is in either the exo or endo configuration or an acid addition salt or quaternary ammonium salt thereof.
Claim 7
Dependent Claim 58 words
Use according to claim 5 wherein R 1 and R 2 independently represent hydrogen, halogen or C 1-4 alkyl, R 3 is hydrogen or C 1-4 alkyl, R 4 is hydrogen, C 1-7 alkyl or aralkyl, the carbonyl group is attached to the 3- position of the indole ring and the azabicyclic ring is in the endo configuration.
Claim 8
Dependent Claim 110 words
Use according to claim 1 wherein the compound which acts as an antagonist of 5-HT at 5-HT "M" receptors is a compound of formula (III) wherein R 5 represents C 1-4 alkyl, C 1-4 alkoxy or halogen; and R 6 and R 7 independently represent hydrogen, C 1-4 alkyl, C 1-4 alkoxy or halogen; provided that (a) when the azabicyclo ring is in the endo configuration and R 7 is hydrogen then R 6 is hydrogen or R 5 and R 6 are both alkyl, and (b) when the azabicyclic ring is in the exo configuration R 5 is a C 1-4 alkyl group; or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim 14 words
Use according to claim 7 wherein the azabicyclo ring is in the endo configuration.
Claim 10
Dependent Claim 94 words
Use according to claim 1 wherein the compound which acts as an antagonist of 5-HT at 5-HT "M" receptors is a compound of formula (IV) wherein R 8 represents C 1-4 alkyl; R 9 represents C 1-4 alkyl, C 1-4 alkoxy or halogen; and p is zero or an integer from 1 to 5; provided that when p is 2 the groups represented by Rg can be the same or different and when p is 3, 4 or 5 the groups represented by R 9 are the same; or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim 168 words
Use according to claim 1 wherein the compound which acts as an antagonist of 5-HT at 5-HT "M" receptors is a compound of formula (V) wherein R 10 represents a C 1-6 alkoxy or amino N-substituted by one or two groups selected from C 1-6 alkyl or C 3-8 cycloalkyl or optionally N-substituted by C 4-5 polymethylene; one of R 11 , R 12 and R13 is hydrogen and the other two are independently selected from hydrogen, chloro, bromo, trifluoromethyl, hydroxy, C 1-6 alkoxy, C 1-6 alkylthio, C 1-6 alkyl and amino; one of R 14 and R 15 represents hydrogen, C 1-6 alkyl, phenyl, or phenylC 1-3 alkyl, which phenyl moieties may be substituted by C 1-6 alkyl, C 1-6 alkoxy, CF 3 or halogen, and the other of R 14 and R 15 is hydrogen or C 1-6 alkyl; q is zero or an integer from 1 to 4; r is zero, or an integer from 1 to 3; and s is zero, 1 or 2.
Claim 12
Dependent Claim 54 words
Use according to claim 10 wherein R1 0 is methoxy, R 11 is hydrogen, R 12 is 4-amino, R 13 is 5-chloro (relative to the benzamide group), R 14 and R 15 independently represent hydrogen or C 1-6 alkyl; q is zero, r is 1 or 2 and s is zero, 1 or 2.
Claim 13
Dependent Claim 29 words
Use according to claim 1 wherein the compound which acts as an antagonist of 5-HT at 5-HT "M" receptors is selected from: 1αH,3α,5αH-tropan-3-yl-3,5-dichlorobenzoate; 1αH,3α,5αH-tropan-3-yl-3,5-dimethylbenzoate; (3α-tropanyl)-1H-indole-3-carboxylic acid ester; and (±)-endo-4-amino-5-chloro-2-methoxy-N-(1-azabicyclo-[3.3.3]-non-4-yl)benzamide.

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