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EP0226266A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Use of a tetrahydrocarbazolone derivative for the manufacture of medicaments

Assignee: Glaxo Group Ltd
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Filing: 1986-06-24
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Granted: —
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Expires: 2006-06-24
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Abstract

Abstract The invention relates to the use of compounds of the general formula (I) wherein R' 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 2 , R 3 and R 4 is a hydrogen atom or a C 1-3 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, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage in radiological examination procedures. The invention also relates to a product containing a therapeutic agent liable to induce nausea and vomiting, e.g. a cytostatic agent such as a cyclophosphamide, an alkylating agent or a platinum complex, and a compound of the general formula (1) as a combined preparation for simultaneous separate or sequential use in therapy.

Inventors

  • 👤 Michael Brian C/O Glaxo Research Limited Tyers
  • 👤 Ian Harold Coates
  • 👤 David Cedric Humber
  • 👤 George Blanch Ewan
  • 👤 James Angus Bell

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-09 21:04
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/415; A61P; A61P1/00; A61P1/08

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 127 words
Use of compounds of the general formula (I) wherein R 1 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 2 3 4 R , R3 and R4 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, for the manufacture of a medicament for the relief of nausea and vomiting and/or the promotion of gastric emptying.
Claim 2
Dependent Claim 127 words
Use of compounds of the general formula (I) wherein R 1 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 2 3 4 R , R3 and R4 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, for the manufacture of a medicament for the relief of nausea and vomiting and/or the promotion of gastric emptying.
Claim 3
Dependent Claim 18 words
Use according to claim 1 for the manufacture of a medicament for the relief of nausea and vomiting.
Claim 4
Dependent Claim 27 words
Use according to claim 1 for the manufacture of a medicament for the promotion of gastric emptying for the relief of gastro-intestinal disorders associated with gastric stasis.
Claim 5
Dependent Claim 21 words
Use according to claim 1 for the manufacture of a medicament for the promotion of gastric emptying in radiological examination procedures.
Claim 6
Dependent Claim 93 words
Use according to any of claims 1 to 3, wherein the compound is a compound of the formula (la) wherein R 1a represents a hydrogen atom or a methyl, ethyl, propyl, prop-2-yl, prop-2-enyl or cyclopentyl group; R 3a represents a hydrogen atom; and either R 2a represents a methyl, ethyl, propyl or prop-2-yl group and R4a represents a hydrogen atom or R 2 a represents a 4a hydrogen atom or R 2a represents a hydrogen atom and R 4a represents a methyl or ethyl group or a physiologically acceptable salt or solvate thereof.
Claim 7
Dependent Claim 24 words
6 . Use according to any of claims 1 to 4, wherein the compound is 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazcl-1-yl)methyl]-4H-carbazol-4-one or a physiologically acceptable salt or solvate thereof.
Claim 8
Dependent Claim 29 words
7 . Use according to any of claims 1 to 4, wherein the compound is selected from 1,2,3,9-tetrahydro-3-[(2-methyl-1H-imidazol-1-yl) methyl]-9-(prop-2-enyl)-4H-carbazol-4-one; 9-cyclopentyl-1,2,3,9-tetrahydro-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carbazol-4-one; 1,2,3,9-tetrahydro-3-[(2-methyl-1H-imidazol-1-yl) methyl]-9-(prop-2-yl)-4H-carbazol-4-one; and physiologically acceptable salts and solvates thereof.
Claim 9
Dependent Claim 43 words
8 . A product containing a therapeutic agent liable to induce nausea and vomiting and a compound of the general formula(I)as defined in any of claims 1 and 4 to 6 as a combined preparation for simultaneous, separate or sequential use in therapy.
Claim 10
Dependent Claim 36 words
A product containing a cytostatic agent and a compound of the general formula(I)as defined in any of claims 1 and 4 to 6 as a combined preparation for simultaneous, separate or sequential use in cytostatic therapy.
Claim 11
Dependent Claim 21 words
A product as claimed in claim 8 wherein the cytostatic agent is a cyclophosphamide, an alkylating agent or a platinum complex.
Claim 12
Dependent Claim 13 words
A product as claimed in claim 9 wherein the cytostatic agent is cisplatin.

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