Carbazole derivatives and their use as 5HT-induced antagonists

The invention relates to compounds of the general formula (I): (I) wherein R1 represents a hydrogen atom or a C1-10 alkyl, C3-7 cycloalkyl, C3-7cycloalkyl-(C1-4)-alkyl, C3-6 alkenyl, C3-10 alkynyl, phenyl or phenyl-(C1-3)alkyl group; one of the groups represented by R2, R3 and R4 is a hydrogen atom...

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Hauptverfasser: BELL, JAMES A, COATES, IAN H, EWAN, GEORGE B, HUMBER, DAVID C
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creator BELL
JAMES A
COATES
IAN H
EWAN
GEORGE B
HUMBER
DAVID C
description The invention relates to compounds of the general formula (I): (I) wherein R1 represents a hydrogen atom or a C1-10 alkyl, C3-7 cycloalkyl, C3-7cycloalkyl-(C1-4)-alkyl, C3-6 alkenyl, C3-10 alkynyl, phenyl or phenyl-(C1-3)alkyl group; one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl or phenyl-(C1-3)alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C1-6 alkyl group; and X represents a halogen atom or a hydroxy, C1-4 alkoxy, phenyl-(C1-3)-alkoxy or C1-6 alkyl group or a group NR5R6 or CONR5R6 wherein R5 and R6, which may be the same or different, each represents a hydrogen atom or a C1-4 alkyl or C3-4 alkenyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring; and physiologically acceptable salts and solvates thereof. The compounds are potent and selective antagonists of "neuronal" 5-hydroxytryptamine receptors and are useful in the treatment of psychotic disorders (e.g. schizophrenia and mania;); anxiety, pain; gastric stasis; symptoms of gastrointestinal dysfunction such as occur with dyspepsia, peptic ulcer, reflux oesophagitis and flatulence; migraine; and nausea and vomiting.
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Carbazole derivatives and their use as 5HT-induced antagonists
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