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Details for Patent: 5,578,632

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Details for Patent: 5,578,632

Title: Medicaments for the treatment of gastrointestinal dysfunction
Abstract:The invention relates to the use of compounds of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group; and one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-C.sub.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.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof in combination with ranitidine, for the treatment of gastrointestinal dysfunction including the relief of nausea and vomiting, the promotion of gastric emptying, and the treatment of dyspepsia, reflux oesophagitis, flatulence, peptic ulcer, and gastric stasis.
Inventor(s): Tyers; Michael B. (Welwyn, GB2)
Assignee: Glaxo Group Limited (London, GB)
Filing Date:Jun 07, 1995
Application Number:08/483,162
Claims:1. A method of treatment of gastrointestinal dysfunction which comprises administering to a human or animal subject an effective amount of a compound of formula (l) ##STR4## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group;

and one of the groups represented by

R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-C.sub.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.sub.1-6 alkyl group;

or a physiologically acceptable salt or solvate thereof, in combination with ranitidine.

2. A method according to claim 1 wherein the compound of formula (l) is 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one or a physiologically acceptable salt or solvate thereof.

3. A method according to claim 2 in which said 1,2,3,9-tetrahydro-9-methyl-3-[2-methyl-1H-imidazol-1-yl)methyl]-4H-carbaz ol-4-one is used in the form of a hydrochloride salt.

4. A method according to claim 2 in which said 1,2,3,9-tetrahydro-9-methyl-3-[2-methyl-1H-imidazol-1-yl)methyl]-4H-carbaz ol-4-one is used in the form of the hydrochloride dihydrate.

5. A method according to claim 1 for the treatment of dyspepsia, reflux oesophagitis, flatulence, peptic ulcer and gastric stasis.

6. A method according to claim 1 for the treatment of nausea and vomiting.

7. A pharmaceutical composition comprising a compound of formula (l) ##STR5## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group;

and one of the groups represented by

R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-C.sub.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.sub.1-6 alkyl group;

or a physiologically acceptable salt or solvate thereof, in combination with ranitidine.

8. A pharmaceutical composition according to claim 7 wherein the compound of formula (l) is 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one or a physiologically acceptable salt or solvate thereof.

9. A pharmaceutical composition according to claim 8 in which said 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one is used in the form of a hydrochloride salt.

10. A pharmaceutical composition according to claim 8 in which said 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one is used in the form of the hydrochloride dihydrate.
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