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Claims for Patent: 4,753,789

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Claims for Patent: 4,753,789

Title: Method for treating nausea and vomiting
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 cycoalkyl-(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, 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 of 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 (I) as a combined preparation for simultaneous separate or sequential use in therapy.
Inventor(s): Tyers; Michael B. (Welwyn, GB2), Coates; Ian H. (Hertford, GB2), Humber; David C. (London, GB2), Ewan; George B. (Gerrards Cross, GB2), Bell; James A. (Royston, GB2)
Assignee: Glaxo Group Limited (GB2)
Application Number:06/877,805
Patent Claims: 1. A method of treatment for the relief of nausea and vomiting which comprises administering to a human or animal subject in need thereof an effective amount for treatment for the relief of nausea and vomiting of 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.

2. A method according to claim 1 wherein the 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one is in the form of its hydrochloride.

3. A method according to claim 1 wherein the 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one is in the form of its hydrochloride dihydrate.

4. A method according to claim 1 wherein said nausea and vomiting is induced by an anticancer drug.

5. A method according to claim 4 wherein the 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one is in the form of its hydrochloride dihydrate.

6. A method according to claim 4 wherein said anticancer drug is a cytostatic agent.

7. A method according to claim 6 wherein the 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one is in the form of its hydrochloride dihydrate.

8. A method according to claim 4 wherein said nausea and vomiting is induced by a platinum complex.

9. A method according to claim 8 wherein the 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one is in the form of its hydrochloride dihydrate.

10. A method according to claim 4 wherein said nausea and vomiting is induced by cisplatin.

11. A method according to claim 10 wherein the 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1)methyl]-4H-carbazol -4-one is in the form of its hydrochloride dihydrate.

12. A method according to claim 1 wherein said nausea and vomiting is induced by an alkylating agent.

13. A method according to claim 1 wherein said nausea and vomiting is induced by cyclophosphamide.

14. A method according to claim 12 wherein the 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one is in the form of its hydrochloride dihydrate.

15. A method according to claim 13 wherein the 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one is in the form of its hydrochloride dihydrate.

16. A method according to claim 1 wherein said nausea and vomiting is induced by radiation.

17. A method according to claim 16 wherein the 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carba zol-4-one is in the form of its hydrochloride dihydrate.
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