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Details for Patent: 4,937,247

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Details for Patent: 4,937,247

Title: 1-acyl indazoles
Abstract:Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CH or N; Y is NH or O; R.sub.1 is hydrogen or halogen; R.sub.2 is a group of formula (a), (b) or (c) ##STR2## wherein n is 2 or 3; p and q are independently 1 to 3; and R.sub.4 or R.sub.5 is C.sub.1-4 alkyl; R.sub.3 i s C.sub.1-10 acyl, C.sub.1-6 alkoxycarbonyl, optionally substituted phenoxycarbonyl or benzyloxycarbonyl, or R.sub.6 R.sub.7 NCO or R.sub.6 R.sub.7 NS(O).sub.m wherein m is 1 or 2 and R.sub.6 and R.sub.7 are independently C.sub.1-6 alkyl groups or together are C.sub.4-6 polymethylene; having 5-HT.sub.3 antagonist activity, a process for their preparation and their use as pharmaceuticals.
Inventor(s): King; Francis D. (Harlow, GB2)
Assignee: Beecham Group p.l.c. (Brentford, GB2)
Filing Date:Sep 25, 1987
Application Number:07/101,081
Claims:1. A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR14## wherein X is N;

Y is NH;

R.sub.1 is hydrogen or halogen;

R.sub.2 is a group of formula (a) ##STR15## wherein n is 2 or 3; R.sub.4 is C.sub.1-4 alkyl; and

R.sub.3 is C.sub.1-10 acyl, C.sub.1-6 alkoxycarbonyl, optionally substituted phenoxycarbonyl or benzyloxycarbonyl, wherein the substituents are selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro or C.sub.1-6 alkylsulphonyl, or R.sub.6 R.sub.7 NCO or R.sub.6 R.sub.7 NS(O).sub.m wherein m is 1 or 2 and R.sub.6 and R.sub.7 are independently C.sub.1-6 alkyl groups or together are C.sub.4-6 polymethylene.

2. A compound according to claim 1 wherein R.sub.1 is hydrogen or 5-fluoro and R.sub.4 is methyl.

3. A compound according to claim 1 wherein R.sub.3 is acetyl or benzoyl.

4. A compound selected from (endo)-N-(9-methyl-9azabicyclo[3.3.1]nonan-3-yl)-1-acetylindazol-3-yl carboxamide; (endo)-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1-benzoylindazol-3-yl carboxamide or a pharmaceutically acceptable salt thereof.

5. (endo-N-(9-Methyl-9-azabicyclo[3.3.1]nonan-3-yl)-1-acetylindazol-3-yl carboxamide.

6. A compound according to claim 1 wherein the CO--Y-- linkage is in the endo configuration with respect to R.sub.2.

7. A pharmaceutical composition for use in the treatment of migraine, cluster headache or trigeminal neuralgia, comprising an effective amount of a compound according to claim 1, and a pharmaceutically acceptable carrier.

8. A pharmaceutical composition for use in the treatment of emesis or irritable bowel syndrome, comprising an effective amount of a compound according to claim 1, and a pharmaceutically acceptable carrier.

9. A method of treatment of migraine, cluster headache or trigeminal neuralgia in a mammal, which comprises the administration to a mammal in need thereof of an effective amount of a compound according to claim 1.

10. A method of treatment of emesis or irritable bowel syndrome in a mammal, which comprises the administration to a mammal in need thereof of an effective amount of a compound according to claim 1.
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