1-acyl indazoles
AssigneeBeecham Group Limited
InventorFrancis D. King
Life of this patent
Estimating the term…
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.
Claims10
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.
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.
(endo-N-(9-Methyl-9-azabicyclo[3.3.1]nonan-3-yl)-1-acetylindazol-3-yl carboxamide.
Dependencies are inferred from the claim text.