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US 6,207,693 B1Granted
Benzamide derivatives having a vasopressin antagonistic activity
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsHiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Yuki Sawada, Teruo Oku
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Abstract
This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by general formula (I): wherein R1 is aryl optionally substituted with lower alkoxy, etc., R2 is lower alkyl, etc., R3 is hydrogen, etc., A is NH, etc., E is etc., X is —CH═CH—, —CH═N—, or S, and Y is a condensed heterocyclic group, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
Claims10
A compound of the formula:
- wherein
- R1 is aryl, substituted aryl, cyclo (lower) alkyl or substituted cyclo (lower) alkyl;
- R2 is hydrogen;
- lower alkyl optionally substituted with hydroxy, aryl or acyl;
- or cyclo (lower) alkyl;
- R3 is hydrogen;
- halogen;
- hydroxyl;
- acyloxy;
- substituted acyloxy;
- lower alkyl optionally substituted with hydroxy or lower alkoxy;
- lower alkoxy optionally substituted with aryl, amino, protected amino, acyl, hydroxy, cyano or lower alkylthio;
- nitro;
- amino;
- acyl;
- substituted acyl;
- or cyclo (lower) alkyloxy;
- A is a single bond or 0;
- E is lower alkylene or
- X is —CH═CH;
- —CH═N— or S and
- Y is benzimidazole or a substituted benzimidazole;
- or a pharmaceutically acceptable salt thereof.
20 more elements
Dependencies are inferred from the claim text.