Benzamide derivatives and their use as vasopressin antagonists
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsHiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Abstract
This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc., R.sup.3 is hydrogen, etc., R.sup.4 is lower alkoxy, etc., R.sup.5 is hydrogen, etc., A is NH, etc., E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, and Y is CH or N, and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
Claims6
A compound of the formula:
- ##STR11## wherein R.sup.1 is aryl which is substituted with alkoxy optionally substituted with acyl, substituted acyl, acylamino or substituted acylamino;
- R.sup.2 is hydrogen;
- lower alkyl optionally substituted with hydroxy, aryl or acyl;
- or cyclo(lower)alkyl;
- R.sup.3 is hydrogen;
- halogen;
- hydroxy;
- 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;
- R.sup.4 is lower alkoxy optionally substituted with hydroxy, aryl, substituted aryl, acyl, substituted acyl, amino, lower alkylamino, acylamino, substituted acylamino, protected amino, a heterocyclic group or guanidino;
- R.sup.5 is hydrogen, lower alkyl, lower alkoxy or halogen;
- A is NH;
- E is ##STR12## X is --CH.dbd.CH--;
- and Y is CH;
- and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.