Benzamide platelet activating factor antagonists
AssigneeMitsubishi Kasei Corporation
InventorsAkihiro Yamamoto, Shuji Morita, Yoshio Hayashi, Noboru Yamada, Toshihito Kitamura
Life of this patent
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Abstract
Benzamide platelet activating factor antagonists of the following formula (I): ##STR1## wherein ##STR2## B, D: hydrogen atom, etc. E: pyridyl group, etc. n: integer from 0 to 2 R.sup.2 : R.sup.3 R.sup.4 N-- etc. (R.sup.3, R.sup.4 : optionally substituted C.sub.6 -C.sub.12 aryl group, etc.) ##STR3## optical antipodes thereof or pharmaceutically acceptable salts thereof, show excellent PAF antagonism and are effective for therapy and prophylaxis of diseases caused by PAF (bronchial asthma, nephritis, shocks, cardiac infarction, cerebral hemorrhage, ulcer, DIC, autoimmune diseases, thrombosis, etc.).
Claims8
A benzamide derivative of the following formula (I):
- ##STR305## wherein:
- R.sup.1 represents a group of the following formula (II) ##STR306## (in the above formula (II), n represents an integer from 0 to 2, B and D each independently represent hydrogen atom or C.sub.1 -C.sub.4 alkyl group, E represents pyridyl or N-oxypyridyl which is unsubstituted or substituted by a C.sub.1 -C.sub.4 alkyl group or a C.sub.1 -C.sub.4 alkoxy group),
- R.sup.2 represents C.sub.6 -C.sub.12 aryl group, C.sub.6 -C.sub.12 aryloxy group, C.sub.6 -C.sub.12 arylthio group, benzyloxy group or C.sub.7 -C.sub.13 arylcarbonyl group, which is unsubstituted or substituted, or a group of the following formula (III):
- R.sup.3 R.sup.4 N (III)
- (in the above formula (III), R.sup.3 represents C.sub.6 -C.sub.12 aryl group which is unsubstituted or substituted and R.sup.4 represents C.sub.6 -C.sub.12 aryl group which is unsubstituted or substituted, hydrogen atom, C.sub.1 -C.sub.4 alkyl group or C.sub.3 -C.sub.8 cycloalkyl group) or a group of the following formula (IV):
- R.sup.5 R.sup.6 CH (IV)
- (in the above formula (IV), R.sup.5 represents C.sub.6 -C.sub.12 aryl group which is unsubstituted or substituted, and R.sup.6 represents C.sub.6 -C.sub.12 aryl group which is unsubstituted or substituted, hydrogen atom, C.sub.1 -C.sub.4 alkyl group or C.sub.3 -C.sub.8 cycloalkyl group), and
- A represents --CO--or --CH.sub.2 and
- optical antipodes thereof or pharmacologically acceptable salts thereof.
Dependencies are inferred from the claim text.