Benzamide derivatives and their use as vasopressin antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 295/185 (2006.01) A61K 31/16 (2006.01) A61K 31/215 (2006.01) A61K 31/27 (2006.01) A61K 31/275 (2006.01) A61K 31/33 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) C07C 235/42 (2006.01) C07C 237/42 (2006.01) C07C 237/44 (2006.01) C07C 243/28 (2006.01) C07C 255/54 (2006.01) C07C 271/16 (2006.01) C07C 271/22 (2006.01) C07C 271/48 (2006.01) C07C 275/16 (2006.01) C07C 279/08 (2006.01) C07C 279/24 (2006.01) C07D 207/34 (2006.01) C07D 209/48 (2006.01) C07D 211/16 (2006.01) C07D 211/46 (2006.01) C07D 211/

Patent

CA 2223869

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., R4 is lower alkoxy, etc., R5 is hydrogen, etc., A is NH, etc., E is (a), etc., X is -CH=CH-, -CH=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.

La présente invention concerne d'une part des dérivés de type benzamide présentant notamment une activité antagoniste de la vasopressine et d'autre part des sels de ces dérivés admis en pharmacologie. L'invention concerne également des procédés de préparation de ces dérivés ou sels ainsi que des compositions à base de ces dérivés ou sels. Ces dérivés sont représentés par la formule générale (I) dans laquelle R?1¿ est aryle à substitution alcoxy inférieur éventuelle, R?2¿ est alkyle inférieur, R?3¿ est alcoxy inférieur, R?5¿ est hydrogène, A est NH, E est (a), X est -CH=CH-, -CH=N- ou S, et Y est CH ou N.

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