BENZOSULPHONES WITH AN ANTAGONIST ACTIVITY OF CALCIUM.

摘要

A compound of Formula I, which has calcium channel blocking activity Formula I or a pharmaceutically acceptable salt thereof, where (a) R1, R2, R3, R4 and R5 are independently selected from the group consisting of H, OH, halogen, cyano, NO2, alkyl, C1-C8 alkoxy, (C1-C8) alkyl sulfonyl, carboalkoxy (C1-C4) alkyl (C1-C8) thio, difluoromethoxy, difluoromethylthio, trifluoromethyl, and oxadiazole (formed by R1 and R2); (b) R6 is selected from the group consisting of H, linear or branched C1-C5 alkyl, alkylamine, aryl, 3-piperidyl, N-substituted 3-piperidyl, and N-substituted 2-pyrrolidinylmethylene, wherein said substituted 3-piperidyl N and said N-substituted 2-pyrrolidinyl may be substituted with straight or branched C1-C5 alkyl or benzyl, and said alkyl substituent may be substituted with C1-C8 alkoxy, C2-C8 alkanoyloxy, phenylacetoxy, benzoyloxy, hydroxy, halogen , p-tosyloxy, mesyloxy, amino, carboalkoxy or NR¿R¿, where (i) R¿ and R¿ are independently selected from the group consisting of H, linear or branched C1-C8 alkyl, C3-C7 cycloalkyl, phenyl, benzyl , and phenethyl, or (ii) R¿ and R¿ together form a heterocyclic ring selected from the group consisting of piperidino, pyrrolidino, morpholino, thiomorpholino, piperazino, 2-thieno, 33-thiene, and an N-substituted derivative of said heterocyclic rings, said N-substituted derivative being substituted with H, at linear or branched C1-C8 chyl, benzyl, benzhydryl, phenyl and / or substituted phenyl (substituted with NO2, halogen, straight or branched C1-C8 alkyl, C1-C8 alkoxy and / or trifluoromethyl); and (c) R7 is selected from the group consisting of H, amino, alkyl, aryl, trifluoromethyl, alkoxymethyl, 2-thieno and 33 thieno.