申请人:WARNER-LAMBERT COMPANY
公开号:EP0037231A2
公开(公告)日:1981-10-07
Octahydro-1-(w-mercaptoalkanoyl)-1H-indole-2-carboxylic acid compounds having the formula
wherein R is hydrogen or lower alkyl; R1 is hydrogen, lower 0 alkyl, or benzyl; R2 is hydrogen or R3-C- where R3 is lower alkyl, heteroaryl containing 4 to 9 carbon atoms and one or two nitrogen, oxygen or sulfur atoms; phenyl, substituted phenyl having 1 or 2 substituents selected from the group consisting of fluorine, chlorine, bromine, lower alkyl or alkoxy; and n is 0 or 1; wherein lower alkyl and lower alkoxy include straight or branched groups containing 1 to 4 carbon atoms, and pharmaceutically acceptable salts of the compounds when R is hydrogen and when R3 is heteroaryl containing 1 or 2 nitrogen atoms, are disclosed. Also disclosed are substituted acyl compounds of octahydro-lH-indole-2-carboxylic acid having the formula
wherein R4 is hydrogen or lower alkyl; R5 is hydrogen, lower alkyl or benzyl; R6 is hydrogen or lower alkyl; Ar is phenyl or phenyl substituted with 1 or 2 substituents selected from the group consisting of fluorine, chlorine, bromine, lower alkyl, lower alkoxy, hydroxy or amino; and m is 0 to 3; wherein lower alkyl and lower alkoxy contain 1 to 4 straight or branched carbon atoms; and the pharmaceutically acceptable salts thereof. The compounds and the salts are useful for treating hypertension.
八氢-1-(w-巯基烷酰基)-1H-吲哚-2-羧酸化合物,其式为
其中 R 是氢或低级烷基;R1 是氢、低级 0 烷基或苄基;R2 是氢或 R3-C-,其中 R3 是低级烷基、含 4 至 9 个碳原子和 1 或 2 个氮、氧或硫原子的杂芳基;苯基、具有 1 或 2 个取代基的取代苯基,取代基选自由氟、氯、溴、低级烷基或烷氧基组成的组;和 n 为 0 或 1;其中低级烷基和低级烷氧基包括含有 1 至 4 个碳原子的直链或支链基团,当 R 为氢和 R3 为含有 1 或 2 个氮原子的杂芳基时,公开了这些化合物的药学上可接受的盐。还公开了八氢-lH-吲哚-2-羧酸的取代酰基化合物,其式为
其中 R4 是氢或低级烷基;R5 是氢、低级烷基或苄基;R6 是氢或低级烷基;Ar 是苯基或被 1 或 2 个选自氟、氯、溴、低级烷基、低级烷氧基、羟基或氨基的取代基取代的苯基;m 是 0 至 3;其中低级烷基和低级烷氧基含有 1 至 4 个直链或支链碳原子;及其药学上可接受的盐。这些化合物及其盐类可用于治疗高血压。