申请人:Otsuka Pharmaceutical Co., Ltd.
公开号:US05227381A1
公开(公告)日:1993-07-13
Carbostyril compounds or salts thereof of the formula ##STR1## wherein A is a C.sub.1 -C.sub.6 alkylene group; R.sup.1 is a C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl group which may have, as a substituent, a group selected from the group consisting of C.sub.1 -C.sub.6 alkoxycarbonyl groups, a carboxy group, C.sub.2 -C.sub.6 alkanoyloxy-C.sub.1 -C.sub.6 alkyl groups, amino-C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkylamino-C.sub.1 -C.sub.6 alkyl groups and hydroxy-C.sub.1 -C.sub.6 alkyl groups, a C.sub.3 -C.sub.8 cycloalkyl group, a tetrahydropyranyl-C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.3 alkylenedioxy group-substituted C.sub.1 -C.sub.6 alkyl group, a phenyl-C.sub.1 -C.sub.6 alkyl group having, as a substituent on the phenyl ring, 1 to 3 groups selected from the group consisting of C.sub.1 -C.sub.6 alkyl groups and a hydroxyl group, or a piperidinyl-C.sub.1 -C.sub.6 alkyl group having a C.sub.1 -C.sub.6 alkyl group as a substituent; R.sup.2 is a 5-membered or 6-membered saturated or unsaturated heterocyclic-C.sub.1 -C.sub.6 alkyl group, said heterocyclic being selected from the group consisting of pyrrolidinyl, morpholino, piperidinyl, thiomorpholino, imidazolyl, 1,2,4-triazolyl, furyl, piperazinyl, pyridyl, tetrahydropyranyl and 1,3-oxathiolranyl groups which may have, as a substituent thereon 1 to 3 groups selected from the group consisting of hydroxy-C.sub. 1 -C.sub.6 alkyl groups, C.sub.2 -C.sub.6 alkanoyloxy-C.sub.1 -C.sub.6 alkyl groups, a hydroxyl group, C.sub.1 -C.sub.6 alkyl groups, amino-C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkylamino-C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkoxy groups, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkoxy groups, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl groups, a thio group and C.sub.1 -C.sub.6 alkylamido groups; the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton being a single bond or a double bond and pharmaceutical compositions containing the compound as the active ingredient.
碳基喹啉化合物或其盐的化学式为##STR1##其中A为C.sub.1 -C.sub.6烷基链;R.sup.1为C.sub.3 -C.sub.8环烷基-C.sub.1 -C.sub.6烷基链,可能具有以下基团之一作为取代基:C.sub.1 -C.sub.6烷氧羰基,羧基,C.sub.2 -C.sub.6烷酰氧-C.sub.1 -C.sub.6烷基群,氨基-C.sub.1 -C.sub.6烷基群,C.sub.1 -C.sub.6烷基氨基-C.sub.1 -C.sub.6烷基群和羟基-C.sub.1 -C.sub.6烷基群,C.sub.3 -C.sub.8环烷基群,四氢吡喃基-C.sub.1 -C.sub.6烷基群,C.sub.1 -C.sub.3烷二氧基基团取代的C.sub.1 -C.sub.6烷基群,苯基-C.sub.1 -C.sub.6烷基群,在苯环上取代基为1至3个来自C.sub.1 -C.sub.6烷基群和羟基的基团,或者带有C.sub.1 -C.sub.6烷基群作为取代基的哌啶基-C.sub.1 -C.sub.6烷基群;R.sup.2为5-或6-成员饱和或不饱和杂环-C.sub.1 -C.sub.6烷基群,所述杂环选自吡咯啉基、吗啉基、哌啶基、硫代吗啉基、咪唑基、1,2,4-三唑基、呋基、哌嗪基、吡啶基、四氢吡喃基和1,3-氧硫杂环基团,可能具有以下基团之一作为取代基:羟基-C.sub.1 -C.sub.6烷基群,C.sub.2 -C.sub.6烷酰氧-C.sub.1 -C.sub.6烷基群,羟基,C.sub.1 -C.sub.6烷基群,氨基-C.sub.1 -C.sub.6烷基群,C.sub.1 -C.sub.6烷基氨基-C.sub.1 -C.sub.6烷基群,C.sub.1 -C.sub.6烷氧基群,C.sub.1 -C.sub.6烷氧-C.sub.1 -C.sub.6烷氧基群,C.sub.1 -C.sub.6烷氧-C.sub.1 -C.sub.6烷基群,硫基和C.sub.1 -C.sub.6烷基酰胺基团;在碳基喹啉骨架的3-位和4-位之间的碳-碳键为单键或双键,其中药物组合物含有该化合物作为活性成分。