申请人:Otsuka Pharmaceutical Co., Ltd.
公开号:US04298739A1
公开(公告)日:1981-11-03
Novel carbostyril derivatives having platelet aggregation inhibitory action, antiinflamatory action, antiulcer action, vasodilatory action and phosphodiesterase inhibitory action and are useful for preventing or curing thrombus, arteriosclerosis, hypertension, asthma and other like diseases, and also useful as an antiinflamatory or anti-ulcer agent, represented by the formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, phenyl-C.sub.1-4 alkyl-; R.sup.2 is hydrogen, a halogen atom, hydroxy, phenyl-C.sub.1-4 alkoxy; R.sup.3 is hydrogen, hydroxy, C.sub.1-4 alkyl; R.sup.4 is C.sub.3-8 cycloalkyl, substituted or unsubstituted phenyl, C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl, 2-(3,4-dimethoxyphenyl)-ethyl, R.sup.5 is hydrogen, C.sub.1-8 alkyl, C.sub.2-4 alkenyl, phenyl, C.sub.3-8 cycloalkyl, phenyl-C.sub.1-4 alkyl, C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl, m is an integer of 1 - 3, l and n which may be same or different, and are respectively 0 or an integer of 1 - 7 and the sum of l and n is not exceeding 7, the carbon-carbon bond at 3- and 4-positions in the carbostyril skelton is either single or double bond.
具有抗血小板聚集抑制作用、抗炎作用、抗溃疡作用、扩血管作用和磷酸二酯酶抑制作用的新型羧基吲哚衍生物,用于预防或治疗血栓、动脉硬化、高血压、哮喘等疾病,同时也可用作抗炎或抗溃疡剂,其结构式如下:其中R.sup.1为氢、C.sub.1-4烷基、C.sub.2-4烯基、苯基-C.sub.1-4烷基-;R.sup.2为氢、卤素原子、羟基、苯基-C.sub.1-4烷氧基;R.sup.3为氢、羟基、C.sub.1-4烷基;R.sup.4为C.sub.3-8环烷基、取代或未取代苯基、C.sub.3-8环烷基-C.sub.1-4烷基、2-(3,4-二甲氧基苯基)-乙基;R.sup.5为氢、C.sub.1-8烷基、C.sub.2-4烯基、苯基、C.sub.3-8环烷基、苯基-C.sub.1-4烷基、C.sub.3-8环烷基-C.sub.1-4烷基;m为1-3的整数,l和n可以相同也可以不同,分别为0或1-7的整数,且l和n的和不超过7,在羧基吲哚骨架的3-和4-位置的碳-碳键为单键或双键。