申请人:Recordati, S. A., Chemical & Pharmaceutical Co.
公开号:US04482561A1
公开(公告)日:1984-11-13
The N-substituted-4-(optionally substituted)-2-, 3- or 4-piperidyl N-(7- or 8-substituted-4-quinolyl)-anthraniloyloxyalkanoates having the structural formula (I): ##STR1## in which R is a straight or branched chain alkyl radical having from 1 to 4 carbon atoms; an alkenyl or alkynyl radical having from 2 to 6 carbon atoms; a benzyl, phenethyl, 4-nitrophenethyl or 4-aminophenethyl radical; or a phenacyl, benzoylethyl, .beta.-hydroxyphenethyl or .alpha.-hydroxyphenylpropyl radical, optionally substituted on the phenyl ring by one or more halogen atom, trifluoromethyl, nitro or amino substituents, or an alkyl substituent having from 1 to 4 carbon atoms or an alkoxy substituent having from 1 to 4 carbon atoms; R.sub.1 is a hydrogen atom or a phenyl radical; each of R.sub.2 and R.sub.3 is independently a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms; one of R.sub.4 and R.sub.5 is a chlorine atom or a trifluoromethyl radical and the other of R.sub.4 and R.sub.5 is a hydrogen atom; and the pharmaceutically acceptable salts of such esters; are effective analgesics, anti-inflammatories and antidepressants; are also strong inhibitors of platelet aggregation, and thus too are useful in the treatment of cerebral thrombosis, cerebral and cardiac infarction, and arteriosclerotic disorders.
具有结构式(I)的N-取代-4-(可选择取代)-2、3或4-哌啶基N-(7-或8-取代-4-喹啉基)-蒽酰氧烷酸酯是有效的镇痛剂、抗炎药和抗抑郁药;它们还是强力的血小板聚集抑制剂,因此在治疗脑血栓形成、脑和心肌梗死以及动脉硬化性疾病方面也很有用。其中R是具有1到4个碳原子的直链或支链烷基基团;具有2到6个碳原子的烯基或炔基基团;苄基、苯乙基、4-硝基苯乙基或4-氨基苯乙基基团;或苯乙酰基、苯乙酰乙基、β-羟基苯乙基或α-羟基苯丙基基团,可选择在苯环上通过一个或多个卤素原子、三氟甲基、硝基或氨基取代基,或具有1到4个碳原子的烷基取代基或具有1到4个碳原子的烷氧基取代基;R.sub.1是氢原子或苯基基团;R.sub.2和R.sub.3中的每一个独立地是具有1到4个碳原子的烷基基团;R.sub.4和R.sub.5中的一个是氯原子或三氟甲基基团,另一个是氢原子;以及这些酯的药用盐。