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1. 发明申请

WO1997012869A1 CARBOSTYRIL DERIVATIVES AS ANTITHROMBOTIC AGENTS 审中-公开
标题翻译： CARBOSTYRIL衍生物作为抗生素代谢物
公开(公告)号：WO1997012869A1
公开(公告)日：1997-04-10
申请号：PCT/JP1996002892
申请日：1996-10-04
申请人： OTSUKA PHARMACEUTICAL COMPANY, LIMITED , KOGA, Yasuo , KIHARA, Yoshito , OKADA, Minoru , NISHI, Takao , INOUE, Yoshihiro , KIMURA, Yukio , HIDAKA, Hiroyoshi , FUKUDA, Norio
发明人： OTSUKA PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07D215/22
CPC分类号： C07D215/227
摘要： A carbostyril derivative of formula (1), wherein A is lower alkylene, R is H, halogen or lower alkoxy, R and R are each lower alkyl being optionally substituted by OH, lower alkoxy, phenyl-lower alkoxy or lower alkanoyloxy; cycloalkyl being optionally substituted by OH, hydroxy-lower alkoxy or lower alkanoyloxy; or amino being optionally substituted by lower alkyl or cycloalkyl, R is H, lower alkyl, lower alkenyl or hydroxy-lower alkyl, and the bond between 3- and 4-positions of the carbostyril nucleus is single or double, provided that when R and R are H, R and R should not be either unsubstituted lower alkyl or unsubstituted cycloalkyl, or a salt thereof, which shows antithrombotic activities, intima thickening inhibitory activity, the platelet mass dissociating activity and increasing activity of the blood flow in the brain and the peripheral vessel, and hence, is useful as medicines in the prophylaxis or treatment of various ischemic diseases.
摘要翻译：式（1）的喹诺酮衍生物，其中A为低级亚烷基，R为H，卤素或低级烷氧基，R 1和R 2各自为低级烷基，任选被OH，低级烷氧基，苯基 - 低级烷氧基或低级烷酰氧基; 任选被OH，羟基 - 低级烷氧基或低级烷酰氧基取代的环烷基; 或任选被低级烷基或环烷基取代的氨基，R 3是H，低级烷基，低级烯基或羟基 - 低级烷基，并且喹诺酮核的3-和4-位之间的键是单或双，条件是当R和R 3为H时，R 1和R 2不应为未经取代的低级烷基或未取代的环烷基或其盐，其显示抗血栓形成活性，内膜增厚抑制活性，血小板质量离解活性并且增加脑和外周血管中的血流的活性，因此可用作预防或治疗各种缺血性疾病的药物。

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