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    CARBOSTYRIL DERIVATIVES AS ANTITHROMBOTIC AGENTS
    2.
    发明申请
    CARBOSTYRIL DERIVATIVES AS ANTITHROMBOTIC AGENTS 审中-公开
    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

    Applicant: OTSUKA PHARMACEUTICAL COMPANY, LIMITED ,  KOGA, Yasuo ,  KIHARA, Yoshito ,  OKADA, Minoru ,  NISHI, Takao ,  INOUE, Yoshihiro ,  KIMURA, Yukio ,  HIDAKA, Hiroyoshi ,  FUKUDA, Norio

    Inventor： OTSUKA PHARMACEUTICAL COMPANY, LIMITED

    IPC: C07D215/22

    CPC classification number: C07D215/227

    Abstract: 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.

    Abstract translation: 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。

    CARBOSTYRIL DERIVATIVES
    5.
    发明申请
    CARBOSTYRIL DERIVATIVES 审中-公开
    卡波斯特灵衍生物

    公开(公告)号：WO1989010919A1

    公开(公告)日：1989-11-16

    申请号：PCT/JP1989000464

    申请日：1989-05-02

    Applicant: OTSUKA PHARMACEUTICAL CO., LTD. ,  NISHI, Takao ,  KOMATSU, Makoto ,  KOGA, Yasuo ,  SHU, Yoshio ,  TAMURA, Katsumi

    Inventor： OTSUKA PHARMACEUTICAL CO., LTD.

    IPC: C07D215/22

    CPC classification number: C07D215/227 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D411/12 ,  C07D417/12

    Abstract: This invention relates to carbostyril derivatives represented by general formula (1), a process for their preparation, and an agent for inhibiting agglutination of platelets containing them as an active ingredient, wherein A represents a lower alkylene group, R1 represents a substituted or unsubstituted cycloalkyl-lower alkyl group, a cycloalkyl group, a tetrahydropyranyl-lower alkyl group, a lower alkylenedioxy-substituted lower alkyl group, a substituted phenyl-lower alkyl group or a lower alkyl-substituted piperidinyl-lower alkyl group, R2 represents a substituted or unsubstituted 5- or 6-membered, saturated or unsaturated heterocyclic-lower alkyl group, a tetrahydropyranylthio-lower alkyl group, a pyridylthio-lower alkyl group, a lower alkylene-dioxy-substituted lower alkyl group or a substituted or unsubstituted lower alkyl group, and the carbon-to-carbon bond between the 3-position and the 4-position of the carbostyril skeleton represents either a single or a double bond.

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