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    OXINDOLE INHIBITORS OF FACTOR Xa
    1.
    发明申请
    OXINDOLE INHIBITORS OF FACTOR Xa 审中-公开
    因子的氧化物抑制剂

    公开(公告)号：WO0172708A3

    公开(公告)日：2002-05-23

    申请号：PCT/US0109374

    申请日：2001-03-26

    Applicant: COR THERAPEUTICS INC ,  MARLOWE CHARLES K ,  KANE MAGUIRE KIM A ,  ZHU BING YAN ,  SCARBOROUGH ROBERT M

    Inventor： MARLOWE CHARLES K ,  KANE-MAGUIRE KIM A ,  ZHU BING-YAN ,  SCARBOROUGH ROBERT M

    IPC: A61P7/02 ,  C07D401/12 ,  A61K31/454

    CPC classification number: C07D401/12

    Abstract: Novel compounds of formula (I), including its pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa is described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.

    Abstract translation: 描述了新的式（I）化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和具有抗哺乳动物因子Xa活性的前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物在体外或体内用于预防或治疗特征在于不期望的血栓形成的哺乳动物中的病症。

    Cyclic diaza compounds as selective factor Xa inhibitors for treating thrombotic related disorders
    8.
    发明专利
    Cyclic diaza compounds as selective factor Xa inhibitors for treating thrombotic related disorders 未知

    公开(公告)号：NZ500354A

    公开(公告)日：2001-11-30

    申请号：NZ50035498

    申请日：1998-04-13

    Applicant: COR THERAPEUTICS INC

    Inventor： SCARBOROUGH ROBERT M ,  ZHU BING-YAN ,  MARLOWE CHARLES K

    IPC: A61K31/495 ,  A61K31/496 ,  A61K31/551 ,  A61P7/02 ,  A61P43/00 ,  C07D211/26 ,  C07D241/08 ,  C07D243/08 ,  C07D295/15 ,  C07D295/205 ,  C07D401/06 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14 ,  C07K5/062 ,  C07K5/083 ,  C07D295/20

    Abstract: A class of cyclic diaza compounds of the general Formula (I) having potent and highly selective inhibitors of factor Xa or factor Xa when assembled in the prothrombinase complex. These compounds show selectivity for factor Xa versus other proteases of the coagulation (e.g. thrombin, fVIIa, flXa) or the fibronolytic cascades (e.g. plasminogen activators, plasmin). The compounds are useful for the treatment or prevention of unstable angina, myocardial infarction, transient ischemic attack, thrombotic stroke, embolic stroke, disseminated intravascular coagulation including the treatment of septic shock, deep venous thrombosis in the prevention of pulmonary embolism or the treatment of reocclusion or restenosis of reperfused coronary arteries. The composition may optionally include anticoagulants, antiplatelet agent, and thrombolytic agents. Wherein; R1 is selected from the group consisting of H, C1-6alkyl, C3-8cycloalkyl, C1-3alkylaryl, C1-3alkyl-C3-8cycloalkyl and aryl and R2 is H, or R1 and R2 are taken together to form a carbocyclic ring; m is an integer from 0-2; n is an integer from 0-6; p is an integer from 0-2; q is an integer from 1-3; r is an integer from 0-4; s is an integer from 0-1; A is selected from the group consisting of R3, -NR3R4, and Formula (II); Q is selected from the group consisting of a direct link, C1-6alkyl, C3-8cycloalkyl, C1-6alkenyl, C1-6alkenylaryl, aryl, and a five to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from the group consisting of N, O and S; D is selected from the group consisting of a direct link, -CO-, -SO2-, -O-CO-, -NR9SO2- and -NR9-CO-, where R9 is selected from the group consisting of H, -OH, C1-6alkyl, aryl and C1-4alkylaryl; E is selected from the group consisting of a direct link, C3-8cycloalkyl, aryl, and a five to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from the group consisting of N, O and S; G is selected from the group consisting of R10, -NR10R11, and Formula (III); X and Y are independently selected from the group consisting of O and H2; W is selected from the group consisting of H, and Formula (IV);

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