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    PHARMACEUTICAL PYRAZOLE COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
    2.
    发明申请
    PHARMACEUTICAL PYRAZOLE COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
    用作蛋白激酶抑制剂的药用吡唑组合物

    公开(公告)号：WO1996014843A2

    公开(公告)日：1996-05-23

    申请号：PCT/US1995014723

    申请日：1995-11-09

    Applicant: COR THERAPEUTICS, INC.

    Inventor： COR THERAPEUTICS, INC. ,  GIESE, Neill, A. ,  LOKKER, Nathalie ,  LAIBELMAN, Alan, M. ,  SCARBOROUGH, Robert, M.

    IPC: A61K31/415

    CPC classification number: A61K31/455 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4439

    Abstract: A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a compound of formula (I), wherein: R1 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, polyaromatic, polyaromatic carbonyl, polyheteroaromatic or polyheteroaromatic carbonyl; R2 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, lower hydrocarboyl, 5- or 6-membered heterocyclic aromatic carbonyl, polyaromatic or polyheteroaromatic; R3 is H or lower alkyl; R5 is H, lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, halogen, or cyano; and R6 is H or lower hydrocarboyl.

    Abstract translation: 公开了选择性抑制激酶的方法，其包括将含有激酶的组合物与式（I）化合物接触，其中：R 1是低级烷基，低级烃基，芳基低级烷基，杂芳基低级烷基，5-或6- 多芳基，多芳基羰基，多杂芳基或多杂芳基羰基; R 2是低级烷基，低级烃基，芳基低级烷基，杂芳基低级烷基，5-或6-元杂环芳族，低级烃基，5-或6-元杂环芳族羰基，多芳族或多杂芳族; R3是H或低级烷基; R5是H，低级烷基，低级烃基，芳基低级烷基，杂芳基低级烷基，5-或6-元杂环芳族，卤素或氰基; R6为H或低级烃基。

    RECOMBINANT THROMBIN RECEPTOR AND RELATED PHARMACEUTICALS
    3.
    发明申请
    RECOMBINANT THROMBIN RECEPTOR AND RELATED PHARMACEUTICALS 审中-公开
    重组血红蛋白受体和相关药物

    公开(公告)号：WO1992014750A1

    公开(公告)日：1992-09-03

    申请号：PCT/US1992001312

    申请日：1992-02-19

    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA ,  COR THERAPEUTICS, INC.

    Inventor： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA ,  COR THERAPEUTICS, INC. ,  COUGHLIN, Shaun, R. ,  SCARBOROUGH, Robert, M.

    IPC: C07K07/00

    CPC classification number: C12N9/6429 ,  A61K38/00 ,  A61K39/00 ,  C07K14/705 ,  C07K16/28 ,  C12Y304/21005 ,  Y10S530/837

    Abstract: The DNA encoding the cell surface receptor for thrombin has been cloned and sequenced. The availability of this DNA permits the recombinant production of thrombin receptor which can be produced at cell surfaces and is useful in assay systems both for the detection of thrombin and for the evaluation of candidate thrombin agonists and antagonists. Further, the elucidation of the structure of the thrombin receptor permits the design of agonist and antagonist compounds which are useful diagnostically and therapeutically. The availability of the thrombin receptor also permits production of antibodies specifically immunoreactive with the receptor per se or with specific regions thereof which are also useful diagnostically or therapeutically.

    Abstract translation: 编码凝血酶细胞表面受体的DNA已被克隆并测序。 该DNA的可用性允许重组产生可在细胞表面产生的凝血酶受体，并且可用于检测凝血酶和用于评价候选凝血酶激动剂和拮抗剂的测定系统。 此外，阐明凝血酶受体的结构允许设计在诊断和治疗上有用的激动剂和拮抗剂化合物。 凝血酶受体的可用性还允许产生与受体本身或其特异性区域特异性免疫反应的抗体，其在诊断或治疗上也是有用的。

    SELECTIVE FACTOR Xa INHIBITORS
    5.
    发明申请
    SELECTIVE FACTOR Xa INHIBITORS 审中-公开
    选择性因子Xa抑制剂

    公开(公告)号：WO1998016547A1

    公开(公告)日：1998-04-23

    申请号：PCT/US1997018312

    申请日：1997-10-10

    Applicant: COR THERAPEUTICS, INC.

    Inventor： COR THERAPEUTICS, INC. ,  ZHU, Bing-Yan ,  SCARBOROUGH, Robert, M.

    IPC: C07K05/06

    CPC classification number: C07K5/06191 ,  A61K38/00

    Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

    Abstract translation: 本发明涉及显示抗哺乳动物因子Xa活性的新化合物，其盐及其组合物。 这些化合物在体外或体内用于凝血障碍的预防性或治疗性治疗。

    SELECTIVE FACTOR Xa INHIBITORS
    6.
    发明申请
    SELECTIVE FACTOR Xa INHIBITORS 审中-公开
    选择性因子Xa抑制剂

    公开(公告)号：WO1998016525A1

    公开(公告)日：1998-04-23

    申请号：PCT/US1997018647

    申请日：1997-10-10

    Applicant: COR THERAPEUTICS, INC.

    Inventor： COR THERAPEUTICS, INC. ,  ZHU, Bing-Yan ,  SCARBOROUGH, Robert, M.

    IPC: C07D417/14

    CPC classification number: C07D417/12 ,  C07F5/025

    Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

    Abstract translation: 本发明涉及具有抗哺乳动物因子Xa活性的新化合物及其盐和相关组合物。 这些化合物在体外或体内可用于预防或治疗凝血病症。

    RECOMBINANT C140 RECEPTOR, ITS AGONISTS AND ANTAGONISTS, AND NUCLEIC ACIDS ENCODING THE RECEPTOR
    8.
    发明申请
    RECOMBINANT C140 RECEPTOR, ITS AGONISTS AND ANTAGONISTS, AND NUCLEIC ACIDS ENCODING THE RECEPTOR 审中-公开
    重组C140受体，其激素和拮抗剂以及编码受体的核酸

    公开(公告)号：WO1996023225A1

    公开(公告)日：1996-08-01

    申请号：PCT/US1996001179

    申请日：1996-01-25

    Applicant: COR THERAPEUTICS, INC.

    Inventor： COR THERAPEUTICS, INC. ,  SUNDELIN, Johan ,  SCARBOROUGH, Robert, M.

    IPC: G01N33/53

    CPC classification number: C07K14/723 ,  A61K38/00 ,  A61K48/00

    Abstract: Nucleic acid molecules encoding the C140 cell surface receptor have been cloned and sequenced. The availability of C140 receptor DNA permits the recombinant production of the C140 receptor which can be produced on the surface of a cell, including an oocyte. The nucleic acid molecules are useful in an assay for detecting a substance which affects C140 receptor activity, either receptor agonists or antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in such assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with one or more antigenic epitopes of the C140 receptor.

    Abstract translation: 编码C140细胞表面受体的核酸分子已被克隆并测序。 C140受体DNA的可用性允许重组产生可在细胞表面（包括卵母细胞）上产生的C140受体。 核酸分子可用于检测影响C140受体活性的物质，即受体激动剂或拮抗剂。 此外，阐明C140受体的结构允许设计可用于此类测定中的激动剂和拮抗剂化合物。 C140受体的可用性还允许产生与C140受体的一个或多个抗原表位特异性免疫反应的抗体。

    ANTITHROMBOSIS AGENTS
    9.
    发明申请
    ANTITHROMBOSIS AGENTS 审中-公开
    抗生素代谢物

    公开(公告)号：WO1992008472A1

    公开(公告)日：1992-05-29

    申请号：PCT/US1991008516

    申请日：1991-11-14

    Applicant: COR THERAPEUTICS, INC.

    Inventor： COR THERAPEUTICS, INC. ,  SCARBOROUGH, Robert, M.

    IPC: A61K37/00

    CPC classification number: C07K14/75 ,  A61K38/00 ,  C07K14/46 ,  C07K16/18 ,  Y10S530/856

    Abstract: Platelet antiadhesives (PAA) which are useful as antithrombotics are obtainable from snake venoms which have been identified using an assay which measures the ability of the venom to inhibit ristocetin- or botrocetin-induced agglutination of platelets in the presence of von Willebrand Factor. The antiadhesives of the invention are 20-24 kd dimers of smaller peptides, or effective portions thereof. Antibodies to these antiadhesives are also prepared and are useful in assays for PAA and for screening expression libraries for PAA encoding DNA.

    Abstract translation: 可用作抗血栓药物的血小板抗粘附剂（PAA）可从蛇毒获得，蛇毒使用测定毒素在血管性血友病因子存在下抑制瑞斯托菌素或博西汀诱导血小板凝集的能力的测定法。 本发明的抗粘附剂是较小肽的20-24kD二聚体或其有效部分。 还制备了这些抗粘附剂的抗体，并且可用于PAA的测定和用于筛选编码DNA的PAA的表达文库。

    PLATELET AGGREGATION INHIBITORS
    10.
    发明申请
    PLATELET AGGREGATION INHIBITORS 审中-公开
    PLATELET聚合抑制剂

    公开(公告)号：WO1990015620A1

    公开(公告)日：1990-12-27

    申请号：PCT/US1990003417

    申请日：1990-06-15

    Applicant: COR THERAPEUTICS, INC.

    Inventor： COR THERAPEUTICS, INC. ,  SCARBOROUGH, Robert, M. ,  WOLF, David, Lawrence ,  CHARO, Israel, F.

    IPC: A61K37/62

    CPC classification number: C07K14/75 ,  A61K38/12 ,  A61K38/1703 ,  A61K38/57 ,  C07K14/46 ,  C07K14/755 ,  C07K14/78

    Abstract: An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K* -(G/Sar)-D wherein K* is a modified lysyl residue of the formula R 2 N(CH2)4CHNHCO- wherein each R is independently H, alkyl(1-6C) or at most one R is R -C=NR wherein R is H, alkyl(1-6C), phenyl or benzyl, or is NR in which each R is independently H or alkyl(1-6C) and R is H, alkyl(1-6C), phenyl or benzyl, or R -C=NR is a radical selected from the group consisting of (a), (b), (c) and (d) where m is an integer of 2-3, and each R is independently H or alkyl(1-6C); and wherein one or two (CH2) may be replaced by O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.

    Abstract translation: 描述了基于特异性受体结合筛选蛇毒用于存在或不存在血小板聚集抑制剂（PAI）的测定法。 使用该测定，完成了广泛的蛇毒样品中PAIs的鉴定和表征。 描述和表征了来自这些活性蛇毒中的几种的分离和纯化的PAI。 另外，缺少Arg-Gly-Asp（RGD）粘附序列但含有K * - （G / Sar）-D的PAI，其中K *是式R 1 N 2（CH 2）4 CHNHCO- 其中每个R 1独立地是H，烷基（1-6C）或至多一个R 1是R 2 -C = NR 3，其中R 2是H，烷基（1-6C） 或苯基或苄基，或为NR 4，其中每个R 4独立地为H或（1-6C）烷基，R 3为H，烷基（1-6C），苯基或苄基， 2 -C-NR 3是选自（a），（b），（c）和（d）中的基团，其中m是2-3的整数，并且每个R 5是 独立地是H或（1-6C）烷基; 并且其中一个或两个（CH 2）可以被O或S替代，条件是所述O或S不与另一个杂原子相邻，并且显示出特异性抑制纤维蛋白原或血管性血友病因子与GP IIb-IIIa的结合。

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