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    THROMBIN RECEPTOR ANTAGONISTS
    4.
    发明申请
    THROMBIN RECEPTOR ANTAGONISTS 审中-公开
    硫蛋白受体拮抗剂

    公开(公告)号：WO1994003479A1

    公开(公告)日：1994-02-17

    申请号：PCT/US1993006428

    申请日：1993-07-08

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

    Inventor： COR THERAPEUTICS, INC.

    IPC: C07K05/00

    CPC classification number: C07K7/06 ,  A61K38/00 ,  C07K5/06078 ,  C07K5/1016 ,  C07K7/02

    Abstract: Peptide derivatives serving as thrombin receptor antagonists are disclosed, which bear specificity for the cellular thrombin receptor without interfering with the catalytic activities of thrombin. The derivatives generally have formula (I) in which R1 and R3 are amide linkages, N-alkylamide linkages, or isosteric replacements of such linkages; R2 is either a neutral amino acid side chain or a hydrophobic radical; R4 is hydrophobic radical; R5 is CO, CH2 or SO; X is either of formula (II) in which R6 and R7 are H, alkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl or arylalkyl, and R8 is a hydrophobic radical, or a hydrophobic residue; Y is alkoxy, hydroxy, amino, alkylamino, dialkylamino, in which any of the alkyl groups may be substituted with a basic moiety; Z is an amino acid or peptide residue; and m is zero or one.

    Abstract translation: 公开了用作凝血酶受体拮抗剂的肽衍生物，其对细胞凝血酶受体具有特异性，而不干扰凝血酶的催化活性。 衍生物通常具有式（I），其中R 1和R 3是酰胺键，N-烷基酰胺键或这种键的等排取代基; R2是中性氨基酸侧链或疏水基团; R4是疏水基; R5是CO，CH2或SO; X为式（Ⅱ）中R6和R7为H，烷基，环烷基烷基，烷氧基烷基，烷硫基烷基或芳基烷基，R8为疏水基团或疏水残基; Y是烷氧基，羟基，氨基，烷基氨基，二烷基氨基，其中任何烷基可被碱部分取代; Z是氨基酸或肽残基; m为0或1。

    MODULATION OF INTEGRIN-MEDIATED SIGNAL TRANSDUCTION
    6.
    发明申请
    MODULATION OF INTEGRIN-MEDIATED SIGNAL TRANSDUCTION 审中-公开
    整合信号传输的调制

    公开(公告)号：WO1997014432A1

    公开(公告)日：1997-04-24

    申请号：PCT/US1996016790

    申请日：1996-10-18

    Applicant: COR THERAPEUTICS, INC.

    Inventor： COR THERAPEUTICS, INC. ,  PHILIPS, David ,  LAW, Debbie, A. ,  ALAIMO, Lisa, N.

    IPC: A61K39/00

    CPC classification number: C07K14/70546

    Abstract: The present invention discloses that phosphorylation of cytoplasmic tyrosine residues in the beta -subunit of integrins is needed for signal protein association. The invention provides methods of identifying signaling partners involved in integrin mediated signaling, methods of identifying agents which block integrin mediated signaling, methods of using agents which block intergrin mediated signaling to modulate biological and pathological processes, and agents which block integrin mediated signaling.

    Abstract translation: 本发明公开了信号蛋白结合所需的β亚单位的胞质酪氨酸残基的磷酸化。 本发明提供识别参与整联蛋白介导的信号传导的信号载体的方法，鉴定阻断整联蛋白介导信号传导的试剂的方法，使用阻断整合蛋白介导的信号传导调节生物和病理过程的试剂的方法，以及阻断整合素介导的信号传导的试剂。

    INHIBITORY IMMUNOGLOBULIN POLYPEPTIDES TO HUMAN PDGF BETA RECEPTOR
    7.
    发明申请
    INHIBITORY IMMUNOGLOBULIN POLYPEPTIDES TO HUMAN PDGF BETA RECEPTOR 审中-公开
    人PDGF受体抑制免疫球蛋白多肽

    公开(公告)号：WO1993010805A1

    公开(公告)日：1993-06-10

    申请号：PCT/US1992010359

    申请日：1992-12-01

    Applicant: COR THERAPEUTICS, INC. ,  RAMAKRISHNAN, Vanitha ,  ESCOBEDO, Maria, A. ,  FRETTO, Larry, J.

    Inventor： COR THERAPEUTICS, INC.

    IPC: A61K37/00

    CPC classification number: C07K16/2863 ,  A61K38/00 ,  C07K14/71 ,  C07K2317/34

    Abstract: The present invention is directed towards immunoglobulin polypeptides that specifically bind to the extracellular domain of the human type beta PDGF receptor. The binding of the immunoglobulin polypeptides to the receptor inhibits PDGF-induced (or stimulated) receptor activation as indicated by inhibition of receptor phosphorylation and dimerisation, and by inhibition of PDGF-mediated mitogenesis, chemotaxis and migration of cells displaying the human PDGF type beta receptor on the cell surface. Nucleic acids encoding the immunoglobulin polypeptides are also included in the invention. The immunoglobulin polypeptides have diagnostic and therapeutic uses.

    Abstract translation: 本发明涉及特异性结合人β型PDGF受体的细胞外结构域的免疫球蛋白多肽。 免疫球蛋白多肽与受体的结合抑制PDGF诱导（或刺激的）受体活化，如通过受体磷酸化和二聚化的抑制以及通过抑制PDGF介导的有丝分裂，趋化性和显示人PDGF型β受体的细胞的迁移所表明的 在细胞表面。 编码免疫球蛋白多肽的核酸也包括在本发明中。 免疫球蛋白多肽具有诊断和治疗用途。

    RECOMBINANT AGENTS AFFECTING THROMBOSIS
    8.
    发明申请
    RECOMBINANT AGENTS AFFECTING THROMBOSIS 审中-公开
    影响血栓形成的重组药物

    公开(公告)号：WO1992004378A1

    公开(公告)日：1992-03-19

    申请号：PCT/US1991006337

    申请日：1991-09-04

    Applicant: COR THERAPEUTICS, INC.

    Inventor： COR THERAPEUTICS, INC. ,  WOLF, David

    IPC: C07K13/00

    CPC classification number: C12N9/647 ,  A61K38/00 ,  C07K14/745 ,  C12N9/6432 ,  C12Y304/21006

    Abstract: Analogs of Factor Xa (Factor Xai) which are inactive as proteases in the prothrombinase reaction are useful in treatment of diseases characterized by thrombosis. These antithrombotic agents can be conveniently prepared using recombinant techniques. In addition, modified forms of Factor Xa that generate Factor Xa in serum but have extended half-lives are useful in treating hemophilic conditions. These modified forms of Factor Xa are typically acylated forms of the serine residue in the active site which are slowly deacylated in vivo.

    IDENTIFICATION OF Bap-1, A PROTEIN THAT BINDS TO INTEGRIN AND IS INVOLVED IN INTEGRIN-MEDIATED SIGNAL TRANSDUCTION
    9.
    发明申请
    IDENTIFICATION OF Bap-1, A PROTEIN THAT BINDS TO INTEGRIN AND IS INVOLVED IN INTEGRIN-MEDIATED SIGNAL TRANSDUCTION 审中-公开
    Bap-1的鉴定，蛋白质在蛋白质整合和参与整合信号转导中的作用

    公开(公告)号：WO1998022583A1

    公开(公告)日：1998-05-28

    申请号：PCT/US1997020951

    申请日：1997-11-18

    Applicant: COR THERAPEUTICS, INC.

    Inventor： COR THERAPEUTICS, INC. ,  LI, Shengfeng ,  PHILLIPS, David, R.

    IPC: C12N15/12

    CPC classification number: C07K14/47 ,  A61K38/00

    Abstract: The present invention provides the amino acid and nucleotide sequence of a protein that binds to beta 3 integrins, alpha IIb and Src kinase and is involved in integrin mediated signaling. Based on this disclosure, the present invention provides methods for identifying agents that block integrin mediated signaling, methods of using agents that block integrin mediated signaling to modulate biological and pathological processes, and agents that block integrin mediated signaling.

    Abstract translation: 本发明提供了结合β3整联蛋白，αIIb和Src激酶并参与整联蛋白介导的信号传导的蛋白质的氨基酸和核苷酸序列。 基于该公开内容，本发明提供了用于鉴定阻断整联蛋白介导的信号传导的试剂的方法，使用阻断整联蛋白介导的信号传导调节生物和病理过程的试剂的方法以及阻断整合素介导的信号传导的试剂。

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