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    PHARMACEUTICAL PYRAZOLE COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
    1.
    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：WO9614843A3

    公开(公告)日：1996-05-23

    申请号：PCT/US9514723

    申请日：1995-11-09

    Applicant: COR THERAPEUTICS INC

    Inventor： GIESE NEILL A ,  LOKKER NATHALIE ,  LAIBELMAN ALAN M ,  SCARBOROUGH ROBERT M

    IPC: C07D231/38 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/455 ,  A61P43/00 ,  C07D231/40 ,  C07D401/06 ,  C07D405/04 ,  C07D409/06

    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. 00000

    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。 00000

    METHOD AND COMPOSITIONS FOR INHIBITING PROTEIN KINASES
    2.
    发明申请
    METHOD AND COMPOSITIONS FOR INHIBITING PROTEIN KINASES 审中-公开
    抑制蛋白激酶的方法和组合物

    公开(公告)号：WO9613259A2

    公开(公告)日：1996-05-09

    申请号：PCT/US9513882

    申请日：1995-10-26

    Applicant: COR THERAPEUTICS INC

    Inventor： GIESE NEILL A ,  LOKKER NATHALIE

    IPC: C12N9/99 ,  A61K31/365 ,  A61K31/366 ,  A61P35/02 ,  C07D313/00

    CPC classification number: A61K31/366 ,  A61K31/365

    Abstract: A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a molecule of formula (I) wherein R1 is H, lower alkyl, or lower alkanoyl; R2 is H, lower alkyl, or lower alkanoyl; R3 and R4 together represent a cis double bond or -O- or each of R3 and R4 independently represents H or OR; R5 is =O, =S, or -H, -OR; R6 and R7 together represent a double bond or -O- or each of R6 and R7 independently represents H or OR; R8 and R9 together represent a double bond or -O- or each of R8 and R9 independently represents H or OR; and each R independently represents H, lower alkyl, or lower alkanoyl.

    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）分子（其中R 1为H，低级烷基或低级烷酰基）接触; R2是H，低级烷基或低级烷酰基; R3和R4一起表示顺式双键或-O-或R 3和R 4各自独立地表示H或OR; R5为= O，= S或-H，-OR; R6和R7一起表示双键或-O-或R6和R7各自独立地表示H或OR; R8和R9一起表示双键或-O-或R8或R9各自独立地表示H或OR; 并且每个R独立地表示H，低级烷基或低级烷酰基。

    RECEPTOR FUNCTION ASSAYS
    4.
    发明公开
    RECEPTOR FUNCTION ASSAYS 失效
    受体功能试验

    公开(公告)号：EP0711341A4

    公开(公告)日：2001-12-19

    申请号：EP94924067

    申请日：1994-07-29

    Applicant: COR THERAPEUTICS INC

    Inventor： GIESE NEILL A

    IPC: G01N33/543 ,  G01N33/50 ,  G01N33/566 ,  C12N9/12 ,  G01N33/53 ,  G01N33/545 ,  G01N33/573

    CPC classification number: G01N33/5008 ,  G01N2333/9121

    Abstract: Methods are provided for assaying the function (e.g., activation) of signal-transducing receptors on cells. The methods are useful for identifying compounds that are agonists or antagonists of receptor function. The assays utilize a two-antibody sandwich assay employing an immobilized first antibody that specifically binds and captures the receptor of interest along with any tightly associated proteins or polypeptides and a second antibody directed against (i) an epitope of the receptor that is characteristic of the activated but not the unactivated state, (ii) an epitope of a protein or molecule characteristically bound to activated receptor but not to unactivated receptor, or (iii) an epitope of the receptor that is characteristic of the unactivated but not the activated state. In one embodiment, the level of binding of the second antibody is determined and correlated with the presence of activated receptor, and thus with activation in response to the treatment received by the cells. The methods provided by the invention will find particular use for detecting activation of tyrosine kinase growth factor receptors.

    5.
    发明专利
    未知

    公开(公告)号：ES2170172T3

    公开(公告)日：2002-08-01

    申请号：ES95941340

    申请日：1995-10-26

    Applicant: COR THERAPEUTICS INC

    Inventor： GIESE NEILL A ,  LOKKER NATHALIE

    IPC: C12N9/99 ,  A61K31/365 ,  A61K31/366 ,  A61P35/02 ,  C07D313/00

    Abstract: A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a molecule of the formular alkanoyl; R2 is H, lower alkyl, or lower alkanoyl; R3 and R4 together represent a cis double bond or -O- or each of R3 and R4 independently represents H or OR; R5 is =O, =S, or -H, -OR; R6 and R7 together represent a double bond or -O- or each of R6 and R7 independently represents H or OR; R4 and R together represent a double bond or -O- or each of R8 and R9 independently represents H or OR; and each R independently represents H, lower alkyl, or lower alkanoyl.

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