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1.发明申请DOMAINS OF EXTRACELLULAR REGION OF HUMAN PLATELET DERIVED GROWTH FACTOR RECEPTOR POLYPEPTIDES 审中-公开人胎盘衍生生长因子受体多肽的细胞外区域
公开(公告)号：WO1992013867A1
公开(公告)日：1992-08-20
申请号：PCT/US1992000730
申请日：1992-01-28
Applicant: COR THERAPEUTICS, INC. , ESCOBEDO, Jaime, A. , WILLIAMS, Lewis, T.
Inventor： COR THERAPEUTICS, INC. , WOLF, David , TOMLINSON, James, E. , FRETTO, Larry, J. , GIESE, Neill, A.
IPC: C07H15/12
CPC classification number: C07K16/2863 , A61K38/00 , C07K14/71 , C07K2319/00
Abstract: Defined constructs of modified human platelet-derived growth factor receptor polypeptides are provided. Extracellular region domain structures are identified and modifications and combinatorial rearrangements of the receptor segments are provided. Both cell bound and soluble forms of modified segments are made available, as are methods for assays using them, allowing for screening or ligand analogues.
Abstract translation: 提供修饰的人血小板衍生生长因子受体多肽的定义构建体。 鉴定细胞外区域结构，并提供受体区段的修饰和组合重排。 修饰片段的细胞结合和可溶形式均可获得，使用它们的测定方法也可用于筛选或配体类似物。
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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。
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公开(公告)号：WO1996013259A3
公开(公告)日：1996-05-09
申请号：PCT/US1995013882
申请日：1995-10-26
Applicant: COR THERAPEUTICS, INC.
Inventor： COR THERAPEUTICS, INC. , GIESE, Neill, A. , LOKKER, Nathalie
IPC: A61K31/365
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公开(公告)号：EP0788356A2
公开(公告)日：1997-08-13
申请号：EP95941340.0
申请日：1995-10-26
Applicant: COR THERAPEUTICS, INC.
Inventor： GIESE, Neill, A. , LOKKER, Nathalie
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.
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Patent Agency Ranking
公开(公告)号：EP0711341A1
公开(公告)日：1996-05-15
申请号：EP94924067.0
申请日：1994-07-29
Applicant: COR THERAPEUTICS, INC.
Inventor： GIESE, Neill, A.
IPC: G01N33
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.
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6.发明授权DOMAINS OF EXTRACELLULAR REGION OF HUMAN PLATELET DERIVED GROWTH FACTOR RECEPTOR POLYPEPTIDES 失效人血小板衍生生长因子受体多肽的胞外区中畴
公开(公告)号：EP0584082B1
公开(公告)日：2000-05-31
申请号：EP92906305.5
申请日：1992-01-28
Inventor： ESCOBEDO, Jaime, A. , WILLIAMS, Lewis, T. , WOLF, David , TOMLINSON, James, E. , FRETTO, Larry, J. , GIESE, Neill, A.
CPC classification number: C07K16/2863 , A61K38/00 , C07K14/71 , C07K2319/00
Abstract: Defined constructs of modified human platelet-derived growth factor receptor polypeptides are provided. Extracellular region domain structures are identified and modifications and combinatorial rearrangements of the receptor segments are provided. Both cell bound and soluble forms of modified segments are made available, as are methods for assays using them, allowing for screening or ligand analogues.
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7.发明公开DOMAINS OF EXTRACELLULAR REGION OF HUMAN PLATELET DERIVED GROWTH FACTOR RECEPTOR POLYPEPTIDES 失效人血小板衍生生长因子受体多肽的胞外区中的结构域。
公开(公告)号：EP0584082A1
公开(公告)日：1994-03-02
申请号：EP92906305.0
申请日：1992-01-28
Applicant: COR THERAPEUTICS, INC. , ESCOBEDO, Jaime, A. , WILLIAMS, Lewis, T.
Inventor： ESCOBEDO, Jaime, A. , WILLIAMS, Lewis, T. , WOLF, David , TOMLINSON, James, E. , FRETTO, Larry, J. , GIESE, Neill, A.
CPC classification number: C07K16/2863 , A61K38/00 , C07K14/71 , C07K2319/00
Abstract: On décrit des produits de recombinaison de polypeptides modifiés récepteurs du facteur de croissance dérivé de plaquettes humaines. Des structures de domaines des régions extracellulaires sont identifiées et des réagencements combinatoires des segments récepteurs sont décrits. Des formes solubles ainsi que des formes à liaison cellulaire de segments modifiés sont disponibles, ainsi que des procédés de titrage les utilisant, permettant la détection d'analogues de ligand.
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公开(公告)号：EP0788356B9
公开(公告)日：2002-10-02
申请号：EP95941340.2
申请日：1995-10-26
Applicant: COR THERAPEUTICS, INC.
Inventor： GIESE, Neill, A. , LOKKER, Nathalie
IPC: A61K31/365
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.
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公开(公告)号：EP0788356B1
公开(公告)日：2001-12-12
申请号：EP95941340.2
申请日：1995-10-26
Applicant: COR THERAPEUTICS, INC.
Inventor： GIESE, Neill, A. , LOKKER, Nathalie
IPC: A61K31/365
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.
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