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1. 发明申请

WO2006047256A1 TRIAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
标题翻译：三氮唑作为蛋白激酶的抑制剂有用
公开(公告)号：WO2006047256A1
公开(公告)日：2006-05-04
申请号：PCT/US2005/037830
申请日：2005-10-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED , DAVIES, Robert, J. , FORSTER, Cornelia, J. , ARNOST, Michael, J. , WANG, Jian
发明人： DAVIES, Robert, J. , FORSTER, Cornelia, J. , ARNOST, Michael, J. , WANG, Jian
IPC分类号： A61K31/4196 , C07D249/14 , C07D401/04 , A61P35/00 , A61P37/08
CPC分类号： C07D249/14 , C07D401/04
摘要： The present invention relates to inhibitors of proteins kinases of formula (I). The invention also provides pharmaceuticals compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
摘要翻译：本发明涉及式（I）的蛋白激酶抑制剂。本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。

2. 发明申请

WO2002088078A3 INHIBITORS OF GSK-3 AND CRYSTAL STRUCTURES OF GSK-3β PROTEIN AND PROTEIN COMPLEXES 审中-公开
公开(公告)号：WO2002088078A3
公开(公告)日：2002-11-07
申请号：PCT/US2002/013511
申请日：2002-04-29
申请人： VERTEX PHARMACEUTICALS INCORPORATED , TER HAAR, Ernst , SWENSON, Lovorka , GREEN, Jeremy , ARNOST, Michael, J.
发明人： TER HAAR, Ernst , SWENSON, Lovorka , GREEN, Jeremy , ARNOST, Michael, J.
IPC分类号： A61K31/495
摘要： The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.

3. 发明申请

WO2003066629A3 HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF GSK-3 审中-公开
公开(公告)号：WO2003066629A3
公开(公告)日：2003-08-14
申请号：PCT/US2003/003655
申请日：2003-02-06
申请人： VERTEX PHARMACEUTICALS INCORPORATED , HARBESON, Scott L. , ARNOST, Michael, J. , GREEN, Jeremy , SAVIC, Vladimir
发明人： HARBESON, Scott L. , ARNOST, Michael, J. , GREEN, Jeremy , SAVIC, Vladimir
IPC分类号： C07D413/04
摘要： The present invention relates to compounds of formula I wherein: Ring A is an optionally substituted 5-7 membered, partially unsaturated or fully unsaturated ring having 0-3 heteroatoms independently selected from nitrogen, oxygen or sulfur, and wherein Ring A is optionally fused to an optionally substituted saturated, partially unsaturated or fully unsaturated 5-8 member ring having 0-3 heteroatoms independently selected from nitrogen, oxygen or sulfur; Ring B is an optionally substituted 5-6 membered ring having 0 to 4 heteroatoms, independently selected from nitrogen, oxygen, or sulfur, wherein said ring has a first substituent, -N(R 1 ) 2 , in the position adjacent to the point of attachment, and is optionally substituted by up to two additional substituents. Compoounds of formula I are useful as inhibitors of GSK-3 and Lck protein kinases. The present invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes, Alzheimer’s disease, and transplant rejection.

4. 发明申请

WO2003011287A1 PYRAZOLON DERIVATIVES AS INHIBITORS OF GSK-3 审中-公开
标题翻译：作为GSK-3的抑制剂的吡唑啉衍生物
公开(公告)号：WO2003011287A1
公开(公告)日：2003-02-13
申请号：PCT/US2002/024726
申请日：2002-08-02
申请人： VERTEX PHARMACEUTICALS INCORPORATED , GREEN, Jeremy , ARNOST, Michael, J. , PIERCE, Albert
发明人： GREEN, Jeremy , ARNOST, Michael, J. , PIERCE, Albert
IPC分类号： A61K31/415
CPC分类号： C07D401/12 , C07D231/20 , C07D231/46 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to compounds of formula (I) that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula (I) or pharmaceutical compositions comprising compounds of formula (I) to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula (I) or pharmaceutical compositions comprising compounds of formula (I). The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula (I) or pharmaceutical compositions comprising compounds of formula (I).
摘要翻译：本发明涉及可用作GSK-3抑制剂的式（I）化合物。本发明还涉及使用式（I）化合物或包含式（I）化合物的药物组合物抑制GSK-3活性的方法。本发明还提供了利用这些化合物和药物组合物治疗和预防各种疾病如糖尿病和阿尔茨海默病的方法。本发明还涉及使用式（I）化合物或包含式（I）化合物的药物组合物来抑制Aurora-2活性和治疗或预防Aurora-2介导的疾病的方法。本发明还涉及使用式（I）化合物或包含式（I）化合物的药物组合物来抑制细胞周期蛋白依赖性激酶-2活性和治疗或预防抑制细胞周期蛋白依赖性激酶2介导的疾病的方法。

5. 发明申请

WO2006127587A1 PYRROLOPYRIDINES USEFUL AS INHIBITORS OF PROTEIN KINASE 审中-公开
标题翻译：吡咯啉可用作蛋白激酶的抑制剂
公开(公告)号：WO2006127587A1
公开(公告)日：2006-11-30
申请号：PCT/US2006/019711
申请日：2006-05-22
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LEDEBOER, Mark, W. , WANNAMAKER, Marion, W. , FARMER, Luc, J. , WANG, Tiansheng , PIERCE, Albert, C. , MARTINEZ-BOTELLA, Gabriel , BETHIEL, Randy, S. , BEMIS, Guy, W. , WANG, Jian , SALITURO, Francesco, G. , ARNOST, Michael, J. , COME, Jon, H. , GREEN, Jeremy , STEWART, Michelle , MARHEFKA, Craig
发明人： LEDEBOER, Mark, W. , WANNAMAKER, Marion, W. , FARMER, Luc, J. , WANG, Tiansheng , PIERCE, Albert, C. , MARTINEZ-BOTELLA, Gabriel , BETHIEL, Randy, S. , BEMIS, Guy, W. , WANG, Jian , SALITURO, Francesco, G. , ARNOST, Michael, J. , COME, Jon, H. , GREEN, Jeremy , STEWART, Michelle , MARHEFKA, Craig
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of formula (I) wherein Q, Z, R 1 , R 2 , and R 3 are as described in claim 1 useful as inhibitors of protein kinases, particularly of JAK family and ROCK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及其中Q，Z，R 1，R 2和R 3的式（I）化合物如权利要求1用作蛋白激酶的抑制剂，特别是JAK家族和ROCK家族激酶的抑制剂。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

6. 发明申请

WO2005013982A1 AMINOTRIAZOLE COMPOUNDS USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
标题翻译：氨基三唑化合物作为蛋白激酶的抑制剂有用
公开(公告)号：WO2005013982A1
公开(公告)日：2005-02-17
申请号：PCT/US2004/025539
申请日：2004-08-06
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LEDEBOER, Mark W. , DAVIES, Robert J. , ARNOST, Michael J. , BEMIS, Guy W. , FORSTER, Cornelia J. , GREY, Ronald, Jr. , LEDFORD, Brian , MARHEFKA, Craig , MESSERSMITH, David , PIERCE, Albert C. , SALITURO, Francesco , WANG, Jian
发明人： DAVIES, Robert J. , ARNOST, Michael J. , BEMIS, Guy W. , FORSTER, Cornelia J. , GREY, Ronald, Jr. , LEDFORD, Brian , MARHEFKA, Craig , MESSERSMITH, David , PIERCE, Albert C. , SALITURO, Francesco , WANG, Jian
IPC分类号： A61K31/4196
CPC分类号： C07D401/04 , C07D249/14 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/04
摘要： The present invention relates to aminotriazole compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的氨基三唑化合物。本发明还提供包含本发明化合物的药物组合物，制备化合物的方法和使用该组合物治疗各种疾病的方法。

7. 发明申请

WO2003066629A2 HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF GSK-3 审中-公开
标题翻译：异氟醚化合物作为GSK-3的抑制剂有用
公开(公告)号：WO2003066629A2
公开(公告)日：2003-08-14
申请号：PCT/US2003/003655
申请日：2003-02-06
申请人： VERTEX PHARMACEUTICALS INCORPORATED , HARBESON, Scott L. , ARNOST, Michael, J. , GREEN, Jeremy , SAVIC, Vladimir
发明人： HARBESON, Scott L. , ARNOST, Michael, J. , GREEN, Jeremy , SAVIC, Vladimir
IPC分类号： C07D413/04
CPC分类号： A61K31/506 , A61K31/4184 , A61K31/4245 , A61K31/4427 , A61K31/4439 , A61K31/501 , A61K31/52
摘要： The present invention relates to compounds of formula I useful as inhibitors of GSK-3 and Lck protein kinases. The present invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes, Alzheimer's disease, and transplant rejection.
摘要翻译：本发明涉及可用作GSK-3和Lck蛋白激酶抑制剂的式I化合物。本发明还提供包含本发明化合物的药学上可接受的组合物和利用这些组合物治疗和预防各种疾病如糖尿病，阿尔茨海默氏病和移植排斥的方法。

8. 发明申请

WO2002088078A2 INHIBITORS OF GSK-3 AND CRYSTAL STRUCTURES OF GSK-3β PROTEIN AND PROTEIN COMPLEXES 审中-公开
标题翻译： GSK-3β蛋白和蛋白复合物的GSK-3和晶体结构的抑制剂
公开(公告)号：WO2002088078A2
公开(公告)日：2002-11-07
申请号：PCT/US2002/013511
申请日：2002-04-29
申请人： VERTEX PHARMACEUTICALS INCORPORATED , TER HAAR, Ernst , SWENSON, Lovorka , GREEN, Jeremy , ARNOST, Michael, J.
发明人： TER HAAR, Ernst , SWENSON, Lovorka , GREEN, Jeremy , ARNOST, Michael, J.
IPC分类号： C07D
CPC分类号： C07D487/04 , C07K2299/00 , C12N9/1205 , G06F19/16
摘要： The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
摘要翻译：本发明涉及GSK-3抑制剂及其制备方法。本发明还提供包含抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病如糖尿病和阿尔茨海默氏病的方法。此外，本发明涉及包含GSK-3β或其同源物的结合口袋的分子或分子复合物。本发明涉及一种计算机，包括用这种结合口袋的结构坐标编码的数据存储介质。本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。本发明涉及使用结构坐标筛选和设计结合GSK-3β蛋白或其同系物的化合物的方法。本发明还涉及可结晶组合物和包含GSK-3β蛋白或GSK-3β蛋白复合物的晶体。

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