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公开(公告)号：WO2008147626A2
公开(公告)日：2008-12-04
申请号：PCT/US2008062331
申请日：2008-05-02
Applicant: VERTEX PHARMA , MORTIMORE MICHAEL , GOLEC JULIAN , ROBINSON DANIEL , DAVIS CHRISTOPHER , STUDLEY JOHN
Inventor： MORTIMORE MICHAEL , GOLEC JULIAN , ROBINSON DANIEL , DAVIS CHRISTOPHER , STUDLEY JOHN
IPC: C07D401/14 , A61K31/4427 , C07D417/14
CPC classification number: C07D401/14 , C07D417/14
Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
Abstract translation: 本发明涉及用作极光蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物以及使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：WO2007056163A3
公开(公告)日：2008-03-27
申请号：PCT/US2006042993
申请日：2006-11-03
Applicant: VERTEX PHARMA , BINCH HAYLEY , MORTIMORE MICHAEL , FRAYSSE DAMIEN , RUTHERFORD ALISTAIR
Inventor： BINCH HAYLEY , MORTIMORE MICHAEL , FRAYSSE DAMIEN , RUTHERFORD ALISTAIR
IPC: C07D403/14 , A61K31/4155 , C07D239/02
CPC classification number: C07D403/12 , C07D239/38 , C07D401/14 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases . The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders . The invention also provides processes for preparing compounds of the invention.
Abstract translation: 本发明涉及可用作Aurora蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物和使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：WO2008137622A3
公开(公告)日：2009-03-05
申请号：PCT/US2008062330
申请日：2008-05-02
Applicant: VERTEX PHARMA , MORTIMORE MICHAEL , GOLEC JULIAN , ROBINSON DANIEL
Inventor： MORTIMORE MICHAEL , GOLEC JULIAN , ROBINSON DANIEL
IPC: C07D403/14 , A61K31/506 , A61P35/00 , C07D417/14
CPC classification number: C07D403/12 , C07D417/14
Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
Abstract translation: 本发明涉及可用作Aurora蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物和使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：WO2008115973A3
公开(公告)日：2008-12-04
申请号：PCT/US2008057465
申请日：2008-03-19
Applicant: VERTEX PHARMA , BINCH HAYLEY , YOUNG STEPHEN , DAVIS CHRISTOPHER , MORTIMORE MICHAEL , GOLEC JULIAN , STUDLEY JOHN , ROBINSON DANIEL , O'DONNELL MICHAEL , BOYALL DEAN , PINDER JOANNE , EVERITT SIMON
Inventor： BINCH HAYLEY , YOUNG STEPHEN , DAVIS CHRISTOPHER , MORTIMORE MICHAEL , GOLEC JULIAN , STUDLEY JOHN , ROBINSON DANIEL , O'DONNELL MICHAEL , BOYALL DEAN , PINDER JOANNE , EVERITT SIMON
IPC: C07D403/14 , A61K31/33 , A61K35/00 , C07D413/14 , C07D417/14 , C07D471/04
CPC classification number: C07D471/04 , C07D403/14 , C07D413/14 , C07D417/14
Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
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公开(公告)号：WO2008094992A3
公开(公告)日：2008-12-04
申请号：PCT/US2008052443
申请日：2008-01-30
Applicant: VERTEX PHARMA , JIMENEZ JUAN-MIGUEL , BEMIS GUY , MALTAIS FRANCOIS , WANG TIANSHENG , KNEGTEL RONALD , DAVIS CHRIS , FRAYSSE DAMIEN , BOYALL DEAN , SETTIMO LUCA , YOUNG STEPHEN , MORTIMORE MICHAEL
Inventor： JIMENEZ JUAN-MIGUEL , BEMIS GUY , MALTAIS FRANCOIS , WANG TIANSHENG , KNEGTEL RONALD , DAVIS CHRIS , FRAYSSE DAMIEN , BOYALL DEAN , SETTIMO LUCA , YOUNG STEPHEN , MORTIMORE MICHAEL
IPC: C07D213/73 , A61K31/444 , A61K31/529 , A61P25/00 , A61P35/00 , C07D401/14 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , C07D487/04 , C07D487/08
CPC classification number: C07D213/73 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , C07D487/04 , C07D487/08
Abstract: The present invention relates to compounds represented by the following structural formula: (I) useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of µsing the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
Abstract translation: 本发明涉及由以下结构式表示的化合物：（I）可用作蛋白激酶的抑制剂。 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组合物治疗各种疾病，病症或病症的方法。 本发明还提供了制备本发明化合物的方法。
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Patent Agency Ranking
公开(公告)号：WO0172707A3
公开(公告)日：2002-05-23
申请号：PCT/US0110182
申请日：2001-03-29
Applicant: VERTEX PHARMA , BEBBINGTON DAVID , CHARRIER JEAN DAMIEN , KAY DAVID , KNEGTEL RONALD , GOLEC JULIAN , MORTIMORE MICHAEL , STUDLEY JOHN
Inventor： BEBBINGTON DAVID , CHARRIER JEAN-DAMIEN , KAY DAVID , KNEGTEL RONALD , GOLEC JULIAN , MORTIMORE MICHAEL , STUDLEY JOHN
IPC: A61K31/403 , A61K31/404 , A61K31/473 , A61K31/496 , A61K31/5415 , A61K31/55 , A61K31/575 , A61P9/00 , A61P19/02 , A61P19/08 , A61P25/32 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/06 , A61P43/00 , C07D209/04 , C07D209/08 , C07D209/82 , C07D209/86 , C07D221/12 , C07D223/22 , C07D223/26 , C07D223/28 , C07D279/30 , C07D279/36 , C07D403/12 , C07J9/00 , A61K31/395 , C07D209/88
CPC classification number: C07D403/12 , C07D209/08 , C07D209/86 , C07D221/12 , C07D223/26 , C07D223/28 , C07D279/30
Abstract: This invention provides caspase inhibitors of formula (I): wherein Z is oxygen or sulfur; R is hydrogen, -CHN2,R, CH2OR, CH2SR, or -CH2Y; Y is an electronegative leaving group; R is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R is a group capable of fitting into the S2 subsite of a caspase enzyme; R and R are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1 beta secretion.
Abstract translation: 本发明提供了式（I）的半胱天冬酶抑制剂：其中Z是氧或硫; R 1是氢，-CHN 2，R 1，CH 2 OR，CH 2 SR或-CH 2 Y; Y是电负离子团; R 2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; R 3是能够适应半胱天冬酶的S2亚位点的基团; R 4和R 5与中间的氮一起形成杂环，R如说明书中所述。 这些化合物是凋亡和IL-1β分泌的有效抑制剂。
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公开(公告)号：WO2008060597A8
公开(公告)日：2009-07-23
申请号：PCT/US2007023999
申请日：2007-11-15
Applicant: VERTEX PHARMA , KNEGTEL RONALD , CHARRIER JEAN-DAMIEN , DURRANT STEVEN , BRENCHLEY GUY , MORTIMORE MICHAEL
Inventor： KNEGTEL RONALD , CHARRIER JEAN-DAMIEN , DURRANT STEVEN , BRENCHLEY GUY , MORTIMORE MICHAEL
IPC: C07D495/04 , C07D513/04 , C07D519/00
CPC classification number: C07D513/04 , A61K31/55 , A61K31/551 , A61K45/06 , C07D495/04 , C07D519/00 , C07K14/81
Abstract: The present invention relates to compounds useful as inhibitors of protein 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. The invention also provides processes for preparing compounds of the inventions.
Abstract translation: 本发明涉及可用作蛋白激酶抑制剂的化合物。 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。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：WO2007056164A3
公开(公告)日：2007-12-13
申请号：PCT/US2006042994
申请日：2006-11-03
Applicant: VERTEX PHARMA , BINCH HAYLEY , MORTIMORE MICHAEL , FRAYSSE DAMIEN , DAVIS CHRIS , O'DONNELL MICHAEL , EVERITT SIMON , ROBINSON DANIEL , PINDER JOANNE , MILLER ANDREW
Inventor： BINCH HAYLEY , MORTIMORE MICHAEL , FRAYSSE DAMIEN , DAVIS CHRIS , O'DONNELL MICHAEL , EVERITT SIMON , ROBINSON DANIEL , PINDER JOANNE , MILLER ANDREW
CPC classification number: C07D403/12 , C07D239/38 , C07D401/14 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
Abstract translation: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物以及使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：WO2007056221A2
公开(公告)日：2007-05-18
申请号：PCT/US2006043096
申请日：2006-11-03
Applicant: VERTEX PHARMA , BINCH HAYLEY , MORTIMORE MICHAEL , DAVIS CHRIS , BOYALL DEAN , EVERITT SIMON , ROBINSON DANIEL , RAMAYA SHARN , FRAYSSE DAMIEN , STUDLEY JOHN , MILIER ANDREW , O'DONNELL MICHAEL , RUTHERFORD ALISTAIR , PINDER JOANNE
Inventor： BINCH HAYLEY , MORTIMORE MICHAEL , DAVIS CHRIS , BOYALL DEAN , EVERITT SIMON , ROBINSON DANIEL , RAMAYA SHARN , FRAYSSE DAMIEN , STUDLEY JOHN , MILIER ANDREW , O'DONNELL MICHAEL , RUTHERFORD ALISTAIR , PINDER JOANNE
IPC: A61K31/513
CPC classification number: C07D403/12 , C07D239/38 , C07D401/14 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
Abstract translation: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物和使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：WO2007015923A2
公开(公告)日：2007-02-08
申请号：PCT/US2006028149
申请日：2006-07-21
Applicant: VERTEX PHARMA , BINCH HAYLEY , MORTIMORE MICHAEL , ROBINSON DANIEL , STAMOS DEAN
Inventor： BINCH HAYLEY , MORTIMORE MICHAEL , ROBINSON DANIEL , STAMOS DEAN
CPC classification number: C07D403/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D487/08
Abstract: The present invention relates to compounds useful as inhibitors of Aurora, FLT-3, or PDKl protein kinase. 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. The invention also provides processes for preparing compounds of the invention.
Abstract translation: 本发明涉及可用作Aurora，FLT-3或PDK1蛋白激酶抑制剂的化合物。 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。 本发明还提供了制备本发明化合物的方法。
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