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71.发明申请PROCESS FOR SYNTHESIZING ASPARTIC AND GLUTAMIC ACID DERIVATIVES ESPECIALLY USEFUL AS INTERMEDIATES IN THE MANUFACTURE OF A CASPASE INHIBITOR 审中-公开合成ASPARTIC和GLUTAMIC ACID衍生物的方法特别适用于CASPASE抑制剂制造中的中间体公开(公告)号：US20080227976A1
公开(公告)日：2008-09-18
申请号：US12030833
申请日：2008-02-13
申请人： Michael Mortimore , Oliver Philps , John Studley
发明人： Michael Mortimore , Oliver Philps , John Studley
IPC分类号： C07D243/10 , C07C229/28 , C07D209/42
CPC分类号： C07C271/20 , C07C269/06 , C07F7/1892
摘要： The invention relates to novel diazoketone derivatives. The invention also relates to processes for homologation of these diazoketone derivatives. The processes are useful for preparing compounds that are caspase inhibitors.
摘要翻译： 本发明涉及新的重氮酮衍生物。 本发明还涉及这些重氮酮衍生物的同系化方法。 该方法可用于制备作为半胱天冬酶抑制剂的化合物。
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公开(公告)号：US20080032963A1
公开(公告)日：2008-02-07
申请号：US11592113
申请日：2006-11-03
IPC分类号： A61K31/397 , A61K31/506 , C07D239/24 , C12N9/99
CPC分类号： C07D403/12 , C07D239/38 , C07D401/14 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： 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.
摘要翻译： 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：US20080015172A1
公开(公告)日：2008-01-17
申请号：US11770093
申请日：2007-06-28
IPC分类号： A61K31/403 , A61K31/404 , A61K31/407 , A61K31/437 , A61K31/495 , A61K31/502 , A61K31/538 , A61K31/5415 , A61K31/55 , A61K31/58 , A61P1/00 , A61P11/00 , A61P13/12 , A61P17/00 , A61P19/02 , A61P25/00 , A61P3/10 , A61P31/00 , A61P35/00 , A61P37/00 , A61P43/00 , A61P9/00 , C07D209/04 , C07D209/82 , C07D219/00 , C07D221/02 , C07D221/12 , C07D223/14 , C07D237/26 , C07D241/36 , C07D279/18 , C07D295/00 , C07J43/00
CPC分类号： A61K31/55 , A61K31/4015 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/45 , A61K31/498 , A61K31/5025 , A61K31/538 , A61K31/54 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
摘要翻译： 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 2，CH 2 OR，CH 2 SR或-CH 2 Y;
R 3和R 4之间代表单键或双键; Y是电负离子团; R 2是CO 2 H，CH 2 CO 2 H，或它们的酯，酰胺或等体醇; R 3是能够适应半胱天冬酶的S2亚位点的基团; R 4是氢或C 1-6烷基或R 3和R 4合在一起形成环 ; 环A和环B各自是杂环，R和R 5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：US20070259869A1
公开(公告)日：2007-11-08
申请号：US11592114
申请日：2006-11-03
申请人： Hayley Binch , Michael Mortimore , Chris Davis , Dean Boyall , Simon Everitt , Daniel Robinson , Sharn Ramaya , Damien Fraysse , John Studley , Andrew Miller , Michael O'Donnell , Alistair Rutherford , Joanne Pinder
发明人： Hayley Binch , Michael Mortimore , Chris Davis , Dean Boyall , Simon Everitt , Daniel Robinson , Sharn Ramaya , Damien Fraysse , John Studley , Andrew Miller , Michael O'Donnell , Alistair Rutherford , Joanne Pinder
IPC分类号： A61K31/506 , A61K31/496 , A61K31/517 , A61K31/5377 , A61P35/00 , A61P35/02 , C07D239/47 , C07D239/48 , C07D239/50 , C07D413/14 , C12N5/02
CPC分类号： C07D403/12 , C07D239/38 , C07D401/14 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： 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.
摘要翻译： 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：US20070249031A1
公开(公告)日：2007-10-25
申请号：US11592119
申请日：2006-11-03
申请人： Hayley Binch , Michael Mortimore , Damien Fraysse , Chris Davis , Michael O'Donnell , Simon Everitt , Daniel Robinson , Joanne Pinder , Andrew Miller
发明人： Hayley Binch , Michael Mortimore , Damien Fraysse , Chris Davis , Michael O'Donnell , Simon Everitt , Daniel Robinson , Joanne Pinder , Andrew Miller
IPC分类号： A61K31/505 , A61P35/00 , C07D239/02 , C12N9/99
CPC分类号： C07D403/12 , C07D239/38 , C07D401/14 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： 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.
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公开(公告)号：US20070173516A1
公开(公告)日：2007-07-26
申请号：US11505637
申请日：2006-08-17
申请人： Michael Mortimore , Julian Golec
发明人： Michael Mortimore , Julian Golec
IPC分类号： A61K31/497 , C07D417/02 , C07D403/14
CPC分类号： C07D241/18 , C07D403/12 , C07D417/12
摘要： 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 inventions.
摘要翻译： 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。 本发明还提供制备本发明化合物的方法。
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公开(公告)号：US20070099920A1
公开(公告)日：2007-05-03
申请号：US11492643
申请日：2006-07-21
申请人： Hayley Binch , Simon Everitt , Michael Mortimore , Daniel Robinson , Dean Stamos
发明人： Hayley Binch , Simon Everitt , Michael Mortimore , Daniel Robinson , Dean Stamos
IPC分类号： A61K31/53 , A61K31/506 , A61K31/501 , A61K31/497 , A61K31/4439 , C07D403/04
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D487/08
摘要： The present invention relates to compounds useful as inhibitors of Aurora, FLT-3, or PDK1 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.
摘要翻译： 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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公开(公告)号：US20060122213A1
公开(公告)日：2006-06-08
申请号：US11170779
申请日：2005-06-29
申请人： Francoise Pierard , Juan-Miguel Jimenez , Ronald Knegtel , Guy Brenchley , Michael Mortimore , Francesca Mazzei
发明人： Francoise Pierard , Juan-Miguel Jimenez , Ronald Knegtel , Guy Brenchley , Michael Mortimore , Francesca Mazzei
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D471/04
摘要： 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 the compounds of the invention.
摘要翻译： 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：US08785444B2
公开(公告)日：2014-07-22
申请号：US13564838
申请日：2012-08-02
IPC分类号： A61K31/50 , C07D239/02
CPC分类号： C07D417/14 , C07D401/14
摘要： 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.
摘要翻译： 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：US20130261114A1
公开(公告)日：2013-10-03
申请号：US13623970
申请日：2012-09-21
IPC分类号： C07D453/02 , A61K45/06 , A61K31/5377 , A61K31/439 , A61K31/496
CPC分类号： C07D453/02 , A61K31/439 , A61K31/496 , A61K31/5377 , A61K45/06
摘要： The present invention relates to compounds useful as inhibitors of choline 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 inventions.
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