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公开(公告)号：US20110144074A1
公开(公告)日：2011-06-16
申请号：US13012180
申请日：2011-01-24
IPC分类号： A61K31/58 , A61K31/405 , A61K31/5415 , A61K31/473 , A61K31/55 , A61K31/496 , A61K31/437 , A61K31/5025 , A61K31/538 , A61K31/498 , A61K31/45 , A61K31/4015 , A61P29/00 , A61P31/00 , A61P19/02 , A61P3/10 , A61P37/06 , A61P35/00 , A61P25/28 , A01N1/02 , C12N5/071
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; R3 is 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; R1是氢，-CHN2，R，CH2OR，CH2SR或-CH2Y; R3和R4之间代表单键或双键; Y是电负离子团; R2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; R3是能够适应胱天蛋白酶的S2亚位点的基团; R4是氢或C1-6烷基或R3和R4一起形成环; 环A和环B各自为杂环，R和R 5如说明书所述。 这些化合物是有效的凋亡抑制剂和IL-1和bgr; 分泌。
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公开(公告)号：US20090215736A1
公开(公告)日：2009-08-27
申请号：US12235820
申请日：2008-09-23
IPC分类号： A61K31/58 , A61K31/403 , C07D209/56 , A61K31/5415 , C07D279/18 , A61K31/473 , C07D221/12 , A61K31/55 , C07D223/18 , A61K31/496 , C07D403/02 , C07J43/00 , A61K31/4439 , C07D471/02 , A61K31/444 , C07D471/12 , A61K31/502 , C07D237/26 , A61K31/542 , C07D513/02 , A61K31/536 , C07D265/38 , A61K31/498 , C07D241/46 , A61K31/445 , A61K31/40 , C07D211/00 , C07D207/00 , A61P35/00 , A61P37/00
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; R3 is 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; R1是氢，-CHN2，R，CH2OR，CH2SR或-CH2Y;
R3和R4之间代表单键或双键; Y是电负离子团; R2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; R3是能够适应胱天蛋白酶的S2亚位点的基团; R4是氢或C1-6烷基或R3和R4一起形成环; 环A和环B各自为杂环，R和R 5如说明书所述。 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：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：US07351702B2
公开(公告)日：2008-04-01
申请号：US10153971
申请日：2002-05-23
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 compounds of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; next to R3 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is 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： 本发明提供式I化合物：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; “img id =”CUSTOM-CHARACTER-00001“he =”1.78mm“wi =”6.01mm“file =”US07351702-20080401-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/> R 3旁边代表单键或双键; 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：US09062008B2
公开(公告)日：2015-06-23
申请号：US13106337
申请日：2011-05-12
申请人： Jean-Damien Charrier , Steven John Durrant , Stephen Clinton Young , Pierre-Henri Storck , Anisa Nizarali Virani , Philip Michael Reaper , Joanne Pinder
发明人： Jean-Damien Charrier , Steven John Durrant , Stephen Clinton Young , Pierre-Henri Storck , Anisa Nizarali Virani , Philip Michael Reaper , Joanne Pinder
IPC分类号： A61K31/497 , A61K31/4965 , C07D241/20 , C07D401/04 , C07D403/04
CPC分类号： C07D241/20 , C07D401/04 , C07D403/04
摘要： The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula V: wherein the variables are as defined herein.
摘要翻译： 本发明涉及可用作ATR蛋白激酶抑制剂的吡嗪和吡啶化合物。 本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。 本发明的化合物具有式V：其中变量如本文所定义。
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公开(公告)号：US08877759B2
公开(公告)日：2014-11-04
申请号：US13440981
申请日：2012-09-04
申请人： Jean-Damien Charrier , David Kay , Somhairle MacCormick , Pierre-Henri Storck , Joanne Pinder , Michael Edward O'Donnell , Ronald Marcellus Alphonsus Knegtel , Stephen Clinton Young , Philip Michael Reaper , Steven John Durrant , Heather Clare Twin , Christopher John Davis
发明人： Jean-Damien Charrier , David Kay , Somhairle MacCormick , Pierre-Henri Storck , Joanne Pinder , Michael Edward O'Donnell , Ronald Marcellus Alphonsus Knegtel , Stephen Clinton Young , Philip Michael Reaper , Steven John Durrant , Heather Clare Twin , Christopher John Davis
IPC分类号： A61K31/4965 , C07D403/00 , A61K31/501 , A61K45/06 , A61K31/55 , A61K31/5377 , A61K31/7068 , C07D413/14 , C07D495/04 , A61K31/7048 , A61K33/24 , A61K31/497 , C07D453/00
CPC分类号： C07D413/14 , A61K31/497 , A61K31/501 , A61K31/5377 , A61K31/55 , A61K31/555 , A61K31/7048 , A61K31/7068 , A61K33/24 , A61K45/06 , C07D453/00 , C07D453/02 , C07D495/04 , A61K2300/00
摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.
摘要翻译： 本发明涉及可用作ATR蛋白激酶抑制剂的化合物。 本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。 本发明的化合物具有式I：其中变量如本文所定义。
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公开(公告)号：US08394952B2
公开(公告)日：2013-03-12
申请号：US13206638
申请日：2011-08-10
申请人： David Kay , Ronald Knetgel , Jean-Damien Charrier , Heather Twin
发明人： David Kay , Ronald Knetgel , Jean-Damien Charrier , Heather Twin
IPC分类号： C07D401/12
CPC分类号： C07D487/04 , A61K31/551 , A61K45/06 , C07D487/14
摘要： The present invention relates to compounds useful as inhibitors of 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 inventions.
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公开(公告)号：US20130034616A1
公开(公告)日：2013-02-07
申请号：US13531467
申请日：2012-06-22
申请人： Pierre-Henri Storck , Jean-Damien Charrier , Alistair Rutherford , Michael Paul Mortimore , Somhairle MacCormick , Ronald Marcellus Alphonsus Knegtel , Steven John Durrant
发明人： Pierre-Henri Storck , Jean-Damien Charrier , Alistair Rutherford , Michael Paul Mortimore , Somhairle MacCormick , Ronald Marcellus Alphonsus Knegtel , Steven John Durrant
IPC分类号： A61K31/4985 , A61K31/5377 , A61K31/7048 , A61K33/24 , A61P35/00 , C07D487/04 , A61K31/551
CPC分类号： C07D487/04
摘要： The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.
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公开(公告)号：US08304414B2
公开(公告)日：2012-11-06
申请号：US12109598
申请日：2008-04-25
IPC分类号： A61K31/50 , A61K31/501 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号： C07D403/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
摘要翻译： 本发明描述了式III的新型吡唑化合物：其中Z1，Z2和Z3如说明书所述; Q是-S - ， - O - ， - N（R4） - 或-CH（R6） - ; R1是T环D，其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; R2和R2'如说明书所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为Aurora-2和GSK-3的抑制剂用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。
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公开(公告)号：US08188281B2
公开(公告)日：2012-05-29
申请号：US12273799
申请日：2008-11-19
申请人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
发明人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
IPC分类号： C07D471/02
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D519/00 , C07F7/0805
摘要： The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical 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。
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