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![Substituted N-(pyrazol-5-yl)-pyrrolo[3,2-D]pyrimidin-4-amine useful as protein kinase inhibitors](/abs-image/US/2013/09/03/US08524720B2/abs.jpg.150x150.jpg)
1.发明授权Substituted N-(pyrazol-5-yl)-pyrrolo[3,2-D]pyrimidin-4-amine useful as protein kinase inhibitors 有权用作蛋白激酶抑制剂的取代的N-（吡唑-5-基） - 吡咯并[3,2-D]嘧啶-4-胺公开(公告)号：US08524720B2
公开(公告)日：2013-09-03
申请号：US12651639
申请日：2010-01-04
申请人： David Bebbington , Hayley Binch , Ronald Knegtel , Julian M.C. Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert Davies , Pan Li , Marion Wannamaker , Cornelia Forster , Albert Pierce
发明人： David Bebbington , Hayley Binch , Ronald Knegtel , Julian M.C. Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert Davies , Pan Li , Marion Wannamaker , Cornelia Forster , Albert Pierce
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , A61P25/28 , A61P3/10
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D491/10 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2′, T, and R3 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IV的新型吡唑化合物：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; R x和R y独立地选自T-R 3，或与它们的插入原子一起形成具有1-3个选自氧，硫或氮的环杂原子的稠合的，不饱和的或部分不饱和的5-8元环; R2，R2'，T和R3如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病的极光-2和GSK-3的抑制剂。
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公开(公告)号：US20110269732A1
公开(公告)日：2011-11-03
申请号：US12595878
申请日：2009-10-14
申请人： Julian M.C. GOLEC , John POLLARD , James WESTCOTT , Hayley Marie BINCH , Michael Paul MORTIMORE , Daniel David ROBINSON
发明人： Julian M.C. GOLEC , John POLLARD , James WESTCOTT , Hayley Marie BINCH , Michael Paul MORTIMORE , Daniel David ROBINSON
IPC分类号： A61K31/397 , A61K31/506 , C07D403/14 , A61K31/496 , G06G7/58 , A61P35/02 , A61P35/04 , C12N9/99 , C12Q1/48 , C07D401/14 , A61P35/00
CPC分类号： C07D403/12 , A61K31/506 , A61K45/06 , C07D401/14 , C12Q1/485 , G01N2500/04 , G16B15/00
摘要： The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational change in the protein AuroraB and whose binding constant for the two-step process is given as Ki*. Finally, this invention also relates to compounds having the features of the pharmacophore.
摘要翻译： 本发明涉及药物发现方法，特别是用于测定化合物作为极光激酶抑制剂的活性的方法。 本发明还涉及描述能够促进蛋白质AuroraB中的构象变化的化合物的药效团，其两步法的结合常数以Ki *给出。 最后，本发明还涉及具有药效团特征的化合物。
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公开(公告)号：US20080199454A1
公开(公告)日：2008-08-21
申请号：US12005068
申请日：2007-12-21
IPC分类号： A61K38/48 , C07D487/06 , C07F9/572 , C07F9/06 , C07F9/6512 , C07F9/59 , C07F9/6547 , C07F9/6506 , C07F9/6553 , A61K31/675 , A61K31/661 , A61K31/67 , A61P35/04 , A61P9/00 , C12N5/02 , A01N1/02
CPC分类号： C07D271/06 , C07C235/52 , C07C237/22 , C07C271/22 , C07C271/28 , C07D209/26 , C07D209/86 , C07D209/94 , C07D211/34 , C07D239/90 , C07F9/10 , C07F9/5728 , C07K5/0202
摘要： The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.
摘要翻译： 本发明涉及式I化合物，其是胱天蛋白酶抑制剂及其药学上可接受的盐的前药。 本发明还涉及通过选择性键切割从这些化合物释放胱天蛋白酶抑制剂。 本发明进一步涉及包含这些化合物的药物组合物，其特别适用于治疗胱天蛋白酶介导的疾病，包括炎性和退行性疾病。 本发明还涉及制备本发明化合物的方法。
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公开(公告)号：US20110046104A1
公开(公告)日：2011-02-24
申请号：US12598277
申请日：2009-10-30
IPC分类号： A61K31/506 , C07D417/14 , C07D403/14 , C07D401/14
CPC分类号： C07D403/12 , 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.
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公开(公告)号：US20120165319A1
公开(公告)日：2012-06-28
申请号：US13293592
申请日：2011-11-10
申请人： Mark James Batchelor , David Bebbington , Guy W. Bemis , Wolf Herman Fridman , Roger John Gillespie , Julian M.C. Golec , Yong Gu , David J. Lauffer , David J. Livingston , Saroop Singh Matharu , Michael D. Mullican , Mark A. Murcko , Robert Murdoch , Philip Nyce , Andrea L.C. Robidoux , Michael Su , M. Woods Wannamaker , Keith P. Wilson , Robert E. Zelle
发明人： Mark James Batchelor , David Bebbington , Guy W. Bemis , Wolf Herman Fridman , Roger John Gillespie , Julian M.C. Golec , Yong Gu , David J. Lauffer , David J. Livingston , Saroop Singh Matharu , Michael D. Mullican , Mark A. Murcko , Robert Murdoch , Philip Nyce , Andrea L.C. Robidoux , Michael Su , M. Woods Wannamaker , Keith P. Wilson , Robert E. Zelle
IPC分类号： A61K31/551 , A61K31/55 , A61P19/02 , A61P1/18 , A61P29/00 , A61P35/02 , A61P1/04 , A61P37/00 , A61P1/16 , A61P25/00 , A61P17/06 , A61P37/06 , C07D487/04 , A61P1/00
CPC分类号： C07D243/12 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/06139 , C07K5/0821
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.
摘要翻译： 本发明涉及作为白介素-1和bgr的抑制剂的新型化合物。 转化酶。 本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗IL-1，细胞凋亡，IGIF和IFN-γ介导的疾病，炎性疾病，自身免疫性疾病 破坏性骨病，增殖性疾病，感染性疾病，退行性疾病和坏死性疾病。 本发明还涉及使用本发明的化合物和组合物来抑制ICE活性，用于治疗白细胞介素-1，细胞凋亡，IGIF和IFN-γ介导的疾病以及减少IGIF和IFN-γ产生的方法。 本发明还涉及制备N-酰基氨基化合物的方法。
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公开(公告)号：US20120077830A1
公开(公告)日：2012-03-29
申请号：US13309117
申请日：2011-12-01
IPC分类号： A61K31/517 , A61P29/00 , C07D239/80
CPC分类号： C07D209/48 , C07D209/46 , C07D213/64 , C07D215/227 , C07D217/24 , C07D239/36 , C07D239/80 , C07D239/88 , C07D239/90 , C07D471/04 , C07D495/04
摘要： This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.
摘要翻译： 本发明提供可用作半胱天冬酶抑制剂的新化合物及其药学上可接受的衍生物。 这些化合物具有通式I：其中R 1，R 2和R 3如本文所述，环A包含0至2个双键，每个X独立地选自氮或碳，环A中的至少一个X为氮， 环A如所述任选被取代，并且可以与含有0至3个杂原子的饱和或不饱和的5至7元环稠合，并且条件是当X 3是碳时，X 3上的取代基被除氮以外的原子连接。
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公开(公告)号：US20120071657A1
公开(公告)日：2012-03-22
申请号：US13094183
申请日：2011-04-26
申请人： David Bebbington , Ronald Knegtel , Hayley Binch , Julian M.C. Golec , Pan Li , Jean-Damien Charrier
发明人： David Bebbington , Ronald Knegtel , Hayley Binch , Julian M.C. Golec , Pan Li , Jean-Damien Charrier
IPC分类号： C07D403/12 , C07D401/12
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D403/14 , 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 triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.
摘要翻译： 本发明描述了式IX的新型三唑化合物：其中Z1是氮或CR9，Z2是氮或CH，条件是Z1和Z2中的至少一个是氮; G是环C或环D; 环C选自苯基，吡啶基，嘧啶基，哒嗪基，吡嗪基或1,2,4-三嗪基，其中所述环C具有一个或两个独立地选自-R 1的邻位取代基; 环D是选自芳基，杂芳基，杂环基或碳环基的5-7元单环或8-10元双环; Rx和Ry独立地选自T-R3，或Rx和Ry与它们的插入原子一起形成稠环; R1，R3和T如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为GSK-3和Aurora的抑制剂，用于治疗诸如糖尿病，癌症和阿尔茨海默病的疾病。
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公开(公告)号：US20110060013A1
公开(公告)日：2011-03-10
申请号：US12601026
申请日：2009-11-20
申请人： Michael Paul Mortimore , Christopher John Davis , Julian M.C. Golec , John Studley , Daniel David Robinson
发明人： Michael Paul Mortimore , Christopher John Davis , Julian M.C. Golec , John Studley , Daniel David Robinson
IPC分类号： A61K31/4439 , C07D401/14 , C07D417/14 , A61P35/00
CPC分类号： C07D401/14 , 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：US20100222367A1
公开(公告)日：2010-09-02
申请号：US12774376
申请日：2010-05-05
IPC分类号： A61K31/497 , A61K31/4965 , A61P35/00
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。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US20100215772A1
公开(公告)日：2010-08-26
申请号：US12598276
申请日：2009-10-30
IPC分类号： A61K33/24 , C07D239/46 , A61K31/495 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/513 , A61P35/00
CPC分类号： C07D403/12 , 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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