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公开(公告)号：US20110021528A1
公开(公告)日：2011-01-27
申请号：US12896535
申请日：2010-10-01
IPC分类号： A61K31/166 , C07C237/42 , C07D209/18 , C07D333/38 , C07D213/82 , C07D215/48 , C07D277/56 , C07D213/56 , C07D207/327 , C07D217/16 , C07D401/04 , C07D241/44 , C07D295/185 , C07D417/06 , C07D405/12 , C07D307/85 , C07D405/06 , A61K31/404 , A61K31/381 , A61K31/465 , A61K31/47 , A61K31/426 , A61K31/4406 , A61K31/402 , A61K31/496 , A61K31/472 , A61K31/498 , A61K31/5375 , A61K31/5377 , A61K31/4025 , A61K31/343 , C07C233/69 , A61K31/195 , A61K31/24 , C07C231/02 , A61P35/00 , A61P35/02
CPC分类号： A61K31/343 , A61K31/18 , A61K31/33 , A61K31/34 , A61K31/4015 , A61K31/4415 , A61K41/00 , A61K45/06 , A61N5/10 , C07C259/10 , C07C2601/02 , C07D207/12 , C07D207/327 , C07D207/34 , C07D209/08 , C07D209/18 , C07D209/42 , C07D209/44 , C07D211/46 , C07D213/56 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/08 , C07D215/18 , C07D215/48 , C07D215/54 , C07D217/04 , C07D217/06 , C07D217/26 , C07D231/56 , C07D235/06 , C07D235/24 , C07D241/52 , C07D249/18 , C07D261/18 , C07D263/58 , C07D277/30 , C07D277/42 , C07D277/56 , C07D277/68 , C07D307/54 , C07D307/68 , C07D307/79 , C07D307/81 , C07D307/85 , C07D307/86 , C07D317/60 , C07D333/16 , C07D333/24 , C07D333/28 , C07D333/38 , C07D333/70 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/04 , C07D417/12 , A61K2300/00
摘要： The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
摘要翻译： 本发明涉及可用于治疗丙型肝炎的某些异羟肟酸衍生物。这些化合物也是组蛋白脱乙酰酶的抑制剂，因此可用于治疗与组蛋白脱乙酰酶活性相关的疾病。 还公开了制备这些化合物的药物组合物和方法。
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公开(公告)号：US20100029605A1
公开(公告)日：2010-02-04
申请号：US12444129
申请日：2007-09-24
申请人： Pamela Albaugh , Gregory S. Chopiuk , Qiang Ding , Shenlin Huang , Zuosheng Liu , Shifeng Pan , Pingda Ren , Xia Wang , Xing Wang , yongping Xie , Chengzhi Zhang , Qiong Zhang , Guobao Zhang , Daniel Poon , Paul Renhowe , Martin Sendzik
发明人： Pamela Albaugh , Gregory S. Chopiuk , Qiang Ding , Shenlin Huang , Zuosheng Liu , Shifeng Pan , Pingda Ren , Xia Wang , Xing Wang , yongping Xie , Chengzhi Zhang , Qiong Zhang , Guobao Zhang , Daniel Poon , Paul Renhowe , Martin Sendzik
IPC分类号： A61K31/506 , C07D413/14 , C07D403/14 , C07D403/04 , A61K31/5377 , A61K31/519
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.
摘要翻译： 本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，ARG，BCR异常活化的疾病或病症 -Abl，BRK，EphB，Fms，Fyn，KDR，c-Kit，LCK，PDGF-R，b-Raf，c-Raf，SAPK2，Src，Tie2和TrkB激酶。
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33.发明申请N-AZASPIROCYCLOALKANE SUBSTITUTED N-HETEROARYL COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2 审中-公开N-烷基环己烷取代的N-HETEROARYL化合物和组合物抑制SHP2的活性公开(公告)号：US20170015680A1
公开(公告)日：2017-01-19
申请号：US15110511
申请日：2015-01-16
申请人： Christine Hiu-Tung Chen , Zhuoliang Chen , Michael Dore , Jorge Garcia Fortanet , Rajesh Karki , Mitsunori Kato , Matthew J. LaMarche , Lawrence Blas Perez , Troy Douglas Smith , Sarah Williams , John William Giraldes , Martin Sendzik , Bakary-Barry Toure
发明人： Christine Hiu-Tung Chen , Zhuoliang Chen , Michael Dore , Jorge Garcia Fortanet , Rajesh Karki , Mitsunori Kato , Matthew J. LaMarche , Lawrence Blas Perez , Troy Douglas Smith , Sarah Williams , John William Giraldes , Martin Sendzik , Bakary-Barry Toure
IPC分类号： C07D498/10 , C07D403/04 , C07D471/10 , C07D491/107 , C07D495/10 , C07D401/04 , C07D401/14
CPC分类号： C07D498/10 , C07B2200/07 , C07D241/18 , C07D241/20 , C07D401/04 , C07D401/14 , C07D403/04 , C07D471/10 , C07D491/107 , C07D495/10
摘要： The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
摘要翻译： 其中p，q，Y1，Y2，R1，R2a，R2b，R3a，R3b，R4a，R4b，R5a，R5b，R7和R8定义在发明概述中; 能够抑制SHP2的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来管理与SHP2的异常活性相关的疾病或病症的方法。
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34.发明申请1-(TRIAZIN-3-YL/PYRIDAZIN-3-YL)-PIPER(-AZINE)IDINE DERIVATIVES AND COMPOSITIONS THEREFOR FOR INHIBITING THE ACTIVITY OF SHP2 有权哌啶衍生物及其组合物，用于抑制SHP2活性的1-（TRIAZIN-3-YL /吡啶-3-基）-PIPER公开(公告)号：US20170001975A1
公开(公告)日：2017-01-05
申请号：US15110504
申请日：2015-01-16
申请人： Zhuoliang CHEN , Michael DORE , Jorge Garcia FORTANET , Rajesh KARKI , Mitsunori KATO , Matthew J. LAMARCHE , Lawrence Blas PEREZ , Sarah WILLIAMS , Martin SENDZIK
发明人： Zhuoliang Chen , Michael Dore , Jorge Garcia Fortanet , Rajesh Karki , Mitsunori Kato , Matthew J. LaMarche , Lawrence Blas Perez , Sarah Williams , Martin Sendzik
IPC分类号： C07D401/04 , C07D401/14
CPC分类号： C07D401/04 , C07D241/26 , C07D249/14 , C07D401/14
摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
摘要翻译： 本发明涉及式I化合物：其中Y1，Y2，Y3，R1，R2a，R2b，R3a，R3b，R4a，R4b，R5a，R5b定义在发明概述中; 能够抑制SHP2的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来管理与SHP2的异常活性相关的疾病或病症的方法。
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公开(公告)号：US08865732B2
公开(公告)日：2014-10-21
申请号：US13396339
申请日：2012-02-14
申请人： Zilin Huang , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
发明人： Zilin Huang , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
IPC分类号： A61K31/505 , C07D241/02
CPC分类号： A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/5383 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04 , A61K2300/00
摘要： New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
摘要翻译： 提供了新的取代的杂环化合物，含有它们的组合物，以及使用它们来抑制Raf激酶活性的方法。 新化合物和组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗Raf激酶介导的病症，例如癌症。
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公开(公告)号：US08202876B2
公开(公告)日：2012-06-19
申请号：US12444129
申请日：2007-09-24
申请人： Pamela Albaugh , Gregory B. Chopiuk , Qiang Ding , Shenlin Huang , Zuosheng Liu , Shifeng Pan , Pingda Ren , Xia Wang , Xing Wang , Yongping Xie , Chengzhi Zhang , Qiong Zhang , Guobao Zhang , Daniel Poon , Paul Renhowe , Martin Sendzik
发明人： Pamela Albaugh , Gregory B. Chopiuk , Qiang Ding , Shenlin Huang , Zuosheng Liu , Shifeng Pan , Pingda Ren , Xia Wang , Xing Wang , Yongping Xie , Chengzhi Zhang , Qiong Zhang , Guobao Zhang , Daniel Poon , Paul Renhowe , Martin Sendzik
IPC分类号： C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D231/00 , C07D403/02 , A01N43/56 , A61K31/415
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.
摘要翻译： 本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，ARG，BCR异常活化的疾病或病症 -Abl，BRK，EphB，Fms，Fyn，KDR，c-Kit，LCK，PDGF-R，b-Raf，c-Raf，SAPK2，Src，Tie2和TrkB激酶。
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公开(公告)号：US08129394B2
公开(公告)日：2012-03-06
申请号：US12383035
申请日：2009-03-19
申请人： Zilin Hunag , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
发明人： Zilin Hunag , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
IPC分类号： A61K31/4965 , A61K31/505 , A01N43/54 , C07D403/00 , C07D401/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号： C07D498/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Novel imidazole compounds of the general formula are disclosed, wherein R1 and R2 comprise heteroaryl groups. These compounds and compositions containing them are useful in methods to treat Raf kinase-mediated disorders such as cancer.
摘要翻译： 公开了通式的新型咪唑化合物，其中R 1和R 2包含杂芳基。 这些含有它们的化合物和组合物可用于治疗Raf激酶介导的疾病如癌症的方法。
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公开(公告)号：US07420089B2
公开(公告)日：2008-09-02
申请号：US11834558
申请日：2007-08-06
IPC分类号： C07C259/04 , C07C239/00 , A61K31/215 , A61K31/19
CPC分类号： A61K31/343 , A61K31/18 , A61K31/33 , A61K31/34 , A61K31/4015 , A61K31/4415 , A61K41/00 , A61K45/06 , A61N5/10 , C07C259/10 , C07C2601/02 , C07D207/12 , C07D207/327 , C07D207/34 , C07D209/08 , C07D209/18 , C07D209/42 , C07D209/44 , C07D211/46 , C07D213/56 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/08 , C07D215/18 , C07D215/48 , C07D215/54 , C07D217/04 , C07D217/06 , C07D217/26 , C07D231/56 , C07D235/06 , C07D235/24 , C07D241/52 , C07D249/18 , C07D261/18 , C07D263/58 , C07D277/30 , C07D277/42 , C07D277/56 , C07D277/68 , C07D307/54 , C07D307/68 , C07D307/79 , C07D307/81 , C07D307/85 , C07D307/86 , C07D317/60 , C07D333/16 , C07D333/24 , C07D333/28 , C07D333/38 , C07D333/70 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/04 , C07D417/12 , A61K2300/00
摘要： The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
摘要翻译： 本发明涉及可用于治疗丙型肝炎的某些异羟肟酸衍生物。这些化合物也是组蛋白脱乙酰酶的抑制剂，因此可用于治疗与组蛋白脱乙酰酶活性相关的疾病。 还公开了制备这些化合物的药物组合物和方法。
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公开(公告)号：US20080004331A1
公开(公告)日：2008-01-03
申请号：US11834558
申请日：2007-08-06
申请人： Erik Verner , Martin Sendzik , Chitra Baskaran , Joseph Buggy , James Robinson
发明人： Erik Verner , Martin Sendzik , Chitra Baskaran , Joseph Buggy , James Robinson
IPC分类号： A61K31/4025 , A61K31/195 , A61K31/403 , A61K31/4523 , C07C229/02 , C07D307/78 , C07D333/52 , C07D405/12
CPC分类号： A61K31/343 , A61K31/18 , A61K31/33 , A61K31/34 , A61K31/4015 , A61K31/4415 , A61K41/00 , A61K45/06 , A61N5/10 , C07C259/10 , C07C2601/02 , C07D207/12 , C07D207/327 , C07D207/34 , C07D209/08 , C07D209/18 , C07D209/42 , C07D209/44 , C07D211/46 , C07D213/56 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/08 , C07D215/18 , C07D215/48 , C07D215/54 , C07D217/04 , C07D217/06 , C07D217/26 , C07D231/56 , C07D235/06 , C07D235/24 , C07D241/52 , C07D249/18 , C07D261/18 , C07D263/58 , C07D277/30 , C07D277/42 , C07D277/56 , C07D277/68 , C07D307/54 , C07D307/68 , C07D307/79 , C07D307/81 , C07D307/85 , C07D307/86 , C07D317/60 , C07D333/16 , C07D333/24 , C07D333/28 , C07D333/38 , C07D333/70 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/04 , C07D417/12 , A61K2300/00
摘要： The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
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40.发明授权公开(公告)号：US08957068B2
公开(公告)日：2015-02-17
申请号：US14347481
申请日：2012-09-26
申请人： Thomas Raymond Caferro , Young Shin Cho , Abran Q. Costales , Huangshu Lei , Francois Lenoir , Julian Roy Levell , Gang Liu , Mark G. Palermo , Keith Bruce Pfister , Martin Sendzik , Cynthia Shafer , Michael David Shultz , Troy Smith , James Clifford Sutton , Bakary-Barry Toure , Fan Yang , Qian Zhao
发明人： Thomas Raymond Caferro , Young Shin Cho , Abran Q. Costales , Huangshu Lei , Francois Lenoir , Julian Roy Levell , Gang Liu , Mark G. Palermo , Keith Bruce Pfister , Martin Sendzik , Cynthia Shafer , Michael David Shultz , Troy Smith , James Clifford Sutton , Bakary-Barry Toure , Fan Yang , Qian Zhao
IPC分类号： C07D413/04 , C07D413/14 , A61K31/506 , C07D487/04 , C07D471/04 , C07D487/08 , C07D417/14 , C07D498/10
CPC分类号： C07D413/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D498/10 , C07D513/04
摘要： The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中R 1 -R 6在本文中定义。 本发明还涉及含有式（I）化合物的组合物以及这些化合物在抑制具有新形态活性的突变体IDH蛋白质中的用途。 本发明还涉及式（I）化合物在治疗与这种突变体IDH蛋白相关的疾病或病症中的用途，包括但不限于细胞增殖病症如癌症。
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