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公开(公告)号：US08415381B2
公开(公告)日：2013-04-09
申请号：US12843494
申请日：2010-07-26
申请人： Paul A. Barsanti , Cheng Hu , Jeff Jin , Robert Keyes , Robert Kucejko , Xiaodong Lin , Yue Pan , Keith B. Pfister , Martin Sendzik , James Sutton , Lifeng Wan
发明人： Paul A. Barsanti , Cheng Hu , Jeff Jin , Robert Keyes , Robert Kucejko , Xiaodong Lin , Yue Pan , Keith B. Pfister , Martin Sendzik , James Sutton , Lifeng Wan
CPC分类号： A61K31/497 , C07D213/74 , C07D241/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.
摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，对映体，立体异构体，旋转异构体，互变异构体，非对映体或其外消旋物。 还提供了治疗由CDK9介导的疾病或病症的方法。
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公开(公告)号：US20120064032A1
公开(公告)日：2012-03-15
申请号：US13209147
申请日：2011-08-12
IPC分类号： A61K31/166 , A61K31/381 , A61K31/4025 , A61K31/704 , A61K31/519 , A61K31/407 , A61K39/395 , A61K31/513 , A61K31/522 , A61K33/24 , A61K38/50 , A61K38/21 , A61K38/20 , A61P35/00 , A61P35/02 , A61K31/343
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：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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25.发明授权6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling 有权6-O-取代的苯并恶唑和苯并噻唑化合物以及抑制CSF-1R信号传导的方法公开(公告)号：US07553854B2
公开(公告)日：2009-06-30
申请号：US11737069
申请日：2007-04-18
申请人： James C Sutton , Marion Wiesmann , Weibo Wang , Mika Lindvall , Jiong Lan , Savithri Ramurthy , Anu Sharma , Elizabeth J. Mieuli , Liana M. Klivansky , William Lenahan , Susan Kaufman , Hong Yang , Simon C. Ng , Keith Pfister , Allan S. Wagman , Victoria Sung , Martin Sendzik
发明人： James C Sutton , Marion Wiesmann , Weibo Wang , Mika Lindvall , Jiong Lan , Savithri Ramurthy , Anu Sharma , Elizabeth J. Mieuli , Liana M. Klivansky , William Lenahan , Susan Kaufman , Hong Yang , Simon C. Ng , Keith Pfister , Allan S. Wagman , Victoria Sung , Martin Sendzik
IPC分类号： C07D215/00 , A61K31/44
CPC分类号： C07D413/12 , C07D417/12
摘要： Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.
摘要翻译： 公开了苯并恶唑和苯并噻唑化合物及其立体异构体，互变异构体，溶剂合物，氧化物，酯和前药及其药学上可接受的盐。 还公开了单独或与至少一种另外的治疗剂组合的化合物与药学上可接受的载体的组合，以及化合物单独或与至少一种另外的治疗剂组合的用途。 这些实施方案可用于抑制细胞增殖，抑制肿瘤的生长和/或复分解，治疗或预防癌症，治疗或预防退行性骨疾病如类风湿性关节炎和/或抑制分子如CSF-1R。
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26.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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27.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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28.发明授权公开(公告)号：US09434719B2
公开(公告)日：2016-09-06
申请号：US14408418
申请日：2014-03-12
申请人： Thomas Raymond Caferro , Zhuoliang Chen , Young Shin Cho , Abran Q. Costales , Julian Roy Levell , Gang Liu , James R. Manning , Martin Sendzik , Cynthia Shafer , Michael David Shultz , James Sutton , Yaping Wang , Qian Zhao
发明人： Thomas Raymond Caferro , Zhuoliang Chen , Young Shin Cho , Abran Q. Costales , Julian Roy Levell , Gang Liu , James R. Manning , Martin Sendzik , Cynthia Shafer , Michael David Shultz , James Sutton , Yaping Wang , Qian Zhao
IPC分类号： C07D413/04 , A61K31/506 , C07D413/14 , C07D417/14 , A61K31/5377
CPC分类号： C07D413/14 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D413/04 , C07D417/14
摘要： The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are 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.
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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：US20140288076A1
公开(公告)日：2014-09-25
申请号：US14295398
申请日：2014-06-04
申请人： Paul A. Barsanti , Cheng Hu , Jeff Jin , Robert Keyes , Robert Kucejko , Xiaodong Lin , Yue Pan , Keith B. Pfister , Martin Sendzik , James Sutton , Lifeng Wan
发明人： Paul A. Barsanti , Cheng Hu , Jeff Jin , Robert Keyes , Robert Kucejko , Xiaodong Lin , Yue Pan , Keith B. Pfister , Martin Sendzik , James Sutton , Lifeng Wan
IPC分类号： C07D409/14 , C07D401/14 , C07D405/14 , C07D401/04
CPC分类号： A61K31/497 , C07D213/74 , C07D241/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.
摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，对映体，立体异构体，旋转异构体，互变异构体，非对映体或其外消旋物。 还提供了治疗由CDK9介导的疾病或病症的方法。
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