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21.发明授权Substituted 1, 4-thiazepine and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效取代的1,4-硫氮杂和类似物作为半胱天冬酶和凋亡诱导剂的活化剂及其用途公开(公告)号：US06861419B2
公开(公告)日：2005-03-01
申请号：US09836548
申请日：2001-04-18
申请人： John A. Drewe , Sui Xiong Cai , Emma Jane Shelton , Joane Litvak , David Sperandio , Jeffrey R. Spencer , Martin Sendzik
发明人： John A. Drewe , Sui Xiong Cai , Emma Jane Shelton , Joane Litvak , David Sperandio , Jeffrey R. Spencer , Martin Sendzik
IPC分类号： A61P35/00 , C07D281/06 , C07D281/10 , C07D405/04 , C07D417/04 , C07D417/14 , C07D513/04 , C07D513/14 , A61K31/55 , C07D281/02
CPC分类号： C07D417/14 , C07D281/06 , C07D281/10 , C07D405/04 , C07D417/04 , C07D513/04 , C07D513/14
摘要： The present invention is directed to substituted 1,4-thiazepine and analogs thereof, represented by the general Formula I: wherein the dashed lines, A1, A2, A3, X1 and R1 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of capases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译： 本发明涉及由通式I表示的取代的1,4-硫氮杂和其类似物：其中虚线A 1，A 2，A 3，X 1和R 3， 1>。 本发明还涉及发现具有式I的化合物是抑制剂的活化剂和凋亡诱导剂。 因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可用于诱导异常细胞发生不受控制的生长和扩散的各种临床病症中的细胞死亡。
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公开(公告)号：US20180186770A1
公开(公告)日：2018-07-05
申请号：US15736925
申请日：2016-06-15
申请人： Zhuoliang Chen , Jorge Garcia Fortanet , Andriana Jouk , Rajesh Karki , Matthew J. LaMarche , Gang Liu , Mark G. Palermo , Lawrence Blas Perez , Patrick James Sarver , Michael David Shultz , Martin Sendzik , Bakary-Barry Toure , Bing Yu
发明人： Zhuoliang Chen , Jorge Garcia Fortanet , Andriana Jouk , Rajesh Karki , Matthew J. LaMarche , Gang Liu , Mark G. Palermo , Lawrence Blas Perez , Patrick James Sarver , Michael David Shultz , Martin Sendzik , Bakary-Barry Toure , Bing Yu
IPC分类号： C07D401/14 , C07D491/107 , C07D498/10 , C07D471/10 , C07D401/04
CPC分类号： C07D401/14 , C07D401/04 , C07D471/10 , C07D491/107 , C07D498/10
摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2, R4a, R5b, R5a, R5b, R6a and R6b 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.
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公开(公告)号：US09580437B2
公开(公告)日：2017-02-28
申请号：US14977273
申请日：2015-12-21
申请人： Ho Man Chan , Xiang-Ju Justin Gu , Ying Huang , Ling Li , Yuan Mi , Wei Qi , Martin Sendzik , Yongfeng Sun , Long Wang , Zhengtian Yu , Hailong Zhang , Ji Yue (Jeff) Zhang , Man Zhang , Qiong Zhang , Kehao Zhao
发明人： Ho Man Chan , Xiang-Ju Justin Gu , Ying Huang , Ling Li , Yuan Mi , Wei Qi , Martin Sendzik , Yongfeng Sun , Long Wang , Zhengtian Yu , Hailong Zhang , Ji Yue (Jeff) Zhang , Man Zhang , Qiong Zhang , Kehao Zhao
IPC分类号： C07D487/04 , A61K31/519 , A61K31/541 , A61K31/551 , A61K45/06 , A61K31/5377
CPC分类号： A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/06 , C07D487/04
摘要： A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein R1, R2, R3, R4, R5, and n are as defined herein.
摘要翻译： 提供式（I）化合物或其药学上可接受的盐，其已被证明可用于治疗PRC2介导的疾病或病症：其中R1，R2，R3，R4，R5和n如所定义 这里。
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公开(公告)号：US20070293540A1
公开(公告)日：2007-12-20
申请号：US11830686
申请日：2007-07-30
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： A61K31/195 , A61K31/34 , A61K31/38 , A61K31/445 , A61P35/00 , C07C259/04 , C07D307/78 , C07D333/52 , C07D405/02
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：US10308660B2
公开(公告)日：2019-06-04
申请号：US15736989
申请日：2016-06-15
申请人： Zhuoliang Chen , Jorge Garcia Fortanet , Matthew J. LaMarche , Martin Sendzik , Victoriano Tamez, Jr. , Bing Yu
发明人： Zhuoliang Chen , Jorge Garcia Fortanet , Matthew J. LaMarche , Martin Sendzik , Victoriano Tamez, Jr. , Bing Yu
IPC分类号： C07D401/04 , C07D491/107 , C07D401/14 , A61P35/00
摘要： The present invention relates to compounds of formula I: in which X1, X2, X3, Y1, Y2, Y3, R1, R2, R3a, R4a, R4b, R5a, R5b, R6a and R6b 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.
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公开(公告)号：US10077276B2
公开(公告)日：2018-09-18
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 , C07D241/18 , C07D241/20 , C07D401/04 , C07D403/04 , C07D471/10 , C07D491/107 , C07D495/10 , C07D401/14
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.
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公开(公告)号：US20180251471A1
公开(公告)日：2018-09-06
申请号：US15736989
申请日：2016-06-15
申请人： Zhuoliang CHEN , Jorge Garcia FORTANET , Matthew J. LAMARCHE , Martin SENDZIK , Victoriano TAMEZ, JR. , Bing YU
发明人： Zhuoliang Chen , Jorge Garcia Fortanet , Matthew J. LaMarche , Martin Sendzik , Victoriano Tamez, JR. , Bing Yu
IPC分类号： C07D491/107 , C07D401/14 , C07D401/04 , A61P35/00
CPC分类号： C07D491/107 , A61P35/00 , C07D401/04 , C07D401/14
摘要： The present invention relates to compounds of formula I: in which X1, X2, X3, Y1, Y2, Y3, R1, R2, R3a, R4a, R4b, R5a, R5b, R6a and R6b 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.
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公开(公告)号：US09938295B2
公开(公告)日：2018-04-10
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 , 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.
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公开(公告)号：US20130210818A1
公开(公告)日：2013-08-15
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： A61K31/444 , A61K31/506 , C07D403/14 , C07D405/14 , A61K31/4439 , C07D417/14 , C07D471/04 , C07D413/14 , A61K31/496 , C07D487/04 , A61K31/4985 , C07D498/04 , A61K31/5383 , A61K31/4709 , A61K31/5377 , A61P35/00 , C07D401/14
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：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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