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公开(公告)号：US10023534B2
公开(公告)日：2018-07-17
申请号：US15521201
申请日：2015-10-23
IPC分类号： A61K31/403 , A61K31/4353 , C07D209/82 , C07D471/04 , C07D209/58 , C07D401/02 , C07D519/00 , A61K31/407 , A61K31/4035 , A61K31/437
摘要： Disclosed are compounds of Formula (I): or a salt thereof, wherein Q is: or; and X, R1a, R1b, R3, R4, and R5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号：US20170066740A1
公开(公告)日：2017-03-09
申请号：US15354613
申请日：2016-11-17
IPC分类号： C07D401/10
CPC分类号： C07D401/10 , C07D209/08 , C07D209/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10
摘要： Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译： 或其盐，其中：X为CR 4或N; R1，R2，R3，R4和A在本文中定义。 还公开了使用这种化合物作为Bruton酪氨酸激酶（Btk）的抑制剂的方法和包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。
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公开(公告)号：US20230322803A1
公开(公告)日：2023-10-12
申请号：US17913206
申请日：2021-03-22
发明人： Andrew P. Degnan , Godwin Kwame Kumi , Andrew J. Tebben , Audris Huang , Peter Kinam Park , Donna M. Bilder , Emily Charlotte Cherney , Ashok Vinayak Purandare
IPC分类号： C07D498/04 , C07D471/04 , C07D401/14
CPC分类号： C07D498/04 , C07D401/14 , C07D471/04
摘要： Disclosed are compounds of Formula (I) or a salt thereof, wherein Ring A is a carbon-linked ring; and Ring A, R1, and n are defined herein. Also disclosed are methods of using such compounds to inhibit Helios protein, and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
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公开(公告)号：US20160115126A1
公开(公告)日：2016-04-28
申请号：US14921347
申请日：2015-10-23
发明人： Qingjie Liu , Scott Hunter Watterson , Douglas G. Batt , Saleem Ahmad , Myra Beaudoin Bertrand , Hua Gong , Weiwei Guo , John E. Macor , Khehyong Ngu , Andrew J. Tebben , Joseph A. Tino
IPC分类号： C07D209/08 , C07D403/10 , C07D403/12 , C07D403/04 , C07D487/10 , C07D487/04 , C07D413/04 , C07D471/04 , C07D401/06 , C07D417/04 , C07D401/04 , C07D401/12
CPC分类号： C07D401/10 , C07D209/08 , C07D209/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10
摘要： Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译： 公开了式（I）的化合物或其盐，其中：X是CR 4或N; R1，R2，R3，R4和A在本文中定义。 还公开了使用这种化合物作为Bruton酪氨酸激酶（Btk）的抑制剂的方法和包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫性疾病和血管疾病）中的疾病或病症的进展。
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公开(公告)号：US10189840B2
公开(公告)日：2019-01-29
申请号：US15558692
申请日：2016-03-17
发明人： Hai-Yun Xiao , Murali T. G. Dhar , Jingwu Duan , Bin Jiang , Andrew J. Tebben
IPC分类号： C07D471/14 , C07D487/06 , A61P37/00 , A61P29/00
摘要： Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: (i) —(CR3R3)1-4—; (ii) —(CR3R3)x—Y—(CR3R3)y—; Or (iii) —Y—(CR3R3)2—Y—; and Y, R1, R2, R3, R5, R6, R8, x, and y are defined herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
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公开(公告)号：US20170355673A1
公开(公告)日：2017-12-14
申请号：US15521201
申请日：2015-10-23
IPC分类号： C07D209/58 , A61K31/4035 , C07D519/00 , A61K31/407 , A61K31/437 , C07D401/02 , C07D471/04
CPC分类号： C07D209/58 , A61K31/4035 , A61K31/407 , A61K31/437 , C07D401/02 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D519/00
摘要： Disclosed are compounds of Formula (I): or a salt thereof, wherein Q is: or; and X, R1a, R1b, R3, R4, and R5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号：US09802915B2
公开(公告)日：2017-10-31
申请号：US15354613
申请日：2016-11-17
IPC分类号： A01N43/00 , A61K31/397 , C07D401/10
CPC分类号： C07D401/10 , C07D209/08 , C07D209/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10
摘要： Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号：US09902740B2
公开(公告)日：2018-02-27
申请号：US15606512
申请日：2017-05-26
发明人： Yong Zhang , Robert M. Borzilleri , Andrew J. Tebben , Erik M. Stang , Andrew F. Donnell , Gretchen M. Schroeder , Heidi L. Perez , Donna D. Wei
IPC分类号： C07D519/00 , C07D498/22 , A61K47/48 , C07K16/30 , A61K31/5513 , A61K31/5517
CPC分类号： C07D498/22 , A61K31/5513 , A61K31/5517 , A61K47/48384 , A61K47/48569 , A61K47/48592 , A61K47/48615 , A61K47/48638 , A61K47/48715 , A61K47/6801 , A61K47/6803 , A61K47/6851 , A61K47/6857 , A61K47/6859 , A61K47/6863 , A61K47/6869 , A61K47/6889 , C07D519/00 , C07K16/30 , C07K16/3023 , C07K16/3046 , C07K16/3069
摘要： Macrocyclic benzodiazepine dimers having a structure represented by formula I where A and B are independently according to formulae Ia or Ib and the other variables in formulae I, Ia, and Ib are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used as the drug component in an antibody-drug conjugate (ADC).
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公开(公告)号：US09708316B2
公开(公告)日：2017-07-18
申请号：US14977709
申请日：2015-12-22
发明人： Brian E. Fink , Yufen Zhao , Robert M. Borzilleri , Liping Zhang , Kyoung S. Kim , Muthoni G. Kamau , Andrew J. Tebben , Yong Zhang , Andrew F. Donnell
IPC分类号： A61K31/4709 , A61K31/501 , C07D487/04 , C07D471/04 , A61K31/5377 , A61K31/437 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/541
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D487/04 , Y02P20/582
摘要： The invention relates generally to compounds that modulate the activity of TGFβR-1 and TGFβR-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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公开(公告)号：US20190292179A1
公开(公告)日：2019-09-26
申请号：US16316714
申请日：2017-07-19
发明人： Robert M. Borzilleri , Peiyung Liu , Andrew J. Tebben , Upender Velaparthi , Hasibur Rahaman , Gopikishan Tonukunuru , Jayakumar Sankara Warrier
IPC分类号： C07D471/04 , A61K31/437 , A61K31/5383 , A61K31/416 , A61K31/5025 , A61K39/395 , C07D403/04 , C07D487/04 , C07D498/04
摘要： The invention relates generally to compounds that modulate the activity of TGFβR-1 and TGFβR-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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