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![Solid forms of (4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl) piperazine-1-yl)(1-hydroxycyclopropyl)methanone](/abs-image/US/2022/03/08/US11267805B2/abs.jpg.150x150.jpg)
公开(公告)号：US11267805B2
公开(公告)日：2022-03-08
申请号：US17006317
申请日：2020-08-28
发明人： George P. Luke , Stephen Hubbs , Matthew W. Martin , Shawn E. R. Schiller , Robert Wenslow , Yawei Shi , Jun Huang
IPC分类号： C07D403/10 , A61K31/665
摘要： The present disclosure reports solid forms of (4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone:
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公开(公告)号：US11254674B2
公开(公告)日：2022-02-22
申请号：US16946159
申请日：2020-06-08
发明人： Shawn E. R. Schiller , Torsten Herbertz , Hongbin Li , Bradford Graves , Steven Mischke , Angela West , Jennifer R. Downing , Anna Ericsson
IPC分类号： C07D471/04
摘要： The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
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公开(公告)号：US10913753B2
公开(公告)日：2021-02-09
申请号：US16077407
申请日：2017-02-13
发明人： David Joseph Guerin , Kenneth W. Bair , Justin A. Caravella , Stephanos Ioannidis, Jr. , David R. Lancia, Jr. , Hongbin Li , Steven Mischke , Pui Yee Ng , David Richard , Shawn E. R. Schiller , Tatiana Shelekhin , Zhongguo Wang
IPC分类号： C07D519/00 , C07D495/04
摘要： The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: where R1, R2, R3, R4, R5, R5′, R6, R7, X, m, and n are described herein.
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公开(公告)号：US09388161B2
公开(公告)日：2016-07-12
申请号：US14546775
申请日：2014-11-18
发明人： Kenneth W. Bair , Torsten Herbertz , Goss S. Kauffman , Katherine J. Kayser-Bricker , George P. Luke , Matthew W. Martin , David S. Millan , Shawn E. R. Schiller , Adam C. Talbot
IPC分类号： C07D401/14 , A61K31/4709 , C07D401/04 , A61K31/5377 , A61K31/517 , C07D487/04 , A61K31/519 , A61K45/06
CPC分类号： C07D487/04 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/5377 , A61K45/06 , C07D215/20 , C07D215/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/14 , C07D471/04 , C07D473/28 , A61K2300/00
摘要： The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I: wherein W, X, Y, Z, R1, R2, R5, and R8 are as described herein.
摘要翻译： 本发明涉及可用于治疗癌症，炎性疾病，糖尿病和肥胖症的溴和额外末端（BET）溴结构域的抑制剂，其具有式I：其中W，X，Y，Z，R 1，R 2，R 5 ，和R8如本文所述。
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公开(公告)号：US11787803B2
公开(公告)日：2023-10-17
申请号：US17669135
申请日：2022-02-10
发明人： Shawn E. R. Schiller , Torsten Herbertz , Hongbin Li , Bradford Graves , Steven Mischke , Angela V. West , Jennifer R. Downing , Anna Ericsson
IPC分类号： C07D471/04 , C07D519/00 , A61P35/00
CPC分类号： C07D471/04 , A61P35/00 , C07D519/00
摘要： The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
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公开(公告)号：US10995078B2
公开(公告)日：2021-05-04
申请号：US15929751
申请日：2020-05-20
发明人： Kenneth W. Bair , David R. Lancia, Jr. , Hongbin Li , James Loch , Wei Lu , Matthew W. Martin , David S. Millan , Shawn E. R. Schiller , Mark J. Tebbe
IPC分类号： C07D295/192 , C07D401/04 , C07D403/04 , C07D405/12 , C07D413/12 , A61K31/4965 , A61P35/00 , A61K45/06 , C07D215/14 , C07D231/56 , C07D417/12 , C07D471/04 , C07D257/04 , C07D487/04 , C07D263/57 , C07D491/048 , C07D271/12 , C07D495/04 , C07D209/18 , C07D277/62 , C07D277/66 , C07D513/04 , C07D213/56 , C07D305/08 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/5025 , A61K31/506 , C07D209/08 , C07D213/65 , C07D213/69 , C07D217/16 , C07D231/12 , C07D235/08 , C07D417/04
摘要： The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号：US10472342B2
公开(公告)日：2019-11-12
申请号：US16383296
申请日：2019-04-12
发明人： Kenneth W. Bair , David R. Lancia, Jr. , Hongbin Li , James Loch , Wei Lu , Matthew W. Martin , David S. Millan , Shawn E. R. Schiller , Mark J. Tebbe
IPC分类号： C07D295/192 , A61K31/4965 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/12 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , C07D213/65 , C07D213/69 , C07D213/56 , C07D231/12 , C07D235/08 , C07D209/08 , C07D209/18 , C07D263/57 , C07D277/66 , C07D277/62 , C07D271/12 , C07D513/04 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K45/06 , C07D217/16 , A61K31/5025 , A61K31/506 , C07D305/08 , C07D257/04 , C07D417/12 , C07D231/56 , C07D215/14
摘要： The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号：US10399951B2
公开(公告)日：2019-09-03
申请号：US16119962
申请日：2018-08-31
发明人： Kenneth W. Bair , David R. Lancia, Jr. , Hongbin Li , James Loch , Wei Lu , Matthew W. Martin , David S. Millan , Shawn E. R. Schiller , Mark J. Tebbe
IPC分类号： C07D295/192 , A61K31/4965 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D491/048 , C07D495/04 , C07D213/65 , C07D213/69 , C07D213/56 , C07D231/12 , C07D235/08 , C07D209/08 , C07D209/18 , C07D263/57 , C07D271/12 , C07D277/66 , C07D277/62 , C07D513/04 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K45/06 , C07D215/14 , C07D231/56 , C07D257/04 , C07D487/04 , C07D305/08 , A61K31/5025 , A61K31/506 , C07D217/16
摘要： The present invention relates to compounds and compositions for inhibition of FASN, their synthesis, applications, and antidotes.
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公开(公告)号：US11292791B2
公开(公告)日：2022-04-05
申请号：US16647478
申请日：2018-09-14
发明人： Shawn E. R. Schiller , Torsten Herbertz , Hongbin Li , Bradford Graves , Steven Mischke , Angela V. West , Jennifer R. Downing , Anna Ericsson
IPC分类号： C07D471/04 , C07D519/00 , A61P35/00
摘要： The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
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公开(公告)号：US11111229B2
公开(公告)日：2021-09-07
申请号：US16774515
申请日：2020-01-28
发明人： Kenneth W. Bair , Torsten Herbertz , Goss S. Kauffman , Katherine J. Kayser-Bricker , George P. Luke , Matthew W. Martin , David S. Millan , Shawn E. R. Schiller , Adam C. Talbot
IPC分类号： C07D401/04 , C07D401/14 , A61K31/4709 , A61K45/06 , A61K31/47 , A61K31/497 , A61K31/506 , A61K31/5377 , C07D405/14 , C07D413/14 , C07D215/20 , C07D215/48 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/04 , C07D473/28 , C07D487/04 , A61K31/517 , A61K31/519 , A61K31/496 , A61K31/501 , A61K31/52 , C07D401/12 , C07D405/04 , C07D417/10
摘要： The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I: wherein W, X, Y, Z, R1, R2, R5, and R8 are as described herein.
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