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公开(公告)号：US11739069B2
公开(公告)日：2023-08-29
申请号：US16658245
申请日：2019-10-21
发明人： Minna D. Balbas , Michael J. Evans , Charles L. Sawyers , Yang Shen , David Hosfield , Geoffrey L. Greene
IPC分类号： C07D401/04 , C07D233/86 , C07D235/02
CPC分类号： C07D401/04 , C07D233/86 , C07D235/02
摘要： The present invention provides compounds useful as modulators, agonists or antagonists of androgen receptor (AR), compositions thereof, and methods of making and using the same.
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公开(公告)号：US20230210778A1
公开(公告)日：2023-07-06
申请号：US17985235
申请日：2022-11-11
发明人： Douglas Alan Lorenz , Sanjay Konagurthu , Randy J. Wald , Jason A. Everett , Sheila Matz , Yuuki Takaishi , Toshiro Sakai , Ryousuke Irie , Shinsuke Oba , Hiroyasu Toyota , Koji Nishimura , Atsushi Kanbayashi
IPC分类号： A61K9/20 , C07D233/86 , A61K9/10 , A61K31/4166 , A61K47/32 , A61K47/38 , A61K9/16 , A61K31/4164
CPC分类号： A61K9/2054 , C07D233/86 , A61K9/10 , A61K31/4166 , A61K47/32 , A61K47/38 , A61K9/16 , A61K9/1652 , A61K9/2095 , A61K31/4164
摘要： This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.
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公开(公告)号：US20180346461A1
公开(公告)日：2018-12-06
申请号：US16048191
申请日：2018-07-27
申请人： Arvinas, Inc.
发明人： Andrew P. Crew , Hanqing Dong , Jing Wang , Xin Chen , Yimin Qian , Kurt Zimmermann , Craig M. Crews , Michael Berlin , Lawrence Snyder
IPC分类号： C07D417/14 , A61P25/28 , A61P35/00 , C07K5/078 , C07D413/14 , C07D417/12 , C07D471/10 , C07D491/107 , C07D401/04 , C07D233/86 , C07D413/12 , A61K45/06
CPC分类号： C07D417/14 , A61K45/06 , A61P25/28 , A61P35/00 , C07D233/86 , C07D401/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/10 , C07D491/107 , C07K5/06165
摘要： The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.
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公开(公告)号：US20180282288A1
公开(公告)日：2018-10-04
申请号：US15764231
申请日：2016-09-29
发明人： Cheryl A. GRICE , Micah NIPHAKIS , Todd K. JONES
IPC分类号： C07D233/80
CPC分类号： C07D233/80 , C07D233/86
摘要： Provided herein are lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitors, pharmaceutical compositions of said inhibitors, and methods of their use for the treatment of disease.
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公开(公告)号：US20180086718A1
公开(公告)日：2018-03-29
申请号：US15655458
申请日：2017-07-20
发明人： Charles L. Sawyers , Michael Jung , Charlie D. Chen , Samedy Ouk , Derek Welsbie , Chris Tran , John Wongvipat , Dongwon Yoo
IPC分类号： C07D235/02 , C07D471/10 , C07D233/74 , C07D233/86 , C07D233/70
CPC分类号： C07D235/02 , C07D233/70 , C07D233/74 , C07D233/86 , C07D471/10
摘要： The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
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公开(公告)号：US09895355B2
公开(公告)日：2018-02-20
申请号：US15411517
申请日：2017-01-20
发明人： Hejun Lu , Piaoyang Sun , Hongbo Fei , Hongjian Jiang , Haowei Wang , Qing Dong
IPC分类号： A61K31/4178 , A61K31/4166 , A61K31/4439 , A61K31/454
CPC分类号： A61K31/4178 , A61K31/4166 , A61K31/4439 , A61K31/454 , C07D233/86 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12
摘要： Methods for treating androgen receptor-mediated diseases, such as breast cancer, with imidazoline derivatives of formula (I) are provided:
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公开(公告)号：US20170342056A1
公开(公告)日：2017-11-30
申请号：US15606064
申请日：2017-05-26
IPC分类号： C07D403/04 , C07C309/29 , C07D231/22 , C07D233/86
CPC分类号： C07D403/04 , C07C309/29 , C07D231/22 , C07D233/86 , C07D401/14
摘要： Imidazolone and pyrazolone derivatives of formula (I) described herein exhibit human neutrophil elastase inhibitory properties and are useful for the therapy of diseases and conditions in which HNE is implicated.
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公开(公告)号：US20170217903A1
公开(公告)日：2017-08-03
申请号：US15417860
申请日：2017-01-27
发明人： Zhihui Qin , Manohar Ratnam
IPC分类号： C07D233/86 , C07D401/12 , C07F9/6506
CPC分类号： C07D233/86 , A61K31/4166 , A61K31/4178 , C07D401/12 , C07F9/6506
摘要： A novel class of drugs for treating androgen receptor (AR) positive cancer including prostate cancer and breast cancer are described. The drugs include the chemical scaffolds of a high affinity androgen receptor ligand and a histone deacetylase inhibitor. Also described are compositions including the novel drugs and methods of treating AR positive cancer using the compositions.
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公开(公告)号：US09611225B2
公开(公告)日：2017-04-04
申请号：US14606390
申请日：2015-01-27
IPC分类号： C07D233/86 , C07C231/12
CPC分类号： C07D233/86 , C07C231/12 , C07C237/30
摘要： The present invention provides an isopropanol solvate of enzalutamide. The present invention also provides a process for the preparation of androgen receptor antagonist. In particular, the present invention provides a process for the preparation of enzalutamide or its pharmaceutically acceptable salts, hydrates, solvates, polymorphs or intermediates thereof.
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公开(公告)号：US20160251316A1
公开(公告)日：2016-09-01
申请号：US15033093
申请日：2014-10-30
IPC分类号： C07D233/86 , C07C237/30 , C07C231/12
CPC分类号： C07D233/86 , C07C231/12 , C07C237/30
摘要： The present invention provides a process for the preparation of enzalutamide.
摘要翻译： 本发明提供了一种制备恩扎拉平的方法。
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