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公开(公告)号：US10772874B2
公开(公告)日：2020-09-15
申请号：US16538208
申请日：2019-08-12
申请人： Forma TM, LLC , Genentech, Inc.
发明人： Kenneth W. Bair , Timm R. Baumeister , Alexandre J. Buckmelter , Karl H. Clodfelter , Peter Dragovich , Francis Gosselin , Bingsong Han , Jian Lin , Dominic J. Reynolds , Bruce Roth , Chase C. Smith , Zhongguo Wang , Po-Wai Yuen , Xiaozhang Zheng
IPC分类号： C07D491/048 , C07D487/04 , A61K31/4355 , A61K31/4365 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K45/06
摘要： The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号：US10730889B2
公开(公告)日：2020-08-04
申请号：US15936086
申请日：2018-03-26
申请人： Forma TM, LLC , Genentech, Inc.
发明人： Kenneth W. Bair , Timm R. Baumeister , Peter Dragovich , Xiongcai Liu , Snahel Patel , Po-Wai Yuen , Mark Zak , Guiling Zhao , Yamin Zhang , Xiaozhang Zheng
IPC分类号： C07D519/00 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , A61K31/438 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K31/444 , A61K31/4545 , A61K31/506 , A61K31/513
摘要： Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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公开(公告)号：US10729738B2
公开(公告)日：2020-08-04
申请号：US15293743
申请日：2016-10-14
申请人： Genentech, Inc.
发明人： Peter Dragovich , Zhonghua Pei , Thomas Pillow , Jack Sadowsky , Jinhua Chen , John Wai
IPC分类号： A61K38/05 , A61K47/54 , A61K47/68 , A61K47/64 , A61K47/55 , A61K31/5365 , A61K31/5517
摘要： The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.
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公开(公告)号：US20200038378A1
公开(公告)日：2020-02-06
申请号：US16590329
申请日：2019-10-01
发明人： ANDREW P. CREW , Jing Wang , Michael Berlin , Peter Dragovich , Huifen Chen , Leanna Staben
IPC分类号： A61K31/427 , A61K31/4035 , A61K31/4439 , A61K31/437 , A61K31/4245 , A61K31/541 , A61K31/496 , A61K47/54
摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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公开(公告)号：US20190105307A1
公开(公告)日：2019-04-11
申请号：US16212360
申请日：2018-12-06
申请人： Forma TM, LLC , Genentech, Inc.
发明人： Kenneth W. Bair , Timm R. Baumeister , Alexandre J. Buckmelter , Karl H. Clodfelter , Peter Dragovich , Francis Gosselin , Bingsong Han , Jian Lin , Dominic J. Reynolds , Bruce Roth , Chase C. Smith , Zhongguo Wang , Po-Wai Yuen , Xiaozhang Zheng
IPC分类号： A61K31/4355 , A61K31/496 , A61K31/4365 , A61K31/437 , A61K31/497 , A61K31/519 , C07D471/04 , A61K31/55 , C07D487/04 , C07D491/048 , A61K45/06 , C07D495/04 , C07D491/04 , A61K31/5377
CPC分类号： A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:
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公开(公告)号：US10035801B2
公开(公告)日：2018-07-31
申请号：US14775405
申请日：2014-03-13
发明人： Brian K. Albrecht , Steven F. Bellon , Victor S. Gehling , Jean-Christophe Harmange , Kwong Wah Lai , Jun Liang , Peter Dragovich , Daniel F. Ortwine , Sharada Labadie , Birong Zhang , James Richard Kiefer
IPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61K31/5377 , A61K31/337 , A61K31/517 , A61K31/437 , C12N9/99 , C07D498/04 , C07D487/14
CPC分类号： C07D487/04 , A61K31/337 , A61K31/437 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D487/14 , C07D498/04 , C12N9/99
摘要： Provided are compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.
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公开(公告)号：US10017577B2
公开(公告)日：2018-07-10
申请号：US15181618
申请日：2016-06-14
申请人： Genentech, Inc.
CPC分类号： C07K16/30 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6889 , A61K2039/505 , C07K16/28 , C07K16/2803 , C07K16/3015 , C07K16/3023 , C07K16/3092 , C07K16/32 , C07K16/40 , C07K2317/515
摘要： The invention provides immunoconjugates and methods of using the same.
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公开(公告)号：US09822129B2
公开(公告)日：2017-11-21
申请号：US14382210
申请日：2013-03-01
申请人： GENENTECH,INC. , FORMA TM, LLC , Po-Wai Yuen
发明人： Kenneth W Bair , Timm R Baumeister , Peter Dragovich , Xiongcai Liu , Snahel Patel , Po-Wai Yuen , Mark Zak , Guiling Zhao , Yamin Zhang , Xiaozhang Zheng
IPC分类号： C07D519/00 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , A61K31/438 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K45/06
CPC分类号： C07D519/00 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04
摘要： Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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公开(公告)号：US20170095570A1
公开(公告)日：2017-04-06
申请号：US15281830
申请日：2016-09-30
申请人： Genentech, Inc.
IPC分类号： A61K47/48 , A61K45/06 , C07K16/32 , A61K31/5517
CPC分类号： A61K45/06 , A61K31/5517 , A61K47/6803 , A61K47/6851 , A61K47/6855 , A61K47/6889 , C07D519/00 , C07K16/2803 , C07K16/32 , C07K2317/40 , C07K2317/522 , C07K2317/567
摘要： The invention provides antibody-drug conjugates comprising an antibody conjugated to a pyrrolobenzodiazepine drug moiety via a disulfide linker, pyrrolobenzodiazepine linker-drug intermediates, and methods of using the antibody-drug conjugates.
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公开(公告)号：US20160060267A1
公开(公告)日：2016-03-03
申请号：US14775405
申请日：2014-03-13
发明人： Brian K. Albrecht , Steven F. Bellon , Victor S. Gehling , Jean-Christophe Harmange , Kwong Wah Lai , Jun Liang , Peter Dragovich , Dan Ortwine , Sharada Labadie , Birong Zhang , Jim Kiefer
IPC分类号： C07D487/04 , A61K45/06 , C12N9/99 , A61K31/337 , A61K31/517 , A61K31/437 , A61K31/519 , A61K31/5377
CPC分类号： C07D487/04 , A61K31/337 , A61K31/437 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D487/14 , C07D498/04 , C12N9/99
摘要： Provided are compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.
摘要翻译： 提供了可用作一种或多种组蛋白脱甲基酶抑制剂的化合物，例如KDM5。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用本发明组合物治疗各种疾病的方法。
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