公开(公告)号：US20240317729A1

公开(公告)日：2024-09-26

申请号：US18667078

申请日：2024-05-17

申请人： YALE UNIVERSITY ,  GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  CAMBRIDGE ENTERPRISE LIMITED

发明人： CRAIG M. CREWS ,  DENNIS BUCKLEY ,  ALESSIO CIULLI ,  WILLIAM L. JORGENSEN ,  PETER C. GAREISS ,  INGE VAN MOLLE ,  JEFFREY GUSTAFSON ,  HYUN-SEOP TAE ,  JULIEN MICHEL ,  DENTON WADE HOYER ,  ANKE G. ROTH ,  JOHN DAVID HARLING ,  IAN EDWARD DAVID SMITH ,  AFJAL HUSSAIN MIAH ,  SEBASTIEN ANDRE CAMPOS ,  JOELLE LE

IPC分类号： C07D413/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/54 ,  A61K47/55 ,  A61K47/64 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07J43/00 ,  C12N9/00

CPC分类号： C07D413/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/545 ,  A61K47/55 ,  A61K47/64 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07J43/003 ,  C12N9/93

摘要： The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. 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 a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

公开(公告)号：US12060333B2

公开(公告)日：2024-08-13

申请号：US17445989

申请日：2021-08-26

申请人： Hoffmann-La Roche Inc.

发明人： Chungen Liang ,  Hongying Yun ,  Weixing Zhang ,  Kun Miao ,  Jianguo Chen ,  Yao Wu

IPC分类号： C07D241/24 ,  C07C243/34 ,  C07C311/35 ,  C07D207/26 ,  C07D209/42 ,  C07D211/76 ,  C07D231/12 ,  C07D233/64 ,  C07D235/24 ,  C07D261/18 ,  C07D401/04 ,  C07D403/12 ,  C07D413/12

CPC分类号： C07D241/24 ,  C07C243/34 ,  C07C311/35 ,  C07D207/26 ,  C07D209/42 ,  C07D211/76 ,  C07D231/12 ,  C07D233/64 ,  C07D235/24 ,  C07D261/18 ,  C07D401/04 ,  C07D403/12 ,  C07D413/12

摘要： The present invention relates to compounds of formula (I),




wherein R1-R5 and L are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.

公开(公告)号：US11987554B2

公开(公告)日：2024-05-21

申请号：US18210555

申请日：2023-06-15

申请人： ACEA Therapeutics, Inc.

发明人： Long Mao ,  Xiao Xu ,  Namir Shaabani ,  Can Jin

IPC分类号： C07D207/26 ,  C07D207/416 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14

CPC分类号： C07D207/26 ,  C07D207/416 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14

摘要： Provided herein, inter alia, are compounds, pharmaceutical compositions and methods related to the treatment of viral infections caused by coronavirus or enterovirus. Provided herein are compounds of Formula (I), (II) and (III)




and methods of using the compounds for therapy. These compounds are peptidomimetics that inhibit protease 3CL of a coronavirus, and are useful for treating conditions caused by viral infections, including COVID-19.

公开(公告)号：US11786521B2

公开(公告)日：2023-10-17

申请号：US17503760

申请日：2021-10-18

申请人： University of Southern California

发明人： Thomas Chen

IPC分类号： A61K31/495 ,  C07D231/12 ,  A61K31/4188 ,  A61K47/54 ,  C07B59/00 ,  A61K31/4015 ,  A61K9/00 ,  A61K31/045 ,  A61K31/415 ,  C07D207/26 ,  C07C33/14 ,  C07D487/04 ,  A61K45/06 ,  A61N5/10 ,  A61K31/635 ,  A61K47/55 ,  A61K31/366

CPC分类号： A61K31/495 ,  A61K9/0043 ,  A61K31/045 ,  A61K31/366 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4188 ,  A61K31/635 ,  A61K45/06 ,  A61K47/54 ,  A61K47/542 ,  A61K47/543 ,  A61K47/55 ,  A61N5/10 ,  C07B59/00 ,  C07C33/14 ,  C07D207/26 ,  C07D231/12 ,  C07D487/04 ,  C07B2200/05 ,  C07C2601/16

摘要： The present methods treat neurofibromatosis by a administering to a subject perillyl alcohol or iso-perillyl alcohol. The present methods also treat neurofibromatosis by administering to a subject a carbamate of perillyl alcohol, or a carbamate of iso-perillyl alcohol. The perillyl alcohol carbamate may comprise perillyl alcohol conjugated with rolipram or temozolomide.

公开(公告)号：US20230322668A1

公开(公告)日：2023-10-12

申请号：US18210555

申请日：2023-06-15

申请人： ACEA Therapeutics, Inc.

发明人： Long Mao ,  Xiao Xu ,  Namir Shaabani ,  Can Jin

IPC分类号： C07D207/26 ,  C07D207/416 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14

CPC分类号： C07D207/26 ,  C07D207/416 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14

摘要： Provided herein, inter alia, are compounds, pharmaceutical compositions and methods related to the treatment of viral infections caused by coronavirus or enterovirus. Provided herein are compounds of Formula (I), (II) and (III)




and methods of using the compounds for therapy. These compounds are peptidomimetics that inhibit protease 3CL of a coronavirus, and are useful for treating conditions caused by viral infections, including COVID-19.

公开(公告)号：US11667673B2

公开(公告)日：2023-06-06

申请号：US16893750

申请日：2020-06-05

申请人： Servier Pharmaceuticals LLC

发明人： Janeta Popovici-Muller ,  Rene M. Lemieux ,  Jeremy Travins ,  Zhenwei Cai ,  Dawei Cui ,  Ding Zhou

IPC分类号： C07D401/14 ,  C07D401/04 ,  A61P35/00 ,  C07K5/065 ,  C07D207/26 ,  C07D205/08 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  A61K38/05 ,  A61K45/06 ,  A61K38/00 ,  C07K5/06 ,  C07D401/12

CPC分类号： C07K5/06078 ,  A61K38/005 ,  A61K38/05 ,  A61K45/06 ,  C07D205/08 ,  C07D207/26 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D401/12 ,  C07K5/06191

摘要： Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.

公开(公告)号：US10076519B2

公开(公告)日：2018-09-18

申请号：US15463288

申请日：2017-03-20

申请人： CYTOKINETICS, INC.

发明人： Luke W. Ashcraft ,  Gustave Bergnes ,  Scott Collibee ,  Chihyuan Chuang ,  Jeff Gardina ,  Bradley P. Morgan ,  Alex R. Muci ,  Xiangping Qian ,  Jeffrey Warrington ,  Zhe Yang ,  Pu-Ping Lu ,  Antonio Romero

IPC分类号： A61K31/501 ,  C07D403/02 ,  A61K31/50 ,  C07D237/06 ,  C07D231/56 ,  A61K31/16 ,  A61K31/166 ,  C07D213/16 ,  C07D207/26 ,  C07D211/76

CPC分类号： A61K31/50 ,  A61K31/16 ,  A61K31/166 ,  C07D207/26 ,  C07D211/76 ,  C07D213/16 ,  C07D231/56 ,  C07D237/06 ,  C07D237/20 ,  C07D237/24 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D405/14 ,  C07D409/14 ,  C07D411/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D487/10 ,  C07D513/04 ,  Y02A50/465

摘要： Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof.Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20180194802A1

公开(公告)日：2018-07-12

申请号：US15809325

申请日：2017-11-10

申请人： Agios Pharmaceuticals, Inc.

发明人： Janeta Popovici-Muller ,  Rene M. Lemieux ,  Jeremy Travins ,  Zhenwei Cai ,  Dawei Cui ,  Ding Zhou

IPC分类号： C07K5/065 ,  C07D401/04 ,  C07D417/04 ,  C07D413/04 ,  C07D403/04 ,  C07D401/14 ,  A61K38/00 ,  C07D207/26 ,  C07D205/08 ,  A61K45/06 ,  A61K38/05 ,  C07K5/06

CPC分类号： C07K5/06078 ,  A61K38/005 ,  A61K38/05 ,  A61K45/06 ,  C07D205/08 ,  C07D207/26 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07K5/06191

摘要： Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.

公开(公告)号：US09920044B2

公开(公告)日：2018-03-20

申请号：US14806360

申请日：2015-07-22

申请人： RADIUS HEALTH, INC.

发明人： Chris P. Miller

IPC分类号： C07D417/04 ,  G01N33/74 ,  C07D233/36 ,  C07D207/26 ,  C07D263/24 ,  C07D417/10

CPC分类号： C07D417/10 ,  C07D207/26 ,  C07D233/36 ,  C07D263/24 ,  C07D417/04 ,  G01N33/74 ,  G01N2333/70567

摘要： This invention provides compounds of formula I, pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds and intermediates useful in the preparation of same.

公开(公告)号：US20170369468A1

公开(公告)日：2017-12-28

申请号：US15694439

申请日：2017-09-01

申请人： The Regents of the University of California

发明人： Anandasankar Ray ,  Christine Krause Pham ,  Sean Michael Boyle

IPC分类号： C07D335/02 ,  C07D317/20 ,  C07D277/04 ,  C07D215/06 ,  C07D207/26 ,  C07D207/16 ,  C07C13/23 ,  C07C13/20 ,  A01N43/78 ,  A01N43/42 ,  A01N43/36 ,  A01N43/32 ,  A01N43/28 ,  A01N43/26 ,  A01N43/20 ,  A01N43/16 ,  A01N43/08 ,  A01N35/06 ,  A01N31/04 ,  A01N27/00 ,  C07D319/06 ,  C07C2601/16

CPC分类号： C07D335/02 ,  A01N27/00 ,  A01N31/04 ,  A01N35/06 ,  A01N43/08 ,  A01N43/16 ,  A01N43/20 ,  A01N43/26 ,  A01N43/28 ,  A01N43/32 ,  A01N43/36 ,  A01N43/42 ,  A01N43/78 ,  C07C13/20 ,  C07C13/23 ,  C07C2601/16 ,  C07D207/16 ,  C07D207/26 ,  C07D215/06 ,  C07D277/04 ,  C07D317/20 ,  C07D319/06

摘要： Compositions and methods for repelling arthropods. The compositions include a carrier and an arthropod repelling compound, which can be a compound discovered by a novel and complex cheminformatic process to demonstrate repellency behavior across a broad spectrum of arthropods. The compound can be a thiane compound, a pyrrolidone compound, a cyclohexadiene compound, a cyclohexenone compound, a cyclohexene compound, a furanone compound, a pyran compound, a tetrahydropyran compound, a thiazolidine compound, a thiazoline compound, a dihydrothiophene compound, a dithiolane compound, a dithiane compound, an epoxide compound, an oxathiane compound, a cyclopentene compound, a cyclohexane compound, a quinoline compound, an oxazoline compound, a tetrahydropyridine compound, and an imidazolidinone compound, or a combination thereof.