公开(公告)号：US20210122763A1

公开(公告)日：2021-04-29

申请号：US17253464

申请日：2019-06-20

申请人： Janssen Pharmaceutica NV

发明人： José Manuel Bartolomé-Nebreda ,  Andrés Avelino Trabanco-Suárez ,  Ana Isabel De Lucas Olivares ,  Francisca Delgado-Jiménez ,  Susana Conde-Ceide ,  Juan Antonio Vega Ramiro

IPC分类号： C07D498/04 ,  C07D491/056 ,  C07D491/048 ,  C07D513/04 ,  C07D405/14 ,  C07D491/052

摘要： The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations.

公开(公告)号：US10961252B2

公开(公告)日：2021-03-30

申请号：US16226378

申请日：2018-12-19

申请人： Achillion Pharmaceuticals, Inc.

发明人： Jason Allan Wiles ,  Avinash Phadke

IPC分类号： C07D401/14 ,  C07D491/056 ,  C07D401/04 ,  C07D401/06 ,  C07D239/94 ,  C07D417/12 ,  A61K31/454 ,  A61K45/06 ,  C07D403/12 ,  C07D487/08 ,  A61K31/662 ,  C07F9/38 ,  C07D403/04 ,  A61K31/517 ,  C07D403/14 ,  C07D417/14 ,  C07D451/02 ,  C07D471/02

摘要： Compounds, methods of use, and processes for making inhibitors of Complement Factor B are provided.

公开(公告)号：US10954220B2

公开(公告)日：2021-03-23

申请号：US16082659

申请日：2017-03-08

申请人： Raze Therapeutics, Inc.

发明人： Nello Mainolfi

IPC分类号： C07D405/12 ,  C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D491/056 ,  A61P35/00

摘要： The present invention provides compounds, compositions thereof, and methods of using the same.

公开(公告)号：US20210069203A1

公开(公告)日：2021-03-11

申请号：US17023597

申请日：2020-09-17

申请人： Vertex Pharmaceuticals Incorporated

发明人： John Patrick Maxwell ,  Paul S. Charifson ,  Qing Tang ,  Steven M. Ronkin ,  Katrina Lee Jackson ,  Albert Charles Pierce ,  David J. Lauffer ,  Pan Li ,  Simon Giroux ,  Jinwang Xu ,  Kevin Michael Cottrell ,  Mark A. Morris ,  Nathan D. Waal ,  John J. Court ,  Wenxin Gu ,  Hongbo Deng

IPC分类号： A61K31/5377 ,  C07D513/04 ,  A61K31/506 ,  A61K31/5386 ,  C07D241/40 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D498/08 ,  C07D413/04 ,  C07D241/44 ,  C07D491/052 ,  C07D241/42 ,  C07D271/12 ,  C07D401/12 ,  C07D413/14 ,  C07D491/056 ,  C07D491/08

摘要： The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：US10913732B2

公开(公告)日：2021-02-09

申请号：US16774596

申请日：2020-01-28

申请人： The University of Toledo

发明人： Isaac Schiefer ,  Zahoor Shah

IPC分类号： C07D413/06 ,  C07D491/048 ,  C07D491/056

摘要： Furoxan compounds, compositions comprising the same, and methods of making and using the same, are described.

公开(公告)号：US20210032202A1

公开(公告)日：2021-02-04

申请号：US16899931

申请日：2020-06-12

申请人： Novartis AG

发明人： Jan JIRICEK ,  Ravinder Reddy KONDREDDI ,  Paul William SMITH

IPC分类号： C07D209/42 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D491/056 ,  A61K31/404

摘要： A compound of Formula (1) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the transportation of essential molecules in the mmpL3 pathway: wherein R1, R2, R3, R4, R5 and R6 are as defined herein.

公开(公告)号：US20200377510A1

公开(公告)日：2020-12-03

申请号：US16887785

申请日：2020-05-29

申请人： Auransa Inc.

发明人： Andrew Asher PROTTER ,  Pek Yee LUM ,  Gregory R. LUEDTKE

IPC分类号： C07D491/056 ,  C07D405/10 ,  C07D211/94 ,  C07D401/06 ,  C07D403/06 ,  C07D401/12 ,  C07D223/10 ,  C07D405/06 ,  C07D405/14 ,  C07D403/14 ,  C07D401/14 ,  C07D405/12 ,  A61P35/00 ,  A61P37/02

摘要： The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer, reducing inflammation and/or treating an autoimmune or inflammatory disease.

公开(公告)号：US10786512B2

公开(公告)日：2020-09-29

申请号：US16282083

申请日：2019-02-21

申请人： Vertex Pharmaceuticals Incorporated

发明人： John Patrick Maxwell ,  Paul S. Charifson ,  Qing Tang ,  Steven M. Ronkin ,  Katrina Lee Jackson ,  Albert Charles Pierce ,  David J. Lauffer ,  Pan Li ,  Simon Giroux ,  Jinwang Xu ,  Kevin Michael Cottrell ,  Mark A. Morris ,  Nathan D. Waal ,  John J. Court ,  Wenxin Gu ,  Hongbo Deng

IPC分类号： A61K31/5377 ,  A61K31/506 ,  A61K31/5386 ,  C07D513/04 ,  C07D241/40 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D498/08 ,  C07D413/04 ,  C07D241/44 ,  C07D491/052 ,  C07D241/42 ,  C07D271/12 ,  C07D401/12 ,  C07D413/14 ,  C07D491/056 ,  C07D491/08

摘要： The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：US10774068B2

公开(公告)日：2020-09-15

申请号：US15738986

申请日：2016-06-24

申请人： The Scripps Research Institute ,  Universität Bremen

发明人： Hank Michael James Petrassi ,  Murali Mohan Reddy Peram Surakattula ,  Kathrin Maedler ,  Amin Ardestani ,  Jason T. Roland ,  Tyler D. Baguley ,  Matthew S. Tremblay ,  Weijun Shen ,  Peter G. Schultz ,  Arnab K. Chatterjee

IPC分类号： C07D401/12 ,  A61K31/47 ,  C12N9/12 ,  A61K31/517 ,  A61K31/4709 ,  C07D215/44 ,  C07D215/46 ,  C07D413/12 ,  C07D471/04 ,  C07D491/052 ,  C07D491/056

摘要： Disclosed herein are compounds, compositions, and methods of their use for the treatment of diabetes.

公开(公告)号：US20200216419A1

公开(公告)日：2020-07-09

申请号：US16799363

申请日：2020-02-24

申请人： Capella Therapeutics, Inc.

发明人： Yun Long

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D498/04 ,  A61K31/55 ,  C07D491/056 ,  A61P35/00

摘要： Provided herein are methods for treating, preventing, or ameliorating one or more symptoms of a condition, disorder, or disease mediated by a lipid kinase or a protein kinase with benzimidazoles, for example, of Formula I or II, and pharmaceutical compositions thereof. Also provided herein are benzimidazoles, and pharmaceutical compositions thereof; and methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.