公开(公告)号：US10519146B2

公开(公告)日：2019-12-31

申请号：US15984855

申请日：2018-05-21

申请人： Amgen Inc.

发明人： Brian Alan Lanman ,  Jian Chen ,  Anthony B. Reed ,  Victor J. Cee ,  Longbin Liu ,  David John Kopecky ,  Patricia Lopez ,  Ryan Paul Wurz ,  Thomas T. Nguyen ,  Shon Booker ,  Nobuko Nishimura ,  Youngsook Shin ,  Nuria A. Tamayo ,  John Gordon Allen ,  Jennifer Rebecca Allen

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D403/04 ,  C07D401/04 ,  C07D475/00 ,  A61K31/496 ,  A61K31/519 ,  A61P35/00 ,  C07D417/04 ,  A61K38/07 ,  C07D487/08 ,  C07D417/12 ,  C07D513/04 ,  C07D487/10 ,  C07D239/80 ,  C07D401/14 ,  C07D237/34 ,  A61K31/416 ,  A61K31/55 ,  A61K31/454 ,  A61K31/517 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/7068 ,  C07D275/04

摘要： Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US10328078B2

公开(公告)日：2019-06-25

申请号：US15545152

申请日：2016-01-22

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： Thomas D. Bannister ,  Hui Wang ,  Chao Wang ,  John L. Cleveland

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61K31/155 ,  A61K31/525 ,  A61K31/4985 ,  C07D475/02 ,  C07D475/00 ,  A61P37/06

摘要： The invention provides compounds effective as inhibitors of monocarboxylate transporters such as MCT1 and MCT4, which can be used for treatment of medical conditions wherein treatment of the condition with a compound having an inhibitor effect on MCT1, MCT4, or both is medically indicated. Compounds of the invention can have antitumor, antidiabetes, anti-inflammatory, or immunosuppressive pharmacological effects, and can be effective for treatment of cancer and of type II diabetes.

公开(公告)号：US20190152974A1

公开(公告)日：2019-05-23

申请号：US16162887

申请日：2018-10-17

申请人： Gilead Sciences, Inc.

发明人： Piet André Maurits Maria HERDEWIJN ,  Steven Cesar Alfons DE JONGHE ,  William John WATKINS ,  Lee Shun CHONG

IPC分类号： C07D475/02 ,  C07D475/08 ,  C07D475/00 ,  C07D475/04 ,  C07D475/06

摘要： The invention provides 4,6-di- and 2,4,6-tri-substituted pteridine derivatives with a specific substitution pattern which exhibit a significant and selective activity against certain types of viral infections, in particular selectively inhibit replication of Flaviridae such as the hepatitis C virus, and are useful for the prevention and treatment of such viral infections.

公开(公告)号：US10272087B2

公开(公告)日：2019-04-30

申请号：US15203424

申请日：2016-07-06

申请人： ASTEX THERAPEUTICS LIMITED

发明人： Gordon Saxty ,  Christopher Charles Frederick Hamlett ,  Valerio Berdini ,  Christopher William Murray ,  Patrick René Angibaud ,  Olivier Alexis Georges Querolle ,  Virginie Sophie Poncelet

IPC分类号： C07D475/00 ,  A61K31/519 ,  A61K45/06

摘要： The invention relates to new pteridine derivative compounds, of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

公开(公告)号：US20190071415A1

公开(公告)日：2019-03-07

申请号：US16167091

申请日：2018-10-22

申请人： Dana-Farber Cancer Institute, Inc.

发明人： James Bradner ,  Dennis Buckley ,  Georg Winter

IPC分类号： C07D401/04 ,  C07J43/00 ,  C07D495/14 ,  C07D487/04 ,  C07D471/04 ,  C07D401/14 ,  C07D471/14 ,  C07D475/00

摘要： The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.

公开(公告)号：US10221154B2

公开(公告)日：2019-03-05

申请号：US15222523

申请日：2016-07-28

申请人： BLUEPRINT MEDICINES CORPORATION

发明人： Neil Bifulco, Jr. ,  Lucian V. DiPietro ,  Brian L. Hodous ,  Chandrasekhar V. Miduturu

IPC分类号： C07D405/12 ,  C07D409/12 ,  A61K31/517 ,  C07D401/04 ,  C07D239/84 ,  C07D403/12 ,  C07D471/04 ,  C07D475/00 ,  C07D401/12 ,  C07D235/30 ,  C07D403/14

摘要： Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

公开(公告)号：US20180022749A1

公开(公告)日：2018-01-25

申请号：US15426208

申请日：2017-02-07

申请人： Boehringer Ingelheim International GmbH

发明人： Johanna BAKONYI ,  Steven Richard BRUNETTE ,  Delphine COLLIN ,  Robert Owen HUGHES ,  Xiang LI ,  Shuang LIANG ,  Robert SIBLEY ,  Michael Robert TURNER ,  Lifen WU ,  Qiang ZHANG

IPC分类号： C07D475/00 ,  C07D487/04 ,  C07D475/10 ,  A61K31/33

CPC分类号： C07D475/00 ,  A61K31/33 ,  C07D475/10 ,  C07D487/04

摘要： The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.

公开(公告)号：US20180009779A1

公开(公告)日：2018-01-11

申请号：US15632023

申请日：2017-06-23

申请人： Dana-Farber Cancer Institute, Inc.

发明人： James Bradner ,  Dennis Buckley ,  Georg Winter

IPC分类号： C07D401/04 ,  C07D495/14 ,  C07D487/04 ,  C07D475/00 ,  C07D471/04 ,  C07J43/00 ,  C07D401/14

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D475/00 ,  C07D487/04 ,  C07D495/14 ,  C07J43/003

摘要： The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.

公开(公告)号：US09598415B2

公开(公告)日：2017-03-21

申请号：US15270029

申请日：2016-09-20

申请人： Boehringer Ingelheim International GmbH

发明人： Johanna Bakonyi ,  Steven Richard Brunette ,  Delphine Collin ,  Robert Owen Hughes ,  Xiang Li ,  Shuang Liang ,  Robert Sibley ,  Michael Robert Turner ,  Lifen Wu ,  Qiang Zhang

IPC分类号： C07D475/00

CPC分类号： C07D475/00 ,  A61K31/33 ,  C07D475/10 ,  C07D487/04

摘要： The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.

公开(公告)号：US20170008894A1

公开(公告)日：2017-01-12

申请号：US15270029

申请日：2016-09-20

申请人： Boehringer Ingelheim International GmbH

发明人： Johanna BAKONYI ,  Steven Richard BRUNETTE ,  Delphine COLLIN ,  Robert Owen HUGHES ,  Xiang LI ,  Shuang LIANG ,  Robert SIBLEY ,  Michael Robert TURNER ,  Lifen WU ,  Qiang ZHANG

IPC分类号： C07D475/00

CPC分类号： C07D475/00 ,  A61K31/33 ,  C07D475/10 ,  C07D487/04

摘要： The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.

摘要翻译： 其中本文所定义的变量适用于RORγ的调节和与RORγ调节有关的疾病的治疗。 本发明还包括制备式（I）化合物和含有它们的药物制剂的方法。