公开(公告)号：EP3404030A1

公开(公告)日：2018-11-21

申请号：EP18169933.1

申请日：2013-12-19

申请人： Gilead Sciences, Inc.

发明人： BACON, Elizabeth M ,  COTTELL, Jeromy J ,  LINK, John O. ,  TREJO MARTIN, Teresa Alejandra

IPC分类号： C07D491/04 ,  A61K31/4188 ,  A61P31/12

CPC分类号： C07D491/052 ,  A61K31/352 ,  A61K31/4188 ,  A61K31/7056 ,  A61K31/7068 ,  A61K31/7072 ,  A61K38/21 ,  A61K45/06 ,  C07D491/04

摘要： The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

公开(公告)号：EP3194402B1

公开(公告)日：2018-11-21

申请号：EP15778411.7

申请日：2015-09-14

申请人： Gilead Sciences, Inc.

发明人： ALLEN, Darin ,  BROWN, Brandon Heath ,  CHAO, Jessica Jade ,  HALCOMB, Randall L. ,  HRVATIN, Paul ,  MCFADDEN, Ryan ,  ROETHLE, Paul ,  RUDIO, Erwina ,  YANG, Hong ,  YU, Richard Hung Chiu

IPC分类号： C07D487/04 ,  C07D207/06 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/545

CPC分类号： C07D475/06 ,  C07D207/06 ,  C07D207/09 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/545 ,  C07D487/04

摘要： The present invention provides methods of preparing 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one and related compounds.

公开(公告)号：EP3186239B1

公开(公告)日：2018-10-10

申请号：EP15759599.2

申请日：2015-08-26

申请人： Gilead Sciences, Inc.

发明人： BRIZGYS, Gediminas ,  CANALES, Eda ,  HALCOMB, Randall, L. ,  HU, Yunfeng, Eric ,  KATO, Darryl ,  LINK, John, O. ,  LIU, Qi ,  SAITO, Roland, D. ,  TSE, Winston, C. ,  ZHANG, Jennifer, R.

IPC分类号： C07D401/14 ,  C07D471/04 ,  C07D403/14 ,  C07D405/14 ,  C07D493/04 ,  C07D413/14 ,  C07D498/04 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/437 ,  A61P31/18

CPC分类号： C07D401/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P31/18 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D493/04 ,  C07D498/04 ,  C07D519/00

摘要： Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

公开(公告)号：EP3355871A1

公开(公告)日：2018-08-08

申请号：EP16785022.1

申请日：2016-09-30

申请人： Gilead Sciences, Inc.

发明人： DI PAOLO, Julie ,  BRECKENRIDGE, David ,  BATES, Jamie ,  TUMAS, Daniel

IPC分类号： A61K31/00 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/519 ,  A61K31/522 ,  A61K31/5375 ,  A61K31/541 ,  A61K31/553 ,  A61P35/00 ,  A61P29/00

CPC分类号： A61K31/522 ,  A61K31/00 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/541 ,  A61K31/553 ,  A61K2300/00

摘要： Provided herein are methods that relate to a therapeutic strategy for treatment of cancer, and allergic, autoimmune, and inflammatory disorders including hematological malignancies. In particular, the methods include administration of a BTK inhibitor and with one or more inhibitor. For example, the one or more inhibitor may be a JAK inhibitor, a ASK1 inhibitor, a BRD4 inhitibor or an MMP9 inhibitor.

公开(公告)号：EP2961742B1

公开(公告)日：2018-08-01

申请号：EP14712844.1

申请日：2014-02-28

申请人： Gilead Sciences, Inc.

发明人： BRIZGYS, Gediminas ,  CANALES, Eda ,  CHOU, Chien-hung ,  GRAUPE, Michael ,  HU, Yunfeng, Eric ,  LINK, John, O. ,  LIU, Qi ,  LU, Yafan ,  SAITO, Roland, D. ,  SCHROEDER, Scott, D. ,  SOMOZA, John, R. ,  TSE, Winston, C. ,  ZHANG, Jennifer, R. ,  HALCOMB, Randall, L.

IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D471/04 ,  A61K31/496 ,  A61P31/14

CPC分类号： C07D401/12 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052

摘要： Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

公开(公告)号：EP3351552A1

公开(公告)日：2018-07-25

申请号：EP18155061.7

申请日：2013-03-11

申请人： Gilead Sciences, Inc.

发明人： CLARKE, Michael O' Neil Hanrahan

IPC分类号： C07H19/23 ,  A61K31/706 ,  A61P31/16

CPC分类号： C07H19/23 ,  A61K31/706 ,  A61K45/06 ,  C07H19/12

摘要： Provided are uses of compounds of Formula I,

as well as compounds of Formula I for use in methods for treating Orthomyxoviridae virus infections, particularly for the treatment of Human Influenza virus infections.

公开(公告)号：EP3342773A1

公开(公告)日：2018-07-04

申请号：EP18156034.3

申请日：2014-12-22

申请人： Gilead Sciences, Inc.

发明人： BLOMGREN, Peter A. ,  CURRIE, Kevin S. ,  KROPF, Jeffrey E. ,  LEE, Seung H. ,  LO, Jennifer R. ,  MITCHELL, Scott A. ,  SCHMITT, Aaron C. ,  XIONG, Jin-Ming ,  XU, Jianjun ,  ZHAO, Zhongdong ,  SWAMINATHAN, Sundaramoorthi

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P25/00

摘要： The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R 1 , R 2 , R 3 , and R 4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.

公开(公告)号：EP3154985B1

公开(公告)日：2018-06-06

申请号：EP15745599.9

申请日：2015-06-09

申请人： Gilead Sciences, Inc.

发明人： BACON, Elizabeth M. ,  COTTELL, Jeromy J. ,  LINK, John O. ,  TREJO MARTIN, Teresa Alejandra ,  ZIPFEL, Sheila

IPC分类号： C07D493/06 ,  A61K31/4178 ,  A61P31/14

CPC分类号： C07D493/06

摘要： The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

公开(公告)号：EP3252058A1

公开(公告)日：2017-12-06

申请号：EP17177433.4

申请日：2014-07-11

申请人： Gilead Sciences, Inc.

发明人： JI, Mingzhe ,  LAZERWITH, Scott E. ,  PYUN, Hyung-Jung

IPC分类号： C07D498/14 ,  C07D471/14 ,  A61K31/553 ,  A61K31/4995 ,  A61P31/18

CPC分类号： A61K31/4985 ,  A61K31/537 ,  A61K31/553 ,  A61K45/06 ,  C07D471/14 ,  C07D471/18 ,  C07D498/14 ,  C07D498/18

摘要： Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I):

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R 1 , X, Y 1 , Y 2 , or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

摘要翻译： 公开了用于治疗人免疫缺陷病毒（HIV）感染的化合物。 该化合物具有下式（I）：包括其立体异构体及其药学上可接受的盐，其中R 1，X，Y 1，Y 2或L如本文所定义。 还公开了与这些化合物的制备和使用有关的方法，以及包含这些化合物的药物组合物。

公开(公告)号：EP3246070A1

公开(公告)日：2017-11-22

申请号：EP17000383.4

申请日：2012-07-12

申请人： Gilead Sciences, Inc.

发明人： Kinzel, Olaf ,  Steeneck, Christoph ,  Kremoser, Claus

IPC分类号： A61P1/16 ,  A61P3/10 ,  A61P35/00 ,  A61K31/42 ,  C07D261/08 ,  C07D413/12 ,  C07D413/14

CPC分类号： A61K31/4439 ,  A61K31/42 ,  A61K31/422 ,  C07D261/08 ,  C07D413/12 ,  C07D413/14

摘要： The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

摘要翻译： 本发明涉及与NR1H4受体（FXR）结合并用作FXR激动剂的化合物。 本发明进一步涉及所述化合物在制备用于通过所述化合物结合所述核受体来治疗疾病和/或病症的药物中的用途以及用于合成所述化合物的方法。