公开(公告)号：US20170088527A1

公开(公告)日：2017-03-30

申请号：US15372077

申请日：2016-12-07

Applicant: Gilead Sciences, Inc.

Inventor： Michael Graupe ,  Yafan Lu ,  Jeff Zablocki

IPC: C07D261/20 ,  C07D417/12 ,  C07D471/04 ,  C07D413/12 ,  C07D413/14

CPC classification number: C07D261/20 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D498/04

Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein X, Y, Z, R2, R3, R4, p and q are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

公开(公告)号：US20160130300A1

公开(公告)日：2016-05-12

申请号：US14996961

申请日：2016-01-15

Applicant: Gilead Sciences, Inc.

Inventor： Kyla Bjornson ,  Eda Canales ,  Jeromy J. Cottell ,  Kapil K. Karki ,  Ashley A. Katana ,  Darryl Kato ,  Tetsuya Kobayashi ,  John O. Link ,  Ruben Martinez ,  Barton W. Phillips ,  Hyung-jung Pyun ,  Michael Sangi ,  Adam J. Schrier ,  Dustin Siegel ,  James G. Taylor ,  Chinh V. Tran ,  Teresa A. Trejo Martin ,  Randall W. Vivian ,  Zheng-Yu Yang ,  Jeff Zablocki ,  Sheila Zipfel

IPC: C07K5/083 ,  C07K5/087

Abstract: Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.

Abstract translation: 公开的式I化合物及其药学上可接受的盐。 还公开了使用所述化合物和含有所述化合物的药物组合物的方法。

公开(公告)号：US20150250805A1

公开(公告)日：2015-09-10

申请号：US14659042

申请日：2015-03-16

Applicant: Gilead Sciences, Inc.

Inventor： Carina E. Cannizzaro ,  Michael Graupe ,  Juan A. Guerrero ,  Yafan Lu ,  Robert G. Strickley ,  Chandrasekar Venkataramani ,  Jeff Zablocki

IPC: A61K31/675 ,  A61K31/4418

CPC classification number: A61K31/675 ,  A61K31/4418 ,  C07D213/64 ,  C07F9/58

Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.

Abstract translation: 公开了具有式（I）结构的新化合物：其可用于治疗依赖于成瘾物质的哺乳动物，例如对多巴胺产生剂如可卡因，吗啡，苯丙胺，尼古丁和/或醇的成瘾。 还公开了包含治疗有效量的式（I）化合物和使用式（I）化合物治疗对多巴胺生成剂成瘾的方法的药物组合物。

公开(公告)号：US20150239904A1

公开(公告)日：2015-08-27

申请号：US14630519

申请日：2015-02-24

Applicant: GILEAD SCIENCES, INC.

Inventor： Britton Kenneth Corkey ,  Elfatih Elzein ,  Robert H. Jiang ,  Rao V. Kalla ,  Dmitry Koltun ,  Xiaofen Li ,  Ruben Martinez ,  Eric Q. Parkhill ,  Thao Perry ,  Jeff Zablocki ,  Chandrasekar Venkataramani ,  Michael Graupe ,  Juan Guerrero

IPC: C07D498/04 ,  C07D413/14 ,  C07D413/12 ,  C07D267/14 ,  C07D413/04

CPC classification number: C07D498/04 ,  C07D267/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14

Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Abstract translation: 本公开涉及作为钠通道抑制剂的化合物及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的用途。 在具体实施方案中，化合物的结构由式I给出：其中Y，Z，n，R 1和R 3如本文所述，涉及化合物的制备和使用方法以及含有该化合物的药物组合物。

公开(公告)号：US08865739B2

公开(公告)日：2014-10-21

申请号：US14101813

申请日：2013-12-10

Applicant: Gilead Sciences, Inc.

Inventor： Matthew Abelman ,  Robert H. Jiang ,  Jeff Zablocki

IPC: C07D215/54 ,  C07D401/06 ,  C07D215/38 ,  C07D413/04 ,  C07D215/18 ,  C07D215/14

CPC classification number: C07D215/54 ,  C07D215/14 ,  C07D215/18 ,  C07D215/38 ,  C07D401/06 ,  C07D413/04

Abstract: The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.

Abstract translation: 本发明涉及式（I）的钠通道抑制剂：其中R1，R2，R3，R4，R5，X，Y和Z如本文所定义，以及它们在治疗各种疾病状态中的用途，包括 心血管疾病和糖尿病。 本发明还涉及制备化合物的方法以及含有这些化合物的药物组合物。

公开(公告)号：US20140296246A1

公开(公告)日：2014-10-02

申请号：US14227736

申请日：2014-03-27

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Gregory Chin ,  Britton Kenneth Corkey ,  Jinfa Du ,  Kristyna Elbel ,  Robert H. Jiang ,  Tetsuya Kobayashi ,  Ruben Martinez ,  Samuel E. Metobo ,  Michael R. Mish ,  Sophie Shevick ,  David Sperandio ,  Hai Yang ,  Jeff Zablocki

IPC: C07D413/14 ,  C07D413/04

CPC classification number: C07D413/14 ,  C07D413/04 ,  C07D417/14

Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, and X are described herein.

Abstract translation: 本申请涉及可用作含溴结构域的蛋白质（包括含溴结构域蛋白质的蛋白质4（BRD4））的抑制剂或其它方式调节其含有活性的蛋白质的化学化合物，以及含有这些化合物的组合物和制剂，以及 使用和制造这些化合物。 化合物包括其中R1a，R1b，R2a，R2b，R3和X在本文中描述的式（I）的化合物。

公开(公告)号：US20140213539A1

公开(公告)日：2014-07-31

申请号：US13970372

申请日：2013-08-19

Applicant: Gilead Sciences, Inc.

Inventor： Jeff Zablocki ,  Elfatih Elzein ,  Robert Seemayer ,  Travis Lemons

IPC: C07H19/16

CPC classification number: C07H19/16 ,  C07H19/167

Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.

Abstract translation: 公开了适用于大规模生产A2A腺苷受体激动剂的合成物，还涉及该化合物的多晶型物以及分离特定多晶型物的方法。

公开(公告)号：US20140051668A1

公开(公告)日：2014-02-20

申请号：US13966029

申请日：2013-08-13

Applicant: Gilead Sciences, Inc.

Inventor： Carina E. Cannizzaro ,  Michael Graupe ,  Juan A. Guerrero ,  Yafan Lu ,  Robert G. Strickley ,  Chandrasekar Venkataramani ,  Jeff Zablocki

IPC: C07F9/58 ,  C07D213/64

CPC classification number: A61K31/675 ,  A61K31/4418 ,  C07D213/64 ,  C07F9/58

Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.

Abstract translation: 公开了具有式（I）结构的新化合物：其可用于治疗依赖于成瘾物质的哺乳动物，例如对多巴胺产生剂如可卡因，吗啡，苯丙胺，尼古丁和/或醇的成瘾。 还公开了包含治疗有效量的式（I）化合物和使用式（I）化合物治疗对多巴胺生成剂成瘾的方法的药物组合物。

公开(公告)号：US20130197001A1

公开(公告)日：2013-08-01

申请号：US13677058

申请日：2012-11-14

Applicant: GILEAD SCIENCES, INC.

Inventor： Dmitry Koltun ,  Eric Parkhill ,  Jeff Zablocki

IPC: A61K31/498

CPC classification number: A61K31/498 ,  C07D241/44

Abstract: The present invention relates to compounds that are late sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein R1, R2, R3, and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Abstract translation: 本发明涉及晚期钠通道抑制剂及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的化合物。 在具体实施方案中，化合物的结构由式（I）给出：其中R 1，R 2，R 3和R 4如本文所述，用于制备和使用化合物的方法以及含有该化合物的药物组合物。

公开(公告)号：US20130096122A1

公开(公告)日：2013-04-18

申请号：US13706786

申请日：2012-12-06

Applicant: Gilead Sciences, Inc.

Inventor： Matthew Abelman ,  Nancy Chu ,  Robert H. Jiang ,  Kwan Leung ,  Jeff Zablocki

IPC: C07D471/04 ,  C07D401/06 ,  C07D413/06 ,  C07D215/227 ,  C07D417/06

CPC classification number: C07D401/06 ,  C07D215/227 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04

Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.

Abstract translation: 本发明涉及式I的钠通道抑制剂：其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如上所定义，并且用于治疗各种疾病状态，包括心血管疾病和糖尿病 。