公开(公告)号：US09045428B2

公开(公告)日：2015-06-02

申请号：US13960636

申请日：2013-08-06

Applicant: Gilead Sciences, Inc.

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

IPC: A01N43/40 ,  A61K31/44 ,  C07D409/00 ,  C07D411/00 ,  C07D213/80 ,  A61K31/435 ,  C07D211/90 ,  C07D215/54 ,  C07D311/74 ,  C07D311/94 ,  C07D401/04 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/147

CPC classification number: C07D213/80 ,  A61K31/435 ,  C07D211/90 ,  C07D215/54 ,  C07D311/74 ,  C07D311/94 ,  C07D401/04 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/147

Abstract: The present invention relates to novel heterocyclic compounds 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 Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.

Abstract translation: 本发明涉及新型杂环化合物及其在治疗各种疾病状态（包括心血管疾病和糖尿病）中的用途。 在具体实施方案中，化合物的结构由式（I）给出：其中Q1，Q2，R2，R3，R4，R5和R6如本文所述。 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：US09000015B2

公开(公告)日：2015-04-07

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: C07D213/62 ,  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：US20140336190A1

公开(公告)日：2014-11-13

申请号：US14273147

申请日：2014-05-08

Applicant: Gilead Sciences, Inc.

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

IPC: C07D471/04 ,  C07D413/14 ,  C07D417/14 ,  C07D413/04

CPC classification number: C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04

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, R2, R2b, R3, R4a, R4b, and R5 are described herein.

Abstract translation: 本申请涉及可用作抑制剂的化合物; 或其它可能调节含溴结构域的蛋白质（包括含有溴结构域的蛋白质4（BRD4））的活性，以及​​含有这些化合物的组合物和制剂，以及使用和制备这些化合物的方法。 化合物包括其中R1a，R1b，R2，R2b，R3，R4a，R4b和R5如本文所述的式（I）化合物。

公开(公告)号：US20140107155A1

公开(公告)日：2014-04-17

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

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：US08664379B2

公开(公告)日：2014-03-04

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 。

公开(公告)号：US20130203704A1

公开(公告)日：2013-08-08

申请号：US13791422

申请日：2013-03-08

Applicant: Gilead Sciences, Inc.

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

IPC: C07D213/64 ,  C07F9/58

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.

公开(公告)号：US20130184255A1

公开(公告)日：2013-07-18

申请号：US13789469

申请日：2013-03-07

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: C07D413/06 ,  C07D471/04

CPC classification number: C07D413/06 ,  A61K31/5513 ,  A61K31/553 ,  C07B59/002 ,  C07B2200/05 ,  C07D243/14 ,  C07D243/24 ,  C07D267/08 ,  C07D267/14 ,  C07D291/08 ,  C07D403/06 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D419/06 ,  C07D471/04 ,  C07D487/04 ,  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 Z1, Z2, Z3, Z4, X, Y, 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Z 1，Z 2，Z 3，Z 4，X，Y，R 2，R 3和R 4如本文所述，用于制备和使用该化合物的方法， 含有该组合物的药物组合物。

公开(公告)号：US20130123280A1

公开(公告)日：2013-05-16

申请号：US13666826

申请日：2012-11-01

Applicant: Gilead Sciences, Inc.

Inventor： Rao V. Kalla ,  Thao Perry ,  Elfatih Elzein ,  Vaibhav Varkhedkar ,  Xiaofen Li ,  Prabha N. Ibrahim ,  Venkata Palle ,  Dengming Xiao ,  Jeff Zablocki

IPC: C07D473/06 ,  C07D473/04

CPC classification number: C07D473/06 ,  A61K31/522 ,  C07D473/04

Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

Abstract translation: 公开了作为A2B腺苷受体拮抗剂的新型化合物，其可用于治疗各种疾病状态，包括哮喘和腹泻。

公开(公告)号：US20130102632A1

公开(公告)日：2013-04-25

申请号：US13706879

申请日：2012-12-06

Applicant: Gilead Sciences, Inc.

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

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

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：US12258346B2

公开(公告)日：2025-03-25

申请号：US18543272

申请日：2023-12-18

Applicant: Gilead Sciences, Inc.

Inventor： Gayatri Balan ,  Mark J. Bartlett ,  Jayaraman Chandrasekhar ,  Julian A Codelli ,  John H. Conway ,  Jennifer L Cosman Ellis ,  Rao V. Kalla ,  Zachary A Kasun ,  Musong Kim ,  Seung H. Lee ,  Jennifer R. Lo ,  Jennifer A. Loyer-Drew ,  Scott A. Mitchell ,  Thao D. Perry ,  Gary B. Phillips ,  Patrick J. Salvo ,  Sundaramoorthi Swaminathan ,  Joshua J. Van Veldhuizen ,  Suet C. Yeung ,  Jeff Zablocki

IPC: C07D471/04 ,  A61K31/437 ,  C07D519/00

Abstract: The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.