公开(公告)号：US20230013585A1

公开(公告)日：2023-01-19

申请号：US17331900

申请日：2021-05-27

Applicant: Gilead Sciences, Inc.

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

IPC: A61K31/4545 ,  A61K31/444 ,  A61K31/5386 ,  C07D471/04 ,  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.

公开(公告)号：US20220213091A1

公开(公告)日：2022-07-07

申请号：US17522628

申请日：2021-11-09

Applicant: Gilead Sciences, Inc.

Inventor： Gayatri Balan ,  Mark J. Bartlett ,  Jayaraman Chandrasekhar ,  Julian A. Codelli ,  John H. Conway ,  Jennifer L. Cosman ,  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 ,  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.

公开(公告)号：US20180148457A1

公开(公告)日：2018-05-31

申请号：US15825993

申请日：2017-11-29

Applicant: Gilead Sciences, Inc.

Inventor： Elfatih Elzein ,  Rao V. Kalla ,  Dmitry Koltun ,  Xiaofen Li ,  Eric Q. Parkhill ,  Thao Perry ,  Scott Preston Simonovich ,  Jeff Zablocki ,  Christopher Allen Ziebenhaus

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0031 ,  A61K9/0075 ,  A61K9/0095 ,  A61K9/02 ,  A61K9/10 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2846 ,  A61K9/2866 ,  A61K9/4866 ,  C07D487/08 ,  C07D491/08 ,  C07D519/00

Abstract: The present disclosure relates to compounds that are CaM Kinase inhibitors and to their use in the treatment of various disease states, including atrial fibrillation and myocardial infarction. In particular embodiments, the general structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, R5, R6, R9 and R10 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：US09655944B2

公开(公告)日：2017-05-23

申请号：US15185273

申请日：2016-06-17

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: A61K38/21 ,  A61K38/06 ,  C07D498/16 ,  A61K31/4985 ,  C07D498/22 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/519 ,  A61K45/06 ,  C07K5/087 ,  C07K5/08 ,  C07K5/083 ,  A61K38/00

CPC classification number: A61K31/498 ,  A61K31/10 ,  A61K31/401 ,  A61K31/4745 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K38/00 ,  A61K38/06 ,  A61K38/21 ,  A61K45/06 ,  C07D241/36 ,  C07D403/14 ,  C07D498/16 ,  C07D498/22 ,  C07K5/08 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0827 ,  A61K2300/00

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.

公开(公告)号：US09193694B2

公开(公告)日：2015-11-24

申请号：US14038646

申请日：2013-09-26

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: C07D243/14 ,  A61K31/5513 ,  C07D243/24 ,  C07D267/14 ,  C07D291/08 ,  C07D403/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D419/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

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：US20150175655A1

公开(公告)日：2015-06-25

申请号：US14412331

申请日：2013-07-02

Applicant: Gilead Sciences, Inc.

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

IPC: C07K5/08 ,  A61K38/06 ,  A61K45/06

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: 公开了式I的化合物，以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：US20150038488A1

公开(公告)日：2015-02-05

申请号：US14448160

申请日：2014-07-31

Applicant: Gilead Sciences, Inc.

Inventor： Kevin S. Currie ,  Zhimin Du ,  Julie Farand ,  Juan A. Guerrero ,  Ashley A. Katana ,  Darryl Kato ,  Scott E. Lazerwith ,  Jiayao Li ,  John O. Link ,  Nicholas Mai ,  Gregory Notte ,  Hyung-Jung Pyun ,  Michael Sangi ,  Aaron C. Schmitt ,  Adam J. Schrier ,  Kirk L. Stevens ,  Chandrasekar Venkataramani ,  William J. Watkins ,  Zheng-Yu Yang ,  Jeff Zablocki ,  Sheila Zipfel

IPC: C07D487/04 ,  C07D417/04 ,  C07D417/12 ,  C07D403/12 ,  C07D471/04 ,  C07D401/14

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D519/00

Abstract: 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 X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.

Abstract translation: 本公开涉及作为Syk抑制剂的化合物及其在治疗各种疾病状态（包括癌症和炎性病症）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X 1，X 2，X 3，R 2，R 3，R 4，R 5和Y如本文所述。 本公开进一步提供包含式I化合物或其药学上可接受的盐的药物组合物，以及使用这些化合物和组合物治疗由Syk介导的病症的方法。

公开(公告)号：US08927582B2

公开(公告)日：2015-01-06

申请号：US13828984

申请日：2013-03-14

Applicant: Gilead Sciences, Inc.

Inventor： Britton Corkey ,  Gregory Notte ,  Jeff Zablocki

IPC: A61K31/44 ,  C07D409/14

CPC classification number: C07D409/14

Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, R, R1, R2 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).

Abstract translation: 本发明涉及式（I）的化合物：其中X1，X2，X3，X4，X5，R，R1，R2如上定义。 这些化合物具有凋亡信号调节激酶（“ASK1”）抑制活性，因此可用于治疗ASK1介导的病症，包括自身免疫性疾病，炎性疾病，心血管疾病，糖尿病，糖尿病肾病，心肾肾病，包括 肾脏疾病，纤维化疾病，呼吸系统疾病，COPD，特发性肺纤维化，急性肺损伤，急性和慢性肝病和神经变性疾病。 本发明还涉及包含一种或多种式（I）化合物的药物组合物和制备式（I）化合物的方法。

公开(公告)号：US20140094460A1

公开(公告)日：2014-04-03

申请号：US14101740

申请日：2013-12-10

Applicant: Gilead Sciences, Inc.

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

IPC: C07D215/227

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：US08575353B2

公开(公告)日：2013-11-05

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: C07D213/62 ,  A61K31/47

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 a human 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：其可用于治疗人类依赖于成瘾物质，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。