公开(公告)号：US20180230157A1

公开(公告)日：2018-08-16

申请号：US15898095

申请日：2018-02-15

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Gediminas Brizgys ,  Elbert Chin ,  Cheinhung Chou ,  Jeromy J. Cottell ,  John O. Link ,  James G. Taylor ,  winston C. Tse ,  Nathan E. Wright ,  Zheng-Yu Yang ,  Jennifer R. Zhang ,  Sheila M. Zipfel

IPC: C07D487/04

CPC classification number: C07D487/04 ,  A61P29/00 ,  C07D453/00 ,  C07D519/00

Abstract: Provided is a compound of Formula (I) wherein the variable groups are defined herein.

公开(公告)号：US09951043B2

公开(公告)日：2018-04-24

申请号：US14771779

申请日：2014-02-28

Applicant: Gilead Sciences, Inc.

Inventor： Gediminas Brizgys ,  Eda Canales ,  Chien-hung Chou ,  Michael Graupe ,  Randall L. Halcomb ,  Yunfeng Eric Hu ,  Scott E. Lazerwith ,  John O. Link ,  Qi Liu ,  Yafan Lu ,  Roland D. Saito ,  Scott D. Schroeder ,  John R. Somoza ,  Winston C. Tse ,  Jennifer R. Zhang

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

CPC classification number: 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

Abstract: 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：US20170152240A1

公开(公告)日：2017-06-01

申请号：US15429086

申请日：2017-02-09

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Gayatri Balan ,  Chien-Hung Chou ,  Christopher T. Clark ,  Jeromy J. Cottell ,  Musong Kim ,  Thorsten A. Kirschberg ,  John O. Link ,  Gary Phillips ,  Scott D. Schroeder ,  Neil H. Squires ,  Kirk L. Stevens ,  James G. Taylor ,  William J. Watkins ,  Nathan E. Wright ,  Sheila M. Zipfel

IPC: C07D401/14

CPC classification number: C07D498/04 ,  C07B59/002 ,  C07B2200/05 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04

Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.

公开(公告)号：US20160368918A1

公开(公告)日：2016-12-22

申请号：US15150038

申请日：2016-05-09

Applicant: Gilead Sciences, Inc.

Inventor： Peter Blomgren ,  Jayaraman Chandrasekhar ,  Kevin S. Currie ,  Zhimin Du ,  Julie Farand ,  Juan A. Guerrero ,  Ashley A. Katana ,  Darryl Kato ,  Jeffrey Kropf ,  Scott E. Lazerwith ,  Seung H. Lee ,  Jiayao Li ,  John O. Link ,  Jennifer R. Lo ,  Nicholas Mai ,  Scott A. Mitchell ,  Gregory Notte ,  Hyung-jung Pyun ,  Michael Sangi ,  Aaron C. Schmitt ,  Adam J. Schrier ,  Kirk L. Stevens ,  Chandrasekar Venkataramani ,  William J. Watkins ,  Jin Ming Xiong ,  Jianjun Xu ,  Zheng-Yu Yang ,  Jeff Zablocki ,  Zhongdong Zhao ,  Sheila Zipfel

IPC: C07D471/04 ,  C07D403/14 ,  C07D401/14 ,  C07D519/00 ,  C07D487/04 ,  C07D498/04 ,  C07D413/14 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D403/12 ,  C07D491/08

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: 其中X1，X2，X3，R2，R3，R4，R5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：US20160362416A1

公开(公告)日：2016-12-15

申请号：US15246074

申请日：2016-08-24

Applicant: Gilead Sciences, Inc.

Inventor： John O. Link ,  Jeromy J. Cottell ,  Teresa Alejandra Trejo Martin ,  Elizabeth M. Bacon

IPC: C07D491/052 ,  A61K31/4188 ,  A61K45/06

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

Abstract: 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：US20160361375A1

公开(公告)日：2016-12-15

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: A61K38/06

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.

Abstract translation: 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：US09376441B2

公开(公告)日：2016-06-28

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 ,  Jennifer R. Lo ,  Seung H. Lee ,  Zhongdong Zhao ,  Jeffrey Kropf ,  Jianjun Xu ,  Peter Blomgren ,  Scott A. Mitchell ,  JinMing Xiong ,  Jayaraman Chandrasekhar

IPC: A61K31/4015 ,  C07D207/12 ,  C07D487/04 ,  C07D401/14 ,  C07D403/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D407/14 ,  C07D417/14

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：US09376392B2

公开(公告)日：2016-06-28

申请号：US14370464

申请日：2013-01-03

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Kyla L. Bjornson ,  Paul Hrvatin ,  Eric Lansdon ,  John O. Link ,  Hongtao Liu ,  Ryan McFadden ,  Michael L. Mitchell ,  Yingmei Qi ,  Paul A. Roethle ,  Lianhong Xu

IPC: C07D215/227 ,  A61K31/4704 ,  C07D519/00 ,  A61K31/4745 ,  C07D491/06 ,  A61K45/06 ,  A61K31/4741 ,  A61K31/497 ,  A61K31/506

CPC classification number: C07D215/227 ,  A61K31/4704 ,  A61K31/4741 ,  A61K31/4745 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  C07D491/06 ,  C07D519/00

Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.

Abstract translation: 本发明提供其化合物及其盐，如本文。 本发明还提供了包含本文公开的化合物的药物组合物，用于制备本文公开的化合物的方法，用于制备本文公开的化合物的中间体和治疗HIV感染的治疗方法，治疗HIV病毒的增殖，治疗AIDS或延迟 使用本文公开的化合物在哺乳动物中的AIDS或ARC症状。

公开(公告)号：US20160083395A1

公开(公告)日：2016-03-24

申请号：US14957988

申请日：2015-12-03

Applicant: Gilead Sciences, Inc.

Inventor： John O. Link ,  Jeromy J. Cottell ,  Teresa Alejandra Trejo Martin ,  Elizabeth M. Bacon

IPC: C07D491/052 ,  A61K45/06 ,  A61K31/4188

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

Abstract: 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：US09233974B2

公开(公告)日：2016-01-12

申请号：US13830346

申请日：2013-03-14

Applicant: Gilead Sciences, Inc.

Inventor： John O. Link ,  Jeromy J. Cottell ,  Teresa Alejandra Trejo Martin ,  Elizabeth M. Bacon

IPC: C07D491/052 ,  A61K31/352 ,  A61K31/4188 ,  A61K31/7056 ,  A61K31/7068 ,  A61K31/7072 ,  A61K38/21 ,  C07D491/04

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

Abstract: 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.