公开(公告)号：US20240182476A1

公开(公告)日：2024-06-06

申请号：US18450646

申请日：2023-08-16

Applicant: GILEAD SCIENCES, INC. ,  CARNA BIOSCIENCES, INC.

Inventor： Masaaki Sawa ,  Mai Arai ,  Ryoko Nakai ,  Hirokazu Matsumoto ,  Catherine Pugh ,  Eric Hu ,  Juan Guerrero ,  Jesse Jacobsen ,  Jonathan William Medley ,  Jie Xu ,  Latesh Lad ,  Leena Patel ,  Michael Graupe ,  Qingming Zhu ,  Stephen Holmbo ,  Tetsuya Kobayashi ,  Will Watkins ,  Yasamin Moazami ,  Suet C. Yeung ,  Julian A. Codelli ,  Heath A. Weaver

IPC: C07D487/04 ,  A61K31/395 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/55 ,  A61K31/553 ,  A61K31/695 ,  A61K31/704 ,  A61K31/7068 ,  A61K35/15 ,  A61K35/17 ,  A61K39/395 ,  A61K45/06 ,  C07D519/00 ,  C07F7/18

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/55 ,  A61K31/553 ,  A61K31/5545 ,  A61K31/695 ,  A61K31/704 ,  A61K31/7068 ,  A61K35/15 ,  A61K35/17 ,  A61K39/3955 ,  A61K45/06 ,  C07D519/00 ,  C07F7/1804

Abstract: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.

公开(公告)号：US11753399B2

公开(公告)日：2023-09-12

申请号：US17584643

申请日：2022-01-26

Applicant: Gilead Sciences, Inc.

Inventor： Gediminas Brizgys ,  Eda Canales ,  Chienhung Chou ,  Michael Graupe ,  Jiayao Li ,  Roland D. Saito ,  Scott D. Schroeder ,  Winston C. Tse ,  Qiaoyin Wu ,  Jennifer R. Zhang

IPC: C07D401/14 ,  A61P31/18 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D401/14 ,  A61P31/18 ,  C07D405/14 ,  C07D413/14

Abstract: The invention provides compounds having Formula (I):




or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising the same, processes for their preparation, and methods of treating and preventing HIV infection by their administration.

公开(公告)号：US20210024494A1

公开(公告)日：2021-01-28

申请号：US16923750

申请日：2020-07-08

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Aesop Cho ,  Michael Graupe ,  Lateshkumar Thakorlal Lad ,  Paulo A. Machicao Tello ,  Jonathan William Medley ,  Samuel E. Metobo ,  Devan Naduthambi ,  Barton W. Phillips ,  Scott Preston Simonovich ,  Peiyuan Wang ,  William J. Watkins ,  Jie Xu ,  Kin Shing Yang ,  Christopher Allen Ziebenhaus

IPC: C07D401/14 ,  A61K31/444 ,  A61K31/497 ,  A61K31/704 ,  A61K31/7068 ,  A61K39/395 ,  C07D471/08

Abstract: Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.

公开(公告)号：US20200157094A1

公开(公告)日：2020-05-21

申请号：US16660219

申请日：2019-10-22

Applicant: Gilead Sciences, Inc.

Inventor： Zhimin Du ,  Michael Graupe ,  Paulo A. Machicao Tello ,  Jonathan William Medley ,  Samuel E. Metobo ,  Eric Q. Parkhill ,  Barton W. Phillips ,  Scott P. Simonovich ,  Peiyuan Wang ,  Jie Xu ,  Christopher A. Ziebenhaus

IPC: C07D471/04 ,  C07D513/04 ,  C07D401/12 ,  C07D413/10 ,  C07D217/04 ,  C07D401/14 ,  C07D471/08 ,  C07D487/04 ,  C07D495/04

Abstract: Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.

公开(公告)号：US20180051005A1

公开(公告)日：2018-02-22

申请号：US15680041

申请日：2017-08-17

Applicant: Gilead Sciences, Inc.

Inventor： Michael Graupe ,  Steven J. Henry ,  John O. Link ,  Charles William Rowe ,  Roland D. Saito ,  Scott D. Schroeder ,  Dimitrios Stefanidis ,  Winston C. Tse ,  Jennifer R. Zhang

IPC: C07D401/14 ,  A61K31/4439 ,  A61K45/06 ,  A61K31/675 ,  A61K31/537 ,  A61K31/7076 ,  C07F5/02 ,  C07D231/54 ,  C07C317/08

CPC classification number: C07D401/14 ,  A61K31/4439 ,  A61K31/537 ,  A61K31/675 ,  A61K31/7076 ,  A61K45/06 ,  C07C317/08 ,  C07D231/54 ,  C07F5/025

Abstract: The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb): which are useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

公开(公告)号：US20170114048A1

公开(公告)日：2017-04-27

申请号：US15280801

申请日：2016-09-29

Applicant: Gilead Sciences, Inc.

Inventor： Tomas Cihlar ,  Michael Graupe ,  Yunfeng Eric Hu ,  Jeffrey Patrick Murry ,  Derek Dean Sloan ,  George Stepan ,  Helen Yu

IPC: C07D405/12 ,  A61K38/06 ,  A61K31/4196 ,  A61K38/07 ,  A61K45/06 ,  A61K31/69

CPC classification number: C07D405/12 ,  A61K31/4196 ,  A61K31/69 ,  A61K38/06 ,  A61K38/07 ,  A61K45/06 ,  C07D249/10

Abstract: Provided are compounds, compositions, combinations, kits, uses, and methods for treating HIV in a human being using such compounds or combinations with proteasome inhibitors.

公开(公告)号：US09416115B2

公开(公告)日：2016-08-16

申请号：US14559011

申请日：2014-12-03

Applicant: Gilead Sciences, Inc.

Inventor： Michael Graupe ,  Yafan Lu ,  Jeff A. Zablocki

IPC: C07D261/20 ,  C07D498/04 ,  C07D471/04 ,  C07D417/12 ,  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.

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X，Y，Z，R 2，R 3，R 4，p和q如本文所述，用于制备和使用化合物和药物组合物的方法 含有相同的

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：US20140135492A1

公开(公告)日：2014-05-15

申请号：US14158595

申请日：2014-01-17

Applicant: Gilead Sciences, Inc.

Inventor： Michael Graupe ,  Randall L. Halcomb

IPC: C07D473/18

CPC classification number: C07D473/18 ,  A61K31/522 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06

Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.

Abstract translation: 本申请包括式I或II化合物或其药学上可接受的盐，溶剂合物和/或酯，含有这些化合物的组合物，包括施用这些化合物的治疗方法，以及包括施用这些化合物的治疗方法 化合物与至少一种另外的活性剂。

公开(公告)号：US20140051656A1

公开(公告)日：2014-02-20

申请号：US13956195

申请日：2013-07-31

Applicant: Gilead Sciences, Inc.

Inventor： Hongyan Guo ,  Darryl Kato ,  Thorsten A. Kirschberg ,  Hongtao Liu ,  John O. Link ,  Michael L. Mitchell ,  Jay P. Parrish ,  Jianyu Sun ,  James Taylor ,  Elizabeth M. Bacon ,  Eda Canales ,  Aesop Cho ,  Choung U. Kim ,  Jeromy J. Cottell ,  Manoj C. Desai ,  Randall L. Halcomb ,  Michael Graupe ,  Evan S. Krygowski ,  Scott E. Lazerwith ,  Qi Liu ,  Richard L. Mackman ,  Hyung-Jung Pyun ,  Joseph H. Saugier ,  James D. Trenkle ,  Winston C. Tse ,  Randall W. Vivian ,  Scott D. Schroeder ,  William J. Watkins ,  Lianhong Xu

IPC: C07D403/14 ,  A61K45/06 ,  A61K31/4184

CPC classification number: C07D403/14 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/427 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  A61P31/12 ,  C07D207/16 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/113 ,  C07D495/04 ,  C07F5/025

Abstract: The invention 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.