公开(公告)号：US20240239807A1

公开(公告)日：2024-07-18

申请号：US18365919

申请日：2023-08-04

Applicant: Gilead Sciences, Inc.

Inventor： Stephen E. Ammann ,  Xinpei Cai ,  Eda Y. Canales ,  Weng K. Chang ,  Gregory F. Chin ,  Henok H. Kinfe ,  Scott E. Lazerwith ,  Jessica L. McKinley ,  Michael R. Mish ,  Devan Naduthambi ,  Jason K. Perry ,  Kevin X. Rodriguez ,  Scott D. Schroeder ,  Christopher J. Swank ,  Joshua J. Van Veldhuizen

IPC: C07D495/04 ,  A61P31/14 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D491/113 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07D495/04 ,  A61P31/14 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D491/113 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: The present disclosure relates to compounds of Formula I:




and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, useful in the treatment of treating viral infections, for example, coronaviridae infections.

公开(公告)号：US12030903B2

公开(公告)日：2024-07-09

申请号：US17178115

申请日：2021-02-17

Applicant: Gilead Sciences, Inc.

Inventor： Daniel H. Byun ,  Gregory F. Chin ,  Michael O. Clarke ,  Bindu Goyal ,  Petr Jansa ,  Richard L. Mackman ,  Michael R. Mish ,  Dustin S. Siegel

IPC: C07F9/6561 ,  A61K45/06

CPC classification number: C07F9/6561 ,  A61K45/06

Abstract: The present disclosure describes 4′-fluoromethyl nucleosides for treating viral infections, including Dengue.

公开(公告)号：US20210017170A1

公开(公告)日：2021-01-21

申请号：US16911643

申请日：2020-06-25

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Andrea Ambrosi ,  Sylvie M. Asselin ,  Florence J. Bachrach ,  Pavel R. Badalov ,  Gregory F. Chin ,  Stephen P. Lathrop ,  Willard Lew ,  Richard L. Mackman ,  Jeffrey E. Merit ,  Samuel E. Metobo ,  Michael R. Mish ,  Beau P. Pritchett ,  Hyung-Jung Pyun ,  Christopher S. Regens ,  Tiago Vieira ,  Xianghong Wang ,  Adam B. Weinstein ,  Todd A. Wenderski ,  Zehua Zheng

IPC: C07D471/04 ,  C07D213/81 ,  C07D413/04

Abstract: The present disclosure provides methods for preparing (R)-2-((2-amino-7-fluoropyrido[3,2-d]pyrimidin-4-yl)amino)-2-methylhexan-1-ol or a salt thereof and related key intermediates.

公开(公告)号：US10370342B2

公开(公告)日：2019-08-06

申请号：US15692093

申请日：2017-08-31

Applicant: Gilead Sciences, Inc.

Inventor： Gregory Chin ,  Richard L. Mackman ,  Michael R. Mish ,  Jeff Zablocki

IPC: C07D239/95 ,  A61K31/517 ,  A61P31/18 ,  A61P35/00 ,  A61K31/519 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.

公开(公告)号：US10035809B2

公开(公告)日：2018-07-31

申请号：US15599151

申请日：2017-05-18

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Zhenhong R. Cai ,  Xiaowu Chen ,  Jeromy J. Cottell ,  Manoj C. Desai ,  Mingzhe Ji ,  Haolun Jin ,  Scott E. Lazerwith ,  Michael R. Mish ,  Philip Anthony Morganelli ,  Hyung-Jung Pyun ,  James G. Taylor ,  Teresa Alejandra Trejo Martin

IPC: A61K31/4985 ,  C07D487/04 ,  C07D498/14 ,  A61K31/537 ,  C07D471/22 ,  A61K31/529 ,  A61K31/551 ,  A61K31/553 ,  C07D471/18 ,  A61K45/06 ,  C07D498/18 ,  C07D487/14 ,  A61K31/498

CPC classification number: C07D498/14 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/529 ,  A61K31/537 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D471/18 ,  C07D471/22 ,  C07D487/14 ,  C07D498/18 ,  A61K2300/00

Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

公开(公告)号：US20180065938A1

公开(公告)日：2018-03-08

申请号：US15692093

申请日：2017-08-31

Applicant: Gilead Sciences, Inc.

Inventor： Gregory Chin ,  Richard L. Mackman ,  Michael R. Mish ,  Jeff Zablocki

IPC: C07D239/95 ,  A61K45/06 ,  A61K31/517 ,  C07D471/04 ,  A61K31/519 ,  C07D495/04 ,  C07D487/04

CPC classification number: C07D239/95 ,  A61K31/517 ,  A61K31/519 ,  A61K45/06 ,  A61P31/18 ,  A61P35/00 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.

公开(公告)号：US20170260204A1

公开(公告)日：2017-09-14

申请号：US15599151

申请日：2017-05-18

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Zhenhong R. Cai ,  Xiaowu Chen ,  Jeromy J. Cottell ,  Manoj C. Desai ,  Mingzhe Ji ,  Haolun Jin ,  Scott E. Lazerwith ,  Michael R. Mish ,  Philip Anthony Morganelli ,  Hyung-Jung Pyun ,  James G. Taylor ,  Teresa Alejandra Trejo Martin

IPC: C07D498/14 ,  C07D471/22 ,  A61K31/529 ,  A61K31/551 ,  A61K31/498 ,  C07D471/18 ,  A61K45/06 ,  C07D498/18 ,  C07D487/14 ,  A61K31/537 ,  A61K31/553

CPC classification number: C07D498/14 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/529 ,  A61K31/537 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D471/18 ,  C07D471/22 ,  C07D487/14 ,  C07D498/18 ,  A61K2300/00

Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

公开(公告)号：US20160289229A1

公开(公告)日：2016-10-06

申请号：US15059070

申请日：2016-03-02

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Gregory Chin ,  Richard L. Mackman ,  Samuel E. Metobo ,  Michael R. Mish ,  Hyung-jung Pyun ,  Jeff Zablocki

IPC: C07D471/04

CPC classification number: A61K31/517 ,  C07D239/84 ,  C07D401/04 ,  C07D471/04

Abstract: The present disclosure relates generally to toll like receptor modulator compounds, such as diamino pyrido[3,2 D]pyrimidine compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them.

Abstract translation: 本公开内容一般涉及诸如二氨基吡啶并[3,2 D]嘧啶化合物等受体调节剂化合物和除其他外调节toll样受体（例如TLR-8）的药物组合物，以及制备和 使用它们。

公开(公告)号：US20250129051A1

公开(公告)日：2025-04-24

申请号：US18922134

申请日：2024-10-21

Applicant: Gilead Sciences, Inc.

Inventor： Robert L. Hoffman ,  Michael R. Mish ,  James G. Taylor

IPC: C07D401/14 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/498 ,  A61P35/00 ,  C07D471/04 ,  C07D491/048

Abstract: Described herein are PARP1 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of cancer.

公开(公告)号：US12110294B2

公开(公告)日：2024-10-08

申请号：US17243911

申请日：2021-04-29

Applicant: Gilead Sciences, Inc.

Inventor： Mark J. Bartlett ,  Gregory F. Chin ,  Michael O. Clarke ,  Jennifer L. Cosman ,  Deeba Ensan ,  Bindu Goyal ,  Stephen Ho ,  Hon C. Hui ,  Richard L. Mackman ,  Michael R. Mish ,  Scott D. Schroeder ,  Nathan D. Shapiro ,  Dustin S. Siegel ,  Doris T. Tang ,  Hai Yang

IPC: C07D487/04 ,  A61K45/06 ,  C07D519/00 ,  C07K16/28

CPC classification number: C07D487/04 ,  A61K45/06 ,  C07D519/00 ,  C07K16/2818 ,  C07K16/2827

Abstract: The present disclosure provides pyrimidine dione compounds of Formula I






and pharmaceutical compositions thereof, for treating cancer, including solid tumors either-used alone or in combination with other anti-cancer agents.