公开(公告)号：US20210078991A1

公开(公告)日：2021-03-18

申请号：US16914034

申请日：2020-06-26

Applicant: Gilead Sciences, Inc.

Inventor： Zhenhong R. Cai ,  Hongyan Guo ,  Mingzhe Ji ,  Haolun Jin ,  Amy Lee ,  Ryan McFadden ,  Michael L. Mitchell ,  Manuel Munoz ,  Hyung-Jung Pyun ,  Lianhong Xu ,  Hong Yang

IPC: C07D417/14 ,  A61P31/18 ,  A61K31/428 ,  A61K31/439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D417/04 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107 ,  C07D498/04

Abstract: Compounds disclosed herein including compounds of Formula I: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.

公开(公告)号：US20210053988A1

公开(公告)日：2021-02-25

申请号：US16868119

申请日：2020-05-06

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

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：US09795602B2

公开(公告)日：2017-10-24

申请号：US15349353

申请日：2016-11-11

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Zhenhong R. Cai ,  Jeromy J. Cottell ,  Mingzhe Ji ,  Haolun Jin ,  Scott E. Lazerwith ,  Philip Anthony Morganelli ,  Hyung-Jung Pyun

IPC: A61K31/4985 ,  C07D491/147 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K45/06 ,  C07D471/04 ,  C07D491/147 ,  C07D491/20

Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (Ia): including stereoisomers and pharmaceutically acceptable salts thereof, wherein A′, R1, R2 and R3 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：US20170119764A1

公开(公告)日：2017-05-04

申请号：US15349353

申请日：2016-11-11

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Zhenhong R. Cai ,  Jeromy J. Cottell ,  Mingzhe Ji ,  Haolun Jin ,  Scott E. Lazerwith ,  Philip Anthony Morganelli ,  Hyung-Jung Pyun

IPC: A61K31/4985 ,  A61K45/06 ,  C07D491/147

CPC classification number: A61K31/4985 ,  A61K45/06 ,  C07D471/04 ,  C07D491/147 ,  C07D491/20

Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (Ia): including stereoisomers and pharmaceutically acceptable salts thereof, wherein A′, R1, R2 and R3 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：US20170057976A1

公开(公告)日：2017-03-02

申请号：US15349934

申请日：2016-11-11

Applicant: Gilead Sciences, Inc.

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

IPC: C07D498/14 ,  A61K31/537 ,  A61K31/553 ,  A61K45/06

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.

Abstract translation: 包括立体异构体及其药学上可接受的盐，其中R1，X，W，Y1，Y2，Z1和Z4如本文所定义。 还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

公开(公告)号：US08871785B2

公开(公告)日：2014-10-28

申请号：US13848593

申请日：2013-03-21

Applicant: Gilead Sciences, Inc.

Inventor： Constantine G. Boojamra ,  Carina E. Cannizzaro ,  James M. Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee S. Chong ,  Maria Fardis ,  Haolun Jin ,  Ralph Hirschmann ,  Alan X. Huang ,  Choung U. Kim ,  Thorsten A. Kirschberg ,  Christopher P. Lee ,  William A. Lee ,  Richard L. Mackman ,  David Y. Markevitch ,  David A. Oare ,  Vidya K. Prasad ,  Hyung-Jung Pyun ,  Adrian S. Ray ,  Rosemarie O'Shea ,  Sundaramoorthi Swaninathan ,  William J. Watkins ,  Jennifer R. Zhang

IPC: A61K31/44 ,  C07D239/00

CPC classification number: C07F9/65616 ,  A61K31/662 ,  A61K31/7072 ,  A61K31/7076 ,  A61K47/548 ,  C07D205/04 ,  C07D211/58 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D475/00 ,  C07F9/4075 ,  C07F9/5728 ,  C07F9/58 ,  C07F9/60 ,  C07F9/65031 ,  C07F9/650905 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/655354 ,  C07F9/6561 ,  C07H15/00 ,  C07H17/00 ,  C07H19/056 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  Y02A50/393 ,  Y02A50/465

Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, 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.

Abstract translation: 本发明涉及具有抗病毒活性的磷取代的化合物，含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US20240238285A1

公开(公告)日：2024-07-18

申请号：US18543923

申请日：2023-12-18

Applicant: Gilead Sciences, Inc.

Inventor： Manoj C. Desai ,  Mingzhe Ji ,  Haolun Jin ,  Hyung-Jung Pyun ,  Teresa Alejandra Trejo Martin

IPC: A61K31/4985 ,  C07D471/14 ,  C07D471/18

CPC classification number: A61K31/4985 ,  C07D471/14 ,  C07D471/18

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 L, R1, R5, W, X, Y1, Y2, and Z 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：US11883397B2

公开(公告)日：2024-01-30

申请号：US17532148

申请日：2021-11-22

Applicant: Gilead Sciences, Inc.

Inventor： Manoj C. Desai ,  Mingzhe Ji ,  Haolun Jin ,  Hyung-Jung Pyun ,  Teresa Alejandra Trejo Martin

IPC: A61K31/4985 ,  C07D487/22 ,  C07D471/18 ,  C07D471/14

CPC classification number: A61K31/4985 ,  C07D471/14 ,  C07D471/18

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 L, R1, R5, W, X, Y1, Y2, and Z 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：US20200215062A1

公开(公告)日：2020-07-09

申请号：US16572159

申请日：2019-09-16

Applicant: Gilead Sciences, Inc.

Inventor： Manoj C. Desai ,  Mingzhe Ji ,  Haolun Jin ,  Hyung-Jung Pyun ,  Teresa Alejandra Trejo Martin

IPC: A61K31/4985 ,  C07D471/18 ,  C07D471/14

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 L, R1, R5, W, X, Y1, Y2, and Z 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：US20190224206A1

公开(公告)日：2019-07-25

申请号：US16251454

申请日：2019-01-18

Applicant: Gilead Sciences, Inc.

Inventor： Haolun Jin ,  Hyung-Jung Pyun ,  Bill J. Smith ,  Raju Subramanian ,  Jianhong Wang

IPC: A61K31/537 ,  A61K45/06 ,  A61K31/706 ,  A61P31/18 ,  G01N33/94 ,  C07H17/00 ,  C07D498/18

Abstract: The present invention provides metabolites of the antiviral drug bictegravir, including compositions and salts thereof, which are useful in the prevention and/or treatment of HIV as well as analytical methods related to the administration of bictegravir.