公开(公告)号：US20220233525A1

公开(公告)日：2022-07-28

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 ,  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：US11213523B2

公开(公告)日：2022-01-04

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 ,  C07D487/22 ,  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：US10456395B2

公开(公告)日：2019-10-29

申请号：US15982197

申请日：2018-05-17

Applicant: Gilead Sciences, Inc.

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

IPC: A61K31/4985 ,  C07D487/04 ,  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：US20190092787A1

公开(公告)日：2019-03-28

申请号：US16017371

申请日：2018-06-25

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 ,  A61K45/06 ,  C07D498/18 ,  A61K31/498 ,  A61K31/551 ,  A61K31/537 ,  C07D471/18 ,  C07D471/22 ,  A61K31/4985 ,  A61K31/529 ,  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：US20180118734A1

公开(公告)日：2018-05-03

申请号：US15716431

申请日：2017-09-26

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

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：US09663528B2

公开(公告)日：2017-05-30

申请号：US14815504

申请日：2015-07-31

Applicant: Gilead Sciences, Inc.

Inventor： Manoj C. Desai ,  Haolun Jin ,  Scott E. Lazerwith ,  Hyung-Jung Pyun ,  James G. Taylor

IPC: A61K31/4985 ,  C07D241/38 ,  C07D487/14

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：US20160289246A1

公开(公告)日：2016-10-06

申请号：US15089342

申请日：2016-04-01

Applicant: Gilead Sciences, Inc.

Inventor： Zhenhong R. Cai ,  Haolun Jin ,  Scott E. Lazerwith ,  Hyung-Jung Pyun

IPC: C07D513/22 ,  A61K31/4985 ,  C07D498/22 ,  C07D498/16 ,  A61K31/5365 ,  C07D491/22 ,  A61K45/06

CPC classification number: C07D513/22 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/5365 ,  A61K45/06 ,  C07D491/14 ,  C07D491/22 ,  C07D498/14 ,  C07D498/16 ,  C07D498/22

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, A′, R1 and R2 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A，A'，R 1和R 2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：US20160194335A1

公开(公告)日：2016-07-07

申请号：US14849453

申请日：2015-09-09

Applicant: Gilead Sciences, Inc.

Inventor： Haolun Jin ,  Scott E. Lazerwith ,  Hyung-Jung Pyun

IPC: C07D498/04 ,  C07D471/18 ,  C07D487/18

CPC classification number: C07D498/18 ,  C07D471/18 ,  C07D471/22 ,  C07D487/18 ,  C07D498/04 ,  C07D498/14

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 R1, X, W, Y1, Y2, Z1, Z2, or 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: 公开了用于治疗人类免疫缺陷病毒（HIV）感染的化合物。 所述化合物具有下式（I）：其包括其立体异构体和药学上可接受的盐，其中R 1，X，W，Y 1，Y 2，Z 1，Z 2或Z 4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：US09216996B2

公开(公告)日：2015-12-22

申请号：US14133858

申请日：2013-12-19

Applicant: Gilead Sciences, Inc.

Inventor： Haolun Jin ,  Scott E. Lazerwith ,  Hyung-Jung Pyun

IPC: A61K31/4985 ,  C07D241/38 ,  C07D498/14 ,  A61K31/537 ,  C07D471/22 ,  A61K31/529 ,  A61K31/551 ,  A61K31/498 ,  C07D471/18 ,  A61K45/06 ,  C07D498/18

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 Z4are 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: 公开了用于治疗人类免疫缺陷病毒（HIV）感染的化合物。 所述化合物具有下式（I）：其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：US09139604B2

公开(公告)日：2015-09-22

申请号：US14309790

申请日：2014-06-19

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 Swaminathan ,  William J. Watkins ,  Jennifer R. Zhang

IPC: A61K31/44 ,  C07F9/6561 ,  A61K31/662 ,  A61K31/7072 ,  A61K31/7076 ,  A61K47/48 ,  C07D205/04 ,  C07D211/58 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D475/00 ,  C07F9/40 ,  C07F9/572 ,  C07F9/58 ,  C07F9/60 ,  C07F9/6503 ,  C07F9/6509 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/655 ,  C07F9/6553 ,  C07H15/00 ,  C07H17/00 ,  C07H21/00 ,  C07H19/056 ,  C07H19/10 ,  C07H19/20

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。