公开(公告)号：US11548901B2

公开(公告)日：2023-01-10

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: A61K31/4985 ,  C07D487/14 ,  C07D498/14 ,  A61K31/537 ,  C07D471/22 ,  A61K31/529 ,  A61K31/551 ,  A61K31/498 ,  C07D471/18 ,  A61K45/06 ,  C07D498/18 ,  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：US20230002412A1

公开(公告)日：2023-01-05

申请号：US17242617

申请日：2021-04-28

Applicant: Gilead Sciences, Inc.

Inventor： Eda Y. Canales ,  Weng K. Chang ,  Laurent P. Debien ,  Petr Jansa ,  Jennifer A. Loyer-Drew ,  Luisruben P. Martinez ,  Stephane Perreault ,  Gary B. Phillips ,  Hyung-Jung Pyun ,  Roland D. Saito ,  Michael S. Sangi ,  Adam J. Schrier ,  Marina E. Shatskikh ,  James G. Taylor ,  Jennifer A. Treiberg ,  Joshua J. Van Veldhuizen

IPC: C07D519/00 ,  C07D471/14 ,  A61K45/06

Abstract: The present disclosure relates to novel compounds for use in therapeutic treatment of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.

公开(公告)号：US11420974B2

公开(公告)日：2022-08-23

申请号：US17070236

申请日：2020-10-14

Applicant: GILEAD SCIENCES, INC.

Inventor： David Alan Gutierrez ,  Tetsuya Kobayashi ,  Scott E. Lazerwith ,  Rick Andrew Lee ,  Philip Anthony Morganelli ,  Hyung-Jung Pyun

IPC: C07D487/04 ,  A61P31/20

Abstract: This application relates generally to certain substituted pyrrolizine compounds, and pharmaceutical compositions which inhibit HBV replication, and methods of making and using them.

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：US20190292187A1

公开(公告)日：2019-09-26

申请号：US16284812

申请日：2019-02-25

Applicant: Gilead Sciences, Inc.

Inventor： David Alan Gutierrez ,  Tetsuya Kobayashi ,  Scott E. Lazerwith ,  Rick Andrew Lee ,  Philip Anthony Morganelli ,  Hyung-Jung Pyun

IPC: C07D487/04 ,  A61P31/20

Abstract: This application relates generally to certain substituted pyrrolizine compounds, and pharmaceutical compositions which inhibit HBV replication, and methods of making and using them.

公开(公告)号：US20190240217A1

公开(公告)日：2019-08-08

申请号：US16053456

申请日：2018-08-02

Applicant: Gilead Sciences, Inc.

Inventor： Mingzhe Ji ,  Scott E. Lazerwith ,  Hyung-Jung Pyun

IPC: A61K31/4985 ,  C07D498/14 ,  C07D471/14 ,  A61K31/537 ,  C07D498/18 ,  A61K45/06 ,  C07D471/18 ,  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, Y1, Y2, or L 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.