公开(公告)号：US12240862B2

公开(公告)日：2025-03-04

申请号：US17558130

申请日：2021-12-21

Applicant: Gilead Sciences, Inc.

Inventor： Daniel H. Byun ,  Eda Y. Canales ,  Laurent P. Debien ,  Petr Jansa ,  Rick A. Lee ,  Jennifer A. Loyer-Drew ,  Stephane Perreault ,  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 ,  Lianhong Xu

IPC: A61P35/02 ,  C07D519/00

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：US20250042922A1

公开(公告)日：2025-02-06

申请号：US18756455

申请日：2024-06-27

Applicant: Gilead Sciences, Inc.

Inventor： Chaodi Dai ,  Julie Farand ,  Juan A. Guerrero ,  Tezcan Guney ,  Hongyan Guo ,  Jason R. Hudlicky ,  Darryl Kato ,  Irene N. Kiburu ,  Scott E. Lazerwith ,  Paulo A. Machicao Tello ,  James B.C. Mack ,  Erik P. McAuley ,  Jessica L. McKinley ,  Jonathan William Medley ,  Hyung-Jung Pyun ,  Thomas P. Stratton ,  Maoqun Tian ,  Jeremy R. Tuck ,  William J. Watkins ,  Jie Xu ,  Jennifer R. Zhang

IPC: C07D519/00 ,  A61K31/55 ,  C07D471/22

Abstract: Provided herein are compounds, and pharmaceutically acceptable salts thereof, useful as KRAS inhibitors, methods of making and using the same (singly or in combination with additional agents), and pharmaceutical compositions thereof.

公开(公告)号：US11253524B2

公开(公告)日：2022-02-22

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 ,  A61K31/553 ,  A61P31/18 ,  A61K31/706 ,  A61K45/06 ,  C07D498/18 ,  C07H17/00 ,  G01N33/94

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.

公开(公告)号：US20210015816A1

公开(公告)日：2021-01-21

申请号：US16832230

申请日：2020-03-27

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 ,  C07D471/04 ,  C07D491/147 ,  C07D491/20 ,  A61K45/06

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：US10800772B2

公开(公告)日：2020-10-13

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: C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  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 ,  C07D471/08 ,  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：US10689399B2

公开(公告)日：2020-06-23

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: A61K31/4985 ,  C07D413/14 ,  C07D498/14 ,  A61K31/537 ,  C07D471/22 ,  A61K31/529 ,  A61K31/551 ,  A61K31/498 ,  C07D471/18 ,  A61K45/06 ,  C07D498/18 ,  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：US20200061024A1

公开(公告)日：2020-02-27

申请号：US16403247

申请日：2019-05-03

Applicant: GILEAD SCIENCES, INC.

Inventor： Jinfa Du ,  Joshua A. Kaplan ,  Thorsten A. Kirschberg ,  Tetsuya Kobayashi ,  Scott E. Lazerwith ,  Rick Andrew Lee ,  Jonathan William Medley ,  Michael L. Mitchell ,  Philip Anthony Morganelli ,  Hyung-Jung Pyun ,  Sophia L. Shevick ,  Neil H. Squires ,  William J. Watkins

IPC: A61K31/403 ,  A61K31/4192 ,  A61K31/38 ,  A61K31/16 ,  A61K31/03 ,  A61P31/20 ,  C07D519/00 ,  C07D487/04

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：US20190134028A1

公开(公告)日：2019-05-09

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 ,  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：US09732092B2

公开(公告)日：2017-08-15

申请号：US15349934

申请日：2016-11-11

Applicant: Gilead Sciences, Inc.

Inventor： Haolun Jin ,  Scott E. Lazerwith ,  Hyung-Jung Pyun ,  Elizabeth M. Bacon ,  Philip Anthony Morganelli ,  Mingzhe Ji

IPC: A61K31/5365 ,  C07D413/14 ,  C07D498/14 ,  A61K45/06 ,  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：US09458159B2

公开(公告)日：2016-10-04

申请号：US14329697

申请日：2014-07-11

Applicant: GILEAD SCIENCES, INC.

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

IPC: A61K31/498 ,  C07D241/38 ,  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.