公开(公告)号：US08841278B2

公开(公告)日：2014-09-23

申请号：US14045717

申请日：2013-10-03

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Eda Canales ,  Aesop Cho ,  Jeromy J. Cottell ,  Manoj C. Desai ,  Michael Graupe ,  Hongyan Guo ,  Randall L. Halcomb ,  Darryl Kato ,  Choung U. Kim ,  Thorsten A. Kirschberg ,  Evan S. Krygowski ,  Scott E. Lazerwith ,  John O. Link ,  Hongtao Liu ,  Qi Liu ,  Richard L. Mackman ,  Michael L. Mitchell ,  Jay P. Parrish ,  Hyung-Jung Pyun ,  Joseph H. Saugier ,  Scott D. Schroeder ,  Jianyu Sun ,  James G. Taylor ,  James D. Trenkle ,  Winston C. Tse ,  Randall W. Vivian ,  William J. Watkins ,  Lianhong Xu

IPC: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07D495/04 ,  A61K31/4178 ,  A61K31/7068 ,  A61K31/7052 ,  A61K31/4184 ,  A61P1/16 ,  A61P31/14

CPC classification number: C07D403/14 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/427 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  A61P31/12 ,  C07D207/16 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/113 ,  C07D495/04 ,  C07F5/025

Abstract: The invention is related to anti-viral compounds, 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.

公开(公告)号：US20140017198A1

公开(公告)日：2014-01-16

申请号：US13934090

申请日：2013-07-02

Applicant: Gilead Sciences, Inc.

Inventor： Kyla Bjornson ,  Eda Canales ,  Jeromy J. Cottell ,  Kapil Kumar Karki ,  Ashley Anne Katana ,  Darryl Kato ,  Tetsuya Kobayashi ,  John O. Link ,  Ruben Martinez ,  Barton W. Phillips ,  Hyung-Jung Pyun ,  Michael Sangi ,  Adam James Schrier ,  Dustin Siegel ,  James G. Taylor ,  Chinh Viet Tran ,  Teresa Alejandra Trejo Martin ,  Randall W. Vivian ,  Zheng-Yu Yang ,  Jeff Zablocki ,  Sheila Zipfel

IPC: C07D498/16 ,  C07D498/22 ,  A61K45/06 ,  A61K31/506 ,  A61K31/519 ,  A61K31/4985 ,  A61K31/4745

CPC classification number: A61K31/498 ,  A61K31/10 ,  A61K31/401 ,  A61K31/4745 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K38/00 ,  A61K38/06 ,  A61K38/21 ,  A61K45/06 ,  C07D241/36 ,  C07D403/14 ,  C07D498/16 ,  C07D498/22 ,  C07K5/08 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0827 ,  A61K2300/00

Abstract: Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.

Abstract translation: 公开的式I化合物及其药学上可接受的盐。 还公开了使用所述化合物和含有所述化合物的药物组合物的方法。

公开(公告)号：US12161625B2

公开(公告)日：2024-12-10

申请号：US18059806

申请日：2022-11-29

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

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：US11878965B2

公开(公告)日：2024-01-23

申请号：US17557860

申请日：2021-12-21

Applicant: Gilead Sciences, Inc.

Inventor： Daniel H. Byun ,  Zhenhong R. Cai ,  Eda Y. Canales ,  Laurent P. Debien ,  Timothy R. Hansen ,  Richard Huang ,  Petr Jansa ,  Rick A. Lee ,  Jennifer A. Loyer-Drew ,  Ryan McFadden ,  Michael L. Mitchell ,  Hyung-Jung Pyun ,  Roland D. Saito ,  Michael S. Sangi ,  Adam J. Schrier ,  Marina E. Shatskikh ,  James G. Taylor ,  Joshua J. Van Veldhuizen ,  Lianhong Xu

IPC: C07D401/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/14 ,  C07D519/00

CPC classification number: C07D401/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/14 ,  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：US20220249499A1

公开(公告)日：2022-08-11

申请号：US17573143

申请日：2022-01-11

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：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：US10668064B2

公开(公告)日：2020-06-02

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 ,  A61K31/553 ,  C07D498/18 ,  A61K31/537 ,  C07D471/18 ,  A61K45/06 ,  C07D471/14 ,  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, 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：US10646486B2

公开(公告)日：2020-05-12

申请号：US15704842

申请日：2017-09-14

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: C07D471/04 ,  A61K31/4985 ,  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：US20190046526A1

公开(公告)日：2019-02-14

申请号：US15867629

申请日：2018-01-10

Applicant: Gilead Sciences, Inc.

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

IPC: A61K31/4985 ,  C07D498/14 ,  C07D471/14 ,  C07D498/18 ,  A61K31/553 ,  A61K45/06 ,  C07D471/18 ,  A61K31/537

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：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.