公开(公告)号：US20170281627A1

公开(公告)日：2017-10-05

申请号：US15496283

申请日：2017-04-25

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Gregory Chin ,  Richard L. Mackman ,  Samuel E. Metobo ,  Michael R. Mish ,  Hyung-Jung Pyun ,  Jeff Zablocki

IPC: A61K31/517 ,  C07D401/04 ,  C07D239/84 ,  C07D471/04

CPC classification number: A61K31/517 ,  C07D239/84 ,  C07D401/04 ,  C07D471/04

Abstract: The present disclosure relates generally to toll like receptor modulator compounds, such as diamino pyrido[3,2 D] pyrimidine compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them.

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：US20150080569A1

公开(公告)日：2015-03-19

申请号：US14312612

申请日：2014-06-23

Applicant: Gilead Sciences, Inc.

Inventor： Aesop Cho ,  Michael O'Neil Hanrahan Clarke ,  Choung U. Kim ,  John O. Link ,  Hyung-Jung Pyun ,  Xiaoning C. Sheng ,  Qiaoyin Wu

IPC: C07D417/14 ,  C07D207/16

CPC classification number: C07D417/14 ,  C07D207/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D487/04 ,  C07K5/0804 ,  C07K5/0808 ,  C07K5/0819 ,  C07K5/0821

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：US20150018298A1

公开(公告)日：2015-01-15

申请号：US14329694

申请日：2014-07-11

Applicant: GILEAD SCIENCES, INC.

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

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

CPC classification number: A61K31/4985 ,  A61K31/537 ,  A61K31/553 ,  A61K45/06 ,  C07D471/14 ,  C07D471/18 ,  C07D498/14 ,  C07D498/18

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 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.

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R 1，X，Y 1，Y 2或L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：US20140221355A1

公开(公告)日：2014-08-07

申请号：US14133855

申请日：2013-12-19

Applicant: Gilead Sciences, Inc.

Inventor： Scott E. LAZERWITH ,  Haolun JIN ,  Hyung-Jung Pyun

IPC: C07D498/14 ,  C07D471/22

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：US20230270719A1

公开(公告)日：2023-08-31

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

CPC classification number: A61K31/403 ,  C07D487/04 ,  C07D519/00 ,  A61P31/20 ,  A61K31/03 ,  A61K31/16 ,  A61K31/38 ,  A61K31/4192

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：US20230148157A1

公开(公告)日：2023-05-11

申请号：US17862896

申请日：2022-07-12

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

CPC classification number: 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：US20230090053A1

公开(公告)日：2023-03-23

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

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.