公开(公告)号：US11084832B2

公开(公告)日：2021-08-10

申请号：US16825142

申请日：2020-03-20

Applicant: Gilead Sciences, Inc.

Inventor： Hang Chu ,  Ana Z. Gonzalez Buenrostro ,  Hongyan Guo ,  Xiaochun Han ,  Lan Jiang ,  Jiayao Li ,  Michael L. Mitchell ,  Hyung-Jung Pyun ,  Scott D. Schroeder ,  Gregg M. Schwarzwalder ,  Nathan D. Shapiro ,  Devleena M. Shivakumar ,  Qiaoyin Wu ,  Hong Yang ,  Jennifer R. Zhang

IPC: C07D498/18 ,  C07D471/18 ,  A61P31/18

Abstract: Compounds for use in treating or preventing human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2, L, W1, W2, X, Y, and Z are as defined herein. Methods associated with the preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

公开(公告)号：US20200215062A1

公开(公告)日：2020-07-09

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 ,  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：US20190282576A1

公开(公告)日：2019-09-19

申请号：US16254333

申请日：2019-01-22

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 ,  C07D471/04 ,  C07D239/84 ,  C07D401/04

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：US20190224206A1

公开(公告)日：2019-07-25

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

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：US10285990B2

公开(公告)日：2019-05-14

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 ,  C07D471/04 ,  C07D239/84 ,  C07D401/04

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：US20180215769A1

公开(公告)日：2018-08-02

申请号：US15669569

申请日：2017-08-04

Applicant: Gilead Sciences, Inc.

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

IPC: C07D498/18 ,  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.

公开(公告)号：US20160176885A1

公开(公告)日：2016-06-23

申请号：US14815504

申请日：2015-07-31

Applicant: Gilead Sciences, Inc.

Inventor： Haolun Jin ,  Scott E. Lazerwith ,  Hyung-Jung Pyun ,  Manoj C. Desai ,  Teresa Alejandra Trejo Martin ,  Elizabeth Bacon ,  Jeromy J. Cottell ,  Zhenhong R. Cai ,  Philip Anthony Morganelli ,  Mingzhe Ji ,  James G. Taylor ,  Xiaowu Chen ,  Michael R. Mish

IPC: 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.

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：US09296782B2

公开(公告)日：2016-03-29

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: A61K6/00 ,  C07K1/00 ,  C07K5/08 ,  C07D498/16 ,  A61K31/4985 ,  C07D498/22 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/519 ,  A61K45/06 ,  C07K5/087 ,  C07K5/083 ,  A61K38/21 ,  A61K38/06 ,  A61K38/00

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：US20240246975A1

公开(公告)日：2024-07-25

申请号：US18527967

申请日：2023-12-04

Applicant: Gilead Sciences, Inc.

Inventor： Hang Chu ,  Hongyan Guo ,  Lan Jiang ,  Jiayao Li ,  David W. Lin ,  Hyung-Jung Pyun ,  Qiaoyin Wu ,  Hong Yang ,  Adam D. Zajdlik ,  Jennifer R. Zhang

IPC: C07D471/18 ,  A61P31/18 ,  C07D491/22

CPC classification number: C07D471/18 ,  A61P31/18 ,  C07D491/22

Abstract: Compounds for use in treating or preventing human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I):




including stereoisomers and pharmaceutically acceptable salts thereof. Methods associated with the preparation and use of the disclosed compounds, as well as pharmaceutical compositions comprising such compounds are also disclosed.

公开(公告)号：US11976083B2

公开(公告)日：2024-05-07

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: C07D471/18 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/437 ,  A61K45/06 ,  A61P3/10 ,  A61P7/02 ,  A61P19/02 ,  A61P35/00 ,  C07D471/12 ,  C07D471/14 ,  C07D487/08 ,  C07D491/22 ,  C07D498/18 ,  C07D498/22 ,  C07D513/18 ,  C07D519/00

CPC classification number: C07D519/00 ,  A61K45/06 ,  C07D471/14

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.