公开(公告)号：US20230374036A1

公开(公告)日：2023-11-23

申请号：US18303813

申请日：2023-04-20

Applicant: Gilead Sciences, Inc.

Inventor： Chaodi Dai ,  Juan A. Guerrero ,  Tezcan Guney ,  Hongyan Guo ,  Darryl Kato ,  Irene N. Kiburu ,  Scott E. Lazerwith ,  Jessica L. McKinley ,  Jonathan William Medley ,  Hyung-Jung Pyun ,  Maoqun Tian ,  Vickie H. Tsui ,  William J. Watkins ,  Adam D. Zajdlik ,  Jennifer R. Zhang

IPC: C07D498/22 ,  C07D471/22 ,  C07F7/10

CPC classification number: C07D498/22 ,  C07D471/22 ,  C07F7/10

Abstract: Provided herein are compounds, and pharmaceutically acceptable salts thereof, useful as KRAS G12D and/or KRAS G12C inhibitors, methods of making and using the same (singly or in combination with additional agents), and pharmaceutical compositions thereof.

公开(公告)号：US11680064B2

公开(公告)日：2023-06-20

申请号：US17357376

申请日：2021-06-24

Applicant: Gilead Sciences, Inc.

Inventor： Chienhung Chou ,  Darryl Kato ,  Scott E. Lazerwith ,  John O. Link ,  Scott D. Schroeder ,  Winston C. Tse ,  Jennifer R. Zhang

IPC: C07D513/06 ,  A61K31/4365 ,  C07D471/04 ,  C07D498/04 ,  A61K45/06 ,  C07D513/04 ,  C07D403/12 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K45/06 ,  C07D403/12 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: The present disclosure relates generally to certain compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of a Retroviridae viral infection, including an infection caused by the HIV virus.

公开(公告)号：US20220143052A1

公开(公告)日：2022-05-12

申请号：US17502559

申请日：2021-10-15

Applicant: Gilead Sciences, Inc.

Inventor： Scott E. Lazerwith ,  Jonathan William Medley ,  Philip A. Morganelli ,  Thomas P. Stratton ,  Peiyuan Wang

IPC: A61K31/685

Abstract: Compounds and methods of using said compounds, alone or in combination with additional agents, and pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.

公开(公告)号：US10975096B2

公开(公告)日：2021-04-13

申请号：US16686912

申请日：2019-11-18

Applicant: Gilead Sciences, Inc.

Inventor： Anna Chiu ,  John Enquist, Jr. ,  Nolan Griggs ,  Christopher Hale ,  Norihiro Ikemoto ,  Katie Ann Keaton ,  Matt Kraft ,  Scott E. Lazerwith ,  Michel Leeman ,  Zhihui Peng ,  Kate Schrier ,  Jonathan Trinidad ,  Jochem Van Herpt ,  Andrew W. Waltman

IPC: C07D498/14 ,  C07D498/22 ,  C07D319/06 ,  C07D309/40 ,  C07C237/20 ,  C07D213/82 ,  C07C235/80 ,  C07C231/02 ,  C07C231/12

Abstract: Methods of making compounds of Formula I are disclosed:

公开(公告)号：US20210053988A1

公开(公告)日：2021-02-25

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: C07D498/14 ,  A61K31/537 ,  C07D471/22 ,  A61K31/529 ,  A61K31/551 ,  A61K31/498 ,  C07D471/18 ,  A61K45/06 ,  C07D498/18 ,  A61K31/4985 ,  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：US10703733B2

公开(公告)日：2020-07-07

申请号：US16410457

申请日：2019-05-13

Applicant: Gilead Sciences, Inc.

Inventor： Hang Chu ,  Juan A. Guerrero ,  Anna E. Hurtley ,  Tae H. Hwang ,  Lan Jiang ,  Darryl Kato ,  Tetsuya Kobayashi ,  John E. Knox ,  Scott E. Lazerwith ,  Xiaofen Li ,  David W. Lin ,  Jonathan W. Medley ,  Michael L. Mitchell ,  Devan Naduthambi ,  Zachary Newby ,  Neil H. Squires ,  Vickie H. Tsui ,  Chandrasekar Venkataramani ,  William J. Watkins ,  Hong Yang

IPC: C07D513/08 ,  C07D267/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  A61K45/06

Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.

公开(公告)号：US20190352271A1

公开(公告)日：2019-11-21

申请号：US16410457

申请日：2019-05-13

Applicant: Gilead Sciences, Inc.

Inventor： Hang Chu ,  Juan A. Guerrero ,  Anna E. Hurtley ,  Tae H. Hwang ,  Lan Jiang ,  Darryl Kato ,  Tetsuya Kobayashi ,  John E. Knox ,  Scott E. Lazerwith ,  Xiaofen Li ,  David W. Lin ,  Jonathan W. Medley ,  Michael L. Mitchell ,  Devan Naduthambi ,  Zachary Newby ,  Neil H. Squires ,  Vickie H. Tsui ,  Chandrasekar Venkataramani ,  William J. Watkins ,  Hong Yang

IPC: C07D267/20 ,  C07D413/12 ,  C07D471/04 ,  C07D417/12 ,  C07D487/04 ,  C07D498/04 ,  C07D413/14

Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.

公开(公告)号：US10328053B2

公开(公告)日：2019-06-25

申请号：US15686499

申请日：2017-08-25

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 ,  A61P31/20 ,  A61K31/03 ,  A61K31/16 ,  C07D487/04 ,  C07D519/00 ,  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：US20190015420A1

公开(公告)日：2019-01-17

申请号：US16008931

申请日：2018-06-14

Applicant: Gilead Sciences, Inc.

Inventor： Ernest A. Carra ,  Irene Chen ,  Katie Ann Keaton ,  Scott E. Lazerwith ,  Vahid Zia

IPC: A61K31/5365 ,  C07D498/18 ,  C07D498/14 ,  A61K31/675 ,  A61K9/20 ,  A61K31/513 ,  A61K45/06 ,  A61K31/683 ,  A61K31/553 ,  A61K31/537

Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.

公开(公告)号：US10005774B2

公开(公告)日：2018-06-26

申请号：US15150038

申请日：2016-05-09

Applicant: Gilead Sciences, Inc.

Inventor： Peter A. Blomgren ,  Jayaraman Chandrasekhar ,  Kevin S. Currie ,  Zhimin Du ,  Julie Farand ,  Juan A. Guerrero ,  Ashley A. Katana ,  Darryl Kato ,  Jeffrey E. Kropf ,  Scott E. Lazerwith ,  Seung H. Lee ,  Jiayao Li ,  John O. Link ,  Jennifer R. Lo ,  Nicholas Mai ,  Scott A. Mitchell ,  Gregory Notte ,  Hyung-jung Pyun ,  Michael Sangi ,  Aaron C. Schmitt ,  Adam J. Schrier ,  Kirk L. Stevens ,  Chandrasekar Venkataramani ,  William J. Watkins ,  Jin-Ming Xiong ,  Jianjun Xu ,  Zheng-Yu Yang ,  Jeff Zablocki ,  Zhongdong Zhao ,  Sheila Zipfel

IPC: C07D471/04 ,  C07D401/14 ,  C07D403/12 ,  C07D417/04 ,  C07D417/12 ,  C07D487/04 ,  C07D407/14 ,  C07D417/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D491/08 ,  C07D498/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D519/00

Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.