公开(公告)号：US20240287061A1

公开(公告)日：2024-08-29

申请号：US18543272

申请日：2023-12-18

Applicant: Gilead Sciences, Inc.

Inventor： Gayatri Balan ,  Mark J. Bartlett ,  Jayaraman Chandrasekhar ,  Julian A. Codelli ,  John H. Conway ,  Jennifer L. Cosman Ellis ,  Rao V. Kalla ,  Zachary A. Kasun ,  Musong Kim ,  Seung H. Lee ,  Jennifer R. Lo ,  Jennifer A. Loyer-Drew ,  Scott A. Mitchell ,  Thao D. Perry ,  Gary B. Phillips ,  Patrick J. Salvo ,  Sundaramoorthi Swaminathan ,  Joshua J. Van Veldhuizen ,  Suet C. Yeung ,  Jeff Zablocki

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present disclosure relates generally to certain 6-azabenzimidazole 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 diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.

公开(公告)号：US20240254091A1

公开(公告)日：2024-08-01

申请号：US18476141

申请日：2023-09-27

Applicant: GILEAD SCIENCES, INC.

Inventor： Gregory Chin ,  Richard L. Mackman ,  Michael R. Mish ,  Jeff Zablocki

IPC: C07D239/95 ,  A61K31/517 ,  A61K31/519 ,  A61K45/06 ,  A61P31/18 ,  A61P35/00 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

CPC classification number: C07D239/95 ,  A61K31/517 ,  A61K31/519 ,  A61K45/06 ,  A61P31/18 ,  A61P35/00 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.

公开(公告)号：US20220218709A1

公开(公告)日：2022-07-14

申请号：US17540563

申请日：2021-12-02

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：USRE48150E1

公开(公告)日：2020-08-11

申请号：US15397344

申请日：2017-01-03

Applicant: Gilead Sciences, Inc.

Inventor： Britton Corkey ,  Gregory Notte ,  Jeff Zablocki

IPC: C07D409/14

Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, R, R1, R2 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).

公开(公告)号：US20200171020A1

公开(公告)日：2020-06-04

申请号：US16668732

申请日：2019-10-30

Applicant: Gilead Sciences, Inc.

Inventor： Gayatri Balan ,  Mark J. Bartlett ,  Jayaraman Chandrasekhar ,  Julian A. Codelli ,  John H. Conway ,  Jennifer L. Cosman ,  Rao V. Kalla ,  Musong Kim ,  Seung H. Lee ,  Jennifer R. Lo ,  Jennifer A. Loyer-Drew ,  Scott A. Mitchell ,  Thao D. Perry ,  Gary B. Phillips ,  Patrick J. Salvo ,  Joshua J. Van Veldhuizen ,  Suet C. Yeung ,  Jeff Zablocki

IPC: A61K31/4545 ,  C07D471/04 ,  A61K31/444 ,  A61K31/5386 ,  C07D519/00

Abstract: The present disclosure relates generally to certain 6-azabenzimidazole 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 diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.

公开(公告)号：US10017501B2

公开(公告)日：2018-07-10

申请号：US15239422

申请日：2016-08-17

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Gregory Chin ,  Britton Kenneth Corkey ,  Jinfa Du ,  Kristyna Elbel ,  Robert H. Jiang ,  Tetsuya Kobayashi ,  Rick Lee ,  Ruben Martinez ,  Samuel E. Metobo ,  Michael Mish ,  Manuel Munoz ,  Sophie Shevick ,  David Sperandio ,  Hai Yang ,  Jeff Zablocki

IPC: C07D413/04 ,  C07D453/02 ,  C07D417/04 ,  C07D413/14 ,  C07D471/04 ,  C07D417/14

CPC classification number: C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04

Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, R4a, R4b, and R5 are described herein.

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.

公开(公告)号：US20170313745A1

公开(公告)日：2017-11-02

申请号：US15455508

申请日：2017-03-10

Applicant: Gilead Sciences, Inc.

Inventor： Kyla L. Bjornson ,  Kapil K. Karki ,  John O. Link ,  Hyung-jung Pyun ,  Adam J. Schrier ,  Kirk L. Stevens ,  James G. Taylor ,  Randall W. Vivian ,  Jeff Zablocki ,  Sheila M. Zipfel

IPC: C07K7/64 ,  C07D487/02 ,  C07D487/00 ,  C07D203/02 ,  A61K31/519 ,  C07D498/22 ,  A61K31/437

CPC classification number: C07K7/64 ,  A61K31/437 ,  A61K31/519 ,  C07D203/02 ,  C07D487/00 ,  C07D487/02 ,  C07D498/22

Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein the various substituents are defined herein, methods of using said compounds, and pharmaceutical compositions containing said compounds.

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：US09695192B2

公开(公告)日：2017-07-04

申请号：US14630519

申请日：2015-02-24

Applicant: GILEAD SCIENCES, INC.

Inventor： Britton Kenneth Corkey ,  Elfatih Elzein ,  Robert H. Jiang ,  Rao V. Kalla ,  Dmitry Koltun ,  Xiaofen Li ,  Ruben Martinez ,  Eric Q. Parkhill ,  Thao Perry ,  Jeff Zablocki ,  Chandrasekar Venkataramani ,  Michael Graupe ,  Juan Guerrero

IPC: A61K31/553 ,  C07D267/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/12 ,  C07D487/04 ,  C07D498/04 ,  C07D413/12

CPC classification number: C07D498/04 ,  C07D267/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14

Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.