公开(公告)号：US10774071B2

公开(公告)日：2020-09-15

申请号：US16510647

申请日：2019-07-12

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Aesop Cho ,  Michael Graupe ,  Lateshkumar Thakorlal Lad ,  Paulo A. Machicao Tello ,  Jonathan William Medley ,  Samuel E. Metobo ,  Devan Naduthambi ,  Barton W. Phillips ,  Scott Preston Simonovich ,  Peiyuan Wang ,  William J. Watkins ,  Jie Xu ,  Kin Shing Yang ,  Christopher Allen Ziebenhaus

IPC: C07D401/14 ,  C07D471/08 ,  A61K31/444 ,  A61K31/497 ,  A61K31/704 ,  A61K31/7068 ,  A61K39/395 ,  A61P31/20

Abstract: Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.

公开(公告)号：US10710986B2

公开(公告)日：2020-07-14

申请号：US16274106

申请日：2019-02-12

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Aesop Cho ,  Zhimin Du ,  Michael Graupe ,  Lateshkumar Thakorlal Lad ,  Paulo A. Machicao Tello ,  Jonathan William Medley ,  Samuel E. Metobo ,  Prasenjit Kumar Mukherjee ,  Devan Naduthambi ,  Eric Q. Parkhill ,  Barton W. Phillips ,  Scott Preston Simonovich ,  Neil H. Squires ,  Peiyuan Wang ,  William J. Watkins ,  Jie Xu ,  Kin Shing Yang ,  Christopher Allen Ziebenhaus

IPC: C07D403/14 ,  A61P31/20 ,  A61P35/02 ,  A61K31/496 ,  C07D519/00 ,  C07D241/20 ,  C07D487/10 ,  C07D405/14 ,  C07D487/08 ,  A61K31/497 ,  C07D491/107 ,  C07D241/18 ,  A61P35/00 ,  C07K16/28

Abstract: Compounds of Formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are 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：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：US20180327437A1

公开(公告)日：2018-11-15

申请号：US16011055

申请日：2018-06-18

Applicant: GILEAD SCIENCES, INC.

Inventor： Thomas Butler ,  Aesop Cho ,  Benjamin R. Graetz ,  Choung U. Kim ,  Samuel E. Metobo ,  Oliver L. Saunders ,  Andrew W. Waltman ,  Jie Xu ,  Lijun Zhang

IPC: C07H1/00 ,  C07H19/23

CPC classification number: C07H1/00 ,  A61K31/7052 ,  A61K31/7056 ,  A61K31/706 ,  C07H19/23

Abstract: Provided are processes and intermediates for the syntheses of nucleosides of pyrrolo[1,2-f][1,2,4]triazinyl and imidazo[1,2-f][1,2,4]triazinyl heterocycles of Formula I.

公开(公告)号：US09670205B2

公开(公告)日：2017-06-06

申请号：US15059070

申请日：2016-03-02

Applicant: Gilead Sciences, Inc.

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

IPC: 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：US20160031868A1

公开(公告)日：2016-02-04

申请号：US14774019

申请日：2014-03-27

Applicant: GILEAD SCIENCES, INC.

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

IPC: C07D413/14

CPC classification number: C07D413/14 ,  C07D413/04 ,  C07D417/14

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, and X are described herein.

Abstract translation: 本申请涉及可用作含溴结构域的蛋白质（包括含溴结构域蛋白质的蛋白质4（BRD4））的抑制剂或其它方式调节其含有活性的蛋白质的化学化合物，以及含有这些化合物的组合物和制剂，以及 使用和制造这些化合物。 化合物包括其中R1a，R1b，R2a，R2b，R3和X在本文中描述的式（I）的化合物。

公开(公告)号：US12037342B2

公开(公告)日：2024-07-16

申请号：US17820374

申请日：2022-08-17

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Jayaraman Chandrasekhar ,  Julian A. Codelli ,  John H. Conway ,  Kristyna M. Elbel ,  Rao V. Kalla ,  Samuel E. Metobo ,  Scott A. Mitchell ,  Thao D. Perry ,  Scott P. Simonovich ,  Christopher A. Ziebenhaus

IPC: C07D498/04 ,  C07D413/14 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D498/04 ,  C07D413/14 ,  C07D471/04 ,  C07D519/00

Abstract: The present disclosure relates generally to certain ene-oxindole compounds, pharmaceutical compositions comprising thereof. Also disclosed are 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：US20230365511A1

公开(公告)日：2023-11-16

申请号：US18164974

申请日：2023-02-06

Applicant: Novartis AG ,  Gilead Sciences, Inc.

Inventor： Zef Konst ,  Yipin Lu ,  Robert Joseph Moreau ,  Naomi Samadara Rajapaksa ,  Galen Shearn-Nance ,  David Charles Tully ,  Michael Robert Turner ,  Joseph Michael Young ,  Qian Zhao ,  Britton K. Corkey ,  Samuel E. Metobo

IPC: C07D243/10

CPC classification number: C07D243/10

Abstract: The invention provides compounds of Formula (I)





as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.

公开(公告)号：US20230183262A1

公开(公告)日：2023-06-15

申请号：US17820374

申请日：2022-08-17

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Jayaraman Chandrasekhar ,  Julian A. Codelli ,  John H. Conway ,  Kristyna M. Elbel ,  Rao V. Kalla ,  Samuel E. Metobo ,  Scott A. Mitchell ,  Thao D. Perry ,  Scott P. Simonovich ,  Christopher A. Ziebenhaus

IPC: C07D498/04 ,  C07D413/14 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D498/04 ,  C07D413/14 ,  C07D471/04 ,  C07D519/00

Abstract: The present disclosure relates generally to certain ene-oxindole compounds, pharmaceutical compositions comprising thereof. Also disclosed are 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.