公开(公告)号：US11827609B2

公开(公告)日：2023-11-28

申请号：US17399984

申请日：2021-08-11

Applicant: GILEAD SCIENCES, INC.

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

IPC: C07D239/95 ,  A61P31/18 ,  A61P35/00 ,  A61K31/517 ,  A61K31/519 ,  A61K45/06 ,  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：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：US20180086755A1

公开(公告)日：2018-03-29

申请号：US15692161

申请日：2017-08-31

Applicant: Gilead Sciences, Inc.

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

IPC: C07D471/04 ,  A61K31/519 ,  A61K45/06

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K45/06

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：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：US10370342B2

公开(公告)日：2019-08-06

申请号：US15692093

申请日：2017-08-31

Applicant: Gilead Sciences, Inc.

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

IPC: C07D239/95 ,  A61K31/517 ,  A61P31/18 ,  A61P35/00 ,  A61K31/519 ,  A61K45/06 ,  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：US20180065938A1

公开(公告)日：2018-03-08

申请号：US15692093

申请日：2017-08-31

Applicant: Gilead Sciences, Inc.

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

IPC: C07D239/95 ,  A61K45/06 ,  A61K31/517 ,  C07D471/04 ,  A61K31/519 ,  C07D495/04 ,  C07D487/04

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：US20160376261A1

公开(公告)日：2016-12-29

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 ,  C07D417/14 ,  C07D413/14 ,  C07D471/04

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.

Abstract translation: 其中R1a，R1b，R2a，R2b，R3，R4a，R4b和R5如本文所述。

公开(公告)号：US20160289229A1

公开(公告)日：2016-10-06

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.

Abstract translation: 本公开内容一般涉及诸如二氨基吡啶并[3,2 D]嘧啶化合物等受体调节剂化合物和除其他外调节toll样受体（例如TLR-8）的药物组合物，以及制备和 使用它们。