公开(公告)号：US11667613B2

公开(公告)日：2023-06-06

申请号：US17030540

申请日：2020-09-24

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: C07D471/04 ,  C07D471/14 ,  A61K31/4162 ,  A61K31/437 ,  A61P31/22 ,  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：US20200017471A1

公开(公告)日：2020-01-16

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 ,  A61K39/395 ,  A61K31/704 ,  A61K31/7068 ,  A61K31/444 ,  A61K31/497

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：US10442804B2

公开(公告)日：2019-10-15

申请号：US15885390

申请日：2018-01-31

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Eda Canales ,  Kevin S. Currie ,  Darryl Kato ,  Jiayao Li ,  John O. Link ,  Samuel E. Metobo ,  Roland D. Saito ,  Scott D. Schroeder ,  Nathan Shapiro ,  Winston C. Tse ,  Qiaoyin Wu ,  Yunfeng Eric Hu

IPC: C07D471/14 ,  C07D491/22 ,  C07D498/14 ,  C07D519/00 ,  A61P31/20 ,  C07B59/00

Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions which may be used in methods of treating a hepatitis B virus infection.

公开(公告)号：US20190270727A1

公开(公告)日：2019-09-05

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 ,  A61P35/02 ,  A61P31/20 ,  C07D519/00 ,  A61K31/496

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：US20180305315A1

公开(公告)日：2018-10-25

申请号：US15957739

申请日：2018-04-19

Applicant: Gilead Sciences, Inc.

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

IPC: C07D213/69 ,  A61K45/06 ,  A61K31/444 ,  C07D401/14 ,  A61K31/4545 ,  C07D213/85 ,  A61K31/44 ,  C07D213/30 ,  C07D295/088 ,  A61K31/5377

CPC classification number: C07D213/69 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/5377 ,  A61K45/06 ,  C07D213/30 ,  C07D213/61 ,  C07D213/64 ,  C07D213/85 ,  C07D295/088 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107 ,  C07D498/04 ,  C07D519/00

Abstract: Compounds according to 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：US10100052B2

公开(公告)日：2018-10-16

申请号：US15596844

申请日：2017-05-16

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Eda Canales ,  Elbert Chin ,  Kevin S. Currie ,  Ashley Anne Katana ,  Darryl Kato ,  John O. Link ,  Samuel E. Metobo ,  Roland D. Saito ,  Zheng-Yu Yang

IPC: C07D471/04

Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions which may be used in methods of treating a hepatitis B virus infection.

公开(公告)号：US20180282316A1

公开(公告)日：2018-10-04

申请号：US16001832

申请日：2018-06-06

Applicant: Gilead Sciences, Inc.

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

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

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, R4a, R4b, and R5 are described herein.

公开(公告)号：US20180251460A1

公开(公告)日：2018-09-06

申请号：US15885390

申请日：2018-01-31

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Eda Canales ,  Kevin S. Currie ,  Darryl Kato ,  Jiayao Li ,  John O. Link ,  Samuel E. Metobo ,  Roland D. Saito ,  Scott D. Schroeder ,  Nathan Shapiro ,  Winston C. Tse ,  Qiaoyin Wu

IPC: C07D471/14 ,  C07D498/14 ,  C07D519/00 ,  C07D491/22 ,  C07B59/00 ,  A61P31/20

CPC classification number: C07D471/14 ,  A61P31/20 ,  C07B59/002 ,  C07B2200/05 ,  C07D491/22 ,  C07D498/14 ,  C07D519/00

Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions which may be used in methods of treating a hepatitis B virus infection.

公开(公告)号：US09458145B2

公开(公告)日：2016-10-04

申请号：US14273147

申请日：2014-05-08

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

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: 本申请涉及可用作抑制剂的化合物; 或其它可能调节含溴结构域的蛋白质（包括含有溴结构域的蛋白质4（BRD4））的活性，以及​​含有这些化合物的组合物和制剂，以及使用和制备这些化合物的方法。 化合物包括其中R1a，R1b，R2，R2b，R3，R4a，R4b和R5如本文所述的式（I）化合物。

公开(公告)号：US09255089B2

公开(公告)日：2016-02-09

申请号：US14227736

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 R. Mish ,  Sophie Shevick ,  David Sperandio ,  Hai Yang ,  Jeff Zablocki

IPC: C07D413/14 ,  C07D413/04 ,  C07D417/14

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。