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11.
公开(公告)号:US20140336190A1
公开(公告)日:2014-11-13
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 , C07D413/14 , C07D417/14 , 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, R2, 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。
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公开(公告)号:US20230212155A1
公开(公告)日:2023-07-06
申请号:US18060934
申请日:2022-12-01
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
CPC classification number: 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 , C07K16/2818
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.
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公开(公告)号:US11453681B2
公开(公告)日:2022-09-27
申请号:US16880134
申请日:2020-05-21
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
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.
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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.
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15.
公开(公告)号:US10988498B2
公开(公告)日:2021-04-27
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 , A61K31/7056 , A61K31/706 , A61K31/7052
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.
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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.
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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.
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18.
公开(公告)号:US20140296246A1
公开(公告)日:2014-10-02
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
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。
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公开(公告)号:US11236085B2
公开(公告)日:2022-02-01
申请号:US16660219
申请日:2019-10-22
Applicant: Gilead Sciences, Inc.
Inventor: Zhimin Du , Michael Graupe , Paulo A. Machicao Tello , Jonathan William Medley , Samuel E. Metobo , Eric Q. Parkhill , Barton W. Phillips , Scott P. Simonovich , Peiyuan Wang , Jie Xu , Christopher A. Ziebenhaus
IPC: C07D471/04 , C07D217/04 , C07D401/12 , C07D401/14 , C07D413/10 , C07D471/08 , C07D487/04 , C07D495/04 , C07D513/04 , C07K16/28 , C07K16/40
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.
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公开(公告)号:US20210323922A1
公开(公告)日:2021-10-21
申请号:US17098171
申请日:2020-11-13
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 , A61K31/5377 , C07D213/85 , A61K31/44 , C07D213/30 , C07D295/088 , A61K31/4545 , C07D401/04 , A61K31/497 , C07D519/00 , C07D487/10 , C07D487/08 , C07D213/64 , C07D491/107 , C07D498/04 , C07D213/61 , C07D405/14
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.
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