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公开(公告)号：US09951065B2
公开(公告)日：2018-04-24
申请号：US15153527
申请日：2016-05-12
Applicant: Gilead Sciences, Inc.
Inventor： Mark J. Bartlett , Julian Andrew Codelli , Britton Kenneth Corkey , Jennifer Leigh Cosman , Kristyna Elbel , Jennifer Alissa Loyer-Drew , David Sperandio , Joshua Van Veldhuizen , Hai Yang , Suet Chung Yeung
IPC: C07D235/06 , C07D235/24 , C07D295/125 , C07D401/12 , C07D471/04 , A61K45/06 , C07D235/08 , A61K31/4184 , A61K31/5377 , A61K31/454 , A61K31/437 , A61K31/506 , A61K31/497 , A61K31/55 , A61K31/541 , A61K31/439 , C07D405/12 , C07D405/14 , C07D471/08 , A61K31/553 , C07D235/30 , C07D235/14 , C07D401/04 , C07D235/12 , A61K31/444 , A61K31/4545 , A61K31/538 , A61K31/5386 , A61K31/438 , C07D403/12 , A61K31/4439 , C07D413/12 , A61K31/496 , C07D487/04 , A61K31/4725 , C07D235/28 , C07D235/16 , C07D409/12
CPC classification number: C07D471/04 , A61K31/4184 , A61K31/437 , A61K31/438 , A61K31/439 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5386 , A61K31/541 , A61K31/55 , A61K31/553 , A61K45/06 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D235/28 , C07D235/30 , C07D295/125 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D471/08 , C07D487/04
Abstract: The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.
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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。
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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。
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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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Patent Agency Ranking
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：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：US20160333009A1
公开(公告)日：2016-11-17
申请号：US15153527
申请日：2016-05-12
Applicant: Gilead Sciences, Inc.
Inventor： Mark J. Bartlett , Julian Andrew Codelli , Britton Kenneth Corkey , Jennifer Leigh Cosman , Kristyna Elbel , Jennifer Alissa Loyer-Drew , David Sperandio , Joshua Van Veldhuizen , Hai Yang , Suet Chung Yeung
IPC: C07D471/04 , C07D235/08 , A61K31/4184 , A61K31/5377 , C07D401/12 , A61K31/454 , A61K31/437 , A61K31/506 , A61K31/497 , A61K31/55 , A61K31/541 , A61K31/439 , C07D405/12 , C07D405/14 , C07D471/08 , A61K31/553 , C07D235/30 , C07D235/14 , C07D401/04 , C07D235/12 , A61K31/444 , A61K31/4545 , A61K31/538 , A61K31/5386 , A61K31/438 , C07D403/12 , A61K31/4439 , C07D235/24 , C07D413/12 , A61K31/496 , C07D487/04 , A61K31/4725 , C07D235/28 , A61K45/06
CPC classification number: C07D471/04 , A61K31/4184 , A61K31/437 , A61K31/438 , A61K31/439 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5386 , A61K31/541 , A61K31/55 , A61K31/553 , A61K45/06 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D235/28 , C07D235/30 , C07D295/125 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D471/08 , C07D487/04
Abstract: The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDOL) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.
Abstract translation: 或其药学上可接受的盐，其中X，L，n，m，R1，R2a，R2b，Rn，Rm和Rt如本文所定义，以及包含式I化合物或其药学上可接受的盐的药物组合物 以及使用其来治疗由IDO1介导的病症的方法。
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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。
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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。
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