公开(公告)号：US20180298011A1

公开(公告)日：2018-10-18

申请号：US15923726

申请日：2018-03-16

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Constantine G. Boojamra ,  Eugene J. Eisenberg ,  Hon Chung Hui ,  Richard L. Mackman ,  Jay P. Parrish ,  Michael Sangi ,  Oliver L. Saunders ,  Dustin Siegel ,  David Sperandio ,  Hai Yang

IPC: C07D487/04 ,  A61K45/06 ,  C07F9/6561 ,  C07D519/00 ,  A61K31/519 ,  C07D495/04 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/675 ,  C07D513/04

Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

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.

公开(公告)号：US09504689B2

公开(公告)日：2016-11-29

申请号：US14635830

申请日：2015-03-02

Applicant: Gilead Sciences, Inc.

Inventor： Dustin Siegel ,  David Sperandio ,  Hai Yang ,  Michael Sangi ,  Jay P. Parrish ,  Hon Chung Hui

IPC: A61K31/519 ,  A61K31/5377 ,  C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  A61K45/06 ,  A61K31/4545 ,  A61K31/5025 ,  A61K31/53

CPC classification number: C07D487/04 ,  A61K31/4545 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

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：US08980878B2

公开(公告)日：2015-03-17

申请号：US13865069

申请日：2013-04-17

Applicant: Gilead Sciences, Inc.

Inventor： Dustin Siegel ,  David Sperandio ,  Hai Yang ,  Michael Sangi ,  Jay P. Parrish ,  Hon Chung Hui

IPC: A61K31/00 ,  C07D413/00

CPC classification number: C07D487/04 ,  A61K31/4545 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

Abstract translation: 提供了用于治疗病毒感染的化合物及其药学上可接受的盐和酯及其组合物。 化合物和组合物可用于治疗肺炎链球菌病毒感染。 提供的化合物，组合物和方法特别可用于治疗人呼吸道合胞病毒感染。

公开(公告)号：US08809330B2

公开(公告)日：2014-08-19

申请号：US14069685

申请日：2013-11-01

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Constantine G. Boojamra ,  Eugene J. Eisenberg ,  Hon Chung Hui ,  Richard L. Mackman ,  Jay P. Parrish ,  Michael Sangi ,  Oliver L. Saunders ,  Dustin Siegel ,  David Sperandio ,  Hai Yang

IPC: A61P31/14

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/675 ,  A61K45/06 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00 ,  C07F9/65616

Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

Abstract translation: 本发明提供了本文所述的式I或式II化合物或其药学上可接受的盐或酯。 其化合物及其组合物可用于治疗肺炎链球菌病毒感染。 提供的化合物，组合物和方法特别可用于治疗人呼吸道合胞病毒感染。

公开(公告)号：US20180179191A1

公开(公告)日：2018-06-28

申请号：US15809296

申请日：2017-11-10

Applicant: Gilead Sciences, Inc.

Inventor： Jinyu Shen ,  Mustapha St. Jules ,  David Sperandio ,  Sankar Mohan

IPC: C07D403/14 ,  C07D235/08 ,  C07D213/30 ,  C07D261/08 ,  C07B37/04 ,  C07B37/10

CPC classification number: C07D403/14 ,  C07B37/04 ,  C07B37/10 ,  C07D213/30 ,  C07D235/08 ,  C07D261/08 ,  C07D413/04 ,  C07D413/14

Abstract: The present disclosure provides processes for the preparation of a compound of formula I: or a salt or co-crystal thereof, that modulates the activity of bromodomain-containing proteins. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

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：US20160130275A1

公开(公告)日：2016-05-12

申请号：US14995486

申请日：2016-01-14

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Constantine G. Boojamra ,  Eugene J. Eisenberg ,  Hon Chung Hui ,  Richard L. Mackman ,  Jay P. Parrish ,  Michael Sangi ,  Oliver L. Saunders ,  Dustin Siegel ,  David Sperandio ,  Hai Yang

IPC: C07D487/04 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/551 ,  A61K31/55 ,  A61K31/519 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/675 ,  A61K45/06 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00 ,  C07F9/65616

Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

Abstract translation: 本发明提供了本文所述的式I或式II化合物或其药学上可接受的盐或酯。 其化合物及其组合物可用于治疗肺炎链球菌病毒感染。 提供的化合物，组合物和方法特别可用于治疗人呼吸道合胞病毒感染。

公开(公告)号：US09238039B2

公开(公告)日：2016-01-19

申请号：US13905410

申请日：2013-05-30

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Constantine G. Boojamra ,  Eugene J. Eisenberg ,  Hon Chung Hui ,  Richard L. Mackman ,  Jay P. Parrish ,  Michael Sangi ,  Oliver L. Saunders ,  Dustin Siegel ,  David Sperandio ,  Hai Yang

IPC: C07D487/04 ,  A61K31/519 ,  A61K31/55 ,  A61K31/551 ,  A61P11/00 ,  A61K31/675 ,  A61K45/06 ,  A61K31/5377 ,  C07D495/04 ,  C07D513/04 ,  C07F9/6561

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/675 ,  A61K45/06 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00 ,  C07F9/65616

Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

Abstract translation: 本发明提供了本文所述的式I或式II化合物或其药学上可接受的盐或酯。 其化合物及其组合物可用于治疗肺炎链球菌病毒感染。 提供的化合物，组合物和方法特别可用于治疗人呼吸道合胞病毒感染。