公开(公告)号：US20140072554A1

公开(公告)日：2014-03-13

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: A61K31/519 ,  A61K45/06 ,  C07D487/04

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.

公开(公告)号：US20170362244A1

公开(公告)日：2017-12-21

申请号：US15639970

申请日：2017-06-30

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

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.

公开(公告)号：US20170088554A1

公开(公告)日：2017-03-30

申请号：US15257482

申请日：2016-09-06

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Michael L. Mitchell ,  Ryan McFadden ,  Paul A. Roethle ,  Lianhong Xu ,  Hong Yang

IPC: C07D491/06 ,  C07D277/64 ,  A61K31/428 ,  A61K9/12 ,  C07D417/10 ,  A61K9/20 ,  A61K9/48 ,  A61K9/00 ,  A61K45/06 ,  A61K31/4741

CPC classification number: C07D491/06 ,  A61K9/0019 ,  A61K9/12 ,  A61K9/20 ,  A61K9/48 ,  A61K31/428 ,  A61K31/4741 ,  A61K45/06 ,  C07D277/62 ,  C07D277/64 ,  C07D277/82 ,  C07D417/04 ,  C07D417/10 ,  C07D491/052

Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provided pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.

公开(公告)号：US20160024104A1

公开(公告)日：2016-01-28

申请号：US14632771

申请日：2015-02-26

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Michael L. Mitchell ,  Ryan McFadden ,  Paul A. Roethle ,  Lianhong Xu ,  Hong Yang

IPC: C07D491/052 ,  A61K45/06 ,  A61K31/4741

CPC classification number: C07D491/06 ,  A61K9/0019 ,  A61K9/12 ,  A61K9/20 ,  A61K9/48 ,  A61K31/428 ,  A61K31/4741 ,  A61K45/06 ,  C07D277/62 ,  C07D277/64 ,  C07D277/82 ,  C07D417/04 ,  C07D417/10 ,  C07D491/052

Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.

Abstract translation: 本发明提供了本文所述的式I化合物或其盐。 本发明还提供了包含式I化合物的药物组合物，制备式I化合物的方法，可用于制备式I化合物的中间体和用于治疗HIV病毒增殖，治疗AIDS或延迟AIDS发作的治疗方法或 哺乳动物使用式I化合物的ARC症状。

公开(公告)号：US09108953B2

公开(公告)日：2015-08-18

申请号：US14549848

申请日：2014-11-21

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Britton K. Corkey ,  Robert H. Jiang ,  David Sperandio ,  Hai Yang

IPC: C07D413/04 ,  C07D413/14 ,  C07D451/04

CPC classification number: C07D413/04 ,  C07D413/14 ,  C07D451/04

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 R1, R2, R3, R4, R7, W, X, and Z are as 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R 1，R 2，R 3，R 4，R 7，W，X和Z如本文所述的式I化合物。

公开(公告)号：US09096586B2

公开(公告)日：2015-08-04

申请号：US13867016

申请日：2013-04-19

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Gediminas Brizgys ,  Hongtao Liu ,  Ryan McFadden ,  Michael L. Mitchell ,  Yingmei Qi ,  Paul A. Roethle ,  Lianhong Xu ,  Hong Yang

IPC: A61K31/425 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/505 ,  A61K31/44 ,  A61K31/415 ,  C07D417/14 ,  C07D417/10 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K31/496 ,  A61K31/428 ,  C07D471/04 ,  A61K31/437 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/454 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/501 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/553 ,  A61K31/551 ,  A61K45/06 ,  A61K31/4741 ,  C07D277/82 ,  C07D491/06 ,  C07D417/04 ,  C07D277/66

CPC classification number: C07D277/82 ,  A61K31/428 ,  A61K31/436 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4741 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D277/66 ,  C07D277/68 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/06 ,  C07D498/04 ,  A61K2300/00

Abstract: Compounds of formula I′: or salts thereof are provided. Pharmaceutical compositions comprising a compound of formula I′, processes for preparing compounds of formula I′, intermediates useful for preparing compounds of formula I′ and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal are also provided.

Abstract translation: 提供式I'化合物或其盐。 包含式I'化合物的药物组合物，制备式I'化合物的方法，可用于制备式I'化合物的中间体和用于治疗HIV病毒增殖的治疗方法，治疗AIDS或延迟AIDS或ARC发作 还提供哺乳动物的症状。

公开(公告)号：US20150111891A1

公开(公告)日：2015-04-23

申请号：US14370466

申请日：2013-01-03

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Gediminas Brizgys ,  Hongyan Guo ,  Paul Hrvatin ,  Eric Lansdon ,  John O. Link ,  Hongtao Liu ,  Ryan McFadden ,  Michael L. Mitchell ,  Yingmei Qi ,  Paul A. Roethle ,  Randall W. Vivian ,  Lianhong Xu ,  Hong Yang

IPC: C07D491/06 ,  A61K45/06 ,  C07C59/64 ,  A61K31/192 ,  C07D213/55 ,  A61K31/5377 ,  A61K31/4406 ,  A61K31/4409 ,  C07D277/30 ,  A61K31/426 ,  A61K31/506 ,  A61K31/436 ,  A61K31/4402

CPC classification number: C07D491/06 ,  A61K31/192 ,  A61K31/426 ,  A61K31/436 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07C59/64 ,  C07D213/55 ,  C07D231/56 ,  C07D277/30 ,  C07D277/34 ,  C07D491/04

Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.

Abstract translation: 本发明提供其化合物及其盐，如本文。 本发明还提供了包含本文公开的化合物的药物组合物，用于制备本文公开的化合物的方法，用于制备本文公开的化合物的中间体和治疗HIV感染的治疗方法，治疗HIV病毒的增殖，治疗AIDS或延迟 使用本文公开的化合物在哺乳动物中的AIDS或ARC症状。

公开(公告)号：US20130281433A1

公开(公告)日：2013-10-24

申请号：US13866997

申请日：2013-04-19

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Gediminas Brizgys ,  Jake Cha ,  Xiaowu Chen ,  Hongyan Guo ,  Randall L. Halcomb ,  Xiaochun Han ,  Richard Huang ,  Hongtao Liu ,  Ryan McFadden ,  Michael L. Mitchell ,  Yingmei Qi ,  Paul A. Roethle ,  Lianhong Xu ,  Hong Yang

IPC: C07D417/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K31/496 ,  A61K31/428 ,  C07D471/04 ,  A61K31/437 ,  A61K31/513 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/454 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/501 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/553 ,  A61K31/551 ,  A61K45/06 ,  C07D417/10

CPC classification number: C07D277/82 ,  A61K31/428 ,  A61K31/436 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4741 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D277/66 ,  C07D277/68 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/06 ,  C07D498/04 ,  A61K2300/00

Abstract: Compounds disclosed herein including compounds of formula I′: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.

Abstract translation: 提供本文公开的化合物，包括式I'化合物及其盐。 还提供了包含本文公开的化合物的药物组合物，用于制备本文公开的化合物的方法，用于制备本文公开的化合物的中间体和使用本文公开的化合物治疗HIV感染的治疗方法。

公开(公告)号：US20180127388A1

公开(公告)日：2018-05-10

申请号：US15658818

申请日：2017-07-25

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Gediminas Brizgys ,  Jacob Y. Cha ,  Xiaowu Chen ,  Hongyan Guo ,  Randall L. Halcomb ,  Xiaochun Han ,  Richard Huang ,  Hongtao Liu ,  Ryan McFadden ,  Michael L. Mitchell ,  Yingmei Qi ,  Paul A. Roethle ,  Lianhong Xu ,  Hong Yang

IPC: C07D277/82 ,  C07D498/04 ,  A61K31/428 ,  C07D487/04 ,  C07D471/04 ,  C07D417/14 ,  C07D417/10 ,  C07D417/04 ,  C07D277/68 ,  C07D277/66 ,  A61K45/06 ,  A61K31/553 ,  A61K31/551 ,  A61K31/5383 ,  A61K31/538 ,  A61K31/5377 ,  A61K31/513 ,  A61K31/506 ,  A61K31/501 ,  A61K31/4985 ,  A61K31/497 ,  A61K31/496 ,  A61K31/4741 ,  A61K31/4709 ,  A61K31/454 ,  A61K31/444 ,  A61K31/4439 ,  A61K31/4375 ,  A61K31/437 ,  A61K31/436 ,  C07D491/06

CPC classification number: C07D277/82 ,  A61K31/428 ,  A61K31/436 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4741 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D277/66 ,  C07D277/68 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/06 ,  C07D498/04 ,  A61K2300/00

Abstract: Compounds disclosed herein including compounds of formula I′: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.

公开(公告)号：US09957275B2

公开(公告)日：2018-05-01

申请号：US15639970

申请日：2017-06-30

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 ,  C07D487/08 ,  C07D495/04 ,  C07D513/04 ,  A61K31/519 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/675 ,  C07F9/6561 ,  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.