公开(公告)号：US09440991B2

公开(公告)日：2016-09-13

申请号：US14576143

申请日：2014-12-18

Applicant: GILEAD SCIENCES, INC.

Inventor： Amy Cagulada ,  Johann Chan ,  Lina Chan ,  Denise A. Colby ,  Kapil Kumar Karki ,  Darryl Kato ,  Katie Ann Keaton ,  Sudha Kondapally ,  Chris Levins ,  Adam Littke ,  Ruben Martinez ,  Dominika Pcion ,  Troy Reynolds ,  Bruce Ross ,  Michael Sangi ,  Adam J. Schrier ,  Pamela Seng ,  Dustin Siegel ,  Nathan Shapiro ,  Donald Tang ,  James G. Taylor ,  Jonathan Tripp ,  Andrew W. Waltman ,  Lawrence Yu

IPC: C07D403/12 ,  C07D413/14 ,  C07D498/16 ,  C07C227/02 ,  C07D453/02 ,  C07C209/00 ,  C07C51/09 ,  C07K5/083

CPC classification number: C07D498/18 ,  C07C51/09 ,  C07C205/57 ,  C07C209/00 ,  C07C227/02 ,  C07C233/09 ,  C07C251/12 ,  C07C255/61 ,  C07C271/34 ,  C07C2601/02 ,  C07D241/44 ,  C07D403/12 ,  C07D453/02 ,  C07D498/16 ,  C07K5/0808

Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. 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：US20160130300A1

公开(公告)日：2016-05-12

申请号：US14996961

申请日：2016-01-15

Applicant: Gilead Sciences, Inc.

Inventor： Kyla Bjornson ,  Eda Canales ,  Jeromy J. Cottell ,  Kapil K. Karki ,  Ashley A. Katana ,  Darryl Kato ,  Tetsuya Kobayashi ,  John O. Link ,  Ruben Martinez ,  Barton W. Phillips ,  Hyung-jung Pyun ,  Michael Sangi ,  Adam J. Schrier ,  Dustin Siegel ,  James G. Taylor ,  Chinh V. Tran ,  Teresa A. Trejo Martin ,  Randall W. Vivian ,  Zheng-Yu Yang ,  Jeff Zablocki ,  Sheila Zipfel

IPC: C07K5/083 ,  C07K5/087

Abstract: Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.

Abstract translation: 公开的式I化合物及其药学上可接受的盐。 还公开了使用所述化合物和含有所述化合物的药物组合物的方法。

公开(公告)号：US20150166546A1

公开(公告)日：2015-06-18

申请号：US14566340

申请日：2014-12-10

Applicant: Gilead Sciences, Inc.

Inventor： Constantine G. Boojamra ,  Hon Chung Hui ,  Petr Jansa ,  Richard L. Mackman ,  Jay P. Parrish ,  Michael Sangi ,  Dustin Siegel ,  David Sperandio ,  Hai Yang

IPC: C07D487/04

CPC classification number: A61K31/5025 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/675 ,  A61K45/06 ,  C07D487/04 ,  C07D487/08 ,  C07D519/00 ,  C07F9/6561

Abstract: The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.

Abstract translation: 本发明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，包括人呼吸道合胞病毒感染。

公开(公告)号：US20130273037A1

公开(公告)日：2013-10-17

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: C07D487/04 ,  C07D471/04 ,  A61K45/06 ,  C07D519/00

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.

公开(公告)号：US10030033B2

公开(公告)日：2018-07-24

申请号：US15227527

申请日：2016-08-03

Applicant: Gilead Sciences, Inc.

Inventor： Amy Cagulada ,  Johann Chan ,  Lina Chan ,  Denise A. Colby ,  Kapil Kumar Karki ,  Darryl Kato ,  Katie Ann Keaton ,  Sudha Kondappally ,  Chris Levins ,  Adam Littke ,  Ruben Martinez ,  Dominika Pcion ,  Troy Reynolds ,  Bruce Ross ,  Michael Sangi ,  Adam J. Schrier ,  Pamela Seng ,  Dustin Siegel ,  Nathan Shapiro ,  Donald Tang ,  James G. Taylor ,  Jonathan Tripp ,  Andrew W. Waltman ,  Lawrence Yu

IPC: C07D498/16 ,  C07D403/12 ,  C07D498/18 ,  C07C271/34 ,  C07D241/44 ,  C07C205/57 ,  C07C233/09 ,  C07C251/12 ,  C07C255/61

Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. 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：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.

公开(公告)号：US20170342079A1

公开(公告)日：2017-11-30

申请号：US15618974

申请日：2017-06-09

Applicant: Gilead Sciences, Inc.

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

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

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：US20170029427A1

公开(公告)日：2017-02-02

申请号：US15191974

申请日：2016-06-24

Applicant: Gilead Sciences, Inc.

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

IPC: C07D487/04 ,  A61K45/06 ,  A61K31/5025

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：US20160368918A1

公开(公告)日：2016-12-22

申请号：US15150038

申请日：2016-05-09

Applicant: Gilead Sciences, Inc.

Inventor： Peter Blomgren ,  Jayaraman Chandrasekhar ,  Kevin S. Currie ,  Zhimin Du ,  Julie Farand ,  Juan A. Guerrero ,  Ashley A. Katana ,  Darryl Kato ,  Jeffrey Kropf ,  Scott E. Lazerwith ,  Seung H. Lee ,  Jiayao Li ,  John O. Link ,  Jennifer R. Lo ,  Nicholas Mai ,  Scott A. Mitchell ,  Gregory Notte ,  Hyung-jung Pyun ,  Michael Sangi ,  Aaron C. Schmitt ,  Adam J. Schrier ,  Kirk L. Stevens ,  Chandrasekar Venkataramani ,  William J. Watkins ,  Jin Ming Xiong ,  Jianjun Xu ,  Zheng-Yu Yang ,  Jeff Zablocki ,  Zhongdong Zhao ,  Sheila Zipfel

IPC: C07D471/04 ,  C07D403/14 ,  C07D401/14 ,  C07D519/00 ,  C07D487/04 ,  C07D498/04 ,  C07D413/14 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D403/12 ,  C07D491/08

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D519/00

Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.

Abstract translation: 其中X1，X2，X3，R2，R3，R4，R5和Y如本文所述。 本公开进一步提供包含式I化合物或其药学上可接受的盐的药物组合物，以及使用这些化合物和组合物治疗由Syk介导的病症的方法。

公开(公告)号：US20160361375A1

公开(公告)日：2016-12-15

申请号：US15185273

申请日：2016-06-17

Applicant: Gilead Sciences, Inc.

Inventor： Kyla Bjornson ,  Eda Canales ,  Jeromy J. Cottell ,  Kapil K. Karki ,  Ashley A. Katana ,  Darryl Kato ,  Tetsuya Kobayashi ,  John O. Link ,  Ruben Martinez ,  Barton W. Phillips ,  Hyung-jung Pyun ,  Michael Sangi ,  Adam J. Schrier ,  Dustin Siegel ,  James G. Taylor ,  Chinh V. Tran ,  Teresa A. Trejo Martin ,  Randall W. Vivian ,  Zheng-Yu Yang ,  Jeff Zablocki ,  Sheila Zipfel

IPC: A61K38/06

CPC classification number: A61K31/498 ,  A61K31/10 ,  A61K31/401 ,  A61K31/4745 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K38/00 ,  A61K38/06 ,  A61K38/21 ,  A61K45/06 ,  C07D241/36 ,  C07D403/14 ,  C07D498/16 ,  C07D498/22 ,  C07K5/08 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0827 ,  A61K2300/00

Abstract: Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.

Abstract translation: 以及其药学上可接受的盐。 还公开了使用所述化合物和含有所述化合物的药物组合物的方法。