公开(公告)号：US20170333438A1

公开(公告)日：2017-11-23

申请号：US15588346

申请日：2017-05-05

Applicant: Gilead Sciences, Inc.

Inventor： Ernest A. Carra ,  Irene Chen ,  Katie Ann Keaton ,  Scott E. Lazerwith ,  Vahid Zia

IPC: A61K31/5365 ,  A61K9/20 ,  A61K45/06 ,  C07D498/18 ,  C07D498/14 ,  A61K31/537

CPC classification number: A61K31/5365 ,  A61K9/20 ,  A61K31/513 ,  A61K31/537 ,  A61K31/553 ,  A61K31/675 ,  A61K31/683 ,  A61K45/06 ,  C07B2200/13 ,  C07D498/14 ,  C07D498/18 ,  Y02A50/395 ,  A61K2300/00

Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.

公开(公告)号：US09732092B2

公开(公告)日：2017-08-15

申请号：US15349934

申请日：2016-11-11

Applicant: Gilead Sciences, Inc.

Inventor： Haolun Jin ,  Scott E. Lazerwith ,  Hyung-Jung Pyun ,  Elizabeth M. Bacon ,  Philip Anthony Morganelli ,  Mingzhe Ji

IPC: A61K31/5365 ,  C07D413/14 ,  C07D498/14 ,  A61K45/06 ,  A61K31/537 ,  A61K31/553

CPC classification number: C07D498/14 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/529 ,  A61K31/537 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D471/18 ,  C07D471/22 ,  C07D487/14 ,  C07D498/18 ,  A61K2300/00

Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

公开(公告)号：US09682084B2

公开(公告)日：2017-06-20

申请号：US14745121

申请日：2015-06-19

Applicant: Gilead Sciences, Inc.

Inventor： Ernest A. Carra ,  Irene Chen ,  Katie Ann Keaton ,  Scott E. Lazerwith ,  Vahid Zia

IPC: A61K31/5365 ,  C07D498/18 ,  A61K45/06 ,  A61K9/20 ,  C07D498/14 ,  A61K31/537

CPC classification number: A61K31/5365 ,  A61K9/20 ,  A61K31/513 ,  A61K31/537 ,  A61K31/553 ,  A61K31/675 ,  A61K31/683 ,  A61K45/06 ,  C07B2200/13 ,  C07D498/14 ,  C07D498/18 ,  Y02A50/395 ,  A61K2300/00

Abstract: The present invention relates to crystalline forms and co-crystals of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, the pharmaceutical formulations, and the therapeutic uses thereof. The present invention also relates to novel crystalline forms of sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.

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：US09376441B2

公开(公告)日：2016-06-28

申请号：US14448160

申请日：2014-07-31

Applicant: Gilead Sciences, Inc.

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

IPC: A61K31/4015 ,  C07D207/12 ,  C07D487/04 ,  C07D401/14 ,  C07D403/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D407/14 ,  C07D417/14

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: 本公开涉及作为Syk抑制剂的化合物及其在治疗各种疾病状态（包括癌症和炎性病症）中的用途。 在具体实施方案中，化合物的结构由式I给出：其中X 1，X 2，X 3，R 2，R 3，R 4，R 5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：US08841278B2

公开(公告)日：2014-09-23

申请号：US14045717

申请日：2013-10-03

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Eda Canales ,  Aesop Cho ,  Jeromy J. Cottell ,  Manoj C. Desai ,  Michael Graupe ,  Hongyan Guo ,  Randall L. Halcomb ,  Darryl Kato ,  Choung U. Kim ,  Thorsten A. Kirschberg ,  Evan S. Krygowski ,  Scott E. Lazerwith ,  John O. Link ,  Hongtao Liu ,  Qi Liu ,  Richard L. Mackman ,  Michael L. Mitchell ,  Jay P. Parrish ,  Hyung-Jung Pyun ,  Joseph H. Saugier ,  Scott D. Schroeder ,  Jianyu Sun ,  James G. Taylor ,  James D. Trenkle ,  Winston C. Tse ,  Randall W. Vivian ,  William J. Watkins ,  Lianhong Xu

IPC: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07D495/04 ,  A61K31/4178 ,  A61K31/7068 ,  A61K31/7052 ,  A61K31/4184 ,  A61P1/16 ,  A61P31/14

CPC classification number: C07D403/14 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/427 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  A61P31/12 ,  C07D207/16 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/113 ,  C07D495/04 ,  C07F5/025

Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

公开(公告)号：US20140030223A1

公开(公告)日：2014-01-30

申请号：US14037296

申请日：2013-09-25

Applicant: Gilead Sciences, Inc.

Inventor： Eda Canales ,  Lee S. Chong ,  Michael O'Neil Hanrahan Clarke ,  Edward Doerffler ,  Scott E. Lazerwith ,  Willard Lew ,  Qi Liu ,  Michael Martzman ,  Philip Anthony Morganelli ,  William J. Watkins ,  Hong Ye

IPC: A61K31/513 ,  A61K31/4436 ,  A61K45/06 ,  A61K31/4709 ,  A61K31/501 ,  C07D417/12 ,  A61K31/427 ,  C07D409/12 ,  A61K31/497

CPC classification number: A61K31/513 ,  A61K31/427 ,  A61K31/4436 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61K45/06 ,  C07D333/68 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D493/04

Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Abstract translation: 提供式I的化合物及其药学上可接受的盐和酯。 所提供的化合物，组合物和方法可用于治疗黄病毒科感染，特别是丙型肝炎感染。

公开(公告)号：US20250049780A1

公开(公告)日：2025-02-13

申请号：US18771751

申请日：2024-07-12

Applicant: Gilead Sciences, Inc.

Inventor： Stephen E. Ammann ,  Eda Y. Canales ,  Weng K. Chang ,  Henok H. Kinfe ,  Scott E. Lazerwith ,  Michael L. Mitchell ,  Yasamin Moazami ,  Scott D. Schroeder ,  Daniel G. Shore

IPC: A61K31/4545 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4706 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D519/00

Abstract: The present disclosure relates generally to certain compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions provided herein may be used for the treatment or prevention of an autoimmune disease and/or inflammatory condition, including systemic lupus erythematosus and cutaneous lupus erythematosus.

公开(公告)号：US12070455B2

公开(公告)日：2024-08-27

申请号：US17930538

申请日：2022-09-08

Applicant: Gilead Sciences, Inc.

Inventor： Stephen E. Ammann ,  Eda Y. Canales ,  Weng K. Chang ,  Henok H. Kinfe ,  Scott E. Lazerwith ,  Michael L. Mitchell ,  Yasamin Moazami ,  Scott D. Schroeder ,  Daniel G. Shore

IPC: C07D519/00 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/4706 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06

CPC classification number: A61K31/4545 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4706 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D519/00

Abstract: The present disclosure relates generally to certain compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions provided herein may be used for the treatment or prevention of an autoimmune disease and/or inflammatory condition, including systemic lupus erythematosus and cutaneous lupus erythematosus.

公开(公告)号：US11963967B2

公开(公告)日：2024-04-23

申请号：US18304270

申请日：2023-04-20

Applicant: Gilead Sciences, Inc.

Inventor： Scott E. Lazerwith ,  Jonathan William Medley ,  Philip A. Morganelli ,  Thomas P. Stratton ,  Peiyuan Wang

IPC: A61K31/685

CPC classification number: A61K31/685

Abstract: Compounds and methods of using said compounds, alone or in combination with additional agents, and pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.