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公开(公告)号：US10072001B2
公开(公告)日：2018-09-11
申请号：US14728562
申请日：2015-06-02
Applicant: Gilead Sciences, Inc.
Inventor： Zhimin Du , Juan Arnaldo Guerrero , Joshua Aaron Kaplan , John Edward Knox, Jr. , Devan Naduthambi , Barton W. Phillips , Chandrasekar Venkataramani , Peiyuan Wang , William J. Watkins , Jeff Zablocki
IPC: C07D471/04 , C07D487/04 , C07D519/00 , C07D473/00
CPC classification number: C07D471/04 , C07D473/00 , C07D487/04 , C07D519/00
Abstract: Compounds having the following formula (I) and methods of their use and preparation are disclosed:
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公开(公告)号：US09938278B2
公开(公告)日：2018-04-10
申请号：US14971825
申请日：2015-12-16
Applicant: Gilead Sciences, Inc.
Inventor： Christian Gege , Claus Kremoser , Olaf Kinzel , Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Aaron C. Schmitt , William J. Watkins , Jianjun Xu
IPC: A61K31/506 , C07D471/08 , C07D401/14 , C07D413/14 , C07D261/08 , C07D413/12 , C07D417/14
CPC classification number: C07D471/08 , C07D261/08 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/14
Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
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公开(公告)号：US20170152240A1
公开(公告)日：2017-06-01
申请号：US15429086
申请日：2017-02-09
Applicant: Gilead Sciences, Inc.
Inventor： Elizabeth M. Bacon , Gayatri Balan , Chien-Hung Chou , Christopher T. Clark , Jeromy J. Cottell , Musong Kim , Thorsten A. Kirschberg , John O. Link , Gary Phillips , Scott D. Schroeder , Neil H. Squires , Kirk L. Stevens , James G. Taylor , William J. Watkins , Nathan E. Wright , Sheila M. Zipfel
IPC: C07D401/14
CPC classification number: C07D498/04 , C07B59/002 , C07B2200/05 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D495/04
Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.
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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。
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Patent Agency Ranking
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。
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公开(公告)号：US20150361068A1
公开(公告)日：2015-12-17
申请号：US14735244
申请日：2015-06-10
Applicant: Gilead Sciences, Inc.
Inventor： Shaopei Cai , Zhimin Du , Musong Kim , Jennifer A. Loyer-Drew , Devan Naduthambi , Leena Patel , Barton W. Phillips , Gary Phillips , Kirk L. Stevens , Jennifer Anne Treiberg , Joshua Van Veldhuizen , William J. Watkins , Suet Chung Yeung
IPC: C07D403/12 , C07D403/14 , C07D487/04 , C07D413/14 , C07D405/14 , C07D473/34 , C07D401/14 , C07D513/04 , C07D471/04
CPC classification number: C07D403/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D473/34 , C07D487/04 , C07D513/04
Abstract: The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein n, W, A′, B′, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.
Abstract translation: 本申请提供式（J）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物，其中本文描述了n，W，A'，B'，R 1，R 2和R 3。 这些化合物是磷脂酰肌醇3-激酶（PI3K）活性的抑制剂，可用于治疗由一种或多种PI3K同种型介导的病症。 本申请还提供包含式（I）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K同种型介导的病症的方法。
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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.
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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。
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公开(公告)号：US20130302280A1
公开(公告)日：2013-11-14
申请号：US13927355
申请日：2013-06-26
Applicant: Gilead Sciences, Inc.
Inventor： Aesop Cho , Lee S. Chong , Michael O'Neil Hanrahan Clarke , Edward Doerffler , Choung U. Kim , Qi Liu , William J. Watkins , Jennifer R. Zhang
IPC: C07F9/6553 , A61K45/06 , A61K31/683 , A61K31/675 , C07F9/6561 , C07F9/6568 , A61K31/67 , C07F9/6558
CPC classification number: C07F9/655345 , A61K31/662 , A61K31/67 , A61K31/675 , A61K31/683 , A61K45/06 , C07F9/65586 , C07F9/6561 , C07F9/65681
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。
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