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公开(公告)号：US09655944B2
公开(公告)日：2017-05-23
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: A61K38/21 , A61K38/06 , C07D498/16 , A61K31/4985 , C07D498/22 , A61K31/4745 , A61K31/506 , A61K31/519 , A61K45/06 , C07K5/087 , C07K5/08 , C07K5/083 , A61K38/00
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.
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公开(公告)号：US20150038488A1
公开(公告)日：2015-02-05
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
IPC: C07D487/04 , C07D417/04 , C07D417/12 , C07D403/12 , C07D471/04 , C07D401/14
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：US11976083B2
公开(公告)日：2024-05-07
申请号：US17242617
申请日：2021-04-28
Applicant: Gilead Sciences, Inc.
Inventor： Eda Y. Canales , Weng K. Chang , Laurent P. Debien , Petr Jansa , Jennifer A. Loyer-Drew , Luisruben P. Martinez , Stephane Perreault , Gary B Phillips , Hyung-Jung Pyun , Roland D. Saito , Michael S. Sangi , Adam J. Schrier , Marina E. Shatskikh , James G. Taylor , Jennifer A. Treiberg , Joshua J. Van Veldhuizen
IPC: C07D471/18 , A61K31/4184 , A61K31/4188 , A61K31/437 , A61K45/06 , A61P3/10 , A61P7/02 , A61P19/02 , A61P35/00 , C07D471/12 , C07D471/14 , C07D487/08 , C07D491/22 , C07D498/18 , C07D498/22 , C07D513/18 , C07D519/00
CPC classification number: C07D519/00 , A61K45/06 , C07D471/14
Abstract: The present disclosure relates to novel compounds for use in therapeutic treatment of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.
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公开(公告)号：US10005774B2
公开(公告)日：2018-06-26
申请号：US15150038
申请日：2016-05-09
Applicant: Gilead Sciences, Inc.
Inventor： Peter A. Blomgren , Jayaraman Chandrasekhar , Kevin S. Currie , Zhimin Du , Julie Farand , Juan A. Guerrero , Ashley A. Katana , Darryl Kato , Jeffrey E. 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 , C07D401/14 , C07D403/12 , C07D417/04 , C07D417/12 , C07D487/04 , C07D407/14 , C07D417/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D491/08 , C07D498/04 , C07D519/00
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.
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公开(公告)号：US20170313745A1
公开(公告)日：2017-11-02
申请号：US15455508
申请日：2017-03-10
Applicant: Gilead Sciences, Inc.
Inventor： Kyla L. Bjornson , Kapil K. Karki , John O. Link , Hyung-jung Pyun , Adam J. Schrier , Kirk L. Stevens , James G. Taylor , Randall W. Vivian , Jeff Zablocki , Sheila M. Zipfel
IPC: C07K7/64 , C07D487/02 , C07D487/00 , C07D203/02 , A61K31/519 , C07D498/22 , A61K31/437
CPC classification number: C07K7/64 , A61K31/437 , A61K31/519 , C07D203/02 , C07D487/00 , C07D487/02 , C07D498/22
Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein the various substituents are defined herein, methods of using said compounds, and pharmaceutical compositions containing said compounds.
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Patent Agency Ranking
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.
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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
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。
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公开(公告)号：US12240862B2
公开(公告)日：2025-03-04
申请号：US17558130
申请日：2021-12-21
Applicant: Gilead Sciences, Inc.
Inventor： Daniel H. Byun , Eda Y. Canales , Laurent P. Debien , Petr Jansa , Rick A. Lee , Jennifer A. Loyer-Drew , Stephane Perreault , Hyung-Jung Pyun , Roland D. Saito , Michael S. Sangi , Adam J. Schrier , Marina E. Shatskikh , James G. Taylor , Jennifer A. Treiberg , Joshua J. Van Veldhuizen , Lianhong Xu
IPC: A61P35/02 , C07D519/00
Abstract: The present disclosure relates to novel compounds for use in therapeutic treatment of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.
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公开(公告)号：US20240376110A1
公开(公告)日：2024-11-14
申请号：US18663952
申请日：2024-05-14
Applicant: Gilead Sciences, Inc.
Inventor： Megan K. Armstrong , Elbert Chin , Chienhung Chou , Laurent P. Debien , Yifan Deng , Joshua D. Farr , Pancham Lal Gupta , Chao-I Hung , Benjamin J. June , Prasenjit K. Mukherjee , Shaina V. Nguyen , Gregory T. Notte , Daniel Roa , Adam J. Schrier , Katie A. Spence , Zheng-Yu Yang
IPC: C07D487/04 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/5386 , A61K31/55 , A61K45/06 , A61P35/00 , C07D487/14 , C07D519/00
Abstract: The present disclosure relates generally to compounds that inhibit PRMT5. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through inhibiting PRMT5. The disclosure further relates to the use of the compounds for the treatment of a disease or condition associated with chromosome 9p21 deletion, MTAP null, or any other MTAP deficiency. The disclosure further relates to the use of the compounds for the treatment of cancers.
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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.
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