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公开(公告)号：US20230012262A1
公开(公告)日：2023-01-12
申请号：US17319507
申请日：2021-05-13
发明人： Brian P. Bestvater , Zhimin Du , Julie Farand , Joshua A. Kaplan , Barton W. Phillips , Doris T. Tang , Chandrasekar Venkataramani , Peiyuan Wang , Kin S. Yang , Anna Zagorska
IPC分类号： C07D401/14 , C07D405/14 , C07D409/14
摘要： The present disclosure relates generally to compounds that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. 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 binding of LPAR1, including fibrosis and liver diseases such as non-alcoholic steatohepatitis (NASH), interstitial lung disease (ILD), or chronic kidney disease (CKD).
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公开(公告)号：US20220411406A1
公开(公告)日：2022-12-29
申请号：US17741991
申请日：2022-05-11
发明人： Brian P. Bestvater , Zhimin Du , Julie Farand , Chandrasekar Venkataramani , Kin S. Yang , Anna Zagorska
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present disclosure relates generally to compounds that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. 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 binding of LPAR1, including fibrosis and liver diseases such as non-alcoholic steatohepatitis (NASH), interstitial lung disease (ILD), or chronic kidney disease (CKD).
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公开(公告)号：US11021467B2
公开(公告)日：2021-06-01
申请号：US14735244
申请日：2015-06-10
发明人： 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分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D473/34 , C07D487/04 , C07D513/04 , C07D405/14 , C07D413/14 , C07D471/04
摘要： 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.
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公开(公告)号：US20190270727A1
公开(公告)日：2019-09-05
申请号：US16274106
申请日：2019-02-12
发明人： Evangelos Aktoudianakis , Aesop Cho , Zhimin Du , Michael Graupe , Lateshkumar Thakorlal Lad , Paulo A. Machicao Tello , Jonathan William Medley , Samuel E. Metobo , Prasenjit Kumar Mukherjee , Devan Naduthambi , Eric Q. Parkhill , Barton W. Phillips , Scott Preston Simonovich , Neil H. Squires , Peiyuan Wang , William J. Watkins , Jie Xu , Kin Shing Yang , Christopher Allen Ziebenhaus
IPC分类号： C07D403/14 , A61P35/02 , A61P31/20 , C07D519/00 , A61K31/496
摘要： Compounds of Formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
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公开(公告)号：US10253019B2
公开(公告)日：2019-04-09
申请号：US16020777
申请日：2018-06-27
发明人： Zhimin Du , Juan A. Guerrero , Joshua A. Kaplan , John E. Knox, Jr. , Jennifer R. Lo , Scott A. Mitchell , Devan Naduthambi , Barton W. Phillips , Chandrasekar Venkataramani , Peiyuan Wang , William J. Watkins , Zhongdong Zhao
IPC分类号： C07D405/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D471/10 , C07D487/04 , C07D491/107 , C07D491/113 , C07D498/04 , A61K31/53 , A61K31/5377 , A61K31/5383 , A61K31/541
摘要： Compounds having the following formula (I) and methods of their use and preparation are disclosed:
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公开(公告)号：US10221197B2
公开(公告)日：2019-03-05
申请号：US14735939
申请日：2015-06-10
发明人： Zhimin Du , Jerry Evarts , Joshua Kaplan , Musong Kim , Devan Naduthambi , Leena Patel , Stephane Perreault , Barton W. Phillips , Gary Phillips , Kirk L. Stevens , Jennifer A. Treiberg , Joshua Van Veldhuizen , William J. Watkins , Suet Chung Yeung
IPC分类号： C07D513/04 , C07D403/12 , C07D413/14 , C07D403/14 , C07D239/91 , C07D487/04 , C07D401/14 , C07D473/34
摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, or a mixture thereof, wherein n, m, q, A′, W1, W2, W3, 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 (J), 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.
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公开(公告)号：US20180305315A1
公开(公告)日：2018-10-25
申请号：US15957739
申请日：2018-04-19
发明人： Evangelos Aktoudianakis , Todd Appleby , Aesop Cho , Zhimin Du , Michael Graupe , Juan A. Guerrero , Salman Y. Jabri , Lateshkumar Thakorlal Lad , Paulo A. Machicao Tello , Jonathan William Medley , Samuel E. Metobo , Prasenjit Kumar Mukherjee , Devan Naduthambi , Gregory Notte , Eric Q. Parkhill , Barton W. Phillips , Scott Preston Simonovich , Neil H. Squires , Chandrasekar Venkataramani , Peiyuan Wang , William J. Watkins , Jie Xu , Kin Shing Yang , Christopher Allen Ziebenhaus
IPC分类号： C07D213/69 , A61K45/06 , A61K31/444 , C07D401/14 , A61K31/4545 , C07D213/85 , A61K31/44 , C07D213/30 , C07D295/088 , A61K31/5377
CPC分类号： C07D213/69 , A61K31/44 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/5377 , A61K45/06 , C07D213/30 , C07D213/61 , C07D213/64 , C07D213/85 , C07D295/088 , C07D401/04 , C07D401/14 , C07D405/14 , C07D487/08 , C07D487/10 , C07D491/107 , C07D498/04 , C07D519/00
摘要： Compounds according to formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
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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
发明人： 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分类号： C07D471/04 , C07D487/04 , C07D519/00 , C07D473/00
CPC分类号： C07D471/04 , C07D473/00 , C07D487/04 , C07D519/00
摘要： Compounds having the following formula (I) and methods of their use and preparation are disclosed:
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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
发明人： 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分类号： 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分类号： 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
摘要： 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.
摘要翻译： 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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公开(公告)号：US09376441B2
公开(公告)日：2016-06-28
申请号：US14448160
申请日：2014-07-31
发明人： 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分类号： A61K31/4015 , C07D207/12 , C07D487/04 , C07D401/14 , C07D403/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D407/14 , C07D417/14
CPC分类号： 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
摘要： 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.
摘要翻译： 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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