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公开(公告)号：US11236085B2
公开(公告)日：2022-02-01
申请号：US16660219
申请日：2019-10-22
发明人： Zhimin Du , Michael Graupe , Paulo A. Machicao Tello , Jonathan William Medley , Samuel E. Metobo , Eric Q. Parkhill , Barton W. Phillips , Scott P. Simonovich , Peiyuan Wang , Jie Xu , Christopher A. Ziebenhaus
IPC分类号： C07D471/04 , C07D217/04 , C07D401/12 , C07D401/14 , C07D413/10 , C07D471/08 , C07D487/04 , C07D495/04 , C07D513/04 , C07K16/28 , C07K16/40
摘要： Compounds and 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：US20210323922A1
公开(公告)日：2021-10-21
申请号：US17098171
申请日：2020-11-13
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 , A61K31/5377 , C07D213/85 , A61K31/44 , C07D213/30 , C07D295/088 , A61K31/4545 , C07D401/04 , A61K31/497 , C07D519/00 , C07D487/10 , C07D487/08 , C07D213/64 , C07D491/107 , C07D498/04 , C07D213/61 , C07D405/14
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：US10710986B2
公开(公告)日：2020-07-14
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 , A61P31/20 , A61P35/02 , A61K31/496 , C07D519/00 , C07D241/20 , C07D487/10 , C07D405/14 , C07D487/08 , A61K31/497 , C07D491/107 , C07D241/18 , A61P35/00 , C07K16/28
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：US20160096827A1
公开(公告)日：2016-04-07
申请号：US14863108
申请日：2015-09-23
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 , C07D405/14 , A61K31/53 , C07D403/14 , C07D409/14 , A61K31/5383 , A61K31/5377 , C07D417/14 , C07D491/107 , C07D471/10 , C07D413/14 , C07D498/04 , A61K31/541 , C07D403/12
CPC分类号： C07D405/12 , A61K31/53 , A61K31/5377 , A61K31/5383 , A61K31/541 , 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
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：US20150361095A1
公开(公告)日：2015-12-17
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 , C07D473/34 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D513/04 , C07D239/91 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D473/34 , C07D487/04
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.
摘要翻译： 本申请提供式（J）化合物或其药学上可接受的盐，异构体或其混合物，其中n，m，q，A'，W 1，W 2，W 3，R 1，R 2和R 3在本文中描述。 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（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：US20150361054A1
公开(公告)日：2015-12-17
申请号：US14735254
申请日：2015-06-10
发明人： Shaopei Cai , Zhimin Du , Joshua Kaplan , Jennifer A. Loyer-Drew , Devan Naduthambi , Barton W. Phillips , Gary Phillips , Joshua Van Veldhuizen , William J. Watkins , Suet Chung Yeung
IPC分类号： C07D239/90 , C07D487/04 , C07D401/14 , C07D405/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D403/14 , C07D513/04
CPC分类号： A61K31/496 , C07D239/04 , C07D239/80 , C07D239/90 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D513/04
摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein W, B, n, m, A′, 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.
摘要翻译： 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W，B，n，m，A'，R 1，R 2和R 3在本文中描述。 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：US20230295111A1
公开(公告)日：2023-09-21
申请号：US18297316
申请日：2023-04-07
发明人： Gayatri Balan , Peter A. Blomgren , Chen Chen , Julian A. Codelli , Zhimin Du , Musong Kim , Dorothée Saddier Axe , Gregg M. Schwarzwalder , Rhiannon Thomas-Tran , Michael T. Tudesco , Chandrasekar Venkataramani , William J. Watkins , Brian M. Weist , Suet C. Yeung , Helen Yu
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07B2200/05
摘要： The present disclosure relates generally to compounds that bind to and act as degraders of an IKAROS Family Zinc Finger (IKZF) protein, such as IKZF2 (Helios) and/or IKZF4 (Eos). 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 and degradation of an IKZF protein, such as IKZF2 and/or IKZF4, including cancer.
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公开(公告)号：US11584738B2
公开(公告)日：2023-02-21
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 , C07D409/14 , C07D405/14
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：US20200157094A1
公开(公告)日：2020-05-21
申请号：US16660219
申请日：2019-10-22
发明人： Zhimin Du , Michael Graupe , Paulo A. Machicao Tello , Jonathan William Medley , Samuel E. Metobo , Eric Q. Parkhill , Barton W. Phillips , Scott P. Simonovich , Peiyuan Wang , Jie Xu , Christopher A. Ziebenhaus
IPC分类号： C07D471/04 , C07D513/04 , C07D401/12 , C07D413/10 , C07D217/04 , C07D401/14 , C07D471/08 , C07D487/04 , C07D495/04
摘要： Compounds and 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：US20150038488A1
公开(公告)日：2015-02-05
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
IPC分类号： C07D487/04 , C07D417/04 , C07D417/12 , C07D403/12 , C07D471/04 , C07D401/14
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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