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公开(公告)号：US11739065B2
公开(公告)日：2023-08-29
申请号：US17537250
申请日：2021-11-29
IPC分类号： C07D261/10 , C07D401/14 , C07D413/12 , C07D413/14 , A61K31/42 , A61K31/44 , C07C13/04 , C07C25/13 , C07C39/28 , C07D205/02
CPC分类号： C07D261/10 , A61K31/42 , A61K31/44 , C07C13/04 , C07C25/13 , C07C39/28 , C07D205/02 , C07D401/14 , C07D413/12 , C07D413/14
摘要： The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. 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 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：US20220226337A1
公开(公告)日：2022-07-21
申请号：US17550591
申请日：2021-12-14
发明人： Peter A. Blomgren , Taryn Campbell , Jayaraman Chandrasekhar , Christopher T. Clark , Julian A. Codelli , Kevin S. Currie , Jeffrey E. Kropf , Yasamin Moazami , Nicole Nava , Leena Patel , Stephane Perreault , Jason K. Perry , Kassandra F. Sedillo , Natalie Seeger , Kirk L. Stevens , Jennifer Anne Treiberg , Suet C. Yeung , Zhongdong Zhao
IPC分类号： A61K31/5377 , A61K31/343 , A61K31/353 , A61K31/357 , A61K31/416 , A61K31/4375 , A61K31/4709 , A61K31/513 , A61K31/519 , A61K31/538 , A61K31/541 , A61K45/06 , C07D295/00 , C07D307/87 , C07D319/18 , C07D405/10 , C07D407/10 , C07D413/14 , C07D471/04
摘要： The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
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公开(公告)号：US10774054B2
公开(公告)日：2020-09-15
申请号：US16541073
申请日：2019-08-14
IPC分类号： C07D261/10 , C07D205/02 , C07C39/28 , C07C25/13 , C07C13/04 , A61K31/44 , A61K31/42 , C07D413/14 , C07D413/12 , C07D401/14
摘要： The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. 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 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：US20200155563A1
公开(公告)日：2020-05-21
申请号：US16667373
申请日：2019-10-29
发明人： Peter A. Blomgren , Taryn Campbell , Jayaraman Chandrasekhar , Christopher T. Clark , Julian A. Codelli , Kevin S. Currie , Jeffrey E. Kropf , Yasamin Moazami , Nicole Nava , Leena Patel , Stephane Perreault , Jason K. Perry , Kassandra F. Sedillo , Natalie Seeger , Kirk L. Stevens , Jennifer Anne Treiberg , Suet C. Yeung , Zhongdong Zhao
IPC分类号： A61K31/5377 , A61K31/541 , A61K45/06 , C07D405/10 , A61K31/4709 , A61K31/357 , C07D319/18 , C07D413/14 , A61K31/513 , C07D307/87 , A61K31/343 , C07D295/00 , A61K31/538 , C07D407/10 , A61K31/353 , A61K31/416 , C07D471/04 , A61K31/4375 , A61K31/519
摘要： The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
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公开(公告)号：US20200155538A1
公开(公告)日：2020-05-21
申请号：US16667306
申请日：2019-10-29
发明人： Peter A. Blomgren , Taryn Campbell , Jayaraman Chandrasekhar , Christopher T. Clark , Julian A. Codelli , Kevin S. Currie , Jeffrey E. Kropf , Yasamin Moazami , Nicole Nava , Leena Patel , Stephane Perreault , Jason K. Perry , Kassandra F. Sedillo , Natalie Seeger , Kirk L. Stevens , Jennifer Anne Treiberg , Suet C. Yeung , Zhongdong Zhao
IPC分类号： A61K31/47 , A61K45/06 , C07D215/14 , C07D401/10 , A61K31/4709 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/14 , C07D407/14 , A61K31/506 , A61K31/501 , A61K31/5355 , C07D413/12 , C07D417/12 , A61K31/541 , A61K31/517 , A61K31/4375 , C07D471/04 , C07D487/04 , A61K31/519
摘要： The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
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公开(公告)号：US20190388419A1
公开(公告)日：2019-12-26
申请号：US16413458
申请日：2019-05-15
发明人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Seung H. Lee , Jennifer R. Lo , Scott A. Mitchell , Aaron C. Schmitt , Sundaramoorthi Swaminathan , Jin-Ming Xiong , Jianjun Xu , Zhongdong Zhao
IPC分类号： A61K31/4985 , A61K31/5377 , A61K9/00 , C07D487/04
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 R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
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公开(公告)号：US20190308962A1
公开(公告)日：2019-10-10
申请号：US16308915
申请日：2017-06-09
IPC分类号： C07D413/14 , C07D401/14 , C07D413/12
摘要： The present disclosure relates generally to compounds (I) which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. 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 said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
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![Substituted imidazo[1,2-a]pyrazines as Syk inhibitors](/abs-image/US/2019/07/09/US10342794B2/abs.jpg.150x150.jpg)
公开(公告)号：US10342794B2
公开(公告)日：2019-07-09
申请号：US15945685
申请日：2018-04-04
发明人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Seung H. Lee , Jennifer R. Lo , Scott A. Mitchell , Aaron C. Schmitt , Sundaramoorthi Swaminathan , Jin-Ming Xiong , Jianjun Xu , Zhongdong Zhao
IPC分类号： A61K31/4985 , C07D487/04 , A61K9/00 , A61K31/5377
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 R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
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公开(公告)号：US20170298068A1
公开(公告)日：2017-10-19
申请号：US14971825
申请日：2015-12-16
发明人： CHRISTIAN GEGE , Claus Kremoser , Olaf Kinzel , Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Aaron C. Schmitt , William J. Watkins , Jianjun Xu
IPC分类号： C07D471/08 , C07D413/12 , C07D261/08 , C07D401/14 , C07D417/14 , C07D413/14
CPC分类号： C07D471/08 , C07D261/08 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： 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：US20220152014A1
公开(公告)日：2022-05-19
申请号：US17508267
申请日：2021-10-22
发明人： Peter A. Blomgren , Taryn Campbell , Jayaraman Chandrasekhar , Christopher T. Clark , Julian A. Codelli , Kevin S. Currie , Jeffrey E. Kropf , Yasamin Moazami , Nicole Nava , Leena Patel , Stephane Perreault , Jason K. Perry , Kassandra F. Sedillo , Natalie Seeger , Kirk L. Stevens , Jennifer Anne Treiberg , Suet C. Yeung , Zhongdong Zhao
IPC分类号： A61K31/47 , A61K31/352 , A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/5377 , A61K31/541 , C07D215/14 , C07D311/58 , C07D401/10 , C07D403/10 , C07D405/10 , C07D413/12 , C07D413/14 , C07D417/10 , C07D471/04 , C07D519/00
摘要： The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
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