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1.发明申请IMIDAZOPYRIDAZINE COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN-ALPHA RESPONSES 审中-公开作为IL-12，IL-23和/或IFN-ALPHA反应调节剂的咪达唑啶化合物有用公开(公告)号：US20160304524A1
公开(公告)日：2016-10-20
申请号：US15102991
申请日：2014-12-10
IPC分类号： C07D487/04 , C07D498/14
CPC分类号： C07D487/04 , C07D487/14 , C07D498/14
摘要： Compounds having the following formula (I), or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
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公开(公告)号：US20220356180A1
公开(公告)日：2022-11-10
申请号：US17244938
申请日：2021-04-29
发明人： Ryan M. Moslin , David S. Weinstein , Stephen T. Wrobleski , John S. Tokarski , Amit Kumar , Douglas G. Batt , Shuqun Lin , Chunjian Liu , Steven H. Spergel , Yanlei Zhang , Qingjie Liu
IPC分类号： C07D417/14 , C07D403/12 , C07D401/14 , C07D413/14 , C07D401/12 , C07D237/24 , C07D403/14 , C07D413/12 , C07D417/12 , C07B59/00
摘要： Compounds having the following formula I. or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
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公开(公告)号：US20220185800A1
公开(公告)日：2022-06-16
申请号：US17439845
申请日：2020-03-25
发明人： Chunjian Liu , David S. Yoon , Wei Wang , Jianxin Feng , Bruce A. Ellsworth , Alicia Regueiro-Ren
IPC分类号： C07D405/14 , C07D417/14
摘要： The present disclosure relates to compounds of Formula (I), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.
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公开(公告)号：US20210179599A1
公开(公告)日：2021-06-17
申请号：US16760810
申请日：2018-10-31
发明人： Jianxin Feng , Chunjian Liu , Yanting Huang
IPC分类号： C07D413/14 , C07D513/04 , C07D417/14 , C07D471/04 , C07D413/12 , C07D413/04 , C07D261/08
摘要： The present invention provides compounds of Formula (I), or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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![1H-PYRROLO[3,2-C]PYRIDINE AND 1H-PYRROLO[2,3-C]PYRIDINE DERIVATIVES AS TLR9 INHIBITORS FOR THE TREATMENT OF FIBROSIS](/abs-image/US/2023/10/05/US20230312565A1/abs.jpg.150x150.jpg)
5.发明公开公开(公告)号：US20230312565A1
公开(公告)日：2023-10-05
申请号：US18042069
申请日：2021-08-18
发明人： Chunjian Liu , Alicia Regueiro-Ren
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to 1H-pyrrolo[3,2-c]pyridine and 1H-pyrrolo[2,3-c]pyridine derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic diseases, such as e.g. liver fibrosis, renal fibrosis, biliary fibrosis or pancreatic fibrosis, nonalcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), chronic kidney disease, diabetic kidney disease, primary sclerosing cholangitis (PSC) or primary biliary cirrhosis (PBC), or idiopathic pulmonary fibrosis (IPF).
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![1H-BENZO[D]IMIDAZOLE DERIVATIVES AS TLR9 INHIBITORS FOR THE TREATMENT OF FIBROSIS](/abs-image/US/2023/09/21/US20230295122A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230295122A1
公开(公告)日：2023-09-21
申请号：US18041719
申请日：2021-08-18
IPC分类号： C07D401/14 , C07D451/04 , C07D471/04 , C07D405/14 , C07D417/14 , C07D413/14 , C07D235/18 , C07D519/00 , C07D405/12 , C07D401/10 , C07D487/10 , C07D487/04 , C07D403/10 , C07D401/12 , C07D451/02
CPC分类号： C07D401/14 , C07D451/04 , C07D471/04 , C07D405/14 , C07D417/14 , C07D413/14 , C07D235/18 , C07D519/00 , C07D405/12 , C07D401/10 , C07D487/10 , C07D487/04 , C07D403/10 , C07D401/12 , C07D451/02
摘要： The present invention relates to 1H-benzo[d]imidazole derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic diseases, such as e.g. liver fibrosis, renal fibrosis, biliary fibrosis or pancreatic fibrosis, non-alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), chronic kidney disease, diabetic kidney disease, primary sclerosing cholangitis (PSC) or primary biliary cirrhosis (PBC), or idiopathic pulmonary fibrosis (IPF).
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公开(公告)号：US20200283430A1
公开(公告)日：2020-09-10
申请号：US16759660
申请日：2018-10-31
发明人： Joseph E. Carpenter , Matthias Broekema , Jianxin Feng , Chunjian Liu , Wei Wang , Ying Wang
IPC分类号： C07D413/14 , C07D417/14 , C07D471/08 , C07D487/04 , C07D471/04 , C07D519/00
摘要： The present invention provides compounds of Formula (I): Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of famesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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公开(公告)号：US20190152948A1
公开(公告)日：2019-05-23
申请号：US16195951
申请日：2018-11-20
发明人： Chunjian Liu , Michael G. Yang , Zili Xiao , Ling Chen , Ryan M. Moslin , John S. Tokarski , David S. Weinstein
IPC分类号： C07D401/14 , C07D401/12 , C07D413/14 , C07D417/14 , C07D405/14 , C07F9/6558 , C07D471/04
摘要： Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
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公开(公告)号：US10273237B2
公开(公告)日：2019-04-30
申请号：US15102991
申请日：2014-12-10
IPC分类号： C07D487/04 , C07D487/14 , C07D498/14
摘要： Compounds having the following formula (I), or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
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10.发明申请公开(公告)号：US20170209426A1
公开(公告)日：2017-07-27
申请号：US15480787
申请日：2017-04-06
发明人： Ryan M. Moslin , David S. Weinstein , Stephen T. Wrobleski , Yanlei Zhang , John S. Tokarski , Michael E. Mertzman , Chunjian Liu
IPC分类号： A61K31/455 , A61K31/506
CPC分类号： A61K31/455 , A61K31/44 , A61K31/444 , A61K31/506 , C07B59/002 , C07B2200/05 , C07D213/56 , C07D213/82 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds having the following formula I: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα by acting on Tyk-2 to cause signal transduction inhibition.
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