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公开(公告)号：US11059854B2
公开(公告)日：2021-07-13
申请号：US16633122
申请日：2018-07-26
发明人： Xiaolin Li , Hualing Xiao , Peng Li , Haiying He , Fei Hao
摘要： The present invention falls within the field of pharmaceutical chemistry, and relates to a method for preparing a steroid derivative FXR agonist and relevant intermediates. In particular, the present invention relates to a method for preparing a compound of formula I, comprising reacting a compound of formula 8 with a compound of formula 9 to obtain a compound of formula 10, obtaining a compound of formula 11 from a reaction of the compound of formula 10, and obtaining the compound of formula I from a reaction of the compound of formula 11, as well as the intermediates used, the methods for preparing the intermediates and the use of the intermediates. The reaction conditions of the preparation method are mild, and some of the steps can convert multiple groups simultaneously, thereby effectively shortening the sequence of steps. The preparation method is suitable for industrialized production.
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公开(公告)号：US11059853B2
公开(公告)日：2021-07-13
申请号：US16633111
申请日：2018-07-26
发明人： Xiaolin Li , Hualing Xiao , Peng Li , Haiying He , Weidong Li
摘要： Disclosed are a crystalline or amorphous form of steroid derivative FXR agonist (formula I), and a preparation method therefor, and a crystalline composition and pharmaceutical composition comprising the crystalline or amorphous form, and the use of same in the preparation of a drug for treating or preventing various conditions associated with FXR.
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公开(公告)号：US10981860B2
公开(公告)日：2021-04-20
申请号：US16099989
申请日：2017-05-11
发明人： Haiying He , Songliang Wu , Zhi Luo , Jianfeng Mou , Fengying Guo , Chuan Wang , Guoqing Li , Minggao Zeng , Shuhui Chen
IPC分类号： C07C225/22 , C07C225/10 , C07C225/18 , C07D205/04 , C07D207/04 , C07D221/22 , C07D221/20 , C07D221/04 , C07D223/04 , C07D265/30 , C07D267/12 , C07D401/06 , A61P43/00 , C07D409/06 , C07D211/62 , C07D451/02 , A61K31/46 , A61K31/445 , C07C237/12 , C07D211/60 , C07D207/06 , C07D227/04 , C07D239/26 , C07D333/10 , C07D333/72 , C07D413/06
摘要： Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.
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公开(公告)号：US20210002235A1
公开(公告)日：2021-01-07
申请号：US16977761
申请日：2019-03-13
发明人： Songliang Wu , Jianfeng Mou , Haiying He
IPC分类号： C07D261/18
摘要： Disclosed herein a crystal structure of a caspase inhibitor, and more specifically a crystal structure of an (S)-3-((S)-2-(5-(2-chlorophenyl)isoxazole-3-formylamide)proponamide)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)valeric acid, a preparation method therefor, a crystal polymer, a pharmaceutical composition and uses thereof. The compound A of formula (I) disclosed herein exhibits high crystal structure stability, low hygroscopicity, and advantageously shows physical properties, safety and metabolic stability while having relatively high pharmaceutical value.
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公开(公告)号：US20200231622A1
公开(公告)日：2020-07-23
申请号：US16633122
申请日：2018-07-26
发明人： Xiaolin Li , Hualing Xiao , Peng Li , Haiying He , Fei Hao
IPC分类号： C07J43/00
摘要： The present invention falls within the field of pharmaceutical chemistry, and relates to a method for preparing a steroid derivative FXR agonist and relevant intermediates. In particular, the present invention relates to a method for preparing a compound of formula I, comprising reacting a compound of formula 8 with a compound of formula 9 to obtain a compound of formula 10, obtaining a compound of formula 11 from a reaction of the compound of formula 10, and obtaining the compound of formula I from a reaction of the compound of formula 11, as well as the intermediates used, the methods for preparing the intermediates and the use of the intermediates. The reaction conditions of the preparation method are mild, and some of the steps can convert multiple groups simultaneously, thereby effectively shortening the sequence of steps. The preparation method is suitable for industrialized production.
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公开(公告)号：US11091450B2
公开(公告)日：2021-08-17
申请号：US16977761
申请日：2019-03-13
发明人： Songliang Wu , Jianfeng Mou , Haiying He
IPC分类号： C07D261/18
摘要： Disclosed herein a crystal structure of a caspase inhibitor, and more specifically a crystal structure of an (S)-3-((S)-2-(5-(2-chlorophenyl)isoxazole-3-formylamide)proponamide)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)valeric acid, a preparation method therefor, a crystal polymer, a pharmaceutical composition and uses thereof. The compound A of formula (I) disclosed herein exhibits high crystal structure stability, low hygroscopicity, and advantageously shows physical properties, safety and metabolic stability while having relatively high pharmaceutical value.
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公开(公告)号：US20190135733A1
公开(公告)日：2019-05-09
申请号：US16099989
申请日：2017-05-11
发明人： Haiying He , Songliang Wu , Zhi Luo , Jianfeng Mou , Fengying Guo , Chuan Wang , Guoqing Li , Minggao Zeng , Shuhui Chen
IPC分类号： C07C225/22 , C07D205/04 , C07D207/06 , C07D227/04 , C07D265/30 , C07D223/04 , C07D221/22 , C07D221/04 , C07D239/26 , C07D333/10 , C07D333/72 , C07D413/06 , C07D401/06
摘要： Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.
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公开(公告)号：US11667667B2
公开(公告)日：2023-06-06
申请号：US17069691
申请日：2020-10-13
发明人： Haiying He , Hualing Xiao , Peng Li , Chunyan Du , Zhi Luo , Shuhui Chen
CPC分类号： C07J43/003 , C07J9/00 , C07J33/002
摘要： The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases.
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公开(公告)号：US11434212B2
公开(公告)日：2022-09-06
申请号：US16479673
申请日：2018-01-23
发明人： Jianfeng Mou , Songliang Wu , Haiying He , Fengying Guo , Chuan Wang , Jie Li , Jian Li , Shuhui Chen
IPC分类号： C07D261/18 , C07D231/14 , C07D233/90 , C07D263/34 , C07D271/06 , C07D277/56
摘要： A compound represented by formula (I), a pharmaceutically acceptable salt or tautomer thereof, and an application of the compound as a caspase inhibitor.
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10.发明申请公开(公告)号：US20200231621A1
公开(公告)日：2020-07-23
申请号：US16633111
申请日：2018-07-26
发明人： Xiaolin Li , Hualing Xiao , Peng Li , Haiying He , Weidong Li
IPC分类号： C07J43/00
摘要： Disclosed are a crystalline or amorphous form of steroid derivative FXR agonist (formula I), and a preparation method therefor, and a crystalline composition and pharmaceutical composition comprising the crystalline or amorphous form, and the use of same in the preparation of a drug for treating or preventing various conditions associated with FXR.
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