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公开(公告)号：US11667629B2
公开(公告)日：2023-06-06
申请号：US16758232
申请日：2018-12-07
Inventor： Jinming Liu , Jiaqiang Cai , Yongyong Wu , Wei Yin , Lichun Wang , Jingyi Wang
IPC: C07D417/14 , C07D451/02 , C07D413/14 , B65D85/00
CPC classification number: C07D417/14 , B65D85/70 , C07D413/14 , C07D451/02
Abstract: The present invention generally relates to an isoxazole derivative, a preparation therefor, and a use thereof. In particular, the present invention provides a farnesoid X receptor (FXR) agonist compound, and a stereoisomer, a tautomer, a polymorph, a solvate (e.g., a hydrate), a pharmaceutically acceptable salt, an ester, a metabolite, and an N-oxide, and the chemically protected forms and prodrugs thereof. The present invention further provides a preparation method for the compound, an intermediate thereof, and a pharmaceutical composition and kit containing the same and used thereof for treating FXR-mediated diseases or conditions.
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公开(公告)号：US11292785B2
公开(公告)日：2022-04-05
申请号：US16959691
申请日：2019-01-18
Inventor： Shuai Song , Qiang Tian , Yongyong Wu , Mingliang Zhao , Chaolei Wang , Jiaqiang Cai , Lichun Wang , Jingyi Wang
IPC: C07D403/12 , A61P1/16
Abstract: Related is a nitrogen-containing benzoheterocycle compound containing a carboxylic acid group as shown in general formula (I), or a stereoisomer or pharmaceutically acceptable salt thereof. The compound has excellent pharmacokinetic properties and extremely remarkable liver targeting properties, and a pharmaceutical composition comprising the same may be used as a CCR antagonist, in particular a CCR2 and/or CCR5 antagonist and can be used in mediated disease, including, but not limited to, nonalcoholic fatty liver disease (NAFLD) or the like.
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公开(公告)号：US11541049B2
公开(公告)日：2023-01-03
申请号：US16965450
申请日：2019-03-18
Inventor： Yongyong Wu , Jiaqiang Cai , Guangchao Zhang , Shuangshuang Duan , Chaolei Wang , Lichun Wang , Jingyi Wang
IPC: C07D403/14 , A61K31/496 , A61P7/02 , A61K31/4725 , A61K45/06 , C07D401/14 , C07D413/14 , C07D401/10
Abstract: Provided are tetrahydroisoquinoline derivatives, the preparation and use thereof. More specifically, provided are the tetrahydroisoquinoline derivatives or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, polymorph, solvate, isotopically labeled compound, metabolite or prodrug thereof. Further provided are a preparation process of the compound, the intermediates, a pharmaceutical composition comprising the compound and the use thereof in the treatment or prevention of a thromboembolic disorder.
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公开(公告)号：US11084847B2
公开(公告)日：2021-08-10
申请号：US16321430
申请日：2017-09-22
Inventor： Jiaqiang Cai , Qiang Tian , Mingliang Zhao , Hong Zeng , Hongmei Song , Nan Yu , Hua Deng , Wei Zhong , Long Yang , Lei Wu , Haitao Huang , Yongyong Wu , Donghai Su , Xin Zhou , Yuting Tan , Lichun Wang , Jingyi Wang
Abstract: The invention relates to a polyamide compound and a use thereof. Specifically, the invention relates to a type of polyamide compound (which preferably comprise one or more amide bonds formed by condensation of same or different L-amino acids or D-amino acids), or stereoisomers, crystalline polymorphs, solvates, metabolites, prodrugs or pharmaceutically acceptable salts or esters thereof, or pharmaceutical compositions thereof, as well as a method for preparing the polyamide compound and a use thereof in the prevention or treatment of diseases associated with κ-opioid receptor. The polyamide compound of the invention has excellent κ-opioid receptor agonistic activity and hydrophilicity, thus having a lesser ability of penetrating the blood-brain barrier and a lower capacity for entering the brain. The compound of the invention has higher selectivity for a κ-opioid receptor, lower addictiveness, improved pharmacokinetic properties, and improved safety (lower toxicity and/or fewer side effects), good patient compliance, and/or lesser propensity for developing tolerance, among other excellent medicinal properties.
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