发明名称 1,4-dihydropyridine-3,5-dicarboxylate derivatives and preparation and use thereof
摘要 The present invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate compound of general compound (I), a process for preparing the same, a use thereof for the manufacture of a medicament for treating and/or preventing kidney injury, cardiovascular diseases and/or endocrine diseases, as well as a pharmaceutical composition and a pharmaceutical formulation containing said compounds, wherein the definitions of R1, R2, R3, R4, R5, R6, R7, R8, m, n1, n2, p and q are the same as those defined in the description.;
申请公布号 US9198902(B2) 申请公布日期 2015.12.01
申请号 US201214114346 申请日期 2012.05.02
申请人 Xuanzhu Pharma Co., Ltd. 发明人 Zhang Hui;Fan Mingwei;Sun Liang
分类号 C07D401/14;C07D401/12;C07D417/14;A61K31/4439;A61K31/444;A61K45/06;A61K31/44 主分类号 C07D401/14
代理机构 Kilpatrick Townsend & Stockton LLP 代理人 Kilpatrick Townsend & Stockton LLP
主权项 1. A compound of general formula (I), a pharmaceutically acceptable salt or a stereoisomer thereof: wherein: R1 and R4 are each independently selected from methyl, ethyl and ethoxymethyl that are unsubstituted or substituted by 1-3 Q1 substituents, and the carbon atom(s) therein can be optionally replaced with 1-3 groups from O, N(H)x or C(O), wherein x is selected from 1 or 2; Q1 is selected from halogen, hydroxy, amino, methoxy and ethoxy; R2 is selected from methyl, ethyl, isopropyl, cyclopropyl, cyclopropylmethyl, azetidinyl, pyrrolidinyl, piperidyl, morpholinyl, pyrrolidinylmethyl and morpholinylmethyl that are unsubstituted or substituted by 1-3 Q2 substituents, Q2 is selected from fluoro, chloro, hydroxy, amino, C1-4alkyl, C1-4alkoxy, and C1-4alkyl and C1-4alkoxy that are substituted by 1-3 fluoro and/or chloro atoms; R3 is selected from hydrogen, fluoro, chloro and nitro; R5 and R6 are each independently selected from methyl or ethyl that is unsubstituted or substituted by 1-3 Q3 substituents, Q3 is selected from fluoro, chloro, hydroxy, amino, methoxy and ethoxy; R7 and R8 are each independently selected from hydrogen, methyl, ethyl, and phenylC0-2alkyl, pyridylC0-2alkyl, furylC0-2alkyl, thienylC0-2alkyl, pyrrolylC0-2alkyl, thiazolylC0-2alkyl and thiadiazolylC0-2alkyl that are unsubstituted or substituted by 1-3 Q4 substituents, and R7 and R8 are not both hydrogen at the same time, Q4 is selected from fluoro, chloro, hydroxy, amino, methyl, ethyl, fluoromethyl, difluoromethyl, trifluoromethyl, methoxy and ethoxy; m is selected from 1, 2 or 3, when m is 2 or 3, R3 can be identical or different; n1 is 2, n2 is 1; p and q are each independently selected from 0, 1, 2 or 3, wherein when q is 0, neither R7 nor R8 is phenylC0-2alkyl.
地址 Jinan, Shandong Province CN