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    • 6. 发明申请
    • UTILITY OF (+) EPICATECHIN AND THEIR ANALOGS
    • (+)天冬酰胺及其类似物的用途
    • WO2017221269A1
    • 2017-12-28
    • PCT/IN2017/050252
    • 2017-06-21
    • SPHAERA PHARMA PVT. LTD.,
    • DUGAR, SundeepSCHREINER, Frederic, George
    • C07H17/06A61K31/00C07D311/74C07D311/62C07D311/64
    • The present invention pertains to the enhanced activity of (+) epicatechin over (-) epicatechin. The present invention is related to novel analogs of (+) epicatechin of the formula (I), which enhances the pharmacokinetics and therefore the pharmacodynamics of (+) epicatechin. The present invention is related to analogs of (+) epicatechin of the formula (I). The general structure of the analogs of the present invention may be represented by Formula (I): Formula (I) wherein A and B are independently OR1 and C and D are independently OH; wherein R1 is independentlyC1 to C10 lower straight or branched chain acyclic or cyclic alkyl, or is selected from the group comprising, hydroxy butyric acid, dichloroacetic acid; phenyl butyric acid; valproic acid.
    • 本发明涉及(+)表儿茶酸对( - )表儿茶素的增强的活性。 本发明涉及式(I)的(+)表儿茶素的新类似物,其增强(+)表儿茶素的药代动力学并因此提高其药效学。 本发明涉及式(I)的(+)表儿茶素的类似物。 本发明类似物的一般结构可由式(I)表示:式(I)其中A和B独立地为OR 1且C和D独立地为OH; 其中R 1独立地为C 1至C 10低级直链或支链无环或环状烷基,或选自羟基丁酸,二氯乙酸; 苯基丁酸; 丙戊酸。