发明名称 Family of analogues and NADP+ or NADPH, their preparation and their application in therapeutics
摘要 A new family of analogues of NADP+ or NADPH, their preparation and their application in therapeutics.
申请公布号 US9409937(B2) 申请公布日期 2016.08.09
申请号 US201214128161 申请日期 2012.06.19
申请人 UNIVERSITE PARIS DESCARTES 发明人 Slama-Schwok Anny;Boucher Jean-Luc;Xu-Li Yun;Deprez Eric;Henry Etienne;Dessy Chantal;Feron Olivier;Tarus Bogdan
分类号 A61K49/00;C07F9/6561;C07H19/16;C07H19/167 主分类号 A61K49/00
代理机构 Young & Thompson 代理人 Young & Thompson
主权项 1. Compounds of formula I:wherein: (i) X represents an electron acceptor group, selected from the group comprising of: —NO2, —CN, —CHO, —COOH, —CF3, —F, —CH═C(CN)2,—SO3H,CONR9R10 or SO2NR9R10, in which R9 and R10 represent each independently of each other an hydrogen, a linear or branched (C1-C3) alkyl group, or an aryl group,COR9, in which R9 represents an hydrogen, a linear or branched (C1-C3) alkyl group, or an aryl group, anda tetrazolyl group, (ii) Y represents an electron donor group, selected from the group consisting of —NR19—, —OC(R19R14)—, and —SC(R19R14)—, in which: R19 is chosen from:a hydrogen,a linear (C1-C8) alkyl group, said alkyl group being optionally substituted by one or more group selected from: —OH group, —NH2 group, —COOH group, CONH-arylCOOH group or NHCOarylCOOH group or NHCOarylsulfate group, or NHCOarylsulfonate group, wherein the aryl group is chosen from phenyl, naphtyl or biphenyl, ora hydrosoluble organic group, includes PEG,R14 represents a hydrogen or a linear or branched (C1-C4) alkyl group, optionally substituted by —OH. (iii) A represents a bond chosen from the group consisting of: (a) —C≡C—, and(b)wherein: M1 and M2 represent independently of each other H, F, Cl, Br or I,n is an integer chosen from 1, 2, or 3, (iv) R1, R2, R3, R4, R5, R6, R7 or R8 are each independently selected from the group consisting of: —H,F, Cl, Br, I, anda linear or branched (C1-C4) alkyl, optionally substituted by one or more substituants chosen from:—OH,NR11R12, in which R11 and R12 represent each independently of each other an hydrogen or a linear or branched (C1-C3) alkyl group, or—COOR11, in which R11 represents hydrogen or a linear or branched (C1-C3) alkyl group,—CONHR13 or NHCOR13, in which R13 represents a linear or branched (C1-C4) alkyl group, (v) L represents a spacer group selected from the group consisting of: wherein m and q represent each independently of each other an integer chosen from 0 to 5, said groups being optionally substituted by one or more OH, (vi) B represents the following formula II:wherein: T represents an oxygen atom, or a sulphur atom, preferably an oxygen atom; R16 and R17 represent each independently of each other OH, H2PO4, HSO4, 0PO3(NH4)2, or any salt of these phosphate or sulphate groups; and R18 represents a purine-base or a pyrimidine-base, adenine, guanine, hypoxanthine, thymine, uracil or cytosine, preferably adenine, wherein the compound of formula (I) includes racemate or isomeric forms, axial or equatorial isomeric forms, and pharmaceutically acceptable salts thereof.
地址 Paris FR