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Synergistic mixture containing dipyridylpropanolamine derivative, useful for treating or preventing disorders of lipid metabolism, includes e.g. cholesterol resorption inhibitor

机译:含有二吡啶基丙醇胺衍生物的增效混合物可用于治疗或预防脂质代谢紊乱,例如包括。胆固醇吸收抑制剂

摘要

A composition comprises a dipyridylpropanolamine (I) or its salt or functional derivative and another active agent (II). A copmposition comprises a dipyridylpropanolamine of formula (I) or its salt or functional derivative and another active agent (II). R1 = phenyl or heteroaryl (both optionally substituted by 1-3 of fluoro, chloro, bromo, iodo, hydroxy, trifluoromethyl, nitro, cyano, 1-8C alkyl or alkoxy, amino, NHR9, NR9R10, formyl, carboxy, COOR11, COR12, 1-6C alkyl (substituted by hydroxy, hydroxy and phenyl, trifluoromethyl, nitro, cyano, amino, NHR9, NR9R10, formyl, carboxy, COOR11, or COR12), 1-6C alkoxy (substituted by trifluoromethyl, nitro, cyano, amino, NHR9, NR9R10, formyl, carboxy, COOR11, or COR12)), NHSO3H, methylsulfonyl, -O(1-6C)alkyl-O(1-6C)alkyl-phenyl, 1-6C alkylthio or pyridyl, and in alkyl residues one or more hydrogen may be replaced by fluoro and phenyl and pyridyl may themselves by substituted once by Me, MeO or halo; R2 = hydrogen, hydroxy, hydroxymethyl, formyl or amino; R3 = mono- to tetra-saccharide residue, optionally substituted one or more times by protecting groups, or is HOSO2 or (HO)2PO-; R4 = hydrogen, Me, fluoro or MeO; R9-R12 = hydrogen or 1-8C alkyl; Z = -NH(0-16C)alkyl-CO-, -O-(0-16C)alkylCO-, -(CO)m-(1-16C)alkyl-(CO)n- or the residue of a (di)amino acid (optionally substituted by protecting groups) or a bond; and n and m = 0 or 1.
机译:组合物包含二吡啶基丙醇胺(I)或其盐或功能衍生物和另一种活性剂(II)。共聚包括式(I)的二吡啶基丙醇胺或其盐或功能衍生物和另一种活性剂(II)。 R 1 =苯基或杂芳基(两者任选被氟,氯,溴,碘,羟基,三氟甲基,硝基,氰基,1-8C烷基或烷氧基,氨基,NHR 9,NR 9的1-3取代> R 10,甲酰基,羧基,COOR 11,COR 12,1-6C烷基(被羟基,羟基和苯基,三氟甲基,硝基,氰基,氨基,NHR 9,NR 9取代) R 10,甲酰基,羧基,COOR 11或COR 12),1-6C烷氧基(被三氟甲基,硝基,氰基,氨基,NHR 9,NR 9 R 10取代,甲酰基,羧基,COOR 11或COR 12)),NHSO 3 H,甲基磺酰基,-O(1-6C)烷基-O(1-6C)烷基-苯基,1-6C烷硫基或吡啶基以及在烷基中一个或多个氢的残基可以被氟和苯基取代,吡啶基本身可以被Me,MeO或卤素取代一次; R 2 =氢,羟基,羟甲基,甲酰基或氨基; R 3 =单糖至四糖残基,任选被保护基取代一次或多次,或者是HOSO 2或(HO)2 PO-; R 4 =氢,Me,氟或MeO; R 9 -R 12 =氢或1-8C烷基; Z = -NH(0-16C)烷基-CO-,-O-(0-16C)烷基CO-,-(CO)m-(1-16C)烷基-(CO)n-或(di )氨基酸(可选地被保护基取代)或键;并且n和m = 0或1。

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