首页> 外国专利> DERIVATIVES OF ((HETERO) CICLOALQUILETINIL-BENCIL) -BENZENE AND ITS USE AS INHIBITORS OF THE SODIUM DEPENDENT GLUCOSE COTRANSPORTADOR (SGLT).

DERIVATIVES OF ((HETERO) CICLOALQUILETINIL-BENCIL) -BENZENE AND ITS USE AS INHIBITORS OF THE SODIUM DEPENDENT GLUCOSE COTRANSPORTADOR (SGLT).

机译:((杂)环喹啉-苯甲酸酯)-苯的衍生物及其作为钠依赖性葡萄糖共转运体(SGLT)抑制剂的用途。

摘要

Glucopyranosyl substituted ((hetero) cycloalkylene-benzyl) -benzene derivatives of the general formula I ** (See formula) ** wherein R 1 indicates hydrogen, fluorine, chlorine, bromine iodine, C 1-4 alkyl, C 2-6 alkynyl , C1-4 alkoxy, (C2-4 alkenyl) - (C1-4 alkoxy), (C2-4 alkynyl) - (C1-4 alkoxy), methyl substituted with 1 to 3 fluorine atoms, ethyl substituted with 1 to 5 fluorine atoms, methoxy substituted with 1 to 3 fluorine atoms, ethoxy substituted with 1 to 5 fluorine atoms, C1-4 alkyl substituted with a hydroxy group or C1-3 alkoxy, C2-4 alkoxy substituted with a hydroxy group or alkoxy C1-3, C2-6 alkenyl, C3-7 cycloalkyl, (C3-7 cycloalkyl) - (C1-3 alkyl), C3-7 cycloalkyloxy, (C3-7 cycloalkyl) - (C1-3 alkoxy), C5- cycloalkenyloxy 7, hydroxy, amino, nitro or cyano, in which in the C5-6 cycloalkyl groups a methylene group may be substituted by O; R2 indicates hydrogen, fluorine, chlorine, bromine, hydroxy, C1-4 alkyl, C1-4 alkoxy, cyano or nitro, in which the alkyl or alkoxy group may be mono- or polysubstituted with fluorine, and R3 indicates C3-7 cycloalkyl , which is substituted with one to four L2 substituents, or tetrahydrofuranyl or tetrahydropyranyl, which may be substituted with one to four substituents L2, and R4, R5 independently of one another, indicate hydrogen, fluorine, chlorine, bromine, iodine, cyano, nitro, C1-3 alkyl, C1-3 alkoxy, or a methyl or methoxy group substituted with 1 to 3 fluorine atoms, L1 independently in each case is selected from fluorine, chlorine, bromine, iodine, hydroxy, cyano, C1-3 alkyl, difluoromethyl, trifluoromethyl, C1-3 alkoxy, difluoromethoxy, trifluoromethoxy, amino, (C1-3 alkyl) -amino and di (C1-3 alkyl) -amino; and L2 independently in each case are selected from fluorine, chlorine, hydroxy, hydroxy-C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, C1-4 alkoxy-C1-4 alkyl, cyano, C1-4 alkyl, trifluoromethyl, amino, C1-4 alkylcarbonylamino, C1-3 alkyl amino and di (C1-3 alkyl) amino; and R6, R7a, R7b, R7c independently of one another, have a meaning selected from hydrogen, (C1-18 alkyl) carbonyl, (C1-18 alkyl) oxycarbonyl, arylcarbonyl and aryl- (C1-3 alkyl) -carbonyl, in the that the aryl groups may be mono- or disubstituted independently of one another with the same or different L1 groups; wherein the aryl groups mentioned in the definition of the above groups are phenyl or naphthyl groups that may be substituted as defined; and in which, unless otherwise indicated, the aforementioned alkyl groups may have straight or branched chain, their tautomers, their stereoisomers, mixtures thereof and their salts.
机译:通式I **(参见式)**的戊二糖基取代的((杂)亚环烷基-苄基)-苯衍生物,其中R 1表示氢,氟,氯,溴碘,C 1-4烷基,C 2-6炔基,C1-4烷氧基,(C2-4烯基)-(C1-4烷氧基),(C2-4炔基)-(C1-4烷氧基),被1-3个氟原子取代的甲基,被1-5个氟取代的乙基原子,被1-3个氟原子取代的甲氧基,被1-5个氟原子取代的乙氧基,被羟基或C1-3烷氧基取代的C1-4烷基,被羟基或C1-3烷氧基取代的C2-4烷氧基, C 2-6烯基,C 3-7环烷基,(C 3-7环烷基)-(C 1-3烷基),C 3-7环烷氧基,(C 3-7环烷基)-(C 1-3烷氧基),C 5-环烯氧基7,羟基,氨基,硝基或氰基,其中在C 5-6环烷基中,亚甲基可以被O取代; R 2表示氢,氟,氯,溴,羟基,C 1-4烷基,C 1-4烷氧基,氰基或硝基,其中烷基或烷氧基可以被氟单或多取代,R 3表示C 3-7环烷基,可以被1-4个取代基L2和R4,R5彼此独立地取代的1-4个L2取代基或四氢呋喃基或四氢吡喃基表示氢,氟,氯,溴,碘,氰基,硝基, C 1-3烷基,C 1-3烷氧基或被1-3个氟原子取代的甲基或甲氧基,L 1分别独立地选自氟,氯,溴,碘,羟基,氰基,C 1-3烷基,二氟甲基,三氟甲基,C 1-3烷氧基,二氟甲氧基,三氟甲氧基,氨基,(C 1-3烷基)-氨基和二(C 1-3烷基)-氨基; L 1和L 2分别独立地选自氟,氯,羟基,羟基-C 1-4烷基,C 1-4烷氧基,三氟甲氧基,C 1-4烷氧基-C 1-4烷基,氰基,C 1-4烷基,三氟甲基,氨基, C1-4烷基羰基氨基,C1-3烷基氨基和二(C1-3烷基)氨基; R 6,R 7a,R 7b,R 7c彼此独立地具有氢,(C 1-18烷基)羰基,(C 1-18烷基)氧羰基,芳基羰基和芳基-(C 1-3烷基)-羰基的含义。芳基可以被相同或不同的L1基团彼此独立地单取代或二取代;其中在上述基团的定义中提及的芳基是可以被定义的取代的苯基或萘基;除非另有说明,否则上述烷基可具有直链或支链,其互变异构体,其立体异构体,其混合物和其盐。

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