首页> 外国专利> Novel derivatives of 7-oxo-2,3,7,14-tetrahydro-1H-benzo b pyrano 3,2-h acridine carboxylate, processes for their preparation and pharmaceutical preparations containing these

Novel derivatives of 7-oxo-2,3,7,14-tetrahydro-1H-benzo b pyrano 3,2-h acridine carboxylate, processes for their preparation and pharmaceutical preparations containing these

机译:7-氧代-2,3,7,14-四氢-1H-苯并[b]吡喃并[3,2-h] a啶羧酸酯的新型衍生物,其制备方法和含有这些衍生物的药物制剂

摘要

7-Oxo-2,3,7,14-tetrahydro-1H-benzo(b)pyrano(3,2-h) acridine derivatives (I), their salts with acids and bases, their isomers, N-oxides, their preparation, and pharmaceutical compositions containing them. The new compounds are of formula (I) X and Y = H, halogen, OH, SH, CN, NO2, 1-6C alkyl, alkoxy, or trihaloalkyl, amino (optionally by one or two 1-6C alkyl groups which may be substituted by alkoxy groups or by a group of formula NR7R8) or together form a methylenedioxy or ethylene dioxy group, the groups X and Y being present on either of the two adjacent benzene rings; R7 and R8 = H or 1-6C alkyl, aryl, or aralkyl; R1 = H or 1-6C alkyl; R2 = H, OH, 1-6C alkyl or alkoxy (optionally substituted by NR9R10, or by a 5-7 membered saturated or unsaturated mono- or bicyclic heterocycle having one or two hetero atoms selected from O, N, and S), alkyl carbonyloxy, or amino (optionally substituted by one or two alkyl, aryl, or aralkyl groups, an alkylcarbonyl group that may be substituted by NR7R8, a group -R11-NR9R10, an alkylene group substituted by a heterocycle, or a group -R11-CO-R12; R9 and R10 = H, or 1-6C alkyl or hydroxyalkyl; R11 = 1-6C alkylene; R12 = OH or 1-6C alkoxy; R3 and R4 = H or 1-6C alkyl; one or both of R5 and R6 = a group -O-CO-U-V, and if only one has this meaning the other represents a group Z; U = 1-8C alkylene, optionally substituted by one or more groups selected from aryl, OH, or 1-6C alkoxy; V = COOH, COOR13, OH, 1-6C alkoxy, -NR7R8, -NR7-COOR13, -NR7-CO-R13, -COR13, or CONR7R8; R13 = 1-6C alkyl optionally substituted OH, aryl, or aralkyl; Z = OH, 1-6C alkoxy, alkoxycarbonyl, alkylcarbonyloxy, arylcarbonyloxy, arylalkyl carbonyloxy, or amino optionally substituted by one or two alkyl groups
机译:7-氧-2,3,7,14-四氢-1H-苯并(b)吡喃并(3,2-h)h啶衍生物(I),其与酸和碱的盐,其异构体,N-氧化物,其制备以及含有它们的药物组合物。新化合物具有式(I)X和Y = H,卤素,OH,SH,CN,NO2、1-6C烷基,烷氧基或三卤代烷基,氨基(可选地一个或两个1-6C烷基,它们可以是被烷氧基或式NR7R8的基团取代或一起形成亚甲基二氧基或亚乙基二氧基,基团X和Y存在于两个相邻的苯环中的任何一个上; R7和R8 = H或1-6C烷基,芳基或芳烷基; R1 = H或1-6C烷基; R 2 = H,OH,1-6C烷基或烷氧基(可选被NR9R10取代,或被具有一个或两个选自O,N和S的杂原子的5-7元饱和或不饱和单环或双环杂环取代),烷基羰氧基或氨基(可选地被一个或两个烷基,芳基或芳烷基取代,可被NR7R8取代的烷基羰基,-R11-NR9R10基团,被杂环取代的亚烷基或-R11-基团CO-R12; R9和R10 = H,或1-6C烷基或羟烷基; R11 = 1-6C亚烷基; R12 = OH或1-6C烷氧基; R3和R4 = H或1-6C烷基; R5中的一个或两个R6 = -O-CO-UV基团,并且如果只有一个具有该含义,则另一个代表Z基团; U = 1-8C亚烷基,任选地被一个或多个选自芳基,OH或1-6C的基团取代烷氧基; V = COOH,COOR13,OH,1-6C烷氧基,-NR7R8,-NR7-COOR13,-NR7-CO-R13,-COR13或CONR7R8; R13 = 1-6C烷基,可选取代的OH,芳基或芳烷基; Z = OH,1-6C烷氧基,烷氧基羰基,烷基羰氧基,芳基核糖氧基,芳基烷基羰氧基或可被一个或两个烷基取代的氨基

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