首页> 外国专利> Therapeutically active 4- (3-methylflavone-8-yl) -1,4-dihydropyridine derivatives, fremgangsnmåder for their preparation and to pharmaceutical compositions containing them

Therapeutically active 4- (3-methylflavone-8-yl) -1,4-dihydropyridine derivatives, fremgangsnmåder for their preparation and to pharmaceutical compositions containing them

机译:具有治疗活性的4-(3-甲基黄酮-8-基)-1,4-二氢吡啶衍生物,弗雷姆冈斯默德用于其制备以及含有它们的药物组合物

摘要

New flavone derivatives of general formula: …CHEM… wherein R and R1 can be equal or different and are alkyl containing from 1 to 4 carbon atoms, hydroxyalkyl having 1-4 carbon atoms, formylalkyl or cyanoalkyl, R2 and R3 could be equal or different and are straight or branched alkyl containing from 1 to 6 carbon atoms, straight or branched alkenyl containing from 2 to 6 carbon atoms, alkynyl containing from 2 to 6 carbon atoms, cycloalkyl having 5-7 carbon atoms, aralkyl, phenyl, cyanoalkyl, haloalkyl, mono- or poly-hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfonylalkyl, acyloxyalkyl, acylalkyl, R4R5N-alkyl straight or branched having 2-6 carbon atoms, where R4 and R5 are equal or different and are hydrogen, alkyl, cycloalkyl, aralkyl, phenyl, 3,3-diphenylpropyl, or alternatively, together with the nitrogen atom they form a satured or unsatured 4-7 membered ring, containing other heteroatoms, like O, N or the NR6 group wherein R6 is alkyl, their optical isomers and diastereoisomers, and pharmaceutically acceptable salts thereof. …??The compounds of general formula (I) exhibit a calcium-antagonistic activity and/or an activity relaxing the smooth musculature (in particular the bladder). …??Some procedures for their preparation, and the pharmaceutical composition containing a derivative of general formula (I) as active constituent, are also described.
机译:新的通式为……的黄酮衍生物:…其中R和R1可以相同或不同,并且是含有1至4个碳原子的烷基,具有1-4个碳原子的羟烷基,甲酰基烷基或氰基烷基,R2和R3可以相同或不同的是含有1至6个碳原子的直链或支链烷基,含有2至6个碳原子的直链或支链烯基,含有2至6个碳原子的炔基,具有5至7个碳原子的环烷基,芳烷基,苯基,氰基烷基,卤代烷基,单或多羟基烷基,烷氧基烷基,烷硫基烷基,烷基磺酰基烷基,具有2-6个碳原子的直链或支链的酰氧基烷基,酰基烷基,R 4 R 5 N-烷基,其中R 4和R 5相同或不同,并且为氢,烷基,环烷基,芳烷基,苯基,3,3-二苯丙基或与氮原子一起形成饱和或不饱和的4-7元环,其中含有其他杂原子,例如O,N或NR6基团,其中R6是烷基,它们的旋光异构体和非对映体聚合物及其药学上可接受的盐。 ……通式(I)的化合物表现出钙拮抗活性和/或使平滑肌组织(特别是膀胱)松弛的活性。还描述了一些制备方法,以及含有通式(I)的衍生物作为活性成分的药物组合物。

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