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PROCESS FOR PRODUCTION OF NEW DERIVATIVES OF QUINOLIN, IZOQUINOLIN AND QUINASOLINE AND MEDICAL PREPARATIVES CONTAINING OF THESE NEW COMPOUNDS

机译:喹诺林,异喹诺林和喹啉新衍生物的生产工艺以及包含这些新化合物的药物制剂

摘要

Amides of formula: IMAGE I in which A is IMAGE V and W are H, halogen, alkyl (1-3C), alkoxy (1-3C), NO2 or CF3, Z is bound in the ortho or para position with respect to B and is phenyl, optionally substituted, thienyl or pyridyl, the chain X-(CH2)n-(CHR)m-CO-NR1R2 is bound in the ortho or para position with respect to B, R is H or alkyl (1-3C), R1 and R2 are alkyl (1-6C), cycloalkyl (3-6C), phenyl, phenylalkyl, cycloalkylalkyl, alkenyl (3-6C), R1 and R2 can also form, with the nitrogen atom to which they are attached, a pyrrolidine, piperidine, morpholine or thiomorpholine ring, X is CH-R3, N-R4, SO, SO2, O or S, R3 is H, alkyl (1-3C), R4 is alkyl (1-3C) m=0 or 1 and n=0, 1 or 2, provided that, if X is SO, SO2 or N-R4, the sum m+n is equal to at least 1, that, when A and B are N and Z is in the para position with respect to B, X cannot denote the group CH-R3 and that when A is CH, B is N, Z is in the ortho position with respect to B, X is an oxygen atom, and R is a hydrogen atom, the sum m+n is other than 1, and excluding 2-phenyl-4-quinolyl N,N-dimethylcarbamate, have useful pharmacological activity, e.g. as anxiolytics, anticonvulsants and antiangina agents.
机译:下式的酰胺:其中A为 V且W为H,卤素,烷基(1-3C),烷氧基(1-3C),NO2或CF3的酰胺,Z结合在邻位或对位相对于B而言,链X-(CH2)n-(CHR)m-CO-NR1R2相对于B为苯基,可以是取代的噻吩基或吡啶基,在相对于B的邻位或对位键合,R为H或烷基(1-3C),R1和R2是烷基(1-6C),环烷基(3-6C),苯基,苯基烷基,环烷基烷基,烯基(3-6C),R1和R2也可以与氮原子形成它们相连的是吡咯烷,哌啶,吗啉或硫代吗啉环,X是> CH-R3,> N-R4,> SO,> SO2,> O或> S,R3是H,烷基(1-3C),R4是烷基(1-3C)m = 0或1和n = 0、1或2,条件是,如果X> SO,> SO2或> N-R4,则m + n的总和至少等于1,其中,当A和B为N且Z相对于B处于对位时,X不能表示基团> CH-R3;当A为CH时,B为N时,Z相对于B为邻位,X是氧原子,R是一个氢原子,总和m + n不为1,并且不包括2-苯基-4-喹啉基N,N-二甲基氨基甲酸酯,具有有用的药理活性,例如。作为抗焦虑药,抗惊厥药和抗心绞痛药。

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