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tricyclic derivatives and their physiologically acceptable salts with psychostimulante properties, antidepressive, analgesic, antitussive, and gastric antisecretoire product

机译:具有精神刺激特性的三环衍生物及其生理上可接受的盐,抗抑郁,镇痛,镇咳和胃抗分泌产品

摘要

1,269,551. Tricyclic compounds. SCIENCE UNION ET CIE SOC. FRANCAISE DE RECHERCHE MEDICALE. 12 March, 1970 [27 March, 1969], No. 16116/69. Heading C2C. Novel tricyclic compounds of the general formula wherein A is -(CH 2 ) m -, -CH=CH-, -(CH 2 ) p O-, -(CH 2 ) p S-, -(CH 2 ) p SO 2 -, -(CH 2 ) p NR 1 - or -SO 2 NR 2 -, in which m is 1, 2 or 3, p is 1 or 2, R 1 is a hydrogen atom or a C 1-5 alkyl group and R 2 is a C 1-5 alkyl group, X and Y are each a hydrogen or halogen atom, R and RSP1/SP are each a hydrogen atom or a C 1-5 alkyl group and n is an integer from 1 to 12 inclusive, and salts thereof are prepared by condensation of an aminoalkanoic acid ester of the general formula RNH(CH 2 ) n COORSP1/SP, wherein RSP1/SP is a C 1-5 alkyl group, with a halide of the general formula wherein Hal is a chlorine or bromine atom, and optional saponification of the resulting ester of the first general formula above to give the corresponding free acid, followed optionally by salification of the product with an acid or base. Halides of the third general formula above are prepared by cyclization of a suitable o- (phenyl-A)-benzoic acid, reduction of the resulting tricyclic ketone and halogenation of the resulting hydroxy compound. Pharmaceutical compositions having psychostimulant, antidepressive, analgesic, antitussive, antihistaminic and gastric antisecretory activity comprise, as active ingredient, a tricyclic compound of the first general formula above or a physiologically tolerable salt thereof, together with a pharmaceutically suitable carrier, and may be administered orally, rectally or parenterally.
机译:1,269,551。三环化合物。科学联盟ET CIE SOC。弗兰卡塞斯德雷赫切医疗公司。 1970年3月12日[1969年3月27日],编号16116/69。标题C2C。具有通式的新型三环化合物,其中A为-(CH 2)m-,-CH = CH-,-(CH 2)p O-,-(CH 2)p S-,-(CH 2)p SO 2 -,-(CH 2)p NR 1-或-SO 2 NR 2-,其中m为1、2或3,p为1或2,R 1为氢原子或C 1-5烷基, R 2是C 1-5烷基,X和Y分别是氢或卤素原子,R和R 1 分别是氢原子或C 1-5烷基,n是通式为RNH(CH 2)n COOR 1 的氨基链烷酸酯缩合制备其盐,其中R 1 为C 1-5烷基,其通式为卤化物,其中Hal为氯或溴原子,以及将上述第一个通式的所得酯任选皂化,得到相应的游离酸,然后任选将其盐化产品与酸或碱。通过合适的邻-(苯基-A)-苯甲酸的环化,所得三环酮的还原和所得羟基化合物的卤化,可以制备上述第三通式的卤化物。具有精神刺激药,抗抑郁药,镇痛药,镇咳药,抗组胺药和胃抗分泌活性的药物组合物包含上述第一通式的三环化合物或其生理上可接受的盐以及药学上合适的载体作为活性成分,并且可以口服给药,直肠或肠胃外。

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