申请人:Egyt Gyogyszervegyeszeti Gyar
公开号:US04342762A1
公开(公告)日:1982-08-03
The invention relates to novel basic ethers of the general formula /I/ and pharmaceutically acceptable acid addition salts and quaternary salts thereof, ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and represent a C.sub.1-5 alkyl group or a C.sub.3-6 cycloalkyl group or they form, together with the adjacent nitrogen atom, a heterocyclic ring containing 4-7 carbon atoms and optionally a further hetero atom, e.g. an oxygen, sulfur or nitrogen atom, and this latter may be optionally substituted by a C.sub.1-3 alkyl, benzyl or phenyl group, R represents a phenyl, phenyl-/C.sub.1-3 alkyl/ or thienyl group optionally substituted by one or more halogen or C.sub.1-3 alkoxy substituent/s/, A represents a C.sub.2-5 straight or branched alkylene chain, and represents a valence bond of .alpha. or .beta. configuration. The new compounds of the general formula /I/ possess valuable anticonvulsive, motility inhibiting, hexobarbital narcose potentiating and analgesic effects, which are, in case of certain compounds, complemented by week antiserotonine, gastro-intestinal-tract inhibiting and antiinflammatory effects, and can be applied to advantage in the therapy.
本发明涉及一种新颖的基础醚,其一般式为/I/,以及其药学上可接受的酸盐和季铵盐,其中,R.sup.1和R.sup.2可以相同也可以不同,表示C.sub.1-5烷基或C.sub.3-6环烷基,或者与相邻的氮原子一起形成含有4-7个碳原子和可选的进一步杂原子(例如氧、硫或氮原子)的杂环,后者可以被C.sub.1-3烷基、苄基或苯基取代;R表示苯基、苯基-/C.sub.1-3烷基/或噻吩基,可选地被一个或多个卤素或C.sub.1-3烷氧基取代;A表示C.sub.2-5直链或支链烷基链,且表示.alpha.或.beta.构型的价键。一般式/I/的新化合物具有有价值的抗惊厥、运动抑制、己巴比妥酸麻醉增强和镇痛作用,对于某些化合物,这些作用还可以通过弱抗血清素、胃肠道抑制和抗炎作用得到补充,并且可以在治疗中得到优越的应用。