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    • 10. 发明授权
    • Pharmaceutical compositions having antiepileptic and antineuralgic action
    • 具有抗癫痫和抗神经功能作用的药物组合物
    • US4431641A
    • 1984-02-14
    • US310197
    • 1981-10-09
    • Cesare MondadoriMarkus Schmutz
    • Cesare MondadoriMarkus Schmutz
    • A61K31/55A61P25/04A61P25/08A61K31/33A61K31/40A61K31/44A61K31/475
    • A61K31/55
    • The present invention relates to novel pharmaceutical compositions having antiepileptic and antineuraglic action and containing (a) at least one anticonvulsive compound of the general formula I ##STR1## wherein X.sub.1 is hydrogen, halogen having an atomic number up to 35, or is cyano, and X.sub.2 and Y together are an additional bond, or X.sub.1 and X.sub.2 together are the oxo radical, or X.sub.1 is hydroxy, X.sub.2 is hydrogen and Y is also hydrogen, and (b) at least one nootropic compound of the vincamine type which has the general formula II ##STR2## wherein Z.sub.1 is lower alkoxycarbonyl, Z.sub.2 is hydroxy and Z.sub.3 is hydrogen, or Z.sub.2 and Z.sub.3 together are an additional bond, or one of Z.sub.1 and Z.sub.2 is hydroxy and the other is hydrogen and Z.sub.3 is also hydrogen, in particular vincamine (DCI rec.), in which Z.sub.1 is methoxycarbonyl, Z.sub.2 is hydroxy and Z.sub.3 is hydrogen, and also e.g., vinpocetin (DCI rec.), in which Z.sub.1 is ethoxycarbonyl and Z.sub.2 and Z.sub.3 together form an additional bond, as well as vincanol (DCI prop.), in which one of Z.sub.1 and Z.sub.2 is hydroxy and the other is hydrogen and Z.sub.3 is hydrogen, and the acid addition salts thereof, or at least one nootropic derivative of 2-pyrrolidinone, e.g. 2-oxo-1-pyrrolidineaetamide (piracetam) or one of its nootropic derivatives. The compounds of the general formula II e.g. vincamine, as well as the nootropic derivatives of 2-pyrrolidinone, e.g. piracetam, have in themselves virtually no anticonvulsive activity but potentiate the action of the compounds of the general formula I, e.g. carbamazepine.
    • 本发明涉及具有抗癫痫和抗神经功能作用的新型药物组合物,并且含有(a)至少一种通式I的抗惊厥药物(I),其中X 1是氢,原子序数高达35的卤素或是 氰基,X2和Y一起是另外的键,或者X 1和X 2一起是氧代基,或者X 1是羟基,X 2是氢,Y也是氢,和(b)至少一种长春胺类的特配化合物, 具有通式II其中Z 1为低级烷氧基羰基,Z 2为羟基,Z 3为氢,Z 2和Z 3为一个附加键,或者Z 1和Z 2中的一个为羟基,另一个为氢和Z 3 也是氢,特别是长春胺(DCI rec。),其中Z1是甲氧基羰基,Z2是羟基,Z3是氢,以及例如长春西林(DCI rec。),其中Z1是乙氧基羰基,Z2和Z3一起形成 额外的粘合剂,以及长春辛醇(DCI prop。),其中一种 的Z 1和Z 2是羟基,另一个是氢,Z 3是氢,及其酸加成盐,或2-吡咯烷酮的至少一种向异性衍生物。 2-吡咯烷酮(吡拉西坦)或其引诱性衍生物之一。 通式II的化合物例如 长春胺,以及2-吡咯烷酮的引诱衍生物,例如。 吡拉西坦本身几乎没有抗惊厥活性,但增强了通式I化合物的作用,例如, 卡马西平。