首页> 外国专利> PHARMACEUTICAL COMPOSITION FOR TREATING PETIT-MAL EPILEPSY COMPRISING AT LEAST ONE COMPOUND HAVING GABAB-ANTAGONISTIC PROPERTIES, PREFERABLY BEING A PHOSPHINIC ACID DERIVATIVE

PHARMACEUTICAL COMPOSITION FOR TREATING PETIT-MAL EPILEPSY COMPRISING AT LEAST ONE COMPOUND HAVING GABAB-ANTAGONISTIC PROPERTIES, PREFERABLY BEING A PHOSPHINIC ACID DERIVATIVE

机译:用于治疗具有至少一种具有GABAB抗性特性的,至少是一种磷酸衍生物的化合物的PET-MAL癫痫病的药物组合物

摘要

Compounds having GABAB-antagonistic properties, for example those of formula I IMAGE (I) wherein one of the radicals R1, R2 and R3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R1 or R2, hydroxy or, in the case of R1, halogen or, in the case of R2 together with R2', oxo, and the remaining radical is hydrogen, R1' is hydrogen or halogen, R2' is hydrogen, hydroxy or, together with R2, is oxo, R4 and R5 are hydrogen or R4 is an araliphatic or heteroarylaliphatic radical and R5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R1 is hydrogen or hydroxy, R2 is an aromatic radical and R1', R2' and R3 are hydrogen, R is methyl, and their pharmaceutically acceptable salts, can be used as active ingredients in medicaments for the treatment of epilepsies of the "petit mal" type. The invention relates also to novel compounds of formula I and processes for the preparation thereof.
机译:具有GABA B拮抗性质的化合物,例如式I (I)的化合物,其中基团R1,R2和R3中的一个为氢或脂族,脂环族,芳脂族或芳族基团,另一个为氢,或在情况下R 1或R 2的基团是羟基,或者在R 1的情况下是卤素,或者在R 2与R 2′一起是氧代,并且剩余的基团是氢,R 1′是氢或卤素,R 2′是氢,羟基或与R 2一起是氧代,R 4和R 5是氢或R 4是芳脂族或杂芳基脂族基团,R 5是氢或脂族基团,并且R是脂族,脂环族,脂环族脂族基,芳脂族,杂芳基脂族或芳族基团具有至少2个碳原子,或当R1为氢或羟基时,R2为芳香族基团,且R1',R2'和R3为氢,R为甲基及其药学上可接受的盐,可用作治疗药物中的活性成分小恶性癫痫病pe。本发明还涉及式I的新型化合物及其制备方法。

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