首页> 外国专利> PYRAZOLE3,4-DPYRIMIDINES SHOWING ANTICONVULSANT AND ANTIALLERGIC/ANTIASTHMATIC EFFECT, METHODS OF THEIR SYNTHESIS (VARIANTS) AND PHARMACEUTICAL COMPOSITION

PYRAZOLE3,4-DPYRIMIDINES SHOWING ANTICONVULSANT AND ANTIALLERGIC/ANTIASTHMATIC EFFECT, METHODS OF THEIR SYNTHESIS (VARIANTS) AND PHARMACEUTICAL COMPOSITION

机译:吡唑并[3,4-D]嘧啶类药物具有抗惊厥作用和镇痛/抗寄生虫作用,其合成方法(变体)和药物组成

摘要

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel pyrazole[3,4-d] pyrimidines showing anticonvulsant and antiallergic/antiasthmatic effect, methods of their synthesis (variants) and pharmaceutical composition based on thereof. Pyrazole[3,4-d]pyrimidines correspond to the general formula (1) or its tautomer where X means oxygen, sulfur atom; Y means halogen atom, C1-44-alkyl, C1-4-alkoxy-group or trifluoromethyl-group; m = 1 or 2. Methods of synthesis of compounds of the general formula (1) involve cyclization of compound of the formula (2) with formamide or interaction of compound of the formula (1) where X means oxygen atom with phosphorus pentasulfide or 2,4-bis-(4-methoxyphenyl)-1,3-dithia-2,4-diphosphoethane-2,4-disulfide. Pharmaceutical composition comprises one or some compounds of the formula (1) and one or some of physiologically tolerant accessory substances and/or carriers. EFFECT: improved methods of synthesis, valuable medicinal properties. 8 cl, 4 tbl, 25 ex
机译:领域:有机化学,药学。发明领域本发明涉及显示出抗惊厥和抗过敏/抗哮喘作用的新型吡唑[3,4-d]嘧啶,其合成方法(变体)和基于其的药物组合物。吡唑[3,4-d]嘧啶对应于通式(1)或其互变异构体,其中X表示氧,硫原子; Y表示卤素原子,C 1-4 4-烷基,C 1-4 -烷氧基或三氟甲基。 m = 1或2。合成通式(1)化合物的方法涉及环化通式(2)的化合物。与甲酰胺或式(1)化合物的相互作用,其中X表示氧原子与五硫化二磷或2,4-双-(4-甲氧基苯基)-1,3-二硫代-2, 4-二磷酸乙烷-2,4-二硫化物。药物组合物包含一种或一些式(1)的化合物以及一种或一些生理上可耐受的辅助物质和/或载体。效果:改进的合成方法,有价值的药物特性。 8厘升,4汤匙,25前

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