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BICYCLIC DERIVATIVES OF AMIDINE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND METHOD OF INHIBITION OF NITROGEN OXIDE SYNTHETASE ACTIVITY
BICYCLIC DERIVATIVES OF AMIDINE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND METHOD OF INHIBITION OF NITROGEN OXIDE SYNTHETASE ACTIVITY
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机译:亚胺二酮的双环衍生物,其合成方法,药物成分和抑制一氧化氮合成酶活性的方法
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摘要
FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention describes bicyclic derivatives of amidine of the formula (I) where D means five-membered heterocyclic aromatic ring containing from 1 to 4 heteroatoms taken among O, N or S and optionally substituted by carbon atom with halogen atom, trifluoromethyl, C1-6-alkyl, nitro- or cyano-group and bound with other moiety of compound of the formula (I) through carbon atom; A means N(X) or CH (-(CH2)m-NXY); U means NH, O or CH2; V means (CH2)a; W means (CH2)b; a, b, m, X and Y have values given in the invention claim. Invention describes also methods of synthesis of compounds and preparing the pharmaceutical composition containing thereof. Compounds of the formula (I) are inhibitors of nitrogen oxide synthetase activity and can be used in therapy. EFFECT: improved method of synthesis, valuable biochemical and therapeutic properties of compounds. 10 cl
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机译:领域:有机化学,生物化学,药学。物质:本发明描述了式(I)的am的双环衍生物。<图像文件=“ 00000002.GIF” he =“ 22” id =“ imag0.2” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 43” />其中D表示五元杂环芳族环,含有从O,N或S中夺取的1-4个杂原子,并任选被碳原子取代为卤素原子,三氟甲基,C 1-6 Sub>-烷基,硝基或氰基并通过碳原子与式(I)化合物的其他部分结合; A表示N(X)或CH(-(CH 2 Sub>) m Sub> -NXY); U表示NH,O或CH 2 Sub>; V表示(CH 2 Sub>) a Sub>; W表示(CH 2 Sub>) b Sub>; a,b,m,X和Y具有本发明权利要求中给出的值。本发明还描述了化合物的合成方法以及制备包含其的药物组合物的方法。式(I)的化合物是氮氧化物合成酶活性的抑制剂,可以用于治疗。效果:改进的合成方法,化合物的重要生化和治疗特性。 10厘升
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