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IMIDAZOLE COMPOUNDS, METHOD FOR THEIR PREPARING, METHOD FOR INHIBITION OF ACTIVITY OF ADENOSINE DEAMINASE AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF

机译:咪唑化合物,其制备方法,基于其的抑制腺苷脱氨酶活性的方法和药物组合物

摘要

FIELD: organic chemistry, biochemistry, medicine, pharmacy.;SUBSTANCE: invention relates to new imidazole compounds of the formula (I):; ;wherein R1 represents hydrogen atom, hydroxy-, protected hydroxy-group or aryl optionally substituted with suitable substitute(s) taken among the group consisting of halogen-(lower)-alkyl, halogen atom, hydroxy-, protected carboxy-group, carbamoyl, lower alkylenedioxy- lower alkoxy-group optionally substituted with aryl and lower alkyl optionally substituted with hydroxy- or protected carboxy-group; R2 represents hydrogen atom or lower alkyl; R3 represents hydroxy- or protected hydroxy-group; R4 represents cyano-group, (hydroxy)-iminoamino-(lower)-alkyl, carboxy-, protected carboxy-group, N-comprising heterocyclic group optionally substituted with amino-group or carbamoyl optionally substituted with suitable substitute(s) taken among the group consisting of amino-, hydroxy-group, lower alkyl, lower alkylsulfonyl and aminoimino-(lower)-alkyl optionally substituted with hydroxy-group; -A- represents -Q- or -O-Q- wherein Q means a single bond or lower alkylene, or its salt under condition that when R2 means lower alkyl then R1 represents hydroxy-, protected hydroxy-group or aryl optionally substituted with suitable substitute(s) given above, and also under condition that compound of the formula (I) doesn't represent 1-(hydroxyethyl)-4-(ethoxycarbonyl)-imidazole or 1-(2-hydroxyethyl)-imidazole 4-carboxylic acid anilide. Also, invention relates to a method for preparing these compounds, to a method for inhibition of activity of adenosine deaminase, and to a pharmaceutical composition eliciting inhibitory effect on activity of adenosine deaminase based on these compounds. Invention provides preparing new compounds and medicinal agents based on thereof used for prophylaxis and treatment of disease wherein adenosine shows the effectiveness.;EFFECT: improved inhibiting and preparing methods, valuable medicinal properties of compounds.;9 cl, 2 tbl, 32 ex
机译:发明领域:本发明涉及式(I)的新型咪唑化合物: ;其中R 1 代表氢原子,羟基,被保护的羟基或任选地被选自卤素-(低级-烷基),卤素原子,羟基的适当取代基取代的芳基-保护的羧基,氨基甲酰基,低级亚烷基二氧基-低级烷氧基-任选地被芳基取代和低级烷基任选地被羟基或保护的羧基取代; R 2 代表氢原子或低级烷基; R 3 代表羟基或受保护的羟基; R 4 表示氰基,(羟基)-亚氨基氨基-(低级)-烷基,羧基,受保护的羧基,含氮的杂环基,其任选地被氨基取代或氨基甲酰基,其任选地被氨基取代。选自由氨基,羟基,低级烷基,低级烷基磺酰基和任选被羟基取代的氨基亚氨基-(低级)-烷基组成的组的合适的取代基; -A-代表-Q-或-OQ-,其中Q表示单键或低级亚烷基或其盐,条件是当R 2 表示低级烷基时,R 1 表示羟基,被保护的羟基或芳基,可选地被上述合适的取代基取代,以及在式(I)的化合物不表示1-(羟乙基)-4-(乙氧基羰基)-咪唑的条件下或1-(2-羟乙基)-咪唑4-羧酸苯胺。此外,本发明涉及制备这些化合物的方法,抑制腺苷脱氨酶活性的方法,以及涉及基于这些化合物引起对腺苷脱氨酶活性的抑制作用的药物组合物。本发明提供了用于预防和治疗其中腺苷显示出有效性的疾病的新化合物和基于其的药物的制备;效果:改进的抑制和制备方法,化合物的有价值的医学特性; 9 cl,2 tbl,32 ex

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