| 摘要 |
organic chemistry, heterocyclic compounds, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of purine of formulas (I) , (II) , (III) and (IV) , pharmaceutical composition based on thereof and method of treatment of morbid state characterized by thrombosis activity. In compounds (I), (II), (III) and (IV) Z1 and Z2 each means -O-; R1 means hydrogen atom or OR10; R2 means +C(NH)-NH2; R3 means +C(O)N-(R10)R11, (1,2)-tetrahydropyrimidinyl (optionally substituted with alkyl), (1,2)-imidazolyl (optionally substituted with alkyl) or (1,2)-imidazolinyl (optionally substituted with alkyl); R4 means hydrogen atom; R5 means alkyl or aralkyl; R6 means alkyl, aralkyl or (C(R7)(R8)n-R9; R7 means alkyl, ; or R7 means aralkyl (optionally substituted with one or more substitutes taken among group comprising of halogen atom, hydroxy-group and OP(O)-(OR10)2); or R7 means imidazolylalkyl or indolylalkyl; R8 means hydrogen atom or alkyl; R9 means -C(O)O-R10 or +C(O)N-(R10)R11; each of R10 and R11 means independently hydrogen atom or alkyl; R12 means linear or branched alkylene chain; and R13 means alkyl or aryl. Invention relates also to pharmaceutical composition showing inhibitory activity with respect to factor Xa that involves therapeutically effective amount of compounds of formulas (I), (II), (III), and (IV) and to method of treatment of human morbid state involving administration of therapeutically effective dose of indicated compounds. EFFECT: improved method of treatment, valuable medicinal properties of compounds and composition. 8 cl |
