FIELD: organic chemistry, heterocyclic compounds, chemical technology, pharmacy. SUBSTANCE: invention relates to new triazolo[4,5-d]pyrimidine compounds of the general formula (I) or their pharmaceutically acceptable salts that elicit effect of P2T-antagonists, in particular, show activity inhibiting platelets aggregation. Invention relates also to methods for preparing compounds of the formula (I) and pharmaceutical composition. In compounds of the general formula (I) R1 represents C1-6-alkyl, C2-6- alkenyl, C2-6-alkynyl, C3-8-cycloalkyl or phenyl group wherein each group is substituted optionally with one or some substituents taken among halogen atom, OR8, NR9R10, SR11 or C1-6-alkyl (that in turn is substituted optionally with one or some halogen atoms); R2 represents C1-8-alkyl optionally substituted with one or some substituents taken among halogen atom, OR8, NR9R10, SR11, C3-8-cycloalkyl, aryl (optionally substituted with one or some C1-6-alkyl groups and/or halogen atoms) or C1-6-alkyl; or R2 represents C3-8-cycloalkyl group optionally substituted with one or some substituents taken among halogen atom, OR8, NR9R10, SR11, C1-6-alkyl or phenyl; two latter groups are substituted optionally with one or some substituents taken among halogen atom, NO2, C(O)R8, OR8, SR11, NR12R13, condensed 5- or 6- membered saturated ring comprising one or two oxygen atoms, phenyl or C1-6-alkyl; two latter groups are substituted optionally with OR8, NR9R10 or one or some halogen atoms; one of R3 and R4 represents hydroxy-group and another represents hydrogen atom, hydroxy-group or NR9R10; R represents group (CR5R6)mOR7 wherein m = 0 or 1; R5 and R6 represent independently hydrogen atom, C1-6-alkyl or phenyl; two latter groups are substituted optionally with halogen atom; R7 represents hydrogen atom, C1-6-alkyl or wherein R5 and R6 are determined above; n = 1-3; R14 represents COOH, OR15, NR16R17 or CONR16R17; or R represents C1-4-alkyl or C2-4-alkenyl group being each of them is substituted with one or some groups taken among =S, =O, =NR20 or OR21 and substituted optionally with one or some groups taken among halogen atom, C1-4-alkyl, phenyl, SR21, NO2 or NR22R23 (wherein R21, R22 and R23 represent independently hydrogen atom, C1-4-alkyl or phenyl; R20 represents OR24 or NR25R26 wherein R24 represents hydrogen atom, C1-4-alkyl or phenyl; R25 and R26 represent independently hydrogen atom, C1-4-alkyl, aryl, C1-6-acyl, arylsulfonyl or arylcarbonyl); R8 represents hydrogen atom, C1-6- alkyl optionally substituted with halogen atom; or R8 represents phenyl optionally substituted with one or some substituents taken among halogen atom, NO2, C(O)6, OR6, SR9, NR10R11; R9, R10, R11 represent independently hydrogen atom or C1-6- alkyl; R12 and R13 represent independently hydrogen atom, C1-6-alkyl, acyl, alkylsulfonyl optionally substituted with halogen atom or phenylsulfonyl optionally substituted with C1-4-alkyl; R15, R16, R17 represent independently hydrogen atom or C1-6-alkyl. EFFECT: improved preparing method, valuable medicinal properties of compounds. 20 cl, 1 tbl, 118 ex
Authors
Dates
2004-03-10—Published
1998-07-15—Filed