Patent RU-2225407-C2 (RU)
Inventor: GAJL SIMON
IPC: C07D487/04
Filed: 1998-07-15
Granted: 2004-03-10
Abstract: 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 P 2T -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) R 1  represents C 1-6 -alkyl, C 2-6 - alkenyl, C 2-6 -alkynyl, C 3-8 -cycloalkyl or phenyl group wherein each group is substituted optionally with one or some substituents taken among halogen atom, OR 8 , NR 9 R 10 , SR 11  or C 1-6 -alkyl (that in turn is substituted optionally with one or some halogen atoms); R 2  represents C 1-8 -alkyl optionally substituted with one or some substituents taken among halogen atom, OR 8 , NR 9 R 10 , SR 11 , C 3-8 -cycloalkyl, aryl (optionally substituted with one or some C 1-6 -alkyl groups and/or halogen atoms) or C 1-6 -alkyl; or R 2  represents C 3-8 -cycloalkyl group optionally substituted with one or some substituents taken among halogen atom, OR 8 , NR 9 R 10 , SR 11 , C 1-6 -alkyl or phenyl; two latter groups are substituted optionally with one or some substituents taken among halogen atom, NO 2 , C(O)R 8 , OR 8 , SR 11 , NR 12 R 13 , condensed 5- or 6- membered saturated ring comprising one or two oxygen atoms, phenyl or C 1-6 -alkyl; two latter groups are substituted optionally with OR 8 , NR 9 R 10  or one or some halogen atoms; one of R 3  and R 4  represents hydroxy-group and another represents hydrogen atom, hydroxy-group or NR 9 R 10 ; R represents group (CR 5 R 6 ) m OR 7  wherein m = 0 or 1; R 5  and R 6  represent independently hydrogen atom, C 1-6 -alkyl or phenyl; two latter groups are substituted optionally with halogen atom; R 7  represents hydrogen atom, C 1-6 -alkyl or   wherein R 5  and R 6  are determined above; n = 1-3; R 14  represents COOH, OR 15 , NR 16 R 17  or CONR 16 R 17 ; or R represents C 1-4 -alkyl or C 2-4 -alkenyl group being each of them is substituted with one or some groups taken among =S, =O, =NR 20  or OR 21  and substituted optionally with one or some groups taken among halogen atom, C 1-4 -alkyl, phenyl, SR 21 , NO 2  or NR 22 R 23  (wherein R 21 , R 22  and R 23  represent independently hydrogen atom, C 1-4 -alkyl or phenyl; R 20  represents OR 24  or NR 25 R 26  wherein R 24  represents hydrogen atom, C 1-4 -alkyl or phenyl; R 25  and R 26  represent independently hydrogen atom, C 1-4 -alkyl, aryl, C 1-6 -acyl, arylsulfonyl or arylcarbonyl); R 8  represents hydrogen atom, C 1-6 - alkyl optionally substituted with halogen atom; or R 8  represents phenyl optionally substituted with one or some substituents taken among halogen atom, NO 2 , C(O) 6 , OR 6 , SR 9 , NR 10 R 11 ; R 9 , R 10 , R 11  represent independently hydrogen atom or C 1-6 - alkyl; R 12  and R 13  represent independently hydrogen atom, C 1-6 -alkyl, acyl, alkylsulfonyl optionally substituted with halogen atom or phenylsulfonyl optionally substituted with C 1-4 -alkyl; R 15 , R 16 , R 17  represent independently hydrogen atom or C 1-6 -alkyl. EFFECT: improved preparing method, valuable medicinal properties of compounds. 20 cl, 1 tbl, 118 ex