| abstract |
FIELD: organic chemistry. SUBSTANCE: product: N-substituted heterocyclic derivatives of the formula (I) given in description where R 1 and R 2 are similar or different and each means independently hydrogen or group taken among C 1 -C 4 -alkyl, cyano, tetrazolyl, methyltetrazolyl, methylsulfonylamino, trifluoromethylsulfonylamino, trifluoromethylsulfonylaminomethyl, N-cyanoacetamide, N-hydroxyacetamide, N-[(4-carboxy)-1,3-thiazole-2-yl]-acetamide, ureido, 2-cyanoguanidinecarbonyl, 2-cyanoguanidinemethyl, 1-imidazolylcarbonyl, 3-cyano-2-methylisothioureidomethyl at condition that at least one of substituents R 1 and R 2 is distinct from hydrogen; R 3 means hydrogen, (C 1 -C 6 )-alkyl that can be free or substituted with one or some halogen atoms, (C 2 -C 6 )-alkenyl, (C 3 -C 7 )-cycloalkyl, phenyl, (C 1 -C 3 )-phenylalkyl; R 4 and R 5 each means independently (C 1 -C 6 )-alkyl, phenyl being alkyl and phenyl were not substituted or substituted with one or some halogen atoms or a single group of (C 1 -C 4 )-perfluoroalkyl; R 4 and R 5 together form group of the formula CR 7 R 8 where R 7 means hydrogen and R 8 - phenyl; or R 4 R 5 combined together mean group of the formula (CH 2 ) n where n = 3-11; if this group is cyclohexane it can be substituted with (C 1 -C 4 )-alkyl or phenyl; or group (CH 2 ) p Y(CH 2 ) q where p = q = 2; -y - HR 6 ; R 6 - acetyl, COF 3 ,COC 6 H 5 , residue of Arg, Asp, Cys or Ile; or R 4 and R 5 combined together with carbon atom to which they bound form indan or adamantane; X means oxygen or sulfur atom; Z and t = 0 or one of their = 0 and another = 1; or their salts and intermediate compounds - derivatives of pyrimidine and imidazoline and pharmaceutical composition containing compound (I) as an active component at effective amount. The synthesized compounds show antagonistic effect with respect to angiotensin-II and can be used in medicine for treatment of cardiovascular illnesses. EFFECT: improved method of synthesis. 11 cl |