TRIAZOLEPYRIMIDINE DERIVATIVES AND PHARMACEUTICAL COMPOSITION SHOWING ANTAGONISTIC ACTIVITY WITH RESPECT TO ANGIOTENSIN II RECEPTORS Russian patent published in 1998 - IPC

FIELD: organic chemistry. SUBSTANCE: invention proposes new derivatives of triazolepyrimidine of the formula (I): where R₁ - lower alkyl or C₃-C₇-cycloalkyl; R₂ - hydrogen, lower alkyl, group NH-NH₂, (CH₂)_mOR₄,(CH₂)_mSR₄ where R₄ - hydrogen, lower alkyl; m = 0-2; group is radical: where R₈ - H, (CH₂)_nOH,-(CH₂)_n--COOH; -R₁₂-,-(CH₂)_nCOOR₁₂, where R₁₂ - lower alkyl; n = 1 or 2; R₉ - hydrogen, -SH; R₁₀ - hydrogen, lower alkyl; R₁₁ - hydrogen, lower alkyl, lower haloidalkyl, phenyl, pyridinyl, ; R₁₃,R₁₄ - hydrogen, lower alkyl; R₃ - phenyl substituted with group -COOH, -CO-NH-, SO₃H, nitrogen- or oxygen-containing heterocycle, thiophene substituted with nitrogen-containing 5-membered heterocycle and their tautomeric forms and pharmaceutically acceptable additive salts. Invention proposes pharmaceutical composition showing antagonistic activity with respect to angiotensin receptors and containing compound of the formula (I) taken at effective dose. The synthesized compounds were used in medicine, in part, in cardiology. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 8 cl, 1 tbl