AMIDINE DERIVATIVES, A METHOD OF THEIR SYNTHESIS AND A DRUG BASED ON SAID SHOWING A PROPERTY TO INHIBIT ACTIVITY OF NITROGEN OXIDE (V) SYNTHETASE Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention proposes derivatives of amidine of the general formula (I) where D means phenyl and 5-membered heterocyclic aromatic ring containing from 1 to 2 heteroatoms taken from O, S and N one group of that is substituted optionally with a group taken from C₁-C₆-alkyl, halogen atom or R¹-perfluoroalkyl; R² means hydrogen, halogen atom; -X(CH₂)_nZCONR³R⁴, means a group or -(CH₂)_qNHC(NH)R⁶; R³ and R⁴ mean hydrogen atom, C₁-C₄-alkyl, -(CH₂)_r-A, -(CH₂)_m-OA or CH(CH₃)(CH₂)_t-A; or NR³N⁴ in combination mean piperonylamino-, piperidinyl-, morpholinyl-group and the others; R⁵ means C₁-C₆-alkyl, C₁-C₆-perfluoroalkyl, -(CH₂)_r-A or -O-(CH₂)_w-A where A means phenyl, pyridinyl, pyrimidinyl or 5-membered heterocyclic ring containing 1 heteroatom taken from O, S or N; R⁶ means phenyl or 5-membered heterocyclic aromatic ring containing 1 heteroatom taken from O, S or N; n and r = 0-4; p and w = 1-4; m = 2-4; q and t = 0-4; s = 1-3; X means O or a bond; Z means O, NR⁷ or a bond; R⁷ means hydrogen atom or C₁-C₆-alkyl, or its pharmaceutically acceptable salts. Method of synthesis of a compound of the formula (I) or its pharmaceutically acceptable salt involves an interaction of compound of the formula (II) where L - a group to be split and D is indicated above with a compound of the formula (III) where R¹ and R² are given above. Invention relates to also a drug showing a property to inhibit activity of nitrogen oxide (V) synthetase. EFFECT: improved method of synthesis, inhibition of nitrogen oxide (V) synthetase. 12 cl, 76 ex