NEW DERIVATIVES OF N-(IMINOMETHYL)AMINES, THEIR PREPARING, THEIR USING AS MEDICINAL AGENTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF Russian patent published in 2004 - IPC

FIELD: organic chemistry, biochemistry, pharmacy.

SUBSTANCE: invention relates to compounds of the formula (I):

wherein Ф represents phenylene radical; A represents radical of the formula:

wherein R₁, R₂, R₃, R₄ and R₅ represent independently hydrogen atom, OH-group or unbranched or branched alkyl or alkoxy-radical comprising from 1 to 6 carbon atoms, or radical of the formula:

wherein R₁, R₂, R₃, R₄ and R₅ represent independently hydrogen atom, OH-group or unbranched or branched alkyl or alkoxy-radical comprising from 1 to 6 carbon atoms; B represents thiophene; W is absent or represents a bond or sulfur atom (S); X represents a bond or radical -(CH₂)_k-NR₁₆-, -O-, -CO-, -NR₁₆-CO- and so on wherein k = 0 or 1; Y represents a bond or radical taken among radicals -(CH₂)_m-, -(CH₂)_m-O-(CH₂)_n, -(CH₂)_m-NR₁₈-(CH₂)_n-, -(CH₂)_m-NR₁₈-CO-(CH₂)_n-, -(CH₂)_m-Q-(CH₂)_n wherein Q represents piperazine radical; m and n mean a whole number from 0 to 5; R₁₆, R₁₇ and R₁₈ represent independently hydrogen atom, or salt of indicated compound. Invention proposes compounds represented by formulas (IS): A-X-Y-Ф-Т (IS) and (IS'):

used as intermediate substances for preparing compounds of the formula (I). Also, invention proposes a pharmaceutical composition eliciting property to inhibit activity of NO-synthase and comprising an active compound. As an active compound the pharmaceutical composition comprises compound of the formula (I) or its pharmaceutically acceptable salt. Invention provides preparing derivatives of N-(iminomethyl)amines showing inhibitory activity with respect to enzymes NO-synthases producing nitrogen monoxide NO.

EFFECT: improved preparing method, valuable medicinal and biochemical properties of compounds.

13 cl, 39 ex