DERIVATIVES OF N-TRIAZOLYLMETHYLPIPERAZINE, METHOD FOR THEIR PREPARING, MEDICINAL AGENT, DERIVATIVES OF PIPERAZINE Russian patent published in 2006 - IPC C07D403/14 C07D413/14 C07D403/06 A61K31/4995 A61P1/06 

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention describes novel derivatives of N-triazolylmethylpiperazine of the general formula (I): , wherein R¹ means hydrogen atom or (lower)-alkyl; R² means (lower)-alkyl, di-(lower)-alkylamino-(lower)-alkyl, (lower)-alkoxycarbonyl-(lower)-alkyl, cycloalkyl with 5-6 carbon atoms in cycle, pyridinyl-(lower)-alkyl, possibly bi-substituted phenyl-(lower)-alkyl, phenyloxy-(lower)-alkyl substituted with halogen atom in phenyl ring; R³ means (lower)-alkyl, (lower)-alkyloxycarbonyl-(lower)-alkyl or (C₅-C₆)-cycloalkyl, or both R² and R³ in common with nitrogen atom to which they are bound form substituted pyrrolidine ring or cyclic group of the formula (a): , wherein A means nitrogen, oxygen atom, methylene or methylidene group wherein its double bond is formed in common with adjacent carbon atom at position 3 of the group (a), and if A means nitrogen atom then this nitrogen atom has substitute R^4', and in this case n means 2 or 3, and R^4' means (lower)-alkyl, possibly substituted phenyl-(lower)-alkyl, possibly substituted pyridyl, pyridyl-(lower)-alkyl, (lower)-alkoxycarbonyl-(lower)-alkyl, pyrimidyl-(C₅-C₆)-cycloalkyl, (C₅-C₆)-cycloalkyl-(lower)-alkyl or morpholinyl-(lower)-alkyl; R⁴ and R⁵ mean hydrogen atom and in all cases n means a whole number from 1 to 2; R⁴ means hydrogen atom, (lower)-alkyl, (lower)-alkoxy-(lower)-alkyl, (lower)-alkoxycarbonyl, (lower)-alkoxycarbonyl-(lower)-alkyl, di-(lower)-alkylamino-(lower)-alkyl, phenyl, pyrrolidinyl, pyrrolidinyl-(lower)-alkyl, pyridyl or piperidinyl, cyclohexyl, cyclohexyl-(lower)-alkyl, phenyl-(lower)-alkyl, pyridyl monosubstituted with (lower)-alkyl, phenyl-(lower)-alkyl monosubstituted with (lower)-alkyl, pyrimidyl, pyridyl-(lower)-alkyl, morpholinyl-(lower)-alkyl; R⁵ means hydrogen atom, (lower)-alkyl or (lower)-alkoxy-(lower)-alkyl, or R⁴ and R⁵ taken in common mean spiroethylenedioxy-group bound with carbon atom of the group (a), (C₃-C₄)-alkylene bound with two adjacent atoms of the group (a) or phenyl anellated by two adjacent carbon atoms of the group (a), and their physiologically acceptable acid-additive salts also. Also, invention relates to methods for synthesis of these compounds, a medicinal agent based on thereof and intermediate compound in synthesis of novel compounds. Novel compounds are antagonists of neurokinin receptors and display effect in peripheral region preferably and can be used in treatment of functional and inflammatory disorders of digestive tract.

EFFECT: improved preparing method, valuable medicinal properties of derivatives.

10 cl, 4 tbl, 4 ex