SUBSTITUTED 1-AMINOALKYL LACTAMES, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD FOR THEIR PREPARING Russian patent published in 2004 - IPC

FIELD: organic chemistry, medicine.

SUBSTANCE: invention describes a compound of the general formula (I):

wherein R¹, R² and R³ mean independently in each case hydrogen, halogen atom, (C₁-C₆)-alkyl, -OR', -SR', -NR'R'', -SOR', -SO₂R', -COOR', -OCOR', -OCONR'R'', -OSO₂R', -OSO₂NR'R'', -NR'SO₂R''. -NR'COR'', -SO₂NR'R'', -SO₂(CH)_1-3CONR'R'', -CONR'R'', cyano-group, halogenalkyl or nitro-group; or if R¹ and R² if there are adjacent then in common with carbon atom to which they are bound can form 5-7-membered aromatic, saturated or unsaturated cycle optionally comprising one or two ring heteroatoms taken among nitrogen atom (N), S(O)_0-2 or oxygen atom (O), and optionally substituted with (C-C₆)-alkyl, halogen atom, cyano-group or (lower)-alkoxy-group; R' and R'' mean independently in each case hydrogen atom, (C₁-C₆)-alkyl, substituted (C₁-C₆)-alkyl, (C₀-C₃)-alkylalkoxy-group, aryl, heterocyclyl, heteroaryl, aryl-(C₁-C₃)-alkyl, heteroaryl-(C₁-C₃)-alkyl, heterocyclyl-(C₁-C₃)-alkyl, cycloalkylalkyl, cycloalkyl; or R' and R'' in common with nitrogen atom to which they are bound can form also 5-7-membered cycle optionally comprising one additional ring heteroatom taken among nitrogen (N), oxygen (O) atom or S(O)_0-2; in each case R⁴ means (C₁-C₆)-alkyl; R⁵ means independently in each case (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkenyl or cycloalkyl; one among X, Y or Z means independently -S-, -O-, -CH₂- or ›N-R⁶ and others mean -CH₂-; R⁶ means hydrogen atom, (C₁-C₆)-alkyl, halogen alkyl, aryl-(C₁-C₆)-alkyl, heteroaryl-(C₁-C₆)-alkyl, -(C₁-C₆)-CR'R'R', -COOR', -SO₂R', -C(O)R', -SO₂(CH₂)_0-3-NR'R'', -CONR'R'', -C(O)OCH₂OC(O)R', -C(O)-CH₂-S-C(O)R' or PO(OR')₂ wherein R' and R'' have values given above; m means a whole number 0-3; n means a whole number 1-6; or invention relates to individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or their solvates. Also, invention describes a pharmaceutical composition eliciting antagonistic effect with respect to muscarinic receptors M2/M3 based on compounds of the formula (I), and methods for preparing compounds of the formula (I). Invention provides preparing novel compounds eliciting useful biological properties.

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

21 cl, 1 tbl, 20 ex