SUBSTITUTED SULPHONAMIDE DERIVATIVES Russian patent published in 2014 - IPC C07D401/14 A61K31/4427 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to substituted sulphonamide derivatives of general formula:

where m equals 0, 1 or 2; n equals 1 or 2; o equals 0, 1 or 2; p equals 0, 1 or 2; q equals 0, 1, 2 or 3; r equals 0, 1 or 2, under the condition that q+r is not greater than 3; v equals 0 or 1; w equals 0 or 1; under the condition that if v equals 0, then w equals 0; An^- denotes a halide anion; Q denotes a single bond, -O- or -CH₂-; R¹ denotes aryl; R² and R³ have values given in (i) or (ii): (i) R² denotes H, C_1-6-alkyl, C_3-8-cycloalkyl, a bicyclic 8-12-member carbocyclyl, CH(aryl)₂ or aryl; or denotes a heteroaryl bonded through a C_1-6-alkylene group, the heteroaryl being selected from pyridinyl; R³ denotes H, C_1-6-alkyl or aryl; or (ii) R² and R³, together with the -N-(CH-)- group bonding them, form a heterocycle which can be annelated with an aryl residue, where the heterocycle is 6-membered, saturated or at least monounsaturated but not aromatic, and together with the N heteroatom to which the residue R² is bonded, can contain at least another O heteroatom; R⁴ denotes aryl or heteroaryl, selected from pyridinyl; R⁵ and R⁶ independently denote H or C_1-6-alkyl, wherein R⁵ and R⁶ do not simultaneously denote H; or R⁵ and R⁶ together denote a substituted or unsubstituted 5- or 6-member heteroaryl which, together with an N atom to which R⁵ and R⁶ are bonded, can contain at least another N heteroatom; or R⁵ and R⁶ together denote a group selected from -(CH₂)_d- or -(CH₂)_e-X-(CH₂)_f, where d denotes 2, 3, 4, 5 or 6 and e and f are independently equal to 1, 2 or 3, under the condition that e+f is not greater than 5; and X denotes NR¹², where R¹² denotes H or C_1-6-alkyl; R²⁰ denotes C_1-6-alkyl; and where said aryl and heteroaryl residues in case can be unsubstituted or monosubustituted or multi-substituted with the same or different residues selected from a group comprising F, Cl, Br, I, O-C_1-6-alkyl, CF₃ and C_1-6-alkyl; and said C_1-6-alkyl residues in each case can be branched or straight; in form of a separate enantiomer or separate diastereomer, racemate, enantiomers, diastereomers, mixtures of enantiomers and/or diastereomers, and in each case in form of bases and/or physiologically compatible salts thereof. The invention also relates to a method of producing the described compound, a drug having antagonistic action on B1R, based on compounds of formula I and use of said compound to produce a drug.

EFFECT: novel compounds which can be used in medicine are obtained and described.

15 cl, 131 ex