NOVEL ESTERS OF QUATERNISED QUINUCLIDINE Russian patent published in 2010 - IPC C07D453/02 A61K31/439 A61P1/00 A61P13/00 A61P31/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula , where B represents a hydrogen atom or a group selected from -R¹, -OR¹, hydroxy, - O(CO)R¹, cyano and non-aromatic heterocycle which is a saturated or unsaturated C₃-C₁₀carbocyclic ring in which one or more carbon atoms, preferably 1 or 2 carbon atoms, are substituted with oxygen atoms as heteroatoms, where R¹ is selected from a group containing hydrogen atoms, C₁-C₈alkyl, C₂-C₈alkenyl and C₃-C₈cycloalkyl, where the alkyl group is unsubstituted or substituted with one or more substitutes selected from halogen atoms and C₁-C₄alkyl, and where the alkenyl group is unsubstituted or substituted with one or more substitutes selected from C₁-C₄alkyl, n equals an integer from 0 to 4, A is selected from a group containing -CH₂-, -CH=CR₃-, -CR³=CH-, -CR³R⁴-, -O-, -CO-, -O-(CH₂)₂-O-, where R³ and R⁴ each independently represents a hydrogen atom or C₁-C₈alkyl, m equals an integer from 0 to 8, p equals 2, and the bicyclic azonium ring contains a substitute on position 3, including all possible configurations of asymmetrical centres, D is selected from a group containing: or where R⁵ is selected from a group containing phenyl, 2-thienyl, 3-thienyl, 2-furanyl, 3-furanyl, R⁶ is selected from a group containing 2-thienyl, 3-thienyl, 2-furanyl, 3-furanyl, C₃-C₈cycloalkyl, C₁-C₈alkyl, C₂-C₈alkenyl and phenylethyl, R⁷ represents a hydrogen atom or a group selected from hydroxyl, hydroxymethyl and methyl, Q represents a single bond or a group selected from -CH₂-, -CH₂CH₂-, -O-, -O-CH₂-, equals an integer from 0 to 3, X represents a pharmaceutically acceptable anion of mono- or polybasic acid, under the condition that the B-(CH₂)_n-A-(CH₂)_m- group does not represent a straight C₁-₄alkyl and that the following compounds are excluded: 1-allyloxycarbonylmethyl-3-(2-hydroxy-2,2-dithiophen-2-ylacetoxy)-1-azoniumbicyclo[2.2.2]octane and 1-carboxymethyl-3-(2-hydroxy-2,2-dithiophen-2-ylacetoxy)-1-azoniumbicyclo [2.2.2]octane. The invention also relates to a method of producing formula (I) compounds, to a pharmaceutical composition, to use of compounds in any of paragraphs 1-14, as well as a combined product.

EFFECT: obtaining novel biologically active compounds with antagonistic activity towards muscarine receptors M3.

21 cl, 64 ex