ALKALOID DERIVATIVES OF AMINOESTERS AND THEREOF-INCLUDING DRUG COMPOSITIONS Russian patent published in 2015 - IPC C07D453/02 A61K31/439 A61P11/00 

Abstract RU 2569846 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds of general formula and their pharmaceutically acceptable salts, which possess activity of antagonist of muscarinic receptors. In formula (I) R1 is selected from the group, consisting of aryl, heteroaryl and aryl-(C1-C6)-alkyl, optionally substituted with one or more substituents, selected from the group, consisting of halogen atoms, CON(R5)2, COR5, CO2R5, (C1-C6)-alkyl and (C1-C6)-alkoxyl; R2 stands for H or (C1-C6)-alkyl; R3 is selected from the group, consisting of phenyl, pyridyl and benzothiophenyl, optionally substituted with one or more substituents, selected from the group, consisting of OH, (C1-C6)-alkoxyl and aryl-(C1-C6)-alkoxyl; R5 is selected independently from H and (C1-C6)-alkyl; Q stands for the group of formula or ; R4 stands for the group of formula , where p stands for 0 or integer number from 1 to 4; q stands for 0 or integer number from 1 to 4; P is absent or is selected from the group, consisting of O, CO and C(O)N(R5); W is selected from the group, consisting of H, (C1-C6)-alkyl, (C2-C6)-alkenyl, aryl and heteroaryl, optionally substituted with one or more substituents, selected from the group, consisting of halogen atoms and OH; A- stands for physiologically acceptable anion, with at least one of R1 and R3 standing for heteroaryl group and when Q represents the group of formula (i) and R3 represents phenyl, R1 is different from 2-(methoxycarbonyl)thiophen-3-yl.

EFFECT: invention relates to pharmaceutical compositions, including formula (I) compound, to device, including said pharmaceutical composition, as well as to thereof application in treatment of bronchial obstructive and inflammatory diseases.

17 cl, 50 ex

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RU 2 569 846 C2

Authors

Amari Gabriehle

Rikkaboni Mauro

Kalidzhuri Antonio

Dates

2015-11-27Published

2011-05-30Filed