DERIVATIVES OF ALKALOID AMINOESTER AND THEIR DRUG COMPOSITIONS Russian patent published in 2015 - IPC C07D453/02 C07D413/06 A61K31/4025 A61K31/439 A61P11/00 

Abstract RU 2567548 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds of general formula

and their pharmaceutically acceptable salts, which have action of antagonist of muscarine receptors. In formula (I) R1 is selected from group, which consists of (C1-C6)alkyl, (C3-C8)cycloalkyl, phenyl, benzyl and thiophenyl, optionally substituted with one or more substituents, selected from atoms of halogen, OH, oxo, SH, NH2, NO2, CN, CONHR5, CON(R5)2, NHCOR5, COR5, CO2R5, etc.; R2 represents H or (C1-C6)alkyl, optionally substituted with one or more substituents, selected from group, which consists of atoms of halogen, OH, oxo, SH, NH2, NO2, CN, CONHR5, CON(R5)2, NHCOR5, COR5, CO2R5, etc.; R3 represents H or is selected from group, which consists of (C1-C6)alkyl, (C3-C8)cycloalkyl, phenyl, thiophenyl, benzothiophenyl and pyridyi, optionally substituted with one or more substituents, selected from group, which consists of atoms of halogen, OH, oxo, SH, NH2, NO2, CN, CONHR5, CON(R5)2, CO2R5, etc.; R6 represents group of formula , where A stands for physiologically acceptable anion; R4 represents group of formula , where p is equal 0 or integer number from 1 to 4; q is equal 0 or integer number from 1 to 4; P represents heteroaryl, selected from oxadiazolyl, oxazolyl, triazolyl, benzoimidazolyl, thiazolyl and isoxazolyl, optionally substituted with one or more substituents, selected from group, which consists of atoms of halogen, OH, oxo, SH, NO2, CN, CON(R5)2, NH2, NHCOR5, CO2R5, etc.; W is selected from group, which consists of (C3-C8)cycloalkyl, phenyl, pyrazolyl, cyclohexyl, dihydrobenzofuranyl, benzothiophenyl, pyridinyl, thiazolyl, oxadiazolyl and thiophenyl, optionally substituted with one or more substituents, selected from group, which consists of atoms of halogen, OH, oxo, SH, NH2, NO2, CN, CONHR5, CON(R5)2, NHCOR5, COR5, CO2R5,etc.; R5 represents H or is selected from group, which consists of (C1-C6)alkyl, (C1-C6)halogenalkyl, (C2-C6)alkenyl and (C3-C8)cycloalkyl, optionally substituted with one or more substituents, selected from group, which consists of atoms of halogen, OH, oxo, SH, NH2, NO2, CN, CONH2, COOH, etc.

EFFECT: invention relates to pharmaceutical compositions, which include compound of formula (I), as well as to their application in treatment of broncho-obstructive or inflammatory diseases, mediated by action of muscarine receptors.

5 cl, 7 tbl, 37 ex

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RU 2 567 548 C2

Authors

Amari Gabriehle

Rikkaboni Mauro

Dates

2015-11-10Published

2011-05-30Filed