GLYCINE DERIVATIVES AND THEIR USE AS MUSCARINIC RECEPTOR ANTAGONISTS Russian patent published in 2016 - IPC C07D207/12 C07D451/10 C07D453/02 A61K31/40 A61K31/46 A61K31/439 A61P11/08 A61P29/02 

Abstract RU 2585767 C2

FIELD: medicine.

SUBSTANCE: invention relates to compounds of general formula (I) or their pharmaceutically acceptable salts having muscarinic receptor antagonist action. In formula (I) R1 is selected from a group consisting of linear or branched (C1-C10)alkyl, (C2-C6)alkenyl, aryl(C3-C8)cycloalkyl, aryl(C1-C6)alkyl and heteroaryl optionally substituted with one or more substitutes selected from a group consisting of halogen atoms, -N(R5)(R6′), -NHCO(R5), -CO2R5, (C1-C10)alkyl, (C1-C10)alkoxy and aryloxy; G is selected from a group consisting of -OC(O)-, -SO2- and -C(O)-; R2 is -H; R3 is selected from a group consisting of (C1-C10)alkyl, aryl, heteroaryl and heteroaryl (C1-C6)alkyl optionally substituted with one or more substitutes selected from a group consisting of halogen, -OH, (C1-C10)alkyl, (C1-C10)alkoxy, aryloxy and aryl(C1-C10)alkyleneoxy; R6 is selected from a group consisting of units of formula (i), (ii) and (iii), where m = 1, 2 or 3; n = 1, 2 or 3; A- is a physiologically acceptable anion; R4 represents a group of formula (Y), wherein p represents 0 or an integer from 1 to 4; q represents 0 or an integer from 1 to 4; P is absent or is selected from a group consisting of -O- and -C(O)-; W is selected from a group consisting of H, linear or branched (C1-C10)alkyl, aryl and heteroaryl optionally substituted with one or more substitutes selected from a group consisting of halogen, -OH, -NO2, -CO2(R5), (C1-C10)alkyl, (C1-C10)alkoxy and aryl; R5 and R6′ are independently selected from a group consisting from -H, (C1-C10)alkyl and (C1-C10)alkoxy. Invention also relates to compounds of general formula (VI), pharmaceutical compositions, a device comprising said composition, and use of compounds of formula (I) or (VI) for manufacture of a medicament for prevention and/or treatment of broncho-obstructive or inflammatory diseases.

EFFECT: manufacture of a medicament for prevention and/or treatment of broncho-obstructive or inflammatory diseases.

13 cl, 6 tbl, 52 ex

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RU 2 585 767 C2

Authors

Amari Gabriele

Rikkaboni Mauro

Farina Marko

Dates

2016-06-10Published

2011-10-27Filed