OXADIAZOLES AS MUSCARINIC RECEPTOR AGONISTS M AND/OR M Russian patent published in 2024 - IPC C07D413/14 C07D451/02 C07D451/14 C07D453/06 C07D471/10 C07D487/10 C07D498/08 C07D498/10 A61K31/5386 A61K31/454 A61K31/46 A61K31/4245 A61K31/55 A61P25/28 A61P29/00 

Abstract RU 2817018 C2

FIELD: medicine; pharmaceutics.

SUBSTANCE: invention relates to a compound of formula (1) or a pharmaceutically acceptable salt thereof, where X1 and X2 are saturated hydrocarbon groups, containing together in total from five to nine carbon atoms and zero or one oxygen atom and bonded together so that the fragment forms a monocyclic or bicyclic ring system, or where X1 and X2 are connected together so that the fragment forms , X3 and X4 are saturated hydrocarbon groups, containing in total from three to six carbon atoms and bonded together in such a way that the fragment forms a monocyclic or bicyclic ring system, R1 is selected from NR5R6, CONR5R6, COOR7, 5- or 6-member ring containing 0, 1 or 2 heteroatoms selected from N, which is optionally substituted with C1-C3 alkyl, CONR5R6, halogen, oxo, CH2OH or pyrazole ring substituted with C1-C3 alkyl, or R1 is bonded to R2 to form a monocyclic or bicyclic ring containing 1 or 2 heteroatoms selected from O and N, which is substituted with one or more substitutes selected from C1-C6 alkyl and oxo, R2 is selected from hydrogen and cyano, R4 is a C1-6 alkyl group, optionally substituted with one or more fluorine atoms, R5 is selected from COCH3, a non-aromatic C1-10 saturated hydrocarbon group, optionally substituted with one or more fluorine atoms, R6 is selected from hydrogen and non-aromatic C1-10 saturated hydrocarbon group and R7 is a non-aromatic C1-6 saturated hydrocarbon group. Invention also relates to a pharmaceutical composition having M1 and/or M4 muscarinic receptor agonist activity based on the compound of formula (1).

EFFECT: obtaining novel compounds and a pharmaceutical composition based on them, which can be used in medicine in treating diseases mediated by muscarinic receptors M1 and / or M4, such as Alzheimer's disease, Lewy body dementia, pain.

23 cl, 4 tbl

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RU 2 817 018 C2

Authors

Brown Giles Albert

Teobald Barry John

Tehan Benjamin Gerald

Dates

2024-04-09Published

2019-06-24Filed