MUSCARINIC RECEPTOR AGONISTS Russian patent published in 2020 - IPC C07D401/08 C07D401/14 C07D405/14 C07D413/14 A61K31/451 A61K31/4523 A61P25/14 A61P25/18 A61P25/28 A61P25/30 A61P29/00 

FIELD: pharmaceuticals.

SUBSTANCE: present invention refers to compounds of formula (1a) or its pharmaceutically acceptable salt, where q equals 1; r is equal to 1 or 2; s equals 0 or 1, wherein sum of r and s equals 1 or 2; Q is CR¹R²NR⁵R⁶, NR⁵R⁶, OR⁷, SR⁷; R¹ is selected from hydrogen or C_1-6 alkyl group; R² is selected from hydrogen or C_1-6 alkyl group; R³ denotes hydrogen; R⁴ represents hydrogen or C_1-6 alkyl group; R⁵ is selected from OR⁷; C_1-6 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and in which one or two but not all carbon atoms of the hydrocarbon group can be optionally replaced with a heteroatom selected from O, N and S and their oxidised forms; and a group W or CH₂W, where W is 5- or 6-member aromatic ring containing 0, 1, 2 or 3 heteroatoms selected from O and N; R⁶ is selected from COR⁷; COOR⁷; CH₂COR⁷; CH₂COOR⁷; C_1-6 non-aromatic hydrocarbon group, which is optionally substituted with one to six fluorine atoms and in which one or two but not all carbon atoms of the hydrocarbon group can optionally be replaced with heteroatom O; or C_3-6 cycloalkyl group; and R⁷ is selected from hydrogen, C_1-6 alkyl group, which is optionally substituted with one to six fluorine atoms and in which one carbon atom can optionally be replaced with heteroatom N; and when Q is group OR⁷ or SR⁷, R⁷ is selected from a group W or (C_1-4 alkyl)W, where W is phenyl; and the dashed line, which shows an optional second carbon-carbon bond, is absent. In addition, specific compounds, pharmaceutical compositions containing compounds of formula (1a) or specific compounds are disclosed.

(1a).

EFFECT: there are prepared and described new compounds which are muscarinic receptor and/or M₄ agonists and are suitable for treating diseases mediated by muscarinic receptors M₁/M₄.

22 cl, 1 dwg, 4 tbl