NOVEL COMPOUNDS Russian patent published in 2020 - IPC C07D207/09 C07D401/12 C07D403/12 C07D403/14 C07D413/12 C07D417/12 C07D417/14 C07D471/04 C07D487/04 A61K31/4025 A61K31/407 A61P25/28 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, having inhibitory activity on ubiquitin-C-terminal hydrolase 30. In formula (I), each of R^1a, R^1b, R^1c, R^1d, R^1e and R^1g is hydrogen; R^1f is hydrogen, or R^1f together with R² forms a pyrrolidine ring substituted with an oxo group; R² is hydrogen or C₁-C₆alkyl, or R² together with R^1f forms a pyrrolidine ring substituted with an oxo group; X is C(R³)(R⁴), where each of R³ and R⁴ independently represents hydrogen, cyano or C₁-C₆alkyl; L is a covalent bond, -SO₂-, -C(O)-, -CONR⁵-, -C(O)-C₁-C₆alkylene, -C(O)-C₂-C₆alkenylene or -C₂-C₆alkenylene; A is substituted 5–6 membered monocyclic heteroaryl or phenyl ring or substituted 8–12-membered bicyclic heteroaryl or naphthyl ring, wherein said heteroaryl rings contain from 1 to 4 heteroatoms independently selected from nitrogen, oxygen and sulfur; R⁵ is hydrogen, where ring A is substituted with one group -Q¹-(R⁶)_n, where n is 1; and additionally optionally substituted with one, two or three groups -Q¹-(R⁶)_n, where n equals 0; n is 0 or 1; when n is equal to 0, Q¹ is halogen, cyano, oxo, -CONR⁷R⁸, -C₁-C₆alkyl or -C₁-C₆alkoxy, wherein said C₁-C₆alkyl is optionally substituted with one or more halogens; when n is 1, Q¹ is a covalent bond, an oxygen atom, -C₁-C₆alkylene or -SO₂NR⁷-; R⁶ denotes a phenyl ring, 3–6 membered cycloalkyl ring, 5–6 membered heterocyclyl ring containing one nitrogen atom, or 5–6 membered heteroaryl ring containing 1 or 2 heteroatoms independently selected from nitrogen, oxygen and sulfur; each of R⁷ and R⁸ independently represents hydrogen or C₁-C₆alkyl, where R⁶ is optionally substituted with one or more substitutes, each of which is independently selected from halogen, cyano, -C₁-C₆alkyl and -C₁-C₆alkoxy, wherein said C₁-C₆alkyl is optionally substituted with one or more halogens. Invention also relates to compounds selected from a group consisting of 3-((quinolin-2-ylamino)methyl)pyrrolidine-1-carbonitrile, 3-(((6-fluorobenzo[d]thiazol-2-yl)amino)methyl)pyrrolidine-1-carbonitrile, 3-((isoquinolin-1-ylamino)methyl)pyrrolidine-1-carbonitrile, etc., and to a pharmaceutical composition containing said compounds together with one or more pharmaceutically acceptable excipients and having the activity of inhibitors of ubiquitin-C-terminal hydrolase.

EFFECT: novel compounds are disclosed.

19 cl, 1 dwg, 4 tbl, 54 ex