KEMP Mark Ien (GB),КЕМП Марк Иэн (GB),STOKLI Martin Li (GB),СТОКЛИ Мартин Ли (GB),MEDIN Endryu (GB),МЭДИН Эндрю (GB)
申请号：
RU2018123779
公开号：
RU0002734256C2
申请日:
2016.12.16
申请国别(地区):
RU
年份:
2020
代理人:
摘要：
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 R1a, R1b, R1c, R1d, R1e and R1g is hydrogen； R1f is hydrogen, or R1f together with R2 forms a pyrrolidine ring substituted with an oxo group； R2 is hydrogen or C1-C6alkyl, or R2 together with R1f 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)
