GALATSIS Paul (US),ГАЛАТСИС Пол (US),HENDERSON Jaclyn Louise (US),ХЕНДЕРСОН Жаклин Луиз (US),KORMOS Bethany Lyn (US),КОРМОС Бетани Лин (US),KURUMBAIL Ravi G. (US),КУРУМБАИЛ Рави Дж. (US),REESE Matthew
申请号：
RU2018108854
公开号：
RU0002722149C1
申请日:
2016.09.07
申请国别(地区):
RU
年份:
2020
代理人:
摘要：
FIELD: organic chemistry.SUBSTANCE: invention relates to a heterocyclic compound of formula (I) or a pharmaceutically acceptable salt thereof, where X is CR7 or N； Z is CR3； R1 is selected from a group consisting of cyano and 5–9 membered heteroaryl, which contains 1–5 heteroatoms independently selected from N, O and S； where 5–9 membered heteroaryl is optionally substituted with 1–2 R8 groups； each of R1a and R1b independently represents hydrogen or halogen； or R1a and R1b together with the carbon atom to which they are bonded are C(O)； R2 is C1-C6 alkyl, C3-C7 cycloalkyl or 5–6-member heterocycloalkyl, which contains 1–3 heteroatoms independently selected from NR and O； where each of C3-C7 cycloalkyl and 5–6-member heterocycloalkyl is optionally substituted with 1–2 R9 groups； and where C1-C6 alkyl is optionally substituted with 1–2 R10 groups； R represents C1-C6 alkyl； R3 is selected from a group consisting of hydrogen, deutero, amino, halogen, cyano, C1-C6 alkyl and C1-C6 alkoxy； where each of C1-C6 alkyl and C1-C 6 alkoxy is optionally substituted with 1–3 halogen groups； R4, R5 and R7 independently represent hydrogen or deutero； R6 denotes hydrogen, deutero, halogen or amino； R8 in each case is independently selected from a group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy and C3-C6 cycloalkyl； where C1-C6 alkyl is optionally substituted with 1–3 halogen, hydroxy or C1-C3 alkoxy groups； R9 at each occurrence is independently selected from the group consisting of halogen, hydroxy, C1-C 6 alkyl and C1-C6 alkoxy, where C1-C6 alkyl and C1-C6 alkoxy are optionally substituted with one to three halogen or cyano groups； and R10 in each case is halogen. Invention also relates to specific compounds, a pharmaceutical composition based on the compound of formula (I) and a method of treating Crohn's disease, Parkinson's disease, dementia with Levy bodies, leprosy, Alzheimer's disease and taupathy..EFFECT: obtaining novel heterocyclic compounds having inhibitory activ
