abstract |
FIELD: chemistry. n SUBSTANCE: invention relates to new compounds of indole with formula (I) or indole pharmaceutically acceptable salts: where: ring A stands for a benzene or a tiofen ring; R 1 stands for a C 1- . 6 alkyl that may be substituted by one or several groups selected from among -OH, - O-C 1-6 alkyl, an amino group that may be substituted by one or two C 1-6 alkyls; -O-C 1-6 alkyl; a halogen; CN; 5-6-membered cyclic amine; n is equal to 0 - 4 and to 0- 2 if ring A is a benzene or a tiofen ring accordingly; R 2 stands for -H, -C 1-6 alkyl; R 3 stands for H, -C 1-6 alkyl that may be substituted by phenyl, C 3-6 cycloalkyl; R 4 stands for C 1-6 alkyl that may be substituted by one or several groups selected from among -OH, -O- C 1-6 alkyl, an amino group that may be substituted by one or two C 1-6 alkyls and 5-6-membered cyclic amine; C 3 - 6 cycloalkyl, phenyl or-OH; X 1 stands for -CH 2 -, -O-, -S-, -CH(R°)-; X 2 stands for -C(R A )(R B )-, -O-; X 3 stands for -C(R C )(R D )-; m is equal to 1 - 3; R° stands for -H, or R°, together with R 4 , form C 3-6 alkylene; R A , R B , R C and R D are identical or different and stand for -H, C 1-6 alkyl where, in case m is equal to 2 or 3, each R C and R° may be identical or different provided 1- methyl-4a-phenyl-2,3,4,4a,5,9b-hexahydro-1H-indeno [1,2-b] pyridine, 4a-phenyl-2,3,4,4a,5,9b-hexahydro-4aH-indeno [1,2-b] pyridine and 2-(1,2,3,4,5,9b-hexahydro-4aH-indeno [1,2-b] pyridine -4a-yl)-N,N-dimethylethanamine are excluded). n EFFECT: compounds possess antagonistic activity regarding NMDA receptor which enables their usage in pharmaceutical compositions for treatment of Alzheimer disease, vascular dementia, Parkinson disease, chronic depression, attention deficit hyperactivity disorder, migraines etc. n 18 cl, 40 tbl, 84 ex |