| 摘要 |
Disclosed are tricyclic quinoline and quinoxaline derivatives of formula (I) as vabicaserin analogues wherein, G is (CR3aR3b)n; X is NR6 or CR7R8; and wherein the remaining substituents are as defined herein. Representative compounds include 1,2,3,4-tetrahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1’-cyclopent[2]en]-6(7H)-one, 8-methyl-8-phenyl-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-6(2H)-one, 8,8-dimethyl-3,4,7,8-tetrahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-6(2H)-one, 12a-methyl-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline, (R)-5,6,7,9,9a,10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline, 9-chloro-8,8-dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinoline, 1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1’-cyclohexane], 9-fluoro-1-methyl-1,2,3,4,6,7-hexahydrospiro[[1,4]diazepino[6,7,1-ij]quinoline-8,1’-cyclobutane], 2,3,5,6,7,8-Hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline, 1-Cyclobutyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline, 1-fluoro-5,6,7,9,9a,10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline, 8-Methyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-8-ol, 2,8-dimethyl-2,3,4,6,7,8-hexahydro-1H-[1,4]diazepino[6,7,1-ij]quinolin-8-ol and 1-propyl-2,3,5,6,7,8-hexahydro-1H-[1,4]diazepino[1,7,6-de]quinoxaline. Also disclosed is a pharmaceutical composition comprising a therapeutically effective amount of at least one compound as defined above, or an N-oxide, a tautomeric form, a stereoisomer or a pharmaceutically acceptable salt thereof, or comprising at least one compound as defined above wherein at least one of the atoms has been replaced by its stable, non-radioactive isotope, in combination with at least one pharmaceutically acceptable carrier and/or auxiliary substance, for the treatment of disorders which respond to the modulation of the 5-HT2c receptor, including disorders such as schizophrenia, depression, bipolar disorders, diabetes, obesity and substance use disorders. |
