| abstract |
Disclosed are compounds of formula 1, salts and stereoisomers thereof, and methods for their preparation. Specific examples of compounds of formula 1 include: N-{ (3S,5S)-1-{ [(3S,4R)-1-tert-butyl-4-(4-chlorophenyl)pyrrolidin-3-yl]carbonyl} -5-[(4-methylpiperazin-1-yl)carbonyl]pyrrolidin-3-yl} -N-(4,4-dimethylcyclohexyl)acetamide, N-{ (3S,5S)-1-{ [(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl} -5-[(4-methylpiperazin-1-yl)carbonyl]pyrrolidin-3-yl} -N-(4,4-dimethylcyclohexyl)-3-hydroxy-2,2-dimethylpropanamide, (2S)-N-{ (3S,5S)-1-{ [(3S,4R)-1-tert-butyl-4-(4-chlorophenyl)pyrrolidin-3-yl]carbonyl} -5-[(4-methylpiperazin-1-yl)carbonyl]pyrrolidin-3-yl} -N-(4,4-difluorocyclohexyl)tetrahydrofuran-2-carboxamide, and (2S)-N-{ (3S,5S)-1-{ [(3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl]carbonyl} -5-[(4-isopropylpiperazin-1-yl)carbonyl]pyrrolidin-3-yl} -N(4,4-dimethylcyclohexyl)tetrahydrofuran-2-carboxamide. Compounds of formula 1 have good agonistic activity to melanocortin receptors and are useful for treating or preventing obesity, diabetes, inflammation and erectile dysfunction. |