| 摘要 |
A compound of Formula I or a pharmaceutically acceptable salt thereof wherein, Ar is phenyl or pyridyl unsubstituted or substituted by from 1 to 3 substituents selected from alkyl, halogen, alkoxy, nitro, amino, NH2CH2, cyano, CF3, NHCONH2, and CO2R1, R1 is hydrogen or straight, branched, or cyclic alkyl of from 1 to 7 carbon atoms, R8 is hydrogen or forms a ring with R1 of from 3 to 7 carbon atoms, R2 is a ring of from 5 to 7 carbon atoms said ring optionally including 1 or 2 oxygen or nitrogen atoms, or R2 is a ring of from 3 to 7 carbon atoms with R9, R9 is hydrogen or forms a ring of from 3 to 7 carbon atoms with R2, Ar1 can be independently selected from phenyl or pyridyl substituted by from 1 to 3 substituents selected from alkyl, halogen, alkoxy, nitro, amino, NH2CH2, cyano, CF3, NHCONH2 and CO2R1; and Ar1 and can also represent pyridyl-N-oxide, indolyl, pyridyl, and imidazole, R4, R5, R6 and R7 are each independently selected from hydrogen and methyl, R3 can be independently selected from Ar or is hydrogen, hydroxy, NMe2, N-methyl-pyrrole, or a group selected from formulae II, III, IV or V wherein Ar2 is phenyl or pyridyl, with the proviso that Ar and R3 cannot both be directly attached to the nitrogen atoms bearing R4 and R6, respectively, and with the proviso that the linkers [(C)0-1R1R8]-(CH2)0-1 and [(CH2)0-3]-[(C)0-1R2R9]-[(CH2)0-2] are not (CH2)1-2 or (CH2)1-6 respectively. These compounds are capable of antagonizing the effects of neuromedin B (NMB) and/or gastrin releasing peptide (GRP) at bombesin receptors and are useful in the treatment of a variety of disorders including depression, psychoses, seasonal affective disorders, cancer, feeding disorders, gastrointestinal disorders including colitis, Crohn's disease and inflammatory bowel disease, sleeping disorders, and memory impairment.
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