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    • 8. 发明授权
    • Non-peptide bombesin receptor antagonists
    • 非肽铃蟾肽受体拮抗剂
    • US06194437B1
    • 2001-02-27
    • US09230933
    • 1999-02-03
    • David Christopher HorwellMartyn Clive Pritchard
    • David Christopher HorwellMartyn Clive Pritchard
    • C07D40112
    • C07D213/40C07D209/20C07D213/56C07D213/89C07D401/12C07D403/12C07D405/12C07D417/12
    • The compounds of the instant invention are novel compounds of Formula I or a pharmaceutically acceptable salt thereof wherein Ar is phenyl or pyridyl unsubstituted or substituted. Ar1 can be independently selected from Ar and can also include pyridyl-N-oxide, indolyl, imidazole, and pyridyl; R3 can be independently selected from Ar or is hydrogen, hydroxy, NMe2, N-methyl-pyrrole, imidazole, tetrazole, thiazole (a), (b), (c), or (d), wherein Ar2 is phenyl or pyridyl. The instant compounds antagonize the bombesin receptors in mammals and are therefore effective in treating and/or preventing depression, psychoses, seasonal affective disorders, cancer, feeding disorders, gastrointestinal disorders, inflammatory bowel disease, sleep disorders, and memory impairment.
    • 本发明的化合物是式I的新化合物或其药学上可接受的盐,其中Ar是未取代或取代的苯基或吡啶基。 Ar 1可以独立地选自Ar,也可以包括吡啶基-N-氧化物,吲哚基,咪唑和吡啶基; R3可以独立地选自Ar或氢,羟基,NMe2,N-甲基 - 吡咯,咪唑,四唑,噻唑(a),(b),(c)或(d),其中Ar2是苯基或吡啶基。 本发明化合物拮抗哺乳动物中的铃蟾肽受体,因此有效地治疗和/或预防抑郁症,精神病,季节性情感障碍,癌症,进食障碍,胃肠道疾病,炎症性肠病,睡眠障碍和记忆障碍。