Bridged tricyclic analogs of 2-(carboxycyclopropyl)glycine as inhibitors of glutamate transport
    10.
    发明授权
    Bridged tricyclic analogs of 2-(carboxycyclopropyl)glycine as inhibitors of glutamate transport 失效
    2-(羧基环丙基)甘氨酸的桥连三环类似物作为谷氨酸转运抑制剂

    公开(公告)号:US06750364B2

    公开(公告)日:2004-06-15

    申请号:US10185489

    申请日:2002-06-27

    IPC分类号: C07D31178

    摘要: This invention provides compounds of the formula: wherein X is (CH2)n, O, S, SO, SO2 or CR1R2; n is 1 or 2; R1 and R2 are H, halogen, hydroxy, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or R1 and R2, taken together form cycloalkyl of 3 to 6 carbon atoms, an alkylidene of up to 6 carbon atoms or a carbonyl; R3, R4 and R5 are H or alkyl of 1 to 6 carbon atoms; Z is H, alkyl of 1 to 6 carbon atoms, alkanoyl of 1 to 6 carbon atoms or alkoxycarbonyl of 2 to 7 carbon atoms; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods for their use in treating or preventing characterized by glutamate hypofunction, including schizophrenia, schizoaffective disorder and schizophreniform disorder, and for the treatment of cognitive deficits due to aging, stroke, Alzheimer's disease or other neurodegenerative diseases.

    摘要翻译: 本发明提供下式的化合物:其中X是(CH 2)n,O,S,SO,SO 2或CR 1 R 2; n为1或2; R 1和R 2是H,卤素,羟基,1至6个碳原子的烷基,1至6个碳原子的烷氧基或R 1和R 2一起形成3至 6个碳原子,最多6个碳原子的亚烷基或羰基; R 3,R 4和R 5是H或1至6个碳原子的烷基; Z是H,1至6个碳原子的烷基,1至6个碳原子的烷酰基或2至7个碳原子的烷氧基羰基; 或其药学上可接受的盐,以及用于治疗或预防特征在于谷氨酸功能低下的药物组合物和方法,包括精神分裂症,分裂情感障碍和精神分裂症样疾病,以及用于治疗由于老化,中风,阿尔茨海默病引起的认知缺陷 或其他神经变性疾病。