申请人:Merck Sharp & Dohme Ltd.
公开号:US06297235B1
公开(公告)日:2001-10-02
A compound of formula I, or a salt or prodrug thereof:
wherein:
Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted;
R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or
R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and
R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alky, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.
一种具有
化学式I的化合物,或其盐或前药:其中:Z代表C1-6烷基,C3-7环烷基,C4-7环烯基,芳基,C3-7杂环烷基,杂芳基或二(C1-6)烷基
氨基,其中任何这些基团均可选择性地被取代;R1代表选择自
噁唑,
噻唑,
异噁唑,异
硫唑,
咪唑,
吡唑,噁二唑,
噻二唑,三唑和
四唑中的一种选择性地取代的五元杂芳环;或R1代表选择自
吡啶,
嘧啶和
吡啶并[1,2-a]
吡嗪中的一种选择性地取代的六元杂芳环;以及R2代表
氰基(C1-6)烷基,羟基(C1-6)烷基,C3-7环烷基(C1-6)烷基,
丙炔基,C3-7杂环烷基羰基(C1-6)烷基,芳基(C1-6)烷基或杂芳基(C1-6)烷基,其中任何这些基团均可选择性地被取代;其用于治疗焦虑和包含它的制药组合物;还公开了一类在增强认知方面有用的化合物,例如阿尔茨海默病。