5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
    9.
    发明申请
    5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 有权
    作为β-分泌酶抑制剂(BACE)的5,6-DIHYDRO-IMIDAZO [1,2-a]吡嗪-8-胺衍生物

    公开(公告)号:US20130274266A1

    公开(公告)日:2013-10-17

    申请号:US13995523

    申请日:2011-12-21

    IPC分类号: C07D487/04

    CPC分类号: C07D487/04

    摘要: The present invention relates to novel 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebrovascular amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.

    摘要翻译: 本发明涉及作为β-分泌酶抑制剂的新的5,6-二氢 - 咪唑并[1,2-a]吡嗪-8-基胺衍生物,也称为β位淀粉样蛋白切割酶,BACE,BACE1,Asp2或 memapsin2。 本发明还涉及包含这些化合物的药物组合物,制备这些化合物和组合物的方法,以及这些化合物和组合物用于预防和治疗其中涉及β-分泌酶的疾病如阿尔茨海默病的用途(例如, AD),轻度认知障碍,衰老,痴呆,路易体痴呆,脑血管淀粉样血管病,多发性梗死性痴呆,唐氏综合征,与中风相关的痴呆,与帕金森病相关的痴呆或与β-淀粉样蛋白相关的痴呆。