首页> 外国专利> 4-amino-6-phenyl-6,7-dihydro1,2,3triazolo1,5-apyrazine derivatives as inhibitors of beta-secretase (BACE)

4-amino-6-phenyl-6,7-dihydro1,2,3triazolo1,5-apyrazine derivatives as inhibitors of beta-secretase (BACE)

机译:4-氨基-6-苯基-6,7-二氢[1,2,3]三唑并[1,5-a]吡嗪衍生物作为β-分泌酶(BACE)的抑制剂

摘要

The present invention relates to novel 6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazin- 6-yl derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, in particular BACE1 and/or BACE2 (wherein BACE1, is also known as Asp2, or memapsin2 and BACE2 is also known as Asp1, Memapsin 1 or DRAP). 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, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, dementia of the Alzheimer's type, dementia associated with beta-amyloid, age- related macular degeneration, type 2 diabetes and other metabolic disorders.
机译:本发明涉及新颖的6,7-二氢[1,2,3]三唑并[1,5-a]吡嗪-6-基衍生物作为β-分泌酶的抑制剂,也称为β-位淀粉样蛋白裂解酶,BACE ,特别是BACE1和/或BACE2(其中BACE1也称为Asp2或memapsin2,BACE2也称为Asp1,Memapsin 1或DRAP)。本发明还涉及包含此类化合物的药物组合物,制备此类化合物和组合物的方法以及此类化​​合物和组合物在预防和治疗涉及β-分泌酶的疾病中的用途,例如阿尔茨海默氏病( AD),轻度认知障碍,衰老,痴呆,路易体痴呆,唐氏综合症,与中风相关的痴呆,与帕金森氏病相关的痴呆,阿尔茨海默氏病类型的痴呆,与β-淀粉样蛋白相关的痴呆,年龄相关性黄斑变性,类型2糖尿病和其他代谢性疾病。

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