首页> 外国专利> 5-(3-AMINOPHENYL)-5-ALKYL-5,6-DIHYDRO-2H-1,4OXAZIN-3-AMINE DERIVATIVES

5-(3-AMINOPHENYL)-5-ALKYL-5,6-DIHYDRO-2H-1,4OXAZIN-3-AMINE DERIVATIVES

机译:5-(3-氨基苯基)-5-烷基-5,6-二氢-2H- [1,4]恶嗪-3-胺衍生物

摘要

The present invention relates to novel 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives of formula (I)where the meanings of derivatives Rand Ar are defined in the claims, as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The present invention also relates 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, cerebral amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
机译:本发明涉及式(I)的新颖的5-(3-氨基苯基)-5-烷基-5,6-二氢-2H- [1,4]恶嗪-3-胺衍生物,其中衍生物Rand Ar的含义是在权利要求书中定义为β-分泌酶的抑制剂,也称为β-位淀粉样蛋白裂解酶,BACE,BACE1,Asp2或memapsin2。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,路易小体痴呆,脑淀粉样血管病,多发性梗塞性痴呆,唐氏综合症,中风相关性痴呆,帕金森氏病相关性痴呆和β-淀粉样蛋白相关性痴呆。

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