embedded image wherein:;R1, R2 and R3 are members independently selected from the group consisting of alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryloxyalkyl, substituted aryloxyalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, heterocycles, substituted heterocycles, heterocyclicalkyl and substituted heterocyclicalkyl; and R5 and R6 are independently selected from the group consisting of hydrogen, halogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryloxyalkyl and substituted aryloxyalkyl; or R5 and R6 and the carbons to which they are bound join to form an optionally substituted carbocyclic or heterocyclic fused ring system having a total of 9- or 10-ring atoms within the fused ring system."/> Methods for treating neurodegenerative disorders using aspartyl protease inhibitors
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Methods for treating neurodegenerative disorders using aspartyl protease inhibitors

机译:使用天冬氨酰蛋白酶抑制剂治疗神经退行性疾病的方法

摘要

The present invention relates to () non-peptide aspartyl protease inhibitors; (ii) methods for modulating the processing of an amyloid precursor protein (APP); (iii) methods for modulating the processing of a tau protein (τ-protein); and (iv) methods for treating neurodegenerative diseases. For instance, in one embodiment, the present invention provides a method for modulating the processing of an amyloid precursor protein (APP), the method comprising contacting a composition containing the APP with an aspartyl protease inhibitor having the formula:; embedded image wherein:;R1, R2 and R3 are members independently selected from the group consisting of alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryloxyalkyl, substituted aryloxyalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, heterocycles, substituted heterocycles, heterocyclicalkyl and substituted heterocyclicalkyl; and R5 and R6 are independently selected from the group consisting of hydrogen, halogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryloxyalkyl and substituted aryloxyalkyl; or R5 and R6 and the carbons to which they are bound join to form an optionally substituted carbocyclic or heterocyclic fused ring system having a total of 9- or 10-ring atoms within the fused ring system.
机译:本发明涉及()非肽天冬氨酰蛋白酶抑制剂; (ii)调节淀粉样前体蛋白(APP)加工的方法; (iii)调节tau蛋白(τ蛋白)加工的方法; (iv)治疗神经退行性疾病的方法。例如,在一个实施方案中,本发明提供了一种调节淀粉样前体蛋白(APP)的加工的方法,该方法包括使含有APP的组合物与下式的天冬氨酰蛋白酶抑制剂接触: “嵌入式图像” 其中:; R 1, R 2 和R 3 是独立地选自烷基,取代烷基,芳基,取代芳基,芳基烷基的成员,取代的芳基烷基,芳氧基烷基,取代的芳氧基烷基,杂芳基,取代的杂芳基,杂芳基烷基,取代的杂芳基烷基,杂环,取代的杂环,杂环烷基和取代的杂环烷基;和R 5 和R 6 独立地选自氢,卤素,烷基,取代的烷基,芳基,取代的芳基,芳基烷基,取代的芳基烷基,芳氧基烷基和芳氧基烷基;或R 5 和R 6 以及与它们键合的碳连接形成任选取代的碳环或杂环稠合环系统,该环系统总共具有9个或10个环稠环系统中的原子。

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