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GSK3 Nitrogen-Containing Heteroaryl Derivatives and Their Use as GSK3 Inhibitors

机译:GSK3含氮杂芳基衍生物及其作为GSK3抑制剂的用途

摘要

The present invention provides a novel compound of formula (I) or a pharmaceutically acceptable salt thereof having GSK3? Inhibitory activity. [Chemical Formula 1] In Formula 1, X is carbon (C) or nitrogen (N); Y is carbon (C) or oxygen (O); R 1 is hydrogen, aryl, -CO-aryl or heteroaryl, wherein said aryl or heteroaryl may be unsubstituted or substituted; R 2 is -CO-NH- (CH 2) n -CO-NH-, -CO-O- (CH 2) n -, -CH = CH- (CH 2) m -CO-NH- or - (CH 2 ) n- CO-NH-, wherein n is an integer from 1 to 3 and m is an integer from 0 to 3; R 3 is C 1-6 alkyl, - (CH 2 ) n -aryl, - (CH 2 ) n -heteroaryl or - (CH 2 ) n -heterocyclyl wherein the aryl, heteroaryl or heterocyclyl May be unsubstituted or substituted. The compound of Formula 1 is useful for preventing or treating a disease associated with GSK3 [beta], i.e., a proliferative disease, a neurodegenerative or neurodegenerative disease, an inflammatory autoimmune disease, a cardiovascular disease, an endocrine disease, and a viral infectious disease.
机译:本发明提供了具有GSK3α的新型式(Ⅰ)化合物或其可药用盐。抑制活性。 [化学式1]式1中,X为碳(C)或氮(N); Y为碳(C)或氧(O); R 1 是氢,芳基,-CO-芳基或杂芳基,其中所述芳基或杂芳基可以是未取代的或取代的; R 2 -CO-NH-(CH 2)n -CO-NH-,-CO-O-(CH 2)n-,-CH = CH- (CH 2)m -CO-NH-或-(CH 2 n- CO-NH-,其中n是1到3的整数,m是一个0到3的整数; R 3 是C 1-6 烷基,-(CH 2 n -芳基,-(CH < Sub> 2 n -杂芳基或-(CH 2 n -杂环基其中芳基,杂芳基或杂环基可以是未取代或取代的。式1的化合物可用于预防或治疗与GSK3β有关的疾病,即增生性疾病,神经变性或神经变性疾病,炎性自身免疫疾病,心血管疾病,内分泌疾病和病毒感染性疾病。 。

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