Structure Activity Optimization of 6H-Pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines As Jak1 Kinase Inhibitors

Bioorganic & medicinal chemistry letters（2015）

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摘要

Previous work investigating tricyclic pyrrolopyrazines as kinase cores led to the discovery that 1-cyclohexyl-6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazine (12) had Jak inhibitory activity. Herein we describe our initial efforts to develop orally bioavailable analogs of 12 with improved selectivity of Jak1 over Jak2.

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关键词

Tricyclic pyrrolopyrazines,6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines,Jak inhibitors,Jak selectivity

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