Preparation of 1-(4-(5-amino-6-(oxazolo[4,5-c]pyridin-2-yl)pyrazin-2-yl)benzoyl)piperazine derivatives as glycogen synthase kinase 3 inhibitors.
2011 (English)Patent (Other (popular science, discussion, etc.))Text
Title compds. I [R1 = H or Me], and their pharmaceutically acceptable salts, are prepd. and disclosed as glycogen synthase kinase 3 (GSK3) inhibitors. Thus, e.g., II was prepd. by cyclization of 3-amino-N-(4-hydroxypyridin-3-yl)pyrazine-2-carboxamide (prepn. given) to get intermediate 3-(oxazolo[4,5-c]pyridin-2-yl)pyrazin-2-amine, which underwent bromination followed by Suzuki reaction with (4-methylpiperazin-1-yl)(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanone. Compds. of the invention were tested for their selective inhibitory activity of GSK3β, e.g., II exhibited Ki value of 2.3 nM. The invention compds. are useful for the treatment of cognitive disorders, diabetes, cancer, etc. [on SciFinder(R)]
Place, publisher, year, edition, pages
AstraZeneca AB, Swed. . , 2011. no WO2011059388A1
aminooxazolopyridinylpyrazinylbenzoylpiperazine prepn glycogen sythase kinase 3 inhibitor diabetes, cancer cognitive disorder aminooxazolopyridinylpyrazinylbenzoylpiperazine prepn GSK3 inhibitor
IdentifiersURN: urn:nbn:se:uu:diva-270231OAI: oai:DiVA.org:uu-270231DiVA: diva2:888178
CAPLUS AN 2011:623456(Patent)2015-12-222015-12-222015-12-22