uu.seUppsala University Publications
Change search
ReferencesLink to record
Permanent link

Direct link
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
Abstract [en]

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
Keyword [en]
aminooxazolopyridinylpyrazinylbenzoylpiperazine prepn glycogen sythase kinase 3 inhibitor diabetes, cancer cognitive disorder aminooxazolopyridinylpyrazinylbenzoylpiperazine prepn GSK3 inhibitor
National Category
Medicinal Chemistry
URN: urn:nbn:se:uu:diva-270231OAI: oai:DiVA.org:uu-270231DiVA: diva2:888178

CAPLUS AN 2011:623456(Patent)

Available from: 2015-12-22 Created: 2015-12-22 Last updated: 2015-12-22

Open Access in DiVA

No full text

Search in DiVA

By author/editor
Yngve, Ulrika.
Medicinal Chemistry

Search outside of DiVA

GoogleGoogle Scholar
The number of downloads is the sum of all downloads of full texts. It may include eg previous versions that are now no longer available

Total: 483 hits
ReferencesLink to record
Permanent link

Direct link