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Preparation of 1-(4...
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.
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Aahlin, Kristofer (author)
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Arvidsson, Per I. (author)
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Huerta, Fernando (author)
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Yngve, Ulrika. (author)
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- AstraZeneca AB, Swed. ., 2011
- English.
- Related links:
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https://urn.kb.se/re...
Abstract
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- 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)]
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Keyword
- aminooxazolopyridinylpyrazinylbenzoylpiperazine prepn glycogen sythase kinase 3 inhibitor diabetes
- cancer cognitive disorder aminooxazolopyridinylpyrazinylbenzoylpiperazine prepn GSK3 inhibitor
Publication and Content Type
- pop (subject category)
- pat (subject category)
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