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Preparation of imidazopyridinecarboxamide derivatives for use as GSK3 modulators.
2008 (English)Patent (Other (popular science, discussion, etc.))Text
Abstract [en]

Title compds. I [Q = halo; R1 = CH2NR3R4; each R2 independently = H or alkyl; R3 and R4 = together with the atoms to which they are attached form an (un)substituted heterocyclic ring contg. one or more heteroatoms selected from N, O, or S; R6 = H or alkyl; R7 = H, (un)substituted alkyl, alkylaryl, aryl, or heteroaryl], and their pharmaceutically acceptable salts, are prepd. and disclosed as glycogen synthase kinase-3 (GSK3) modulators. Thus, e.g., II•HCl was prepd. by cyclocondensation of 5-bromopyridine-2,3-diamine with terephthalic monomethyl ester followed by chlorination, iodination, sapon., amidation with morpholine, redn., and coupling with carbon monoxide and 3-methoxy-1-propanamine. I were evaluated in GSK3β scintillation proximity assays, e.g., II•HCl demonstrated an Ki value of 390 nM. [on SciFinder(R)]

Place, publisher, year, edition, pages
AstraZeneca AB, Swed. . , 2008. no WO2008121063A1
Keyword [en]
imidazopyridinecarboxamide deriv prepn GSK3 modulator
National Category
Medicinal Chemistry
URN: urn:nbn:se:uu:diva-270233OAI: oai:DiVA.org:uu-270233DiVA: diva2:888181

CAPLUS AN 2008:1210930(Patent)

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

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Yngve, Ulrika.
Medicinal Chemistry

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