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

Title compds. I [A = (un)substituted aryl or heteroaryl; Q = halo; R1 = C(O)NR6R7; R2 and R4 independently = H, halo, CN, NO2, alkyl, or haloalkyl; R3 and R5 independently = H, halo, alkyl, or haloalkyl; R6 and R7 = 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;], 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 N-methylpiperazine, and coupling with 4-methoxyphenyl boronic acid. I were evaluated in GSK3β scintillation proximity assays, e.g., II•HCl demonstrated an Ki value of 97 nM. [on SciFinder(R)]

Place, publisher, year, edition, pages
AstraZeneca AB, Swed. . , 2008. no WO2008121064A1
Keyword [en]
imidazopyridine aryl deriv prepn GSK3 modulator
National Category
Medicinal Chemistry
URN: urn:nbn:se:uu:diva-270234OAI: oai:DiVA.org:uu-270234DiVA: diva2:888180

CAPLUS AN 2008:1210769(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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