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Preparation of aryl...
Preparation of arylimidazopyridine derivatives for use as GSK3 modulators.
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Arvidsson, Per (författare)
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Burrows, Jeremy (författare)
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Soederman, Peter (författare)
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visa fler...
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Yngve, Ulrika. (författare)
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visa färre...
- AstraZeneca AB, Swed. ., 2008
- Engelska.
- Relaterad länk:
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https://urn.kb.se/re...
Abstract
Ämnesord
Stäng
- 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)]
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Nyckelord
- imidazopyridine aryl deriv prepn GSK3 modulator
Publikations- och innehållstyp
- pop (ämneskategori)
- pat (ämneskategori)