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Preparation of imidazolyl-pyrimidine derivatives as GSK3 inhibitors.
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2008 (English)Patent (Other (popular science, discussion, etc.))
Resource type
Text
Abstract [en]

Title compds. I [R1 = sulfamoyl, carbamoyl or -R5-R6 and N linked (un)substituted 4- to 7-membered satd. ring which optionally contains an addnl. N, O or S; R5 = O, C(O), C(O)O, C(O)NH, etc., R6 = (un)substituted alkyl, carbocyclyl or heterocyclyl; at least one of X1, X2, X3 and X4 = N, the other three independently = N or C(R9), wherein R9 = H, halo, CN, OH, NH2, alkyl or alkoxy; provided that not more than two of X1, X2, X3 or X4 = N; R2 = halo or CN; R3 = Me, (un)substituted 3-tetrahydropyranyl or 4-tetrahydropyranyl; R4 = H, halo, CN or (un)substituted alkyl], and their pharmaceutically acceptable salts, are prepd. and disclosed as glycogen synthase kinase 3 (GSK3) inhibitors. Thus, e.g., II was prepd. by amidation of 3,5-dichloro-2-pyridinecarboxylic acid with piperidine followed by coupling reaction with 5-fluoro-4-[2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl]pyrimidin-2-amine, which was prepd. starting from 5-methyl-4-aminoisoxazole and tetrahydro-2H-pyran-4-one in 5 steps. All the exemplar compds. were evaluated for their GSK3 inhibitory activity in GSK3 inhibition assays with typical Ki values ranging from 0.001 to 10,000 nM. For instance, II exhibited a Ki value of 7 nM. As inhibitors of GSK3, I should prove useful in treatment and prevention of GSK3 assocd. diseases including Alzheimer's disease. [on SciFinder(R)]

Place, publisher, year, edition, pages
AstraZeneca AB, Swed. . , 2008. no WO2008002244A2
Keyword [en]
pyrimidine imidazolyl prepn GSK3 inhibitor Alzheimer disease treatment
National Category
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-270235OAI: oai:DiVA.org:uu-270235DiVA: diva2:888179
Note

CAPLUS AN 2008:9934(Patent)

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

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Yngve, Ulrika.

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