Preparation of imidazolylpyrimidine derivatives for treatment of glycogen synthase kinase 3 related disorders such as Alzheimer's disease.
2010 (English)Patent (Other (popular science, discussion, etc.))Text
Title compds. I [R1 = H or F; R2 and R3 independently = H or Me], and their pharmaceutically acceptable salts, are prepd. and disclosed as agents for treatment of glycogen synthase kinase 3 (GSK3) related disorders such as Alzheimer's disease. Thus, e.g., II.HCl was prepd. by reductive amination of 4-bromo-3-fluorobenzaldehyde with (S)-3-methylmorpholine followed by amination with 2-amino-5-fluoro-4-(2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl)pyrimidine. Select I were evaluated for GSK3β inhibitory activity, and e.g., II·HCl demonstrated a Ki value of 30 nM. [on SciFinder(R)]
Place, publisher, year, edition, pages
AstraZeneca AB, Swed. . , 2010. no WO2010120237A1
pyrimidine imidazolyl deriv prepn GSK3 inhibitor treatment Alzheimer disease
IdentifiersURN: urn:nbn:se:uu:diva-270232OAI: oai:DiVA.org:uu-270232DiVA: diva2:888192
CAPLUS AN 2010:1315131(Patent)2015-12-222015-12-222015-12-22