Preparation of azetidinotriazole compounds as gamma secretase modulators useful for treatment of Aβ-related diseases.
2014 (English)Patent (Other (popular science, discussion, etc.))Text
The invention relates to azetidinotriazole compds. of formula I and pharmaceutically acceptable salts and pharmaceutical compns. thereof, as well as processes for making these compds. for use in the treatment and/or prevention of Aβ-related diseases. I [wherein A is (un)substituted 5- or 6-membered heteroaryl ring comprising at least one N; R1 is H, C1-3-alkyl, cyano, etc.; R2 is (un)substituted C1-6-alkyl, C3-7-cycloalkyl-C1-3-alkyl, heterocyclyl-C1-3-alkyl, etc.; R3, R5, and R7 are each independently selected from H, (un)substituted C1-3-alkyl, C3-7-cycloalkyl, etc.; R4, R6, R8 are each independently selected from H, F, C1-3-alkyl, etc.; or R3 and R4, or R5 and R6, or R7 and R8, together with the carbon to which they are attached, form (un)substituted 3- to 7-membered satd. ring optionally contg. an O or N] or pharmaceutically acceptable salts thereof are claimed and exemplified. Example compd. II was prepd. from the reaction of III with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline under Buchwald-Hartwig conditions in 26% yield. Nine compds. of I were evaluated for activity on Aβ formation utilizing electrochemiluminescence anal. and HEK cells expressing amyloid precursor protein (data given). [on SciFinder(R)]
Place, publisher, year, edition, pages
Acturum Life Science AB, Swed. . , 2014. no WO2014195321A1
azetidinotriazole compd prepn gamma secretase modulator amyloid beta disease
IdentifiersURN: urn:nbn:se:uu:diva-270226OAI: oai:DiVA.org:uu-270226DiVA: diva2:888174
CAPLUS AN 2014:2053612(Patent)2015-12-222015-12-222015-12-22