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Preparation of pyrimidinylamine compounds as gamma secretase modulators useful for treatment of Aβ-related diseases.
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2014 (English)Patent (Other (popular science, discussion, etc.))Text
Abstract [en]

The invention relates to pyrimidinylamine 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 and R3 are each independently selected from C1-3-alkyl and fluoro-C1-3-alkyl; or R2 and R3 together with the carbon to which they are attached form a 3- to 6-membered satd. carbocyclic ring, optionally substituted with one or more fluoro substituents; R4 is C1-3-alkyl, fluoro-C1-3-alkyl, or C3-6-cycloalkyl-C1-3-alkyl; R5 is H, C1-3-alkyl, fluoro, etc.; R6 is, for example, CH3NH-, CNCH2-, or MeO-] 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 77% yield. Fifty-two 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 WO2014195323A1
Keyword [en]
pyrimidinylamine compd prepn gamma secretase modulator amyloid beta disease
National Category
Medicinal Chemistry
URN: urn:nbn:se:uu:diva-270225OAI: oai:DiVA.org:uu-270225DiVA: diva2:888176

CAPLUS AN 2014:2054594(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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