C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 333/34 (2006.01) A61K 31/381 (2006.01) A61P 25/28 (2006.01) C07D 231/18 (2006.01) C07D 333/62 (2006.01)
Patent
CA 2517155
Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
L'invention porte sur des composés de formule (I) dans laquelle: T est CHO, COR¿8?, ou C(OH)R¿1?R¿2?; R¿1? et R¿2? sont hydrogène, alkyle inférieur facultativement substitué, CF¿3?, alcényle facultativement substitué, ou alkynyle facultativement substitué; R¿3? est hydrogène ou alkyle inférieur facultativement substitué; R¿4? est (CF¿3?)¿n?alkyle, (CF¿3?)¿n?(alkyle substitué), (CF¿3?)¿n?alkylphényle, (CF¿3?)¿n?alkyl(phényle substitué), ou (F)¿n?cycloalkyle; n=1-3; R¿5? est hydrogène, halogène, CF¿3?, diène fusionné avec Y quand Y=C, ou diène substitué fusionné avec Y quand Y=C; W, Y et Z sont C, CR¿6? ou N lorsqu'un au moins l'un de W, Y ou Z est C; R¿6? est hydrogène, halogène, ou alkyle inférieur facultativement substitué; X est O, S, SO¿2?, ou NR¿7?; R¿7? est hydrogène, alkyle inférieur facultativement substitué, benzyle facultativement substitué, ou phényle facultativement substitué; et R¿8? est alkyle inférieur, CF¿3?, ou phényle facultativement substitué. L'invention porte également sur les procédés de préparation de ces composés inhibant la production de bêta amyloïde et traitant la maladie d'Alzheimer et le syndrome de Down.
Cole Derek Cecil
Diamantidis George
Galante Rocco John
Harrison Boyd Lynn
Hoke Molly
Torys Llp
Wyeth
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