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Fluoro-and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof

机译:β淀粉样蛋白生产的含氟和三氟烷基杂环磺酰胺抑制剂及其衍生物

摘要

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.
机译:提供了式(I)的化合物,其中T为CHO,COR8或C(OH)R1R2; R1和R2为氢,任选取代的低级烷基,CF3,任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4为(CF3)n烷基,(CF3)n(取代烷基),(CF3)n烷基苯基,(CF3)n烷基(取代苯基)或(F)n环烷基。 n = 1-3; R5是氢,卤素,CF3,当Y = C时稠合于Y的二烯或当Y = C时稠合于Y的取代的二烯; W,Y和Z为C,CR6或N,其中W,Y或Z中的至少一个为C; R6是氢,卤素或任选取代的低级烷基; X是O,S,SO2或NR7; R7为氢,任选取代的低级烷基,任选取代的苄基或任选取代的苯基; R8是低级烷基,CF3或任选取代的苯基。还描述了制备和使用这些化合物抑制β淀粉样蛋白产生以及治疗阿尔茨海默氏病和唐氏综合症的方法。

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