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    Fluoro-and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof
    4.
    发明申请
    Fluoro-and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
    含有氟和三氟烷基的杂环磺酰胺抑制剂β淀粉样蛋白产生及其衍生物

    公开(公告)号：US20070254929A1

    公开(公告)日：2007-11-01

    申请号：US11818630

    申请日：2007-06-15

    申请人： Anthony Kreft ,  Lynn Resnick ,  Scott Mayer ,  George Diamantidis ,  Derek Cole ,  Boyd Harrison ,  Minsheng Zhang ,  Molly Hoke ,  Tingzhong Wang ,  Rocco Galante

    发明人： Anthony Kreft ,  Lynn Resnick ,  Scott Mayer ,  George Diamantidis ,  Derek Cole ,  Boyd Harrison ,  Minsheng Zhang ,  Molly Hoke ,  Tingzhong Wang ,  Rocco Galante

    IPC分类号： A61K31/433 ,  A61P25/00 ,  C07D285/08

    CPC分类号： C07D333/62 ,  C07D231/18 ,  C07D333/34

    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.

    摘要翻译： 提供式（I）化合物，其中T是CHO，COR 8或C（OH）R 1 R 2 2; R 1和R 2均为氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R 3是氢或任选取代的低级烷基; R 4是（CF 3）n烷基，（CF 3 N）N（S） （取代的烷基），（CF 3）n烷基苯基，（CF 3）n烷基（取代的苯基）或（C 3 -C 6）烷基 （F）环烷基; n = 1-3; 当Y-C时，R 5是氢，卤素，CF 3 O，与Y稠合的二烯，或Y-C时与Y稠合的取代的二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R 6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 和R 8是低级烷基，CF 3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-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。