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    FLUORO-AND TRIFLUOROALKYL-CONTAINING HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION AND DERIVATIVES THEREOF
    28.
    发明申请
    FLUORO-AND TRIFLUOROALKYL-CONTAINING HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION AND DERIVATIVES THEREOF 审中-公开
    含氟和含三氟甲磺酸的苯甲酰胺酰胺抑制剂的制备及其衍生物

    公开(公告)号：WO2004092155A1

    公开(公告)日：2004-10-28

    申请号：PCT/US2004/009268

    申请日：2004-03-26

    Applicant: WYETH ,  KREFT, Anthony, Frank ,  RESNICK, Lynn ,  MAYER, Scott, Christian ,  DIAMANTIDIS, George ,  COLE, Derek, Cecil ,  WANG, Tingzhong ,  GALANTE, Rocco, John ,  HOKE, Molly ,  HARRISON, Boyd, Lynn ,  ZHANG, Minsheng

    Inventor： KREFT, Anthony, Frank ,  RESNICK, Lynn ,  MAYER, Scott, Christian ,  DIAMANTIDIS, George ,  COLE, Derek, Cecil ,  WANG, Tingzhong ,  GALANTE, Rocco, John ,  HOKE, Molly ,  HARRISON, Boyd, Lynn ,  ZHANG, Minsheng

    IPC: C07D333/34

    CPC classification number: C07D333/62 ,  C07D231/18 ,  C07D333/34

    Abstract: Compounds of Formula (I), are provided where T is CHO, COR 8 , or C(OH)R 1 R 2 ; R 1 and R 2 are hydrogen, optionally substituted lower alkyl, CF 3 , optionally substituted alkenyl, or optionally substituted alkynyl; R 3 is hydrogen or optionally substituted lower alkyl; R 4 is (CF 3 ) n alkyl, (CF 3 ) n (substitutedalkyl), (CF 3 ) n alkylphenyl, (CF 3 )nalkyl(substitutedphenyl), or (F) n cycloalkyl; n=1-3; R 5 is hydrogen, halogen, CF 3 , diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR 6 or N where at least one of W, Y or Z are C; R 6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO 2 , or NR 7 ; R 7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R 8 is lower alkyl, CF 3 , 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.

    Abstract translation: 提供式（I）化合物，其中T是CHO，COR8或C（OH）R 1 R 2; R 1和R 2是氢，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; R3是氢或任选取代的低级烷基; R4是（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; 当Y = C时，R 5为氢，卤素，CF 3，与Y稠合的二烯，或Y = C时与Y稠合的取代二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6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; 且R 8为低级烷基，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。

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