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    BRIDGED PIPERIDINE DERIVATIVES
    8.
    发明申请
    BRIDGED PIPERIDINE DERIVATIVES 审中-公开
    桥连哌啶衍生物

    公开(公告)号：WO2012116965A1

    公开(公告)日：2012-09-07

    申请号：PCT/EP2012/053301

    申请日：2012-02-28

    Applicant: F. HOFFMANN-LA ROCHE AG ,  BAUMANN, Karlheinz ,  GREEN, Luke ,  LIMBERG, Anja ,  LUEBBERS, Thomas ,  THOMAS, Andrew

    Inventor： BAUMANN, Karlheinz ,  GREEN, Luke ,  LIMBERG, Anja ,  LUEBBERS, Thomas ,  THOMAS, Andrew

    IPC: C07D471/04 ,  C07D519/00 ,  A61K31/4196 ,  A61P25/00

    CPC classification number: C07D451/04

    Abstract: The present invention relates to compounds of formula (l); hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from S or N; hetaryl II is a six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, or N, wherein at least one ring is aromatic in nature; R 1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen or halogen; R 2 is lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, cycloalkyl substituted by lower alkyl or lower alkyl substituted by halogen, or is lower alkyl substituted by hydroxy, or is furyl, or is O-benzyl, (CH2)p-phenyl, optionally substituted by halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkyl or by cyano; R 3 is hydrogen or lower alkyl; Y is (CH 2 )n-, -CH 2 OCH 2 -, -CH 2 O-, CH 2 S-, -CH 2 SCH 2 - and is bonded to two of the ring carbon atoms, bonding being to either the ring carbon atoms a and b or the ring carbon atoms c and d; p is 0 or 1; m is 0, 1 or 2; if m is 2 then R 1 may be the same or different; -75- n is 2 or 3; o is 0, 1 or 2, if o is 2, then R 2 may be the same or different; or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimers disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

    Abstract translation: 本发明涉及式（I）化合物; 杂芳基I是含有1至3个选自S或N的杂原子的五或六元杂芳基; 杂芳基II是含有1至3个选自S或N的杂原子或是含有1至4个选自S或N的杂原子的二元环体系的六元杂芳基，其中至少一个环在本质上是芳族的; R1是低级烷基，低级烷氧基，被卤素或卤素取代的低级烷基; R2是低级烷基，被卤素取代的低级烷基，卤素，低级烷氧基，被低级烷基取代的环烷基或被卤素取代的低级烷基，或被羟基取代的低级烷基，或是呋喃基，或是O-苄基，（CH2）p 苯基，任选被卤素，低级烷氧基，被卤素，低级烷基或氰基取代的低级烷基取代; R3是氢或低级烷基; Y是（CH 2）n - ， - CH 2 OCH 2 - ， - CH 2 O - ，CH 2 S - ， - CH 2 SCH 2 - 并键合到两个环碳原子上，键合为环碳原子a和b或环碳原子c 和d p为0或1; m为0,1或2; 如果m为2，则R1可以相同或不同; -75- n为2或3; o为0,1或2，如果o为2，则R2可以相同或不同; 或其药物活性的酸加成盐。 本发明式I化合物是淀粉样蛋白β的调节剂，因此它们可用于治疗或预防与脑中β-淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默病和其它疾病如脑淀粉样蛋白 血管病，遗传性脑出血伴淀粉样变性，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合征。

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