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    Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors
    4.
    发明申请
    Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors 审中-公开
    取代的N-芳基磺酰基杂环胺作为γ-分泌酶抑制剂

    公开(公告)号：US20100087425A1

    公开(公告)日：2010-04-08

    申请号：US12633286

    申请日：2009-12-08

    申请人： Hubert B. Josien ,  John W. Clader ,  Thomas A. Bara ,  Ruo Xu ,  Hongmei Li ,  Dmitri A. Pissarnitaki ,  Zhiqiang Zhao

    发明人： Hubert B. Josien ,  John W. Clader ,  Thomas A. Bara ,  Ruo Xu ,  Hongmei Li ,  Dmitri A. Pissarnitaki ,  Zhiqiang Zhao

    IPC分类号： A61K31/5377 ,  C07D413/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  A61K31/541 ,  A61P25/00 ,  A61P25/28

    CPC分类号： C07D265/30 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08

    摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: L is —O—, —N(R6)—, —S—, —S(O)—, or —S(O2)—; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, —C(O)—Y, —X—C(O)—Y, -alkylene-X—C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-X—C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-X—C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-X—C(O)—Y, -cycloalkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-X—C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of —NR8R9, —N(R6)—(CH2)b—NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and aryl heterocycloalkyl; or Y is selected from the group consisting of: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

    摘要翻译： 本发明公开了下式的新型γ-分泌酶抑制剂：其中：L是-O - ， - N（R6） - ， - S - ， - S（O） - 或-S（O 2） - ; R 1选自芳基和杂芳基; R 2选自烷基，-C（O）-Y，-X-C（O）-Y， - 亚烷基-X-C（O）-Y， - 亚烷基-C（O）-Y， - 亚烷基 - 亚环烷基-X-C（O）-Y-亚烷基 - 亚环烷基-C（O）-Y-亚烷基 - 亚烷基-X-C（O）-Y-亚烷基 - 亚烷基-C（O） （O）-Y-亚烷基-C（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-X-C（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-C（O ）-Y，芳基和杂芳基; R 3选自芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基和烷氧基烷基; 每个R 4和R 5独立地选自H和烷基; 并且Y选自-NR8R9，-N（R6） - （CH2）b-NR8R9，芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基和芳基杂环烷基; 或Y选自：一种或多种式I化合物或包含该化合物的制剂可用于，例如， 治疗阿尔茨海默病。

    GAMMA SECRETASE MODULATORS
    10.
    发明申请
    GAMMA SECRETASE MODULATORS 审中-公开
    GAMMA秘密调节器

    公开(公告)号：US20110263529A1

    公开(公告)日：2011-10-27

    申请号：US13125995

    申请日：2009-11-05

    申请人： Ruo Xu ,  John W. Clader

    发明人： Ruo Xu ,  John W. Clader

    IPC分类号： A61K31/695 ,  A61P25/28 ,  A61K31/437 ,  C07F7/10 ,  C07D498/04

    CPC分类号： C07D498/04 ,  C07F7/0812

    摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

    摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的杂环化合物作为γ-分泌酶的调节剂，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法和方法 使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病。