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    Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production Containing an Azole
    3.
    发明申请
    Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production Containing an Azole 审中-公开
    包含唑类的β淀粉样蛋白的杂环磺酰胺抑制剂

    公开(公告)号：US20100144812A1

    公开(公告)日：2010-06-10

    申请号：US12708557

    申请日：2010-02-19

    申请人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    发明人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    IPC分类号： A61K31/4155 ,  A61K31/415 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4025 ,  A61P25/28 ,  A61P25/00 ,  C07D409/02 ,  C07D231/10

    CPC分类号： A61K31/416 ,  C07D231/12 ,  C07D409/12

    摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.

    摘要翻译： 提供了可用于降低β淀粉样蛋白水平的化合物。 所述化合物具有式Ia的结构：其中，R 1为低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2 R 5; R5是苯基，取代的苯基，杂环，取代的杂环，烷基或取代的烷基; R2是低级烷基，取代的低级烷基，CF3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基或环烷基; R3是氢，低级烷基或取代的低级烷基; R4是苯基，取代的苯基，杂环，取代的杂环，噻吩或取代的噻吩; R 6是氢，低级烷基，取代的低级烷基，CF 3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基，环烷基或取代的环烷基; W，X和Y独立地为CR 7或N; 并且R 7是氢，卤素，低级烷基或取代的低级烷基。

    Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole
    4.
    发明授权
    Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole 失效
    含有唑类的β-淀粉样蛋白产生的杂环磺酰胺抑制剂

    公开(公告)号：US07674813B2

    公开(公告)日：2010-03-09

    申请号：US12142306

    申请日：2008-06-19

    申请人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    发明人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    IPC分类号： A01N43/50 ,  A01N43/56 ,  C07D231/00

    CPC分类号： A61K31/416 ,  C07D231/12 ,  C07D409/12

    摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.

    摘要翻译： 提供了可用于降低β淀粉样蛋白水平的化合物。 所述化合物具有式Ia的结构：其中，R 1为低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2 R 5; R5是苯基，取代的苯基，杂环，取代的杂环，烷基或取代的烷基; R2是低级烷基，取代的低级烷基，CF3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基或环烷基; R3是氢，低级烷基或取代的低级烷基; R4是苯基，取代的苯基，杂环，取代的杂环，噻吩或取代的噻吩; R 6是氢，低级烷基，取代的低级烷基，CF 3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基，环烷基或取代的环烷基; W，X和Y独立地为CR 7或N; 并且R 7是氢，卤素，低级烷基或取代的低级烷基。

    Small molecule activators of mitochondrial function
    8.
    发明授权
    Small molecule activators of mitochondrial function 有权
    线粒体功能的小分子激活剂

    公开(公告)号：US09000009B2

    公开(公告)日：2015-04-07

    申请号：US13139162

    申请日：2009-12-10

    申请人： Robert B. Wilson ,  Maria Grazia Cotticelli ,  Phillip A. Benedetti ,  Amos Smith ,  Jason E. Melvin ,  Donna M Huryn

    发明人： Robert B. Wilson ,  Maria Grazia Cotticelli ,  Phillip A. Benedetti ,  Amos Smith ,  Jason E. Melvin ,  Donna M Huryn

    IPC分类号： A61K31/47

    CPC分类号： C07D409/06 ,  A61K31/47 ,  C07D215/14 ,  C07D405/06 ,  C12Q1/025 ,  G01N2333/39 ,  G01N2500/10

    摘要： Methods for improving mitochondrial function, decreasing iron accumulation, and/or decreasing oxidative stress by exposing cells or treating a subject to compounds or compositions of the general formula (I) are described that are beneficial in treating, for example, diseases and conditions such as Friedreich's ataxia, normal aging, and various neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. Furthermore, such compounds are useful as probes for identifying defects in mitochondrial metabolism, mitochondrial iron accumulation, cellular stress among other mitochondrial diseases and helping to identify compounds active in overcoming such defects.

    摘要翻译： 描述了通过使细胞暴露或治疗受试者对通式（I）的化合物或组合物来改善线粒体功能，减少铁积累和/或降低氧化应激的方法，其有益于治疗例如疾病和病症如 弗里德里希的共济失调，正常老化和各种神经变性疾病如阿尔茨海默病和帕金森病。 此外，这些化合物可用作鉴定线粒体代谢缺陷，线粒体铁积累，其他线粒体疾病中的细胞应激以及有助于鉴别克服这些缺陷的活性物质的探针。