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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。

    Process for the synthesis of chirally pure beta-amino-alcohols
    5.
    发明授权
    Process for the synthesis of chirally pure beta-amino-alcohols 失效
    手性纯合β-氨基醇的合成方法

    公开(公告)号：US06800764B2

    公开(公告)日：2004-10-05

    申请号：US10304322

    申请日：2002-11-26

    申请人： Anthony Frank Kreft ,  Madelene Miyoko Antane ,  Derek Cecil Cole ,  Dennis Martin Kubrak ,  Lynn Resnick ,  Joseph Raymond Stock ,  Zheng Wang

    发明人： Anthony Frank Kreft ,  Madelene Miyoko Antane ,  Derek Cecil Cole ,  Dennis Martin Kubrak ,  Lynn Resnick ,  Joseph Raymond Stock ,  Zheng Wang

    IPC分类号： C07D33332

    CPC分类号： C07C215/20 ,  C07B2200/07 ,  C07C215/08 ,  C07C215/24 ,  C07C215/28 ,  C07C215/56 ,  C07C229/08 ,  C07C229/28 ,  C07C229/30 ,  C07C229/36 ,  C07C247/12 ,  C07C323/63 ,  C07D263/26 ,  C07D333/34

    摘要： A process is provided for preparing chirally pure S-enantiomers of &agr;-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an &agr;-azido acid; h) reducing the &agr;-azido acid to the &agr;-amino acid; and i) recrystallizing the &agr;-amino acid to the chirally pure &agr;-amino acid. A process is also provided for preparing chirally pure S-enantiomers of &bgr;-amino alcohols further comprising the steps of reducing the crude &agr;-amino acid to the &bgr;-amino alcohol and recrystallizing the &bgr;-amino alcohol to the chirally pure &bgr;-amino alcohol. A process is further provided for preparing chirally pure S enantiomers of N-sulfonyl &bgr;-amino alcohols further comprising the steps of sulfonylating the &bgr;-amino alcohol with 5-chloro-thiophene-2-sulfonyl halide; and recrystallizing to afford the chirally pure N-sulfonyl &bgr;-amino alcohols.

    摘要翻译： 提供了一种用于制备α-氨基酸的手性纯的S-对映异构体的方法，包括以下步骤：a）由式（R）2CH（CH 2）n CH 2 X的烷基卤制备有机金属试剂; b）将有机金属试剂加入到二氧化碳中，得到羧酸; c）在叔胺碱存在下用酰氯，三氯化磷，酸酐或亚硫酰氯活化羧酸; d）使步骤c）的产物与S-4-苄基-2-恶唑烷酮的碱金属盐反应; e）用强非亲核碱处理步骤d）的产物以形成烯醇化物阴离子; f）用2,4,6-三异丙基苯磺酰叠氮化物捕获烯醇化阴离子，得到恶唑烷酮叠氮化物; g）用碱水溶液水解恶唑烷酮叠氮化物，得​​到α-叠氮基; h）将α-叠氮基还原成α-氨基酸; 和i）将α-氨基酸重结晶至手性纯的α-氨基酸。 还提供了制备β-氨基醇的手性纯的S-对映异构体的方法，该方法还包括将β-氨基酸的粗α-氨基酸还原成β-氨基醇，并将β-氨基醇重结晶至手性纯的β-氨基醇 。 还提供了制备N-磺酰基β-氨基醇的手性纯S对映异构体的方法，其还包括用5-氯 - 噻吩-2-磺酰卤磺酰化β-氨基醇的步骤; 并重结晶得到手性纯的N-磺酰基β-氨基醇。