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174 条记录 (耗时 0.054 秒)

    Process for making optically active .alpha.-amino ketones and selected novel optically active .alpha.-amino ketones
    112.
    发明授权
    Process for making optically active .alpha.-amino ketones and selected novel optically active .alpha.-amino ketones 失效
    制备光学活性α-氨基酮和选择的新型光学活性α-氨基酮的方法

    公开(公告)号：US6107512A

    公开(公告)日：2000-08-22

    申请号：US541767

    申请日：1995-10-10

    申请人： John J. Talley

    发明人： John J. Talley

    IPC分类号： B01J31/24 ,  C07C231/12 ,  C07C233/47 ,  C07C229/00

    CPC分类号： B01J31/2409 ,  C07C231/12 ,  C07C233/47 ,  B01J2231/645 ,  B01J2531/822 ,  B01J31/24

    摘要： The invention includes selected novel optically active .alpha.-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.

    摘要翻译： 本发明包括选择性的新型光学活性α-氨基酮，其本身可用或用作制备用作抗生素，抗生素增强剂或酶抑制剂的已知酮亚甲基伪肽的中间体。 此外，本发明提供了一种脱氢/不对称氢化的方法，以获得具有两个手性中心的基本上纯的对映体。

    Substituted isoxazoles for the treatment of inflammation
    115.
    发明授权
    Substituted isoxazoles for the treatment of inflammation 失效
    用于治疗炎症的取代的异恶唑

    公开(公告)号：US5633272A

    公开(公告)日：1997-05-27

    申请号：US473884

    申请日：1995-06-07

    申请人： John J. Talley ,  David L. Brown ,  Srinivasan Nagarajan ,  Jeffery S. Carter ,  Richard M. Weier ,  Michael A. Stealey ,  Paul W. Collins ,  Roland S. Rogers, deceased ,  Karen Seibert

    发明人： John J. Talley ,  David L. Brown ,  Srinivasan Nagarajan ,  Jeffery S. Carter ,  Richard M. Weier ,  Michael A. Stealey ,  Paul W. Collins ,  Roland S. Rogers, deceased ,  Karen Seibert

    IPC分类号： A61P29/00 ,  C07D261/08 ,  C07D261/10 ,  C07D261/12 ,  C07D261/18 ,  C07D413/04 ,  C07D261/06 ,  A61K31/42 ,  C07D261/14

    CPC分类号： C07D261/10 ,  C07D261/08 ,  C07D261/12 ,  C07D261/18 ,  C07D413/04

    摘要： A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.3 is optionally substituted at a substitutable position with one or more radicals independently selected from lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; and wherein R.sup.4 is selected from lower alkyl, hydroxyl and amino; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类用于治疗炎症和炎症相关疾病的取代的异恶唑基化合物。 特别感兴趣的化合物由式II其中R1选自羟基，低级烷基，羧基，低级羧基烷基，低级氨基羰基烷基，低级烷氧基羰基烷基，低级芳烷基，低级烷氧基烷基，低级芳烷氧基烷基，低级烷硫基烷基，低级芳烷硫基烷基，低级 低级芳氧基烷基，低级芳基硫代烷基，低级卤代烷基，低级羟基烷基，环烷基，环烷基烷基和芳烷基; 其中R 3选自环烷基，环烯基，芳基和杂芳基; 其中R 3在可取代的位置任选被一个或多个独立地选自低级烷基亚磺酰基，低级烷基，氰基，羧基，低级烷氧基羰基，低级卤代烷基，羟基，低级羟烷基，低级卤代烷氧基，氨基，低级烷基氨基，低级芳基氨基，低级 氨基烷基，硝基，卤素，低级烷氧基，氨基磺酰基和低级烷硫基; 并且其中R 4选自低级烷基，羟基和氨基; 或其药学上可接受的盐。

    Process for making optically active .alpha.-amino ketones
    120.
    发明授权
    Process for making optically active .alpha.-amino ketones 失效
    制备光学活性α-氨基酮的方法

    公开(公告)号：US5364961A

    公开(公告)日：1994-11-15

    申请号：US898853

    申请日：1992-06-15

    申请人： John J. Talley

    发明人： John J. Talley

    IPC分类号： B01J31/24 ,  C07C231/12 ,  C07C233/47 ,  C07C233/11 ,  C07D295/18

    CPC分类号： B01J31/2409 ,  C07C231/12 ,  C07C233/47 ,  B01J2231/645 ,  B01J2531/822 ,  B01J31/24

    摘要： The invention includes selected novel optically active .alpha.-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.

    摘要翻译： 本发明包括选择性的新型光学活性α-氨基酮，其本身可用或用作制备用作抗生素，抗生素增强剂或酶抑制剂的已知酮亚甲基伪肽的中间体。 此外，本发明提供了一种脱氢/不对称氢化的方法，以获得具有两个手性中心的基本上纯的对映体。