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26 条记录 (耗时 0.081 秒)

    Tetrapeptide inhibitors of β-secretase
    5.
    发明授权
    Tetrapeptide inhibitors of β-secretase 失效
    β-分泌酶的四肽抑制剂

    公开(公告)号：US07169759B1

    公开(公告)日：2007-01-30

    申请号：US09594667

    申请日：2000-06-15

    申请人： Varghese John ,  Jay Tung ,  Lawrence Fang ,  Shumeye S. Mamo

    发明人： Varghese John ,  Jay Tung ,  Lawrence Fang ,  Shumeye S. Mamo

    IPC分类号： A61K38/00

    CPC分类号： A61K38/07

    摘要： Statine-derived peptide inhibitors of the β-secretase enzyme are provided which are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of Aβ peptide in a mammal. The compounds of the invention provide useful methods of treatment by administration of these inhibitors to reduce Aβ peptide formation and pharmaceutical compositions.

    摘要翻译： 提供了β-分泌酶的来自Statine的肽抑制剂，其可用于治疗阿尔茨海默氏病和以哺乳动物中Abeta肽沉积为特征的其它疾病。 本发明的化合物提供了通过施用这些抑制剂以减少Aβ肽形成和药物组合物的有效治疗方法。

    Method for the preparation of substituted 1,4-dihydro-4-oxo-cinnoline-3-carboxylic acid, esters and salts thereof, and intermediates used in their preparation
    10.
    发明授权
    Method for the preparation of substituted 1,4-dihydro-4-oxo-cinnoline-3-carboxylic acid, esters and salts thereof, and intermediates used in their preparation 失效
    制备取代的1,4-二氢-4-氧代 - 噌啉-3-羧酸的方法，其酯和盐及其制备中使用的方法

    公开(公告)号：US5183891A

    公开(公告)日：1993-02-02

    申请号：US434077

    申请日：1989-11-09

    申请人： Jeffrey Labovitz ,  William J. Guilford ,  Lawrence Fang ,  Yi Liang

    发明人： Jeffrey Labovitz ,  William J. Guilford ,  Lawrence Fang ,  Yi Liang

    IPC分类号： C07D237/28

    CPC分类号： C07D237/28

    摘要： A method for the preparation of compounds of the formula ##STR1## wherein X represents a group of the formula OR.sub.1 or NR.sub.1 R.sub.2, wherein R.sub.1 and R.sub.2 independently represent H or an organic group that forms a stable covalent bond with the N or O of said X; Y is H or an organic group that forms a stable ester with the adjacent COO group; R is an alkyl or aryl group optionally substituted with one or more stable organic substituents; each R.sub.3 independently represents a stable organic group; and n is an integer from 0 to 3;the method using new intermediates of the formula ##STR2## wherein R.sub.3 and Y have the foregoing meanings; W is either F or Cl;and R.sub.9 is a hydrocarbon such as a C.sub.1 -C.sub.4 alkyl or alkenyl group.

    摘要翻译： 制备式（I）的化合物的方法，其中X表示式OR1或NR1R2的基团，其中R1和R2独立地表示H或与N或O形成稳定的共价键的有机基团 的X Y是H或与相邻COO基形成稳定酯的有机基团; R是任选被一个或多个稳定的有机取代基取代的烷基或芳基; 每个R 3独立地表示稳定的有机基团; n为0〜3的整数， 使用式（VI）的新中间体的方法，其中R3和Y具有上述含义; W是F或Cl; 并且R 9是烃，例如C 1 -C 4烷基或烯基。