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    Substituted pyrrolidine hydroxamate metalloprotease inhibitors
    6.
    发明授权
    Substituted pyrrolidine hydroxamate metalloprotease inhibitors 失效
    取代的吡咯烷异羟肟酸盐金属蛋白酶抑制剂

    公开(公告)号：US06329418B1

    公开(公告)日：2001-12-11

    申请号：US09274564

    申请日：1999-03-23

    申请人： Menyan Cheng ,  Michael George Natchus ,  Biswanath De ,  Neil Gregory Almstead ,  Yetunde Olabisi Taiwo ,  Stanislaw Pikul

    发明人： Menyan Cheng ,  Michael George Natchus ,  Biswanath De ,  Neil Gregory Almstead ,  Yetunde Olabisi Taiwo ,  Stanislaw Pikul

    IPC分类号： A61K3140

    CPC分类号： C07D401/12 ,  C07D207/48 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12

    摘要： The invention provides compounds which are potent inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to compounds having a structure according to the following Formula (I): wherein R1, R2, X, Z, m, and n are defined below. to This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of diseases and conditions which are characterized by unwanted metalloprotease activity. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for metalloprotease-related maladies using these compounds or the pharmaceutical compositions containing them.

    摘要翻译： 本发明提供了作为金属蛋白酶的有效抑制剂的化合物，其有效治疗以这些酶的过度活性为特征的病症。 特别地，本发明涉及具有根据下式（I）的结构的化合物：其中R1，R2，X，Z，m和n定义如下。本发明还包括光学异构体，非对映异构体和对映异构体 上式，及其可药用盐，生物可水解酰胺，酯和酰亚胺。 本发明的化合物可用于治疗以不需要的金属蛋白酶活性为特征的疾病和病症。 因此，本发明还提供包含这些化合物的药物组合物。 本发明还提供了使用这些化合物或含有它们的药物组合物治疗金属蛋白酶相关疾病的方法。