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    Protease inhibitors
    1.
    发明授权
    Protease inhibitors 失效
    蛋白酶抑制剂

    公开(公告)号：US4935493A

    公开(公告)日：1990-06-19

    申请号：US105768

    申请日：1987-10-06

    申请人： William W. Bachovchin ,  Andrew G. Plaut ,  Charles A. Kettner

    发明人： William W. Bachovchin ,  Andrew G. Plaut ,  Charles A. Kettner

    IPC分类号： C07K5/06 ,  C07K5/08

    CPC分类号： C07K5/0827 ,  C07K5/0606 ,  C07K5/06191

    摘要： A compound having the structure ##STR1## where T is of the fomrula ##STR2## where each D.sup.1 and D.sup.2, independently, is a hydroxyl group of a group which is capable of being hydrolysed to a hydroxyl group in aqueous solution at physiological pH; a group of the formula ##STR3## where G is either H,F or an alkyl group containing 1 to about 20 carbon atoms and optional heteroatoms which can be N, S, or O; or a phosphonate group of the formula ##STR4## where J is O-alkyl, N-alkyl, or alkyl, each comprising about 1-20 carbon atoms and, optionally, heteroatoms which can be N, S, or O; T being able to form a complex with the catalytic site of an enzyme, X is a group having at least one amino acid, ##STR5## and each R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 is separately a group which does not interfere significantly (i.e., does not lower than Ki of the compound to less than 10.sup.-7 M) with site-specific recognition of the compound by the enzyme, and allows a complex to be formed with the enzyme.

    摘要翻译： 具有结构的化合物，其中T是所述的“IMAGE”，其中每个D1和D2独立地是能够在生理pH下在水溶液中水解成羟基的基团的羟基; 其中G是H，F或含有1至约20个碳原子的烷基和可以是N，S或O的任选的杂原子的式 或其中J为O-烷基，N-烷基或烷基的式（IMAGE）的膦酸酯基团，各自包含约1-20个碳原子，以及任选的可以是N，S或O的杂原子; T能够与酶的催化位点形成复合物，X是具有至少一个氨基酸的基团，每个R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8 分别是通过酶对化合物的位点特异性识别而不会显着干扰（即不低于化合物的Ki至小于10-7M）的基团，并且允许与酶形成复合物。

    Inhibitors of dipeptidyl-aminopeptidase type IV
    10.
    发明授权
    Inhibitors of dipeptidyl-aminopeptidase type IV 失效
    II型二肽基氨基肽酶的抑制剂

    公开(公告)号：US07230074B2

    公开(公告)日：2007-06-12

    申请号：US10775598

    申请日：2004-02-10

    申请人： William W. Bachovchin ,  Andrew G. Plaut ,  George R. Flentke

    发明人： William W. Bachovchin ,  Andrew G. Plaut ,  George R. Flentke

    IPC分类号： C07K5/10

    CPC分类号： C07F5/025

    摘要： Peptide inhibitors of dipeptidyl-aminopeptidase type IV (DP-IV) are provided. The peptide inhibitors have an isomeric purity of about 96–99 percent. The peptide inhibitors include one or more amino acids covalently coupled to boroproline moiety. The compounds are useful as DP-IV inhibitors, in vivo and in vitro.

    摘要翻译： 提供IV型二肽基氨基肽酶（DP-IV）的肽抑制剂。 肽抑制剂的异构纯度约为96-99％。 肽抑制剂包括共价偶联到硼脯氨酸部分的一个或多个氨基酸。 该化合物在体内和体外可用作DP-IV抑制剂。