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14 条记录 (耗时 0.018 秒)

    Peptide boronic acid inhibitors of trypsin-like proteases
    11.
    发明授权
    Peptide boronic acid inhibitors of trypsin-like proteases 失效
    胰蛋白酶样蛋白酶的肽硼酸抑制剂

    公开(公告)号：US5242904A

    公开(公告)日：1993-09-07

    申请号：US848296

    申请日：1992-03-09

    申请人： Charles A. Kettner ,  Ashokkumar B. Shenvi

    发明人： Charles A. Kettner ,  Ashokkumar B. Shenvi

    IPC分类号： C07F5/02 ,  C07K5/00

    CPC分类号： C07F5/025 ,  C07K5/00

    摘要： Peptides comprising C-terminal boronic acid derivatives of lysine, ornithine, and arginine, homoarginine and corresponding isothiouronium analogs thereof, are reversible inhibitors of trypsin-like serine proteases such as thrombin, plasma kallikrein and plasmin.

    摘要翻译： 包含赖氨酸，鸟氨酸和精氨酸的C末端硼酸衍生物，精氨酸及其相应的异硫脲类似物的肽是胰蛋白酶样丝氨酸蛋白酶如凝血酶，血浆激肽释放酶和纤溶酶的可逆抑制剂。

    Protease inhibitors
    12.
    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。

    &agr;-aminoboronic acids prepared by novel synthetic methods
    13.
    发明授权
    &agr;-aminoboronic acids prepared by novel synthetic methods 失效
    通过新型合成方法制备α-氨基硼酸

    公开(公告)号：US06586615B1

    公开(公告)日：2003-07-01

    申请号：US10043865

    申请日：2002-01-09

    申请人： Charles A. Kettner ,  Sharada Jagannathan ,  Timothy Patrick Forsyth

    发明人： Charles A. Kettner ,  Sharada Jagannathan ,  Timothy Patrick Forsyth

    IPC分类号： C07F504

    CPC分类号： C07F5/025

    摘要： The present invention relates to a novel class of &agr;-aminoboronic acids of Formula (V), which are useful as intermediates in synthetic processes for inhibitors of the serine proteases, leukocyte elastase, pancreatic elastase, cathepsin G, and chymotrypsin. More specifically, the &agr;-aminoboronic acids are useful as intermediates for the synthesis of Hepatitis C Virus (HCV) protease inhibitors. This invention also generally relates to novel methods for the preparation of &agr;-aminoboronic acids.

    摘要翻译： 本发明涉及一类新颖的式（Ⅴ）的α-氨基硼酸，其可用作丝氨酸蛋白酶，白细胞弹性蛋白酶，胰弹性蛋白酶G，胰凝乳蛋白酶抑制剂合成过程中的中间体。 更具体地说，α-氨基硼酸可用作合成丙型肝炎病毒（HCV）蛋白酶抑制剂的中间体。 本发明还通常涉及制备α-氨基硼酸的新方法。