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    Chromogenic amino acid esters and peptide esters
    2.
    发明授权
    Chromogenic amino acid esters and peptide esters 失效
    显色氨基酸酯和肽酯

    公开(公告)号：US4723020A

    公开(公告)日：1988-02-02

    申请号：US710623

    申请日：1985-03-11

    申请人： Herbert Hugl ,  Eugen Schnabel

    发明人： Herbert Hugl ,  Eugen Schnabel

    IPC分类号： C07D279/02 ,  C07D231/56 ,  C07D275/04 ,  C12Q1/34 ,  C12Q1/37 ,  C12Q1/44 ,  G01N33/493 ,  G01N33/50

    CPC分类号： C12Q1/44 ,  C07D231/56 ,  C07D275/04 ,  C12Q1/37 ,  C12Q2334/70 ,  C12Q2337/00 ,  Y10S435/81

    摘要： The present invention relates to new chromogenic amino acid esters and peptide esters of hydroxybenzo(iso)thiazoles and hydroxybenzopyrazoles, processes for their preparation and the use of the new esters as substrates for the analytical detection of esterolytic and/or proteolytic enzymes, for example in body fluids, the esters being incorporated into test agents, in particular test strips, in a suitable manner. The new esters are preferably used for the detection of leukocytes, in particular in urine.

    摘要翻译： 本发明涉及羟基苯并（异）噻唑和羟基苯并吡唑的新的显色氨基酸酯和肽酯，其制备方法以及新酯作为分解检测酯水解和/或蛋白水解酶的底物的用途，例如 体液，以合适的方式将酯并入测试剂，特别是测试条中。 新的酯优选用于检测白细胞，特别是在尿液中。

    Derivatives, having an inhibitory action against protease and an antiphlogistic action, of the trypsin-kallikrein inhibitor obtained from cattle organs (BPTI), their preparation and their use as medicaments
    7.
    发明授权
    Derivatives, having an inhibitory action against protease and an antiphlogistic action, of the trypsin-kallikrein inhibitor obtained from cattle organs (BPTI), their preparation and their use as medicaments 失效
    从牛器官（BPTI）获得的胰蛋白酶激肽释放酶抑制剂对蛋白酶和消炎作用具有抑制作用的衍生物，其制备及其作为药物的用途

    公开(公告)号：US4153687A

    公开(公告)日：1979-05-08

    申请号：US847886

    申请日：1977-11-02

    申请人： Eugen Schnabel ,  Gerd Reinhardt ,  Horst D. Schlumberger ,  Ernst Truscheit ,  Harold Tschesche

    发明人： Eugen Schnabel ,  Gerd Reinhardt ,  Horst D. Schlumberger ,  Ernst Truscheit ,  Harold Tschesche

    IPC分类号： C07G99/00 ,  A61K38/00 ,  A61K38/55 ,  A61P29/00 ,  A61P37/00 ,  C07K14/81 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K14/8117 ,  A61K38/00

    摘要： The invention provides derivatives of kallikrein-trypsin inhibitor (BPTI) in which one or both of the 10- or 21-tyrosine residues are linked, in the o-position relative to the phenolic hydroxyl group, to an aptionally substituted carbocyclic or heterocyclic aromatic radical via an azo group and the other if only one of the said residues is substituted is either unsubstituted or carries a nitro group or an amino group in the o-position relative to the phenolic hydroxyl group.The azo-BPTI derivatives of the invention can be used, as medicaments for the therapy of diseases which are caused either by over-production of proteases as a result of increased liberation from the zymogens or of release during cell decomposition or by a deficiency or lack of natural indogenous inhibitors of these enzymes in organs and tissue fluids. Diseases which have this type of etiology are the various forms of shock and post-traumatic or post-operative complications, disorders in blood clotting and acute and chronic inflammatory reactions and, in particular, also chronic inflammatory reactions with necrotic and degenerative damage to connective tissue, such as pancreatitis and also vasculitides, glomerulonephritides, rheumatoid arthritis and other collagenoses caused by immune complexes and also arthritides caused by deposits due to metabolic processes (gout), but also degenerative changes in the elastic elements of vascular walls (arterioscleroses) or in the lung (pulmonary emphysema).

    摘要翻译： 本发明提供激肽释放酶 - 胰蛋白酶抑制剂（BPTI）的衍生物，其中10位或21位酪氨酸残基中的一个或两者在相对于酚羟基的o位置连接到易位的碳环或杂环芳族基团 如果只有一个所述残基被取代，则通过偶氮基团和另一个是未取代的或在相对于酚羟基的o位置携带硝基或氨基。