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    Inhibitors, obtained from bacilli, for glycoside hydrolases
    64.
    发明授权
    Inhibitors, obtained from bacilli, for glycoside hydrolases 失效
    抑制剂，从杆菌获得，用于糖苷水解酶

    公开(公告)号：US4307194A

    公开(公告)日：1981-12-22

    申请号：US858036

    申请日：1977-12-06

    Applicant: Werner Frommer ,  Lutz Muller ,  Delf Schmidt ,  Walter Puls ,  Hans-Peter Krause ,  Ulrich Heber

    Inventor： Werner Frommer ,  Lutz Muller ,  Delf Schmidt ,  Walter Puls ,  Hans-Peter Krause ,  Ulrich Heber

    IPC: C12P17/12 ,  A23K1/17 ,  A23K1/18 ,  A61K31/445 ,  A61K35/74 ,  C07D211/46 ,  C12N1/20 ,  C12N9/99 ,  C12P1/04 ,  C12P19/26 ,  C12R1/07 ,  C12R1/12 ,  C12R1/125

    CPC classification number: C12R1/07 ,  A23K20/195 ,  A23K50/30 ,  A61K31/445 ,  C12N1/20 ,  C12P1/04 ,  Y10S435/832 ,  Y10S435/839

    Abstract: According to the present invention inhibitors for glycoside hydrolases, and in particular glucosidase inhibitors especially saccharase inhibitors, which are active in the digestive tract are formed by culturing organisms of the family Bacillaceae, particularly by strains of the genus Bacillus.It has also been found that certain strains of organisms of the family Bacillaceae, especially strains DSM 7, DSM 704 and DSM 675 produce the antibiotic known as 1-desoxynojirimycin. The invention therefore provides a method of producing 1-desoxynojirimycin which comprises culturing a 1-desoxynojirimycin producing organism of the genus Bacillus. Inhibitors for glycoside hydrolases and the invention includes methods for producing such inhibitors, pharmaceutical compositions containing the inhibitors and methods of treatment involving the use of the inhibitors.

    Abstract translation: 根据本发明，通过培养家蚕科的生物体，特别是通过芽孢杆菌属的菌株形成糖苷水解酶抑制剂，特别是在消化道中有活性的葡糖苷酶抑制剂，特别是糖酶抑制剂。 还已经发现，芽孢杆菌科的特定菌株DSM 7，DSM 704和DSM 675的生物体产生称为1-脱氧野尻霉素的抗生素。 因此，本发明提供了一种生产1-脱氧野尻霉素的方法，该方法包括培养产生芽孢杆菌属的1-脱氧诺伊霉素生物的生物。 糖苷水解酶和本发明的抑制剂包括制备这种抑制剂的方法，含有抑制剂的药物组合物和涉及使用抑制剂的治疗方法。

    Glycoside-hydrolase enzyme inhibitors
    65.
    发明授权
    Glycoside-hydrolase enzyme inhibitors 失效
    糖苷 - 水解酶抑制剂

    公开(公告)号：US4013510A

    公开(公告)日：1977-03-22

    申请号：US493463

    申请日：1974-07-31

    Applicant: Werner Frommer ,  Walter Puls ,  Dietmar Schafer ,  Delf Schmidt

    Inventor： Werner Frommer ,  Walter Puls ,  Dietmar Schafer ,  Delf Schmidt

    IPC: C12P1/04 ,  C12P1/06 ,  C12D13/00

    CPC classification number: A61K31/70 ,  C12P1/04 ,  C12P1/06 ,  Y10S435/803 ,  Y10S435/822 ,  Y10S435/827 ,  Y10S435/886 ,  Y10S435/889 ,  Y10S435/896 ,  Y10S435/907 ,  Y10S435/911

    Abstract: This invention relates to inhibitors for glycosidehydrolases derived from bacteria of the order Actinomycetales, means for their production comprising cultivation of a microorganism of the order Actinomycetales in appropriate nutrient solutions under conditions most favorable to growth and production of the enzyme inhibitor and recovering, as a new product, glycoside-hydrolase enzyme inhibitors, from the culture as well as the use of said enzyme inhibitors in pharmaceutically acceptable therapeutic compositions in the treatment of conditions indicating obesity, diabetes, pre-diabetes, gastritis, gastric ulcer, hyperlipidemia (arteriosclerosis) and the like. The invention also contemplates the provision of methods of inhibiting the reaction of carbohydrates and glycoside-hydrolase enzymes and particularly carbohydrate-splitting glycoside-hydrolase enzymes of the digestive tract by means of conducting said reaction of said carbohydrates and glycoside-hydrolase enzymes in the presence of a glycoside-hydrolase enzyme inhibitor for said glycoside-hydrolase enzyme derived from a strain of microorganism of the order Actinomycetales. The invention further contemplates the provision of methods for the treatment of indications of the group consisting of obesity, adipose, hyperlipidemia (arteriosclerosis), diabetes, pre-diabetes, gastritis, gastric ulcer, duodenal ulcer, and caries induced by the action of glycoside-hydrolase enzymes and carbohydrates, the improvement which comprises employing an enzyme inhibitor for glycoside-hydrolase enzymes produced by a strain of microorganism of the order Actinomycetales.

    Abstract translation: 本发明涉及来自放线菌纲序列的细菌的糖苷水解酶的抑制剂，其生产方法包括在最有利于生长和产生酶抑制剂的条件下，在适当的营养液中培养放线菌纲的微生物，并作为新的 产品，糖苷 - 水解酶抑制剂，以及所述酶抑制剂在药学上可接受的治疗组合物中用于治疗指示肥胖，糖尿病，前期糖尿病，胃炎，胃溃疡，高脂血症（动脉硬化）和 喜欢。 本发明还考虑提供通过在所述碳水化合物和糖苷 - 水解酶的存在下进行所述碳水化合物和糖苷 - 水解酶的反应来抑制碳水化合物和糖苷 - 水解酶，特别是消化道的碳水化合物 - 裂解糖苷 - 水解酶的反应的方法 一种衍生自放线菌纲的微生物菌株的糖苷 - 水解酶的糖苷 - 水解酶抑制剂。 本发明进一步考虑了提供治疗由肥胖，脂肪，高脂血症（动脉硬化），糖尿病，前期糖尿病，胃炎，胃溃疡，十二指肠溃疡以及由糖苷 - 水解酶和碳水化合物，其改进包括使用由抑制放线菌的微生物菌株产生的糖苷 - 水解酶的酶抑制剂。

    Masking background fluorescence and luminescence in optical analysis of biomedical assays
    70.
    发明授权
    Masking background fluorescence and luminescence in optical analysis of biomedical assays 有权
    掩蔽背景荧光和发光在生物医学测定的光学分析

    公开(公告)号：US06420183B1

    公开(公告)日：2002-07-16

    申请号：US09194099

    申请日：1998-11-20

    Applicant: Thoams Krahn ,  Wolfgang Paffhausen ,  Andreas Schade ,  Martin Bechem ,  Delf Schmidt

    Inventor： Thoams Krahn ,  Wolfgang Paffhausen ,  Andreas Schade ,  Martin Bechem ,  Delf Schmidt

    IPC: G01N2100

    CPC classification number: G01N33/542 ,  G01N33/5005 ,  G01N33/5306 ,  G01N33/54393 ,  Y10S436/80 ,  Y10S436/805 ,  Y10S436/823 ,  Y10T436/13

    Abstract: In a process for the quantitative optical analysis of fluorescently labelled biological cells 5, a cell layer on a transparent support at the bottom 2 of a reaction vessel 1 is in contact with a solution 3 containing the fluorescent dye 4. The sensitivity of analytical detection can be considerably improved if to the fluorescent dye 4 already present in addition a masking dye 9, which absorbs the excitation light 6 for the fluorescent dye 4 and/or its emission light 7, is added to the solution 3 and/or if a separating layer 10 permeable to the solution and absorbing and/or reflecting the excitation light 6 or the emission light 7 is applied to the cell layer at the bottom 2. The separating layer 10 must be composed such that it has a high power of reflection for the luminescent light 11. Analogously, these process principles can also be used in receptor studies for the masking of the interfering background radiation in the quantitative optical analysis of fluorescently or luminescently labelled reaction components. In this case, a receptor layer 12 at the bottom 2 of a reaction vessel 1 is in contact with a solution in which a fluorescent or luminescent ligand 13 is dissolved. The sensitivity and accuracy of the analytical detection can be considerably improved here if a masking dye 9 which absorbs the excitation light 6 for the fluorescent dye and/or its emission light or the luminescent light is added to the supernatant 3. Instead of the masking dye in the solution 3 or optionally as an additional measure, a separating layer 10 permeable to the solution 3 and absorbing and/or reflecting the excitation light 6 and/or the emission light or the luminescent light can be applied to the cell or receptor layer 12 at the bottom 2.

    Abstract translation: 在荧光标记的生物细胞5的定量光学分析的过程中，反应容器1的底部2的透明支持体上的细胞层与含有荧光染料4的溶液3接触。分析检测的灵敏度可以 对于已经存在的荧光染料4而言，如果将吸收用于荧光染料4和/或其发光7的激发光6的掩蔽染料9添加到溶液3中和/或如果分离层 10可溶解并且吸收和/或反射激发光6或发射光7被施加到底部2处的电池层。分离层10必须被构成为使得其具有用于发光的高反射功率 类似地，这些过程原理也可以用于受体研究中用于在荧光或发光的定量光学分析中掩蔽干扰背景辐射 标记反应组分。 在这种情况下，反应容器1的底部2处的受体层12与其中溶解有荧光或发光配体13的溶液接触。 如果将吸收用于荧光染料的激发光6和/或其发光或遮光染料的掩蔽染料9加入到上清液3中，则可以显着改善分析检测的灵敏度和精度。代替掩蔽染料 在溶液3中或任选地作为另外的措施，可以将溶液3可透过并吸收和/或反射激发光6和/或发射光或发光的分离层10施加到细胞或受体层12 在底部2。

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