Substituted 1,8-naphthyridines and their use in medicaments
    31.
    发明授权
    Substituted 1,8-naphthyridines and their use in medicaments 失效
    取代的1,8-萘啶并用于药物

    公开(公告)号:US5034399A

    公开(公告)日:1991-07-23

    申请号:US496757

    申请日:1990-03-21

    CPC classification number: C07D471/04

    Abstract: Inhibitors of 3-hydrooxy-3-methyl-glutarylcoenzyme A reductase which are 1,8-naphthyridines of the formula ##STR1## in which Arepresents a 3- to 7-membered heterocycle which is optionally substituted, or aryl which is optionally substituted,Brepresents cycloalkyl or alkyl which is optionally substituted, aryl which is optionally substituted,D and E are identical or different andrepresents hydrogen, halogen, mercapto, hydroxyl, alkoxy, alkyl which is optionally substituted, or a group of the formula --NR.sup.1 R.sup.2, aryl, aryloxy or arylthio having 6 to 10 carbon atoms, which is optionally substituted,Yrepresents a group of the formula ##STR2## in which Jdenotes hydrogen, hydroxyl, mercapto or halogen, or alkyl, alkoxy or alkylthio which are optionally substituted, aryloxy, benzyloxy or arylthio or a group of the formula --NR.sup.1 R.sup.2,Zdenotes oxygen or sulphur,Gdenotes hydrogen, alkyl or alkenyl which is optionally substituted,Xrepresents a group of the formula --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,andRrepresents a group of the formula ##STR3## in which R.sup.5denotes hydrogen or alkyl, andR.sup.6denotes hydrogen or alkyl, which may be substituted by phenyl, ordenotes aryl or a cation,and their salts.

    Abstract translation: 作为式“IMAGE”的1,8-萘啶的3-羟基-3-氧代-3-甲基 - 戊二酰辅酶A还原酶的抑制剂,其中A表示任选取代的3-至7-元杂环,或任选取代的芳基, B代表任选取代的环烷基或烷基,任选取代的芳基,D和E相同或不同,代表氢,卤素,巯基,羟基,烷氧基,任选被取代的烷基,或式-NR1R2的基团, 芳基,芳氧基或具有6至10个碳原子的芳硫基,其任选被取代,Y表示下式的基团,其中J表示氢,羟基,巯基或卤素,或任选被取代的烷基,烷氧基或烷硫基, 芳氧基,苄氧基或芳硫基或式-NR1R2的基团,Z表示氧或硫,G表示氢,任选被取代的烷基或烯基,X表示式-CH 2 -CH 2 - 或-CH = CH- ,和R 表示式为“IMAGE”的基团,其中R5表示氢或烷基,R6表示氢或可被苯基取代的烷基,或表示芳基或阳离子及其盐。

    Pharmaceutical compositions containing a saccharase inhibitor
    34.
    发明授权
    Pharmaceutical compositions containing a saccharase inhibitor 失效
    含有SACCHARASE抑制剂的药物组合物

    公开(公告)号:US3937817A

    公开(公告)日:1976-02-10

    申请号:US481224

    申请日:1974-06-20

    CPC classification number: C12P1/06 A61K38/005 C07K14/365 Y10S435/827

    Abstract: The invention relates to a saccharase inhibitor derived from Actinoplanaceae Strain CBS 961.70, including mutants and variants thereof, means for the production of said saccharase inhibitors comprising cultivation of Actinoplanaceae Strain CBS 961.70, including mutants and variants thereof, in appropriate nutrient solutions which are characterized by being starch free under conditions most favorable to growth and production of said saccharase inhibitor and recovering a saccharase inhibitor from culture broths of said nutrient solutions, as well as the use of said inhibitor in pharmaceutically acceptable therapeutic compositions suitable for use in the treatment and relief of conditions indicative of adiposity, diabetes, pre-diabetes, hyperlipaemia (atherosclerosis), caries and the like.

    Masking of the background fluorescence and luminescence in the optical analysis of biomedical assays
    35.
    发明授权
    Masking of the background fluorescence and luminescence in the optical analysis of biomedical assays 有权
    在生物医学测定的光学分析中掩盖背景荧光和发光

    公开(公告)号:US08178359B2

    公开(公告)日:2012-05-15

    申请号:US09966522

    申请日:2001-09-28

    Abstract: A process for the quantitative optical analysis of fluorescently labeled biological cells involves contacting a cell layer on a transparent support at the bottom of a reaction vessel with a solution containing the fluorescent dye. This process can also be used for improving the sensitivity in the quantitative optical analysis of a luminescent biological cell layer. 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 at the bottom of a reaction vessel is in contact with a solution in which a fluorescent or luminescent ligand is dissolved.

    Abstract translation: 用于荧光标记的生物细胞的定量光学分析的方法包括使反应容器底部的透明支持体上的细胞层与含有荧光染料的溶液接触。 该方法也可用于提高发光生物细胞层的定量光学分析中的灵敏度。 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标记的反应组分的定量光学分析中掩蔽干扰背景辐射。 在这种情况下,反应容器底部的受体层与荧光或发光配体溶解的溶液接触。

    MASKING BACKGROUND FLUORESCENCE AND LUMINESCENCE IN THE OPTICAL ANALYSIS OF BIOMEDICAL ASSAYS

    公开(公告)号:US20080318270A1

    公开(公告)日:2008-12-25

    申请号:US12199317

    申请日:2008-08-27

    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. This process can also be used for improving the sensitivity in the quantitative optical analysis of a luminescent biological cell layer. The separating layer 10 must in this case 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 (supernatant 3) 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 (in the case of luminescent ligands) 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.

    Masking of the background fluorescence and luminescence in the optical analysis of biomedical assays
    37.
    发明授权
    Masking of the background fluorescence and luminescence in the optical analysis of biomedical assays 有权
    在生物医学测定的光学分析中掩盖背景荧光和发光

    公开(公告)号:US07138280B2

    公开(公告)日:2006-11-21

    申请号:US10263607

    申请日:2002-10-03

    Abstract: In a process for the quantitative optical analysis of biological cells labelled with a fluorescent dye, the sensitivity of analytical detection can be considerably improved if a masking dye, which absorbs the excitation light for the fluorescent dye and/or its emission light is added to the solution surrounding the biological cells and/or if a separating layer permeable to the solution and absorbing and/or reflecting the excitation light or the emission light is applied to a layer of the biological cells at the bottom of a reaction vessel. This process can also be used for improving the sensitivity in the quantitative optical analysis of a luminescent biological cell layer. 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.

    Abstract translation: 在用荧光染料标记的生物细胞的定量光学分析的过程中,如果将吸收荧光染料的激发光和/或其发射光的掩蔽染料加入到分析检测的灵敏度,则可以显着改善 并且或者如果对溶液可渗透并且吸收和/或反射激发光或发射光的分离层被施加到反应容器底部的生物细胞层。 该方法也可用于提高发光生物细胞层的定量光学分析中的灵敏度。 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标记的反应组分的定量光学分析中掩蔽干扰背景辐射。

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