PEPTIDE SUB-LIBRARY KITS
    34.
    发明授权
    PEPTIDE SUB-LIBRARY KITS 失效
    肽在图书馆试台

    公开(公告)号:EP0642669B1

    公开(公告)日:1997-03-12

    申请号:EP93910302.4

    申请日:1993-05-20

    IPC分类号: G01N33/68

    摘要: The subjects of the invention are kits comprising free or support bound peptide mixtures (sub-libraries) as components, methods for their preparation and method for their use in discovery of bioactive peptides as potential drugs. Groups of free peptide mixtures (sub-libraries) forming components of the kit may carry different color or fluorescent labels facilitating their identification. The solid support in kits comprising support bound peptides may carry color or fluorescent labels as well, but the size or the specific gravity of the beads are also used as markers. The kits can be applied in all kinds of biological screening tests, including binding tests with macromolecules (like proteins), cells or tissues. The amino acid sequences of bioactive peptides can generally be determined in three stages: (i) determination of amino acid occurrence list by use of amino acid tester sub-kit, (ii) determination of occurrence library by use of the first sub-kit, and (iii) determination of sequences by use of second sub-kits.

    ANTI-SINN-OLIGONUKLEOTIDE ZUR AROMATASE-INHIBIERUNG
    36.
    发明公开
    ANTI-SINN-OLIGONUKLEOTIDE ZUR AROMATASE-INHIBIERUNG 失效
    反义寡核苷酸TO-芳香酶抑制

    公开(公告)号:EP0715632A1

    公开(公告)日:1996-06-12

    申请号:EP95924929.0

    申请日:1995-06-23

    IPC分类号: C12N15 A61K31 A61K48 A61P35 C07H21

    CPC分类号: C12N15/1137 C07H21/00

    摘要: The invention concerns an anti-sense oligonucleotide which is suitable for use in inhibiting the expression of aromatase, the anti-sense oligonucleotide being obtained by the following steps: a) construction of anti-sense oligonucleotides along the whole length of coding and regulating zones of aromatase DNA and/or transcripts thereof, the anti-sense oligonucleotides overlapping each other, b) incubation of an aromatase-expressing cell with one or more of the anti-sense oligonucleotides from a) and c) analysis of the inhibition of aromatase expression in the usual way, as well as identification of the anti-sense oligonucleotide(s) responsible. The invention also concerns a method of preparing such an anti-sense oligonucleotide as well as its use.

    FLUORESZENZBESTIMMUNG DER AKTIVITÄT LIPOLYTISCHER ENZYME
    37.
    发明公开
    FLUORESZENZBESTIMMUNG DER AKTIVITÄT LIPOLYTISCHER ENZYME 失效
    FLUORESZENZBESTIMMUNG DERAKTIVITÄTLIPOLYTISCHER ENZYME

    公开(公告)号:EP0710225A1

    公开(公告)日:1996-05-08

    申请号:EP95920070.0

    申请日:1995-05-19

    IPC分类号: C07C229 C09K11 C12Q1

    摘要: A fluorometric method was developed to determine the activity of lipases of animal, vegetable and microbial origin, in particular of lipases detectable in serum. For that purpose, fluorescent triglyceride analogues were synthesised in which an acyl or alkyl chain bears a fluorophore at the φ-end and another acyl or alkyl chain bears a fluorescence quencher. The fluorescent lipid is solubilised with amphiphiles in the form of liposomes, vesicles, micelles or emulsions in order to determine lipase activity. The fluorescent substrate may also be dissolved as such in an aqueous medium or be dissolved in organic solvents to be presented to the enzyme. The invention for the first time describes complexes of fluorescent triglycerides with appropriate proteins (for example albumin) in an aqueous medium as new substrate solubilisation forms for lipase analysis. The activity of lipolytic enzymes is determined through hydrolysis of the fluorescent substrate that results in a continuous increase in fluorescence intensity.

    摘要翻译: 开发了一种荧光测定方法来确定动物,植物和微生物来源的脂肪酶的活性,特别是在血清中可检测的脂肪酶的活性。 为此,合成了荧光甘油三酯类似物,其中酰基或烷基链在ω-end处带有荧光团,另一个酰基或烷基链带有荧光猝灭剂。 荧光脂质以脂质体,囊泡,胶束或乳液形式的两亲物溶解,以确定脂肪酶活性。 荧光底物也可以原样溶于水性介质中或溶于有机溶剂中以供给酶。 本发明首次描述了荧光甘油三酸酯与水性介质中适当蛋白质(例如白蛋白)的复合物,作为用于脂肪酶分析的新的底物溶解形式。 脂肪分解酶的活性通过荧光底物的水解测定,导致荧光强度的连续增加。

    1,4-BENZOTHIAZEPINE DERIVATIVE
    38.
    发明授权
    1,4-BENZOTHIAZEPINE DERIVATIVE 失效
    1,4-苯并吖庚因衍生物

    公开(公告)号:EP0565721B1

    公开(公告)日:1995-07-26

    申请号:EP92901899.2

    申请日:1991-12-27

    申请人: KANEKO, Noboru

    CPC分类号: C07D417/06 C07D417/14

    摘要: To provide a compound which inhibits the kinetic cell death of cardiac muscles without inhibiting cardiac functions. A 1,4-benzothiazepine derivative represented by general formula (I) and a pharmaceutically acceptable salt thereof, wherein R represents H or C1 to C3 lower alkoxy; X represents O or H2; n represents 1 or 2; R1 represents H, substituted phenyl (wherein the substituent is OH or C¿1? to C3 lower alkoxy), (a), C1 to C3 lower alkoxy, or (b) wherein R?2¿ represents C¿1? to C3 acyl; and ph represents phenyl.

    摘要翻译: 提供抑制心肌动力学细胞死亡而不抑制心脏功能的化合物。 由通式(I)表示的1,4-苯并硫氮杂衍生物及其药学上可接受的盐,其中R代表H或C1至C3低级烷氧基; X代表O或H 2; n代表1或2; R1代表H,取代的苯基(其中取代基是OH或C 1至C 3低级烷氧基),(a),C 1至C 3低级烷氧基,或(b)其中R 2'代表C 1〜 到C3酰基; 并且ph代表苯基。

    SPROUT INHIBITOR FOR POTATOES
    39.
    发明公开
    SPROUT INHIBITOR FOR POTATOES 失效
    发芽马铃薯产品。

    公开(公告)号:EP0653912A1

    公开(公告)日:1995-05-24

    申请号:EP94918387.0

    申请日:1994-06-03

    IPC分类号: A01N31 A01N37

    摘要: The invention relates to a sprout inhibitor for potatoes which, as the main component, contains rape oil methylester and/or specific long-chain alcohols, eventually in mixture with the medium- and/or long-chain alcohols known for said purpose, and/or ethereal oil and/or the known chemical sprout-inhibiting agents, or to the use of rape oil methylester alone or the use of C18 to > C36-alcohols such as Espum EGA 162 (now Dehysan) alone, or in a mixture with rape oil methylester and/or other known sprout-inhibiting agents.

    2-Aryl-1,3-propanediol and dioxane derivatives and their preparation
    40.
    发明公开
    2-Aryl-1,3-propanediol and dioxane derivatives and their preparation 失效
    衍生化2-芳基-1,3-丙二醇和二恶烷和Herstellung。

    公开(公告)号:EP0641757A1

    公开(公告)日:1995-03-08

    申请号:EP94113242.5

    申请日:1994-08-24

    申请人: KURARAY Co. LTD.

    摘要: A compound that can be converted, at a low cost and in a simple way, into 2-aryl-1,3-propanediols serving as precursors for synthesizing felbamate acting as an antiepileptic has a structure represented by Formula (1):

    wherein Ar represents an aryl group; R¹ represents a hydrogen atom or is R⁴ or R⁵, where R⁴ represents an alkoxy group having 1 to 10 carbon atoms and R⁵ represents a hydroxy group or an acyloxy group having 1 to 10 carbon atoms; and R² and R³ are hydrogen atoms at the same time or R² and R³ together form a group represented by Formula (2):

    wherein R⁶ and R⁷ each independently represent a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, or R⁶ and R⁷ together form an oligomethylene group having 2 to 10 carbon atoms.

    摘要翻译: 可以以低成本和简单的方式转化成用作合成作为抗癫痫药的纤维蛋白酸的前体的2-芳基-1,3-丙二醇的化合物具有由式(1)表示的结构: 其中Ar表示芳基; R 1表示氢原子或R 4或R 5,其中R 4表示具有1〜10个碳原子的烷氧基,R 5表示羟基或具有1个 至10个碳原子; R 2和R 3同时为氢原子或R 2和R 3一起形成由式(2)表示的基团:其中R 6和R 7为 >各自独立地表示氢原子或具有1〜5个碳原子的烷基,或者R 6和R 7一起形成具有2〜10个碳原子的低聚亚乙基。