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    • 1. 发明授权
    • Diagnostic agents for the detection of proteolytic enzymes
    • 用于检测蛋白水解酶的诊断剂
    • US4278763A
    • 1981-07-14
    • US99180
    • 1979-11-30
    • Dieter BergerFranz BraunWerner GuthleinManfred KuhrWolfgang Werner
    • Dieter BergerFranz BraunWerner GuthleinManfred KuhrWolfgang Werner
    • C07D209/36C07D209/12C07D333/64C07K1/113C07K5/04C07K7/06C12Q1/37G01N33/48G01N33/50C12Q1/38
    • C12Q1/37C12Q2334/50
    • The present invention provides a diagnostic agent for the detection of proteolytic enzymes, comprising an absorbent carrier, a film layer, a powder mixture, a lyophilisate, a solution or a reagent tablet, containing at least one chromogen and an appropriate buffer substance, wherein the chromogen used is an indoxyl- and/or thioindoxyl-amino acid ester and/or peptide ester of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which can be the same or different, are hydrogen or halogen atoms, lower alkyl, lower alkoxy, aryl, aralkyl, aralkoxy, hydroxyl, carboxy, carboxy lower alkoxy, aralkoxycarbonyl, aralkyloxycarbonyl lower alkoxy, nitro or lower acylamino radicals, whereby two adjacent substituents can also represent an optionally halogenated fused benzene ring, X is a sulphur atom or an imino group optionally substituted by a lower alkyl, aryl, aralkyl or acyl radical, A is an amino acid or peptide residue and B is a nitrogen protective group conventional in peptide chemistry or derived therefrom.The present invention also provides new compounds of the above-given general formula and processes for the preparation thereof.Furthermore, the present invention is concerned with the use of the compounds of the above-given general formula for the production of diagnostic agents for the detection of proteolytic enzymes.
    • 本发明提供了用于检测蛋白水解酶的诊断剂,其包含含有至少一种色原体和适当的缓冲物质的吸收剂载体,膜层,粉末混合物,冻干物,溶液或试剂片剂,其中 使用的色原是通式为:其中R 1,R 2,R 3和R 4可以相同或不同,为氢或卤素原子的通式如下的吲哚氧基和/或硫代吲哚氧基 - 氨基酸酯和/或肽酯: 低级烷基,低级烷氧基,芳基,芳烷基,芳烷氧基,羟基,羧基,羧基低级烷氧基,芳烷氧基羰基,芳烷氧基羰基低级烷氧基,硝基或低级酰基氨基,其中两个相邻的取代基也可以表示任选卤代的稠合苯环,X是硫 原子或任选被低级烷基,芳基,芳烷基或酰基取代的亚氨基,A是氨基酸或肽残基,B是肽化学中常规的氮保护基或 从其衍生。 本发明还提供了上述给出的通式的新化合物及其制备方法。 此外,本发明涉及上述给出的通式的化合物用于产生用于检测蛋白水解酶的诊断剂的用途。
    • 3. 发明授权
    • Diagnostic composition for the detection of leukocytes and chromogens
useful therein
    • 用于检测其中有用的白细胞和色原体的诊断组合物
    • US4296202A
    • 1981-10-20
    • US63211
    • 1979-08-02
    • Dieter BergerFranz BraunGunter FreyWerner GuthleinManfred Kuhr
    • Dieter BergerFranz BraunGunter FreyWerner GuthleinManfred Kuhr
    • C09B43/20C09B43/18C09B43/28G01N33/50
    • C09B43/18G01N33/5094
    • Novel diagnostic composition for the detection of leukocytes in body fluids, comprising an absorbent carrier impregnated with a buffer substance and a chromgen, wherein the chromogen is an azo dyestuff ester of the formulaA--N.dbd.N--B(OR).sub.nwhereinA is a five- or six-membered heterocyclic radical of up to 2 hetero ring atoms selected from nitrogen, sulfur and oxygen, and wherein the heterocyclic ring may be substituted with at least one member of the group selected from halogen, lower alkyl and lower alkoxy; orA is phenyl substituted by at least one member of the group selected from lower alkyl, lower alkoxy, nitro, sulphanato and acylamino;B is benzene, naphthalene or quinolone, optionally substituted with one or two radicals selected from sulphanato, lower alkoxy and lower alkoxypoly-alkyleneoxy;R is a carboxylic acid residue or an amino acid or peptide residue having a nitrogen protective group; andn is 1 or 2.
    • 用于检测体液中白细胞的新型诊断组合物,其包含浸渍有缓冲物质和染色剂的吸收剂载体,其中所述色原是式AN = NB(OR)n的偶氮染料酯,其中A是五或 多至2个选自氮,硫和氧的杂环原子的六元杂环基,其中杂环可以被选自卤素,低级烷基和低级烷氧基中的至少一个基团取代; 或A是被选自低级烷基,低级烷氧基,硝基,磺酰基和酰氨基中的至少一个基团取代的苯基; B是苯,萘或喹诺酮,任选地被一个或两个选自磺酰基,低级烷氧基和低级烷氧基聚 - 亚烷氧基的基团取代; R是具有氮保护基团的羧酸残基或氨基酸或肽残基; n为1或2。
    • 8. 发明授权
    • Process for the detection of substances with hydrolase activity
    • 检测具有水解酶活性的物质的方法
    • US5202233A
    • 1993-04-13
    • US816795
    • 1992-01-03
    • Rupert HerrmannHans-Joachim GuderWerner GuthleinManfred KuhrJohann BergerHarvey Buck
    • Rupert HerrmannHans-Joachim GuderWerner GuthleinManfred KuhrJohann BergerHarvey Buck
    • C12Q1/34G01N33/58
    • C12Q1/34G01N33/581C12Q2334/30G01N2333/924Y10S435/805
    • A process for the detection of substances with hydrolase activity in a sample by mixing the sample with a hydrolase substrate and an oxidizing agent, and the evaluating the resultant color intensity, wherein, as hydrolase substrate, there is used at least one compound of the formula ##STR1## in which R.sup.1 is hydrogen or an alkoxy radical,R.sup.2 is hydrogen or halogen, an amino group or an alkoxy or aralkoxy radical,R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which can be the same or different, are hydrogen, halogen, carboxyl, a carbamoyl group, sulpho, an amino groups alkyl, an alkoxy radical, aralkoxy, alkylcarbonyl or alkoxycarbonyl, andX is a glycosyl, phosphate or acyl residue.Optionally R.sup.2 and R.sup.3, R.sup.3 and R.sup.4, R.sup.4 and R.sup.5, and R.sup.5 and R.sup.6 can be joined to form a ring system. At least one of R.sup.1 and R.sup.2 must be hydrogen and at least one of R.sup.1, R.sup.2 and R.sup.3 must not be hydrogen. Compounds in which X is .beta.-galactosyl are new.
    • 一种用于通过将样品与水解酶底物和氧化剂混合来检测样品中水解酶活性的物质并评估所得颜色强度的方法,其中作为水解酶底物,使用至少一种式 其中R 1是氢或烷氧基,R 2是氢或卤素,氨基或烷氧基或芳烷氧基,可以相同或不同的R 3,R 4,R 5和R 6是氢,卤素, 羧基,氨基甲酰基,磺基,氨基烷基,烷氧基,芳烷氧基,烷基羰基或烷氧基羰基,X是糖基,磷酸酯或酰基残基。 任选地,R 2和R 3,R 3和R 4,R 4和R 5以及R 5和R 6可以连接形成环系。 R 1和R 2中的至少一个必须是氢,R 1,R 2和R 3中的至少一个不能是氢。 X是β-半乳糖基的化合物是新的。