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1. 发明授权

US4622389A Novel substrate for determining the activity of blood coagulation factor Xa (Stuart-Prower factor) 失效
标题翻译：确定凝血因子Xa活性的新型底物（Stuart-Prower因子）
公开(公告)号：US4622389A
公开(公告)日：1986-11-11
申请号：US732396
申请日：1985-05-09
申请人： Takeshi Nagasawa , Yoshio Nakamura , Tsuyoshi Enomoto , Katsumasa Kuroiwa
发明人： Takeshi Nagasawa , Yoshio Nakamura , Tsuyoshi Enomoto , Katsumasa Kuroiwa
IPC分类号： G01N33/86 , C07K5/08 , C07K14/745 , C07K14/755 , C12Q1/56
CPC分类号： C12Q1/56 , C12Q2337/10 , G01N2333/96444 , Y10S530/802
摘要： A novel chromogenic and fluorescent substrate for determining the activity of blood coagulation factor Xa and Xa-like enzymes. The novel substrate according to the present invention has very excellent selectivity as compared with the hitherto disclosed substrates and enables specific determination of blood coagulation factor Xa. The present substrate is therefore useful for the studies of chemical reactions involving formation, inhibition and consumption of factor Xa and can be also used for the determination of various factors associated therewith such as factor X, anti-Xa factor, factor VII, factor VIII, factor IX and heparin.
摘要翻译：一种用于测定凝血因子Xa和Xa样酶的活性的新型显色和荧光底物。根据本发明的新型底物与迄今为止公开的基材相比具有非常优异的选择性，并能够进行血液凝固因子Xa的特异性测定。因此，本底物可用于涉及形成，抑制和消耗因子Xa的化学反应的研究，并且还可用于测定与其相关的各种因素，如因子X，抗Xa因子，因子VII，因子VIII，因子IX和肝素。

2. 发明授权

US4877727A Substrate for determining leucine aminopeptidase or gamma-glutamyltranspeptase activity 失效
标题翻译：用于测定亮氨酸氨基肽酶或γ-谷氨酰转肽酶活性的底物
公开(公告)号：US4877727A
公开(公告)日：1989-10-31
申请号：US248347
申请日：1988-09-20
申请人： Akira Miike , Yukio Katsumata , Toshio Tatano
发明人： Akira Miike , Yukio Katsumata , Toshio Tatano
IPC分类号： C12Q1/37 , C12Q1/48
CPC分类号： C12Q1/48 , C12Q1/37 , C12Q2337/10
摘要： Leucine aminopeptidase (LAP) activity or .gamma.-glutamyltranspeptidase (.gamma.-GTP) activity in a sample is determined by converting a substrate represented by the formula (I): ##STR1## wherein Z represents (CH.sub.3).sub.2 CHCH.sub.2 CH(NH.sub.2)--or (NH.sub.2)(COOH) CHCH.sub.2 CH.sub.2 --, R.sub.1 represents hydrogen, alkyl or substituted alkyl, R.sub.2 represents alkylene or hydroxyalkylene, R.sub.3 and R.sub.4 are the same or different and represents hydrogen, halogen, nitro, hydroxyl, sulfo, carboxyl, alkyl, and alkoxy, and salts thereof into a compound represented by the formula (II): ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the same meanings as defined above. The compound (II) is reacted with a chromogen to form a pigment or converted into a diazonium salt which is reacted with a coupling agent to form an azo dye. Absorption of a resultant colored reaction solution is measured.
摘要翻译：通过转化由式（I）表示的底物来确定样品中的亮氨酸氨基肽酶（LAP）活性或γ-谷氨酰转肽酶（γ-GTP）活性：其中Z表示（CH 3）2 CHCH 2 CH（NH 2） - 或（NH 2）（COOH）CHCH 2 CH 2 - ，R 1表示氢，烷基或取代的烷基，R 2表示亚烷基或羟基亚烷基，R 3和R 4相同或不同，表示氢，卤素，硝基，羟基，磺基，羧基，烷基和（II）表示的化合物：其中R 1，R 2，R 3和R 4具有与上述相同的含义。使化合物（II）与色原反应形成颜料或转化为重氮盐，其与偶联剂反应以形成偶氮染料。测量所得有色反应溶液的吸收。

3. 发明授权

US4520100A Method for measuring thrombin 失效
标题翻译：凝血酶测定方法
公开(公告)号：US4520100A
公开(公告)日：1985-05-28
申请号：US578805
申请日：1984-02-10
申请人： Takeshi Nagasawa , Katsumasa Kuroiwa , Katsuyuki Takabayashi
发明人： Takeshi Nagasawa , Katsumasa Kuroiwa , Katsuyuki Takabayashi
IPC分类号： C07K5/02 , C07K5/08 , C07K5/083 , C07K5/087 , C12Q1/00 , C12Q1/56 , C12Q1/38
CPC分类号： C07K5/0804 , C07K5/0812 , C12Q1/56 , C12Q2337/10 , G01N2333/974
摘要： A novel substrate for measuring thrombin which has chromophoric and fluorescent properties on thrombin or a thrombin-like enzymes and is represented by a compound of the following general formula or a salt thereof: ##STR1## wherein R represents ##STR2##

4. 发明授权

US4508644A Chromogenic compounds, a process for their preparation and their use 失效
标题翻译：显色化合物，其制备方法及其用途
公开(公告)号：US4508644A
公开(公告)日：1985-04-02
申请号：US554942
申请日：1983-11-25
申请人： Helmut Heber , Reinhard Eberle , Volker Teetz
发明人： Helmut Heber , Reinhard Eberle , Volker Teetz
IPC分类号： G01N33/52 , C07K1/06 , C07K5/00 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/097 , C07K5/10 , C07K5/103 , C07K5/117 , C07K7/06 , C07K14/745 , C12Q1/37 , C12Q1/56 , G01N33/50 , C07C103/52
CPC分类号： C07K7/06 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/1002 , C07K5/101 , C07K5/1024 , C12Q1/37 , C12Q1/56 , C12Q2337/10 , C12Q2337/12 , Y02P20/55 , Y10S930/28
摘要： Chromogenic compounds of the formula I ##STR1## and a process for their preparation are described, X denoting a hydrogen atom, a protective group customarily used in peptide chemistry or a group which irreversibly blocks the terminal amino group,A and P being identical or different and denoting an alpha-, beta- or gamma-amino acid which is composed of 2 to 15 carbon atoms with up to 3 nitrogen atoms, 2 sulfur atoms and 6 oxygen atoms, the side-chain of which can be substituted, and P also denoting a dipeptide formed from amino acids of these types,B denoting arginine, homoarginine, lysine, homolysine, ornithine or histidine andR denoting a substituent in the 2- or 3-position.The compounds can be used as substrates for the detection and the quantitative determination of hydrolytic enzymes of enzyme class 3.4.21.
摘要翻译：描述了式I（I）的显色化合物及其制备方法，X表示氢原子，肽化学中通常使用的保护基或不可逆阻断末端氨基的基团，A和P为相同或不同，并且表示由具有至多3个氮原子，2个硫原子和6个氧原子的2至15个碳原子组成的α-，β-或γ-氨基酸，其侧链可以被取代，并且P还表示由这些类型的氨基酸形成的二肽，B表示精氨酸，高精氨酸，赖氨酸，高赖氨酸，鸟氨酸或组氨酸，R表示2-或3-位的取代基。该化合物可用作酶类3.4.21的水解酶的检测和定量测定的底物。

5. 发明授权

US4275153A Analytical fluorogenic substrates for proteolytic enzymes 失效
标题翻译：用于蛋白水解酶的分析荧光底物
公开(公告)号：US4275153A
公开(公告)日：1981-06-23
申请号：US930826
申请日：1978-08-03
申请人： Robert J. Gargiulo , Gary A. Mitchell , Patricia M. Hudson , Sharon P. Pochron , Rolf M. Huseby , Robert E. Smith
发明人： Robert J. Gargiulo , Gary A. Mitchell , Patricia M. Hudson , Sharon P. Pochron , Rolf M. Huseby , Robert E. Smith
IPC分类号： C07K5/083 , C07K5/087 , C07K5/093 , C07K5/097 , C07K5/103 , C12Q1/37 , C12Q1/56 , C12Q1/36 , C07G7/00 , C12Q1/38
CPC分类号： C07K5/0823 , C07K5/0804 , C07K5/0812 , C07K5/0819 , C07K5/1013 , C12Q1/37 , C12Q1/56 , C12Q2337/10 , C12Q2337/30 , G01N2333/968 , G01N2333/974 , G01N2400/40 , Y10S530/802 , Y10S930/28
摘要： Fluorogenic substrates for proteolytic enzymes having the formula: ##STR1## or acid salts thereof wherein: R.sub.1 is hydrogen-L, hydrogen-D, benzoyl, benzenesulfonyl, glutaryl, pyroglutamyl, carbobenzoxy, D-serine, or carbobenzoxy-serine;R.sub.2 is hydrogen, phenyl, a straight, branched or cyclic alkyl having 1 to 4 carbons, or propionic acid;R.sub.3 is hydrogen, straight or branched or cyclic alkyl having 1 to 4 carbons, 4-aminobutane, or 3-guanidylpropane;R.sub.4 is methyl, 4-aminobutane, or 3-guanidylpropane;R.sub.5 is a fluorogenic moiety, severable from said compound by a proteolytic enzyme and having different fluorescent property when severed from said compound than when forming part of said compound.The enzymes, when reacting with the substrate, remove the fluorogenic group R.sub.5 producing an increase in its fluorescence. The increase of the fluorescence is an indication of the activity of the enzyme present. Specific enzymes thusly detectable include plasmin, thrombin, the factors X.sub.a, XI.sub.a, & XII.sub.a, kallikrein, trypsin, elastase, urokinase, and cathepsin B.sub.1.
摘要翻译：用于具有下式的蛋白水解酶的荧光底物：其中：R 1是氢-L，氢-D，苯甲酰基，苯磺酰基，戊二酰基，焦谷氨酰基，苄氧羰基，D-丝氨酸或苄氧羰基丝氨酸; R2是氢，苯基，具有1-4个碳原子的直链，支链或环状烷基或丙酸; R3是氢，具有1至4个碳的直链或支链或环状烷基，4-氨基丁烷或3-胍基丙烷; R4是甲基，4-氨基丁烷或3-胍基丙烷; R5是荧光部分，当与所述化合物形成一部分时，所述化合物与蛋白水解酶可从所述化合物中分离，并且在从所述化合物切断时具有不同的荧光特性。

6. 发明申请

US20030044877A1 Novel enzymatic substrates for detecting pseudomonas aeruginosa, compositions containing same and method for detecting said species 有权
标题翻译：用于检测铜绿假单胞菌的新型酶底物，含有其的组合物和用于检测所述物种的方法
公开(公告)号：US20030044877A1
公开(公告)日：2003-03-06
申请号：US10148327
申请日：2002-05-29
发明人： Mireille Desmonceaux , Daniel Monget
IPC分类号： C12Q001/37 , C12Q001/04 , C07D311/02
CPC分类号： C12Q1/04 , C07C237/04 , C07D209/40 , C07D311/16 , C12Q1/37 , C12Q2326/90 , C12Q2337/10 , C12Q2337/12 , C12Q2337/22 , C12Q2337/30
摘要： This invention concerns an enzyme substrate consisting of a target part and a marker part, hydrolysis of the substrate leading to separation of the target part from the marker part, and said target part being specific for the enzyme activity being assayed. It also concerns a formulation containing at least one such substrate, and a method for detecting the bacterial species Pseudomonas aeruginosa. The target part of the substrate is specific for null-alanine aminopeptidase activity and the marker part is a compound which reveals whether a hydrolysis reaction has taken place or not. The invention is particularly applicable in the field of diagnosis.
摘要翻译：本发明涉及由目标部分和标记部分组成的酶底物，底物的水解导致目标部分与标记部分的分离，并且所述目标部分对被测定的酶活性是特异性的。它还涉及含有至少一种这样的底物的制剂，以及用于检测细菌种类铜绿假单胞菌的方法。底物的目标部分对β-丙氨酸氨基肽酶活性是特异性的，标记部分是揭示水解反应是否发生的化合物。本发明特别适用于诊断领域。

7. 发明授权

US4675290A Assaying peptidase enzyme activity 失效
标题翻译：测定肽酶活性
公开(公告)号：US4675290A
公开(公告)日：1987-06-23
申请号：US713242
申请日：1985-03-18
申请人： Kunio Matsumoto , Yoshitaka Kagimoto , Tsutomu Hirata , Susumu Watanabe , Akira Ohtsuka , Kiyoharu Takahashi
发明人： Kunio Matsumoto , Yoshitaka Kagimoto , Tsutomu Hirata , Susumu Watanabe , Akira Ohtsuka , Kiyoharu Takahashi
IPC分类号： C12Q1/26 , C12Q1/37 , C12Q1/52 , C12Q1/36
CPC分类号： C12Q1/52 , C12Q1/26 , C12Q1/37 , C12Q2337/10 , Y10S435/817
摘要： A method for assay of enzyme activity which comprises treating an amide compound of the formula ##STR1## with peptidase; treating thus-liberated amine of the formula ##STR2## with an oxidase which consume oxygen and forms pigment by oxidative condensation of said amine with a coupler of the formula ##STR3## and quantitatively measuring the detectable changes. Also disclosed is an assay method which comprises treating an amide compound of the formula ##STR4## or a salt thereof, with peptidase to liberate an aniline derivative of the formula ##STR5## oxidizing said aniline derivative; and quantitatively measuring detectable change.
摘要翻译：一种测定酶活性的方法，其包括用肽酶处理式“酰基”的酰胺化合物; 用消耗氧气的氧化酶处理如此释放的式“IMAGE”的胺，并通过所述胺与式“IMAGE”的成色剂的氧化缩合形成颜料并定量测量可检测的变化。还公开了一种测定方法，其包括用肽酶处理式IMA的酰胺化合物或其盐，以释放氧化所述苯胺衍生物的式IMA的苯胺衍生物; 并定量测量可检测的变化。

8. 发明授权

US4452736A Substrates for measuring plasmin 失效
标题翻译：用于测量纤溶酶的底物
公开(公告)号：US4452736A
公开(公告)日：1984-06-05
申请号：US417377
申请日：1982-09-13
申请人： Takeshi Nagasawa , Katsumasa Kuroiwa , Katsuyuki Takabayashi , Yoshio Nakamura
发明人： Takeshi Nagasawa , Katsumasa Kuroiwa , Katsuyuki Takabayashi , Yoshio Nakamura
IPC分类号： G01N33/52 , C07K5/083 , C07K5/09 , C07K5/093 , C12Q1/37 , C12Q1/56 , G01N33/50 , C07C103/52
CPC分类号： C07K5/0808 , C07K5/0806 , C07K5/0815 , C07K5/0819 , C12Q1/37 , C12Q2337/10 , C12Q2337/12 , G01N2333/968
摘要： A novel substrate for measuring plasmin which has chromophoric and fluoroescent properties against plasmin or a plasmin-like enzyme, which is characterized by being a compound of the formula or a salt thereof: ##STR1## wherein ##STR2## wherein ##STR3## .
摘要翻译：一种用于测量纤溶酶的新型底物，其具有针对纤溶酶或纤溶酶样酶的发色和荧光特性，其特征在于下式化合物或其盐：其中m = 1,2,3或4，其中R1 = （n = 0,1,2或3，R3 = H或CH3），（CH2）nCH（CH3）2（n = 0,1,2或3 R2 =（CH2）n + 1CH3（n = 0,1,2或3）图像（n = 0,1,2或3，R4，R4和R4“为H或CH3）。

9. 发明授权

US4336186A Analytical fluorogenic substrates for proteolytic enzymes 失效
标题翻译：用于蛋白水解酶的分析荧光底物
公开(公告)号：US4336186A
公开(公告)日：1982-06-22
申请号：US232942
申请日：1981-02-09
申请人： Robert J. Gargiulo , Gary A. Mitchell , Patricia M. Hudson , Sharon P. Pochron , Rolf M. Huseby , Robert E. Smith
发明人： Robert J. Gargiulo , Gary A. Mitchell , Patricia M. Hudson , Sharon P. Pochron , Rolf M. Huseby , Robert E. Smith
IPC分类号： C07K5/083 , C07K5/087 , C07K5/093 , C07K5/097 , C07K5/103 , C12Q1/37 , C12Q1/56 , C07C103/52
CPC分类号： C07K5/0823 , C07K5/0804 , C07K5/0812 , C07K5/0819 , C07K5/1013 , C12Q1/37 , C12Q1/56 , C12Q2337/10 , C12Q2337/30 , G01N2333/968 , G01N2333/974 , G01N2400/40 , Y10S530/802 , Y10S930/28
摘要： Fluorogenic substrates for proteolytic enzymes having the formula: ##STR1## or acid salts thereof wherein: R.sub.1 is hydrogen-L, hydrogen-D, benzoyl, benzenesulfonyl, glutaryl, pyroglutamyl, carbobenzoxy, D-serine, or carbobenzoxy-serine;R.sub.2 is hydrogen, phenyl, a straight, branched or cyclic alkyl having 1 to 4 carbons, or propionic acid;R.sub.3 is hydrogen, straight or branched or cyclic alkyl having 1 to 4 carbons, 4-aminobutane, or 3-guanidylpropane;R.sub.4 is methyl, 4-aminobutane, or 3-guanidylpropane;R.sub.5 is a fluorogenic moiety, severable from said compound by a proteolytic enzyme and having different fluorescent property when severed from said compound than when forming part of said compound.The enzymes, when reacting with the substrate, remove the fluorogenic group R.sub.5 producing an increase in its fluorescence. The increase of the fluorescence is an indication of the activity of the enzyme present. Specific enzymes thusly detectable include plasmin, thrombin, the factors X.sub.a, XI.sub.a, and XII.sub.a, kallikrein, trypsin, elastase, urokinase, and cathepsin B.sub.1.
摘要翻译：用于具有下式的蛋白水解酶的荧光底物：其中：R 1是氢-L，氢-D，苯甲酰基，苯磺酰基，戊二酰基，焦谷氨酰基，苄氧羰基，D-丝氨酸或苄氧羰基丝氨酸; R2是氢，苯基，具有1-4个碳原子的直链，支链或环状烷基或丙酸; R3是氢，具有1至4个碳的直链或支链或环状烷基，4-氨基丁烷或3-胍基丙烷; R4是甲基，4-氨基丁烷或3-胍基丙烷; R5是荧光部分，当与所述化合物形成一部分时，所述化合物与蛋白水解酶可从所述化合物中分离，并且在从所述化合物切断时具有不同的荧光特性。酶与底物反应时，除去荧光基团R5，产生荧光增加。荧光的增加是酶存在的活性的指示。因此可检测的特异性酶包括纤溶酶，凝血酶，因子Xa，XIa和XIIa，激肽释放酶，胰蛋白酶，弹性蛋白酶，尿激酶和组织蛋白酶B1。

10. 发明授权

US4209459A Novel L-leucyl-4-hydroxyanilide derivatives 失效
标题翻译：新型L-亮氨酰-4-羟基苯胺衍生物
公开(公告)号：US4209459A
公开(公告)日：1980-06-24
申请号：US36094
申请日：1979-05-04
申请人： Takeshi Nagasawa , Katsumasa Kuroiwa , Tadami Akatsuka , Osamu Kodama , Mitoshi Shimamoto
发明人： Takeshi Nagasawa , Katsumasa Kuroiwa , Tadami Akatsuka , Osamu Kodama , Mitoshi Shimamoto
IPC分类号： C07C237/04 , C07C67/00 , C07C301/00 , C07C309/51 , C12Q1/37 , C07C143/44 , C07C101/72
CPC分类号： C12Q1/37 , C12Q2337/10
摘要： Novel L-leucyl-4-hydroxyanilide derivatives of the formula, ##STR1## wherein R represents a carboxyl group or a sulfo group or an acid addition salt thereof, which are useful for assay of leucine-aminopeptidase activity.
摘要翻译：新颖的下式的L-亮氨酰-4-羟基苯胺衍生物，其中R表示羧基或磺基或其酸加成盐，可用于测定亮氨酸 - 氨基肽酶活性。

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