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1. 发明专利

JPS6119635A Cytotoxic substance and protein complex 失效
标题翻译：细胞毒性物质和蛋白质复合物
公开(公告)号：JPS6119635A
公开(公告)日：1986-01-28
申请号：JP14015884
申请日：1984-07-05
申请人： Sumitomo Chem Co Ltd
发明人： MURAKAMI YOSHIAKI , SHIBA KUNIO , SHIYOUNO FUMIAKI , YOSHITAKE AKIRA
IPC分类号： C08G81/00
摘要： PURPOSE: The titled complex useful as a target-directing carcino-static agent, prepared by binding a physiologically active protein with a specified polysuccinimide derivative through mercapto groups.
CONSTITUTION: A cytotoxic substance/physiologically active protein complex is obtained by binding the mercapto groups of a physiologically active protein (e.g., urokinase) with the mercapto groups of a polysuccinimide derivative of an average MW of 2,000W1,000,000 comprising the structural units of formulas I WVI [wherein X is a reaction residue of a cytotoxic substance having an amino or imino group in the molecule, Y is a water-soluble aliphatic primary amine residue, Z is H or a group of the formula: Z' (when Z is H, one -SH group represented by -SZ, together with another -SH group can form an intramolecular or intermolecular -S-S- bond in equilibrium, these are represented inclusively by -SH), and Z' is a group which, together with an adjacent S, can form a reactive disulfide], wherein the numbers of said structural units of formulas I WVI are m, l, r, p, and q which are each 0 or a natural number and satisfy the relationships of formulas VII and VIII.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：标题化合物可用作通过巯基与特定的聚琥珀酰亚胺衍生物结合生理活性蛋白质而制备的靶向靶向抗癌剂。构成：通过将生理活性蛋白质（例如尿激酶）的巯基与平均MW为2,000-1,000,000的聚琥珀酰亚胺衍生物的巯基结合，获得细胞毒性物质/生理活性蛋白质复合物，其包含式I的结构单元 -VI [其中X是分子中具有氨基或亚氨基的细胞毒性物质的反应残基，Y是水溶性脂族伯胺残基，Z是H或下式的基团Z'（当Z是 H，由-SZ表示的一个-SH基团与另一个-SH基团可以在平衡中形成分子内或分子间-SS-键，这些由-SH包括），Z'是与相邻的S可以形成活性二硫化物]，其中式I-VI的所述结构单元的数目为m，l，r，p和q，其各自为0或自然数，并且满足式VII和VIII的关系。

2. 发明专利

JPS59215321A Reactive polymer having bound bifunctional ligand 失效
标题翻译：具有双重功能配体的反应性聚合物
公开(公告)号：JPS59215321A
公开(公告)日：1984-12-05
申请号：JP9121783
申请日：1983-05-23
申请人： Sumitomo Chem Co Ltd
发明人： MURAKAMI YOSHIAKI , SHIBA KUNIO , YOSHITAKE AKIRA , TAKAHASHI HIROYOSHI , UEDA NOBUO , HAZUE MASAAKI
IPC分类号： C08G73/00 , A61K51/00 , A61K51/08 , A61K51/10 , C08G69/48 , C08G73/10
CPC分类号： C08G73/1092 , A61K51/088 , A61K51/1093 , A61K2123/00 , C08G69/48 , Y10S514/802 , Y10S514/836
摘要： PURPOSE: The titled reactive polymer useful in the production of a radioactive metal-bound radiodiagnostic agent for nuclear-medical applications for detection of a particular disease, comprising a specified polysuccinimide derivative.
CONSTITUTION: A polysuccinimide of formula I (wherein k is a natural number) is reacted with an amino group-containing bifunctional ligand compound, a compound of formula II (wherein W is a lower alkylene, Z is H or a group which forms, together with the adjacent S, an active disulfide, and which, when Z is H, may form together with another -SH, an intramolecular or intermolecular -S-S- bond in equilibrium, these are covered by -SH), and optionally, a water-soluble aliphatic amine to obtain a polysuccinimide derivative having an MW (in terms of globular protein) of 2,000W1,000,000 and represented by formula III (wherein X is the residue of component B, Y is a water-soluble aliphatic prim. amine residue, n, m, l, r, p, and q are each 0 or a natural number representing the number of repeating units, m+n≥2, and 0.001≤p+q/n+m+l+r+p+q≤0.50).
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：用于生产用于检测特定疾病的核医学应用的放射性金属结合放射诊断剂的标题反应性聚合物，其包含特定的聚琥珀酰亚胺衍生物。构成：将式I的聚琥珀酰亚胺（其中k为天然数）与含氨基的双官能配体化合物，式II化合物（其中W为低级亚烷基，Z为H或一起形成的基团）反应与相邻的S是活性二硫化物，当Z是H时，它们可以与另一个-SH，分子内或分子间-SS-键平衡形成，这些被-SH覆盖），并且任选地，可溶性脂族胺，得到MW（以球状蛋白质计）为2,000-1,000,000并由式III表示的聚琥珀酰亚胺衍生物（其中X为组分B的残基，Y为水溶性脂族基团，胺残基，n ，m，l，r，p和q分别为0或表示重复单元数的自然数，m + n> = 2，0.001 <= p + q / n + m + 1 + r + p + q <= 0.50）。

3. 发明专利

JPS59211861A Preparation of enzyme labeled oxy-toxin for measuring oxy-toxin 失效
标题翻译：用于测量氧化铁的酶标签氧化铁的制备
公开(公告)号：JPS59211861A
公开(公告)日：1984-11-30
申请号：JP8715783
申请日：1983-05-17
申请人： Sumitomo Chem Co Ltd
发明人： YASUDA TAEKO , MOURI ZENICHI , MURAKAMI YOSHIAKI , TANIZAWA OSAMU
IPC分类号： G01N33/53 , C07K1/113 , C07K7/16 , C07K14/00 , C07K14/575 , C07K19/00 , C12Q1/34 , G01N33/535
CPC分类号： G01N33/535
摘要： PURPOSE:To obtain enzyme labeled oxy-toxin for enabling highly sensitive quantitative analysis of oxy-toxin, by reacting a specific chemical coupling agent and oxy-toxin while bonding specific enzyme to the resulting reaction product. CONSTITUTION:A coupling agent represented by formula I (wherein X is a functional group capable of forming a sulfide bond or a disulfide bond upon reaction with SH of protein, A is a lower alkylene group and Y is COOH or a reactive derivative thereof), for example, a chemical coupling agent selected from compounds shown by formulae II, III is reacted with oxy-toxin (parts posterior hypophysis hormone), if necessary, in the presence of a condensing agent such as water-soluble carbodiimide to form a composite. beta-D-galactositase is bonded to this composite to obtain enzyme labeled oxy- toxin. On the other hand, a rabbit is immunized with a composite obtained by bonding oxy-toxin to albumin to obtain anti-serum. An oxy-toxin-containing specimen, enzyme labeled oxy-toxin and anti-serum are reacted while the formed precipitate is added to a substrate to measure enzymatic activity. This measured value is compared with a caliburation curve preliminarily calculated from known oxy-toxin specimens to enable the quantitative analysis of oxy-toxin in a specimen with good accuracy.
摘要翻译：目的：为了获得酶标记的氧 - 毒素，通过使特定的化学偶联剂和氧 - 毒素反应，将特异性酶与所得的反应产物结合，从而实现对氧 - 毒素的高敏感定量分析。构成：由式I表示的偶联剂（其中X是能与蛋白质与SH反应形成硫键或二硫键的官能团，A为低级亚烷基，Y为COOH或其反应性衍生物），例如，如果需要，在缩合剂如水溶性碳二亚胺的存在下，选自式II，III所示化合物的化学偶联剂与氧 - 毒素（部分后垂体激素）反应以形成复合物。将β-D-半乳糖酶与该复合物结合，得到酶标记的氧 - 毒素。另一方面，通过将氧 - 毒素与白蛋白结合获得的复合物免疫兔子，得到抗血清。使含氧素毒素的标本，酶标记的氧 - 毒素和抗血清反应，同时将形成的沉淀物加入到底物中以测量酶活性。将该测量值与由已知的氧 - 毒素样品预先计算的加成曲线进行比较，以使得能够以高精度定量分析样品中的氧 - 毒素。

4. 发明专利

JPS6115899A Difunctional ligand compound and conjugated protein 失效
标题翻译：功能性配体化合物和结合蛋白
公开(公告)号：JPS6115899A
公开(公告)日：1986-01-23
申请号：JP13599484
申请日：1984-06-29
申请人： Sumitomo Chem Co Ltd
发明人： MURAKAMI YOSHIAKI , SHIBA KUNIO , YOSHITAKE AKIRA , TAKAHASHI HIROYOSHI , UEDA NOBUO , HAZUE MASAAKI
IPC分类号： G01N33/534 , A61K38/00 , A61K38/16 , A61K38/46 , A61K39/00 , A61K51/00 , C07K16/00 , C07K17/08 , C08G73/10 , C08G81/00
摘要： PURPOSE: A physiologically active protein and polysuccinimide derivative are linked utilizing mercapto groups included in both compounds to enable industrially advantageous production of the titled conjugated protein which has a specific structural unit, composition and average molecular weight and is used as a radioactive diagnostic.
CONSTITUTION: The mercapto group in a physiologically active protein such as fibrinogen or mercapto groups which has been newly introduced into a physiologically active protein and the mercapto group in a polysuccinimide derivative are utilized to bond the two substances to give the objective conjugated protein which has structural units of formula I (X is reaction residue of amino group- containing difunctional ligand), formula II, formula III (Y is residue of water- soluble aliphatic primary amine), formula IV, formula V (W is lower alkylene; Z is H, group capable of forming an active disulfide bond together with adjacent S) and formula VI where individual numbers of each structural unit satisfy equations VII and VIII and has an average molecular weight of 2,000W1,000,000.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：使用两种化合物中包含的巯基连接生理活性蛋白和聚琥珀酰亚胺衍生物，使工业上有利地生产具有特定结构单元，组成和平均分子量的标题缀合蛋白，并用作放射性诊断。构成：将新引入生理活性蛋白质的生物活性蛋白质例如纤维蛋白原或巯基中的巯基和聚琥珀酰亚胺衍生物中的巯基用于结合两种物质，得到具有结构的目标缀合蛋白式I的单元（X是含氨基的双官能配体的反应残基），式II，式III（Y是水溶性脂族伯胺的残基），式IV，式V（W是低级亚烷基; Z是H 能够与相邻的S）和式VI形成活性二硫键的基团，其中每个结构单元的个数满足式VII和VIII，并且平均分子量为2,000-1,000,000。

5. 发明专利

JPS6113156A Reagent for quantitative analysis of human interferon-alpha and determination method thereof 失效
标题翻译：人类干扰素定量分析试剂及其测定方法
公开(公告)号：JPS6113156A
公开(公告)日：1986-01-21
申请号：JP13470784
申请日：1984-06-28
申请人： Sumitomo Chem Co Ltd
发明人： MIYAI KIYOSHI , KATSUMARU HIROYUKI , MOURI ZENICHI , MURAKAMI YOSHIAKI
IPC分类号： G01N33/53 , A61K39/00 , A61K39/395 , C12Q1/34 , G01N33/535 , G01N33/563
摘要： PURPOSE: To measure the concn. of HuIFN (human interferon)-α, by reducing an anti-HuIFN-α antibody or its pepsine hydrolysate F(ab')
2 while bonding the resulting reduced product to β-D-galactosidase through a dimaleimide compound.
CONSTITUTION: An anti-HuIFN-α antibody or F(ab')
2 being a pepsine hydrolysate thereof is reduced to form a thiol group and a large excess of a dimaleimide compound is reacted with one of said thiol group or that of β-D-galactosidase and subsequently reacted with the other thiol group, after the unreacted dimaleimide compound was removed, to prepare an enzyme labelled antibody wherein the antibody is bonded to the enzyme. By determining HuIFN-α according to a sandwich method using this enzyme labelled antibody, 1I.U./ml of HulFN-α can be determined.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：测量浓度的HuIFN（人类干扰素）-α，通过还原抗HuIFN-α抗体或其肽水解产物F（ab'）2，同时将得到的还原产物通过二马来酰亚胺化合物结合到β-D-半乳糖苷酶。构成：将抗HuIFN-α抗体或作为其胰蛋白酶水解产物的F（ab'）2还原成硫醇基团，并将大量过量的二马来酰亚胺化合物与所述硫醇基团或β-D 然后在除去未反应的二马来酰亚胺化合物之后与另一硫醇基团反应，制备其中抗体与酶结合的酶标记抗体。通过使用该酶标记的抗体根据夹心法测定HuIFN-α，可以测定1I.U./ml的HulFN-α。

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