-
1.发明授权Bisphosphonic acid derivative and compound thereof labeled with radioactive nuclide 失效二膦酸衍生物及其与放射性核素标记的化合物公开(公告)号：US06607710B1
公开(公告)日：2003-08-19
申请号：US09686372
申请日：2000-10-12
申请人： Osamu Ito , Nobuhiko Kanazashi , Aki Morishita , Masamichi Hara , Masaru Kanagawa , Yasuko Watanabe , Yoshitoshi Itaya
发明人： Osamu Ito , Nobuhiko Kanazashi , Aki Morishita , Masamichi Hara , Masaru Kanagawa , Yasuko Watanabe , Yoshitoshi Itaya
IPC分类号： A61K5100
CPC分类号： A61K51/0497 , C07B59/004 , C07F9/3865 , C07F9/3869 , C07F9/3873
摘要： An object of the present invention is to provide a bisphosphonic acid derivative and said bisphosphonic acid derivative being labeled with a radioactive nuclide, which has properties of rapid accumulation to the bone and rapid urinary excretion. The present invention relates to a bisphosphonic acid derivative and said bisphosphonic acid derivative being labeled with a radioactive nuclide, which is represented by the following general formula (1), R—Y—A (1) wherein A is a bisphosphonic acid or a salt thereof, having P—C—P bond; Y is a bonding portion such as a methylene, an amido etc.; R is a group of any one of a polyaminopolycarboxylic acid, an aliphatic carboxylic acid, a mercaptoacetylpolyamino acid or its derivatives and a compound represented by the formula (2), X is a halogen atom or an isotope thereof or an alkyl tin; Z is a group of any one of compounds of an aminocarboxylic acid, an alkylcarboxylic acid or a substituted-alkylcarboxylic acid, an alkylsulfonic acid or a substituted-alkylsulfonic acid.
摘要翻译： 本发明的目的是提供双膦酸衍生物和所述双膦酸衍生物，其被放射性核素标记，其具有快速积累到骨骼和快速排尿的性质。 本发明涉及用下列通式（1）表示的放射性核素标记的双膦酸衍生物和二膦酸衍生物，其中A为具有P-C-P键的双膦酸或其盐; Y是亚甲基，酰氨基等的结合部分; R是聚氨基多羧酸，脂肪族羧酸，巯基乙酰基聚氨基酸或其衍生物中的任何一种和式（2）表示的化合物，X是卤素原子或其同位素或烷基锡; Z是氨基羧酸，烷基羧酸或取代的烷基羧酸的化合物，烷基磺酸或取代的烷基磺酸中的任何一种。
-
公开(公告)号：US5770178A
公开(公告)日：1998-06-23
申请号：US575863
申请日：1995-12-20
CPC分类号： C07K7/08 , A61K51/08 , A61K51/088 , C07K5/0812 , C07K5/0815 , C07K5/0819 , A61K2121/00 , A61K2123/00 , Y02P20/55
摘要： The invention provides a metal chelate forming peptide having an amino acid sequence of three amino acid residues represented by: X1-X2-Cys, wherein X1 represents an amino acid residue other than Cys residue; X2 represents an amino acid residue other than Cys residue and Pro residue; functional groups at the N-terminus, C-terminus and side chain may be substituted with protecting groups; and each of the amino acid residues may be any of D-form and L-form. Further, the invention provides a complex of the peptide with a physiologically active peptide, protein or other substance; a labeled reagent obtained by labeling the peptide or the complex with a metal radionuclide; and a radiodiagnostic and radiotherapeutic composition comprising the metal radionuclide-labeled reagent.
摘要翻译： 本发明提供一种形成金属螯合物的肽，其具有由以下基团表示的三个氨基酸残基的氨基酸序列：X1-X2-Cys，其中X1表示除Cys残基以外的氨基酸残基; X2表示除Cys残基和Pro残基之外的氨基酸残基; N-末端，C-末端和侧链的官能团可以被保护基团取代; 并且每个氨基酸残基可以是D型和L-型中的任何一种。 此外，本发明提供了肽与生理活性肽，蛋白质或其他物质的复合物; 通过用金属放射性核素标记肽或配合物获得的标记试剂; 以及包含金属放射性核素标记试剂的放射诊断和放射治疗组合物。
-
3.发明授权Metal chelate forming peptides and use thereof represented by three amino acid sequences 失效金属螯合物形成肽及其用途由三个氨基酸序列表示
公开(公告)号：US5785948A
公开(公告)日：1998-07-28
申请号：US815530
申请日：1997-03-12
CPC分类号： C07K7/08 , A61K51/08 , A61K51/088 , C07K5/0812 , C07K5/0815 , C07K5/0819 , A61K2121/00 , A61K2123/00 , Y02P20/55
摘要： The invention provides, inter alia, metal radionuclide-labelled reagent comprising a metal radionuclide coordinated with a metal chelate forming peptide having an amino acid sequence of three amino acid residues represented by: X1-X2-Cys, wherein X1 represents an Asp residue, a Tyr residue or a Lys residue; X2 represents an amino acid residue other than a Cys residue and a Pro residue, provided that X2 does not represent a Gly residue when X1 represents an Asp residue; wherein functional groups at the N-terminus, C-terminus and side chain may be optionally substituted with protecting groups; and wherein each of the amino acid residues may be either D-form or L-form.
摘要翻译： 本发明尤其提供了金属放射性核素标记的试剂，其包含与形成有金属螯合物的肽配位的金属放射性核素，所述金属螯合物具有由以下基团表示的三个氨基酸残基的氨基酸序列：X1-X2-Cys，其中X1表示Asp残基， 酪氨酸残基或赖氨酸残基; X2表示除Cys残基和Pro残基以外的氨基酸残基，条件是当X1表示Asp残基时X 2不表示Gly残基; 其中N末端，C末端和侧链上的官能团可以任选被保护基取代; 并且其中每个氨基酸残基可以是D-型或L-型。
-
4.发明授权
公开(公告)号：US5827498A
公开(公告)日：1998-10-27
申请号：US463230
申请日：1995-06-05
CPC分类号： A61K51/1018 , A61K51/1045 , C07K16/18 , C07K16/30 , A61K38/00
摘要： A peptide having affinity with tumor or a salt thereof, which comprises an amino acid sequence containing 20 or less amino acid residues, said amino acid sequence being described as X.sub.1 -YCAREPPT-X.sub.2 wherein A, C, E, P, R, T and Y represent amino acid residues expressed by standard one-letter symbols, each of amino acid residues A, C, R and Y in the amino acid sequence YCAR may be in either L-form or D-form, X.sub.1 represents a basic organic compound having 1-3 amino groups, and X.sub.2 represents any given amino acid sequence, is provided together with a radioactive diagnostic agent and a radioactive therapeutic agent containing the above peptide or a salt thereof. The present tumor affinity peptide is high in radioactive metal labeling yield, useful for imaging and treating pathological tissues such as of breast cancer, ovarian cancer and colon cancer of mammals including human, and difficult to be readily metabolized in organisms and to accumulate in normal tissues especially at kidney and liver.
摘要翻译： 一种与肿瘤或其盐具有亲和力的肽，其包含含有20个或更少氨基酸残基的氨基酸序列，所述氨基酸序列描述为X1-YCAREPPT-X2，其中A，C，E，P，R，T和 Y代表由标准单字母符号表示的氨基酸残基，氨基酸序列YCAR中的氨基酸残基A，C，R和Y中的每一个可以是L-型或D-型，X1表示具有 1-3个氨基，X2代表任何给定的氨基酸序列，与放射性诊断剂和含有上述肽或其盐的放射性治疗剂一起提供。 本发明的肿瘤亲和肽具有放射性金属标记产率高，可用于成像和治疗诸如乳腺癌，卵巢癌和包括人在内的哺乳动物的结肠癌的病理组织，并且难以在生物体中代谢并积累在正常组织中 特别是在肾脏和肝脏。
-
5.发明授权Peptide having inflammation affinity and radioactive diagnostic containing the same 失效具有炎症亲和力的肽和包含其的放射性诊断
公开(公告)号：US5821330A
公开(公告)日：1998-10-13
申请号：US327459
申请日：1994-10-21
CPC分类号： A61K51/1093 , A61K51/088 , C07K16/00
摘要： A peptide having affinity with inflammation is disclosed, which contains at least one of the following amino acid sequences: LLGGPS (SEQ ID NO:1), LLGGPSV (SEQ ID NO:2), KEYKAKVSNKALPAPIEKTISK (SEQ ID NO:3), KEYKCKVSNKALPAPIEKTISK (SEQ ID NO:4), KTKPREQQYNSTYR (SEQ ID NO:5), and KTKPREQQYNSTYRVV (SEQ ID NO:6), wherein A, C, E, G, I, K, L, N, P, Q, R, S, T, V, and Y represent amino acid residues expressed by standard one-letter symbols. According to the present invention, a peptide and its chemically modified substances, radioactive metal labeled peptides derived therefrom, and radioactive diagnostics comprising such peptide are provided, which are useful for imaging inflammation region and easy in preparation handling, and accumulate at inflammation site immediately after administration while being excellent in clearance into urine. The imaging is possible in several ten minutes after administration.
摘要翻译： 公开了具有炎症亲和力的肽，其含有以下氨基酸序列中的至少一个：LLGGPS（SEQ ID NO：1），LLGGPSV（SEQ ID NO：2），KEYKAKVSNKALPAPIEKTISK（SEQ ID NO：3），KEYKCKVSNKALPAPIEKTISK（ SEQ ID NO：4），KTKPREQQYNSTYR（SEQ ID NO：5）和KTKPREQQYNSTYRVV（SEQ ID NO：6），其中A，C，E，G，I，K，L，N，P，Q，R，S ，T，V和Y表示由标准单字母符号表示的氨基酸残基。 根据本发明，提供肽及其化学修饰物质，由其衍生的放射性金属标记肽和包含该肽的放射性诊断物，其可用于成像炎症区域并且易于制备处理，并且在紧随其后的炎症部位积聚 同时排尿良好。 在施用后几十分钟内成像是可能的。
-
-
-
-
搜索结果
5 条记录 (耗时 0.016 秒)