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DRUG FOR PRODUCING RADIOLABELED POLYPEPTIDE REDUCING NON-SPECIFIC RENAL ACCUMULATION

外国特許コード F130007411
整理番号 S2012-0175-N0
掲載日 2013年6月19日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2012JP081033
国際公開番号 WO 2013081091
国際出願日 平成24年11月30日(2012.11.30)
国際公開日 平成25年6月6日(2013.6.6)
優先権データ
  • 特願2011-263647 (2011.12.1) JP
発明の名称 (英語) DRUG FOR PRODUCING RADIOLABELED POLYPEPTIDE REDUCING NON-SPECIFIC RENAL ACCUMULATION
発明の概要(英語) Provided is a radiolabeled drug which contains a compound expressed in the following formula (I); the compound to which polypeptide is bound which is capable of being bound to a target site, or a pharmacologically acceptable salt of the compound; and a complex which includes a complex structure which contains the compound to which the polypeptide is bound which is capable of being bound to the target site, or the pharmacologically acceptable salt thereof, and a radioisotope. (I) Herein, R1 is a hydrogen atom, a methyl group, or a carboxymethyl group; R2 is CH2-CH2-NH-CH2-COOH, CH2-CH2-N(CH2-COOH)2, CH2-CH2-NH2, CH2-CH2-NHR3, the carboxymethyl group, or CH2-CH2-NR3R4; R3 and R4 are alkyl groups which may be different; X, Y, and Z are amino acids which may be different; and F is a functional group which is capable of being bound to the polypeptide. Using the compound according to the present invention, the radiolabeled drug is provided which is prepared through a simple operation, has high accumulation toward the target site, and reduces non-specific renal accumulation.
従来技術、競合技術の概要(英語) BACKGROUND ART
The agent is a radioactive label, a radioisotope label (RI) by pharmaceutical and, disease diagnosis and treatment of, for example is widely used for diagnosis and treatment of tumor are. Radioactive labeling agents in the diagnosis and treatment using, the selection of useful nuclides, the agent can be integrated in a specific tissue or cell have been made for drug design.
Labeled with a radioactive isotope such as a small polypeptide is an antibody fragment, including cancer as a probe for molecular imaging, β-ray emitting nuclide further internal radiation as a therapeutic agent which is expected to be applied. However, a small polypeptide by administering RI and labeled, administered from an early kidney radioactivity is observed for a long time. Therefore, there is a fear of exposure of the kidney and nephropathy and, is necessary to adjust the dose to. In this way, integration is radioactive labeled polypeptide of the kidney, image diagnosis and treatment and their applicability to large obstacles.
On the other hand the inventors have found that, a small polypeptide and labeling agents and high urinary excretion, kidney brush border membrane of the substrate for the enzyme is attached via the drug design has been developed. Then, from an examination of the radioactive iodine is used, the usefulness of such drug design (non-patent document 1) revealed. Further, the metal to the radioactive isotope label to drug design in order to verify the applicability of the present invention, and deployment of the organic rhenium compounds, to demonstrate the feasibility thereof (non-patent document 2, patent document 1).
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • NATIONAL UNIVERSITY CORPORATION CHIBA UNIVERSITY
  • 発明者(英語)
  • ARANO, Yasushi
  • UEHARA, Tomoya
  • HANAOKA, Hirofumi
  • SUZUKI, Chie
国際特許分類(IPC)
指定国 National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IS JP KE KG KM KN KP KR KZ LA LC LK LR LS LT LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

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