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Polymer-metal complex composite having MRI contrast ability and MRI contrasting and/or antitumor composition using the same

外国特許コード F110005825
整理番号 AF12-02WO
掲載日 2011年10月19日
出願国 アメリカ合衆国
出願番号 200913000836
公報番号 20110123458
公報番号 8961949
出願日 平成21年6月26日(2009.6.26)
公報発行日 平成23年5月26日(2011.5.26)
公報発行日 平成27年2月24日(2015.2.24)
国際出願番号 JP2009061772
国際公開番号 WO2009157561
国際出願日 平成21年6月26日(2009.6.26)
国際公開日 平成21年12月30日(2009.12.30)
優先権データ
  • 特願2008-167823 (2008.6.26) JP
  • 2009JP061772 (2009.6.26) WO
発明の名称 (英語) Polymer-metal complex composite having MRI contrast ability and MRI contrasting and/or antitumor composition using the same
発明の概要(英語) The present invention provides a polymer-metal complex composite, which comprises a block copolymer capable of serving as a constituent member of a polymeric micelle and a metal complex having MRI contrast ability, accumulates in a tumor-specific manner, achieves high image contrast even in a small amount, and has reduced side effects and a long retention time in blood.
The polymer-metal complex composite of the present invention comprises a block copolymer (A) represented by general formula (a) and a metal complex (B) having MRI contrast ability, wherein the composite comprises a structure in which a carboxyl anion of poly(carbo) in the copolymer (A) is attached to the metal complex (B) via a metal atom (M).
特許請求の範囲(英語) [claim1]
1. A polymer-metal complex composite, which comprises a block represented by the following general formula (1) or (2):
wherein R1 represents a hydrogen atom or an unsubstituted or substituted linear or branched C1-12 alkyl group, L1 and L2 each represent a linker group, R2 independently represents a methylene group or an ethylene group, R3 independently represents a hydrogen atom, a protecting group for an amino group, a hydrophobic group or a polymerizable group, R4 represents a hydroxyl group or an initiator residue, R5 independently represents a hydrogen atom, an alkali metal ion, or a group represented by the following general formula (3) and/or (4):
wherein R6 represents a metal atom or a group derived from a metal complex, and R7 represents a group derived from a metal complex having MRI contrast ability,
provided that at least one R5 comprises the group represented by general formula (3) in which each R6 is independently a group derived from a metal complex having antitumor activity represented by the following formula (5-a) or (6-a):
each R7 is independently a group represented by the following formula (7-a), (8-a), (9-a) or (10-a):
m represents an integer of 5 to 20,000, n represents an integer of 2 to 5,000, and x represents an integer of 0 to 5,000provided that x <= n.
[claim2]
2. The composite according to claim 1, which is represented by the following general formula (1-a) or (2-a):
[claim3]
3. The composite according to claim 1 or 2, wherein the group represented by general formula (3) is independently a group represented by the following formula (15-a), (16-a), (17-a) or (18-a):
[claim4]
4. The composite according to claim 1, which when dispersed in an aqueous medium forms micellar particles.
[claim5]
5. The composite according to claim 4, which has an average dispersed particle size of 10 nm to 1 mu m in an aqueous medium, as measured by dynamic light scattering.
[claim6]
6. An MRI contrasting and antitumor composition, which comprises the composite according to claim 1.
[claim7]
7. An MRI contrasting method for tumor detection, which comprises administering the composite according to claim 1 to the body of an animal subject.
[claim8]
8. An MRI contrasting and antitumor kit, which comprises the composite according to claim 1.
[claim9]
9. The composite according to claim 1 or 2, wherein the group represented by general formula (3) is independently a group represented by the following formula (11-a), (12-a), (13-a), or (14-a):
  • 発明者/出願人(英語)
  • KATAOKA KAZUNORI
  • KAIDA SACHIKO
  • CABRAL HORACIO
  • KUMAGAI MICHIAKI
  • SEKINO MASAKI
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
国際特許分類(IPC)
米国特許分類/主・副
  • 424/78.37
  • 424/1.21
  • 424/1.29
  • 424/1.33
  • 424/1.37
  • 424/1.65
  • 424/9.34
  • 424/9.364
  • 424/9.365
参考情報 (研究プロジェクト等) CREST Establishment of Innovative Manufacturing Technology Based on Nanoscience AREA
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