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NOVEL BSH COMPLEX FOR BORON NEUTRON CAPTURE THERAPY

Foreign code F180009464
File No. S2017-0130-C0
Posted date Jul 31, 2018
Country WIPO
International application number 2017JP043220
International publication number WO 2018097335
Date of international filing Nov 24, 2017
Date of international publication May 31, 2018
Priority data
  • P2016-229302 (Nov 25, 2016) JP
Title NOVEL BSH COMPLEX FOR BORON NEUTRON CAPTURE THERAPY
Abstract The present invention provides: a complex of a mercaptoundecahydrodecaborate (BSH) and a peptide, the complex for boron neutron capture therapy (BNCT); a method for producing the complex; and a cancer therapy using the complex.
Scope of claims [claim1]
1. A hydrophobic amino acid residue in the aqueous solution with a basic amino acid residues (BSH) mercapto undeca hydrodecaborate peptide and mixing, the manufacturing method of a complex comprising metallopeptide BSH.
[claim2]
2. 1 -1000 BSH1 With respect to the peptide mixture in the ratio of moles R′O, method according to claim 1.
[claim3]
3. The diameter of the complexes can be adjusted and further characterized in that, the method of claims 1 or 2.
[claim4]
4. A diameter of about 20nm - to about 200nm of the composite body of any one of claims 1-3 spherical.
[claim5]
5. : Where the peptide KCMD_f (1) in the formula, m amino acid residues X may each independently be alanine, valine, leucine or Glycine, n amino acid residues Z are each independently - NHCH (COOH) R1and, R1is-(CH2)pNHR2and, R2is (NH) NH -H or -C2and, m is 4-10, n is 1-2, in which p is 1-6. Wherein the method of any one of claims 1-4 are indicated.
[claim6]
6. X is alanine, where m is 6, lysine Z, arginine, homoarginine, ornithine, 2,7 - diaminoheptane acid, 2,4 - diaminobutanes acid, or 2-amino acid and -4 - guanidinobutanoic, where n is 1, the method according to claim 5.
[claim7]
7. X and alanine, and m is 6, lysine or arginine and Z, where n is 1, the method according to claim 6.
[claim8]
8. A hydrophobic amino acid residues in the peptide comprising the amino acid residues and basic complex comprising BSH.
[claim9]
9. A diameter of about 20nm - to about 200nm of the composite body according to claim 8 spherical in shape.
[claim10]
10. : Where the peptide KCMD_f (1) in the formula, m amino acid residues X may each independently be alanine, valine, leucine or Glycine, n amino acid residues Z are each independently - NHCH (COOH) R1and, R1is-(CH2)pNHR2and, R2is (NH) NH -H or -C2and, m is 4-10, n is 1-2, in which p is 1-6. Claims 8 or 9 as indicated by the composite.
[claim11]
11. X is alanine, where m is 6, lysine Z, arginine, homoarginine, ornithine, 2,7 - diaminoheptane acid, 2,4 - diaminobutanes acid, or 2-amino acid and -4 - guanidinobutanoic, where n is 1, according to claim 10 CReRf.
[claim12]
12. X and alanine, and m is 6, lysine or arginine and Z, where n is 1, the composite body according to claim 11.
[claim13]
13. Comprising a composite of any one of claims 8-12, boron neutron capture therapy of a medicament for cancer.
[claim14]
14. Any one of claims 8-12 Baboon administered to a patient and the patient for the cancer, cancer patient comprising irradiating neutron radiation, a method for treating cancer.
[claim15]
15. In which the boron neutron capture therapy FZDlO used, any one of claims 8-12 sarcosin.
[claim16]
16. Boron neutron capture therapy FZDlO for manufacture of a medicament for, the use of the conjugates of any one of claims 8-12.
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • OKAYAMA UNIVERSITY
  • Inventor
  • MATSUI HIDEKI
  • FURUYA SHUICHI
  • MICHIUE HIROYUKI
  • KAKUTA HIROKI
  • TAKEUCHI YASUAKI
IPC(International Patent Classification)

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