Patent · US Expired

Synthesis of macrocyclic polyaminocarboxylates and their use for preparing stable radiometal antibody immunoconjugates for therapy, spect and pet imaging

US5428156A · kind A · utility

18Cited by
17References
2Claims
0Family size

Assignee

Inventors

Key dates

Filing dateApr 2, 1993
Grant dateJun 27, 1995
Priority date
Expiry dateApr 2, 2013

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D257/02
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A simple method for the synthesis of 1,4,7,10-tetraazacyclododecane N,N'N",N'"-tetraacetic acid and 1,4,8,11-tetraazacyclotetradecane N,N',N",N'"-tetraacetic acid involves cyanomethylating 1,4,7,10-tetraazacyclododecane or 1,4,8,11-tetraazacyclotetradecane to form a tetranitrile and hydrolyzing the tetranitrile. These macrocyclic compounds are functionalized through one of the carboxylates and then conjugated to various biological molecules including monoclonal antibodies. The resulting conjugated molecules are labeled with radiometals for SPECT and PET imaging and for radiotherapy.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.