专利号:US-5428155-A 优先权日:1984-10-18 标题 :Synthesis of polyazamacrocycles with more than one type of side-chain chelating groups 发明人:SHERRY A DEAN; WESTRENEN JEROEN VAN 权利人:UNIV TEXAS 摘要:The pH controlled selectivity of the sulfomethylation reaction is used to prepare a series of di-, tri-, tetra- and hexaazacyclomacrocycles with specified patterns of pendent side-chain chelating groups. The prepared mono and diacetic acid derivatives, together with monomethylenephosphonate and monomethylenephosphinate derivatives of [12]aneN4, [12]aneN3 and [9]aneN3, make these types of ligands easily available by a synthetic pathway that avoids the use of protective groups. The invention thus comprises a variety of compounds, methods and uses characterized by relatively high synthetic yields of polyazamacrocyclic ligands exhibiting a wide and predictable choice of metal ion binding constants water and lipid solubilities by reason of their substituent pendent groups.
专利号:US-5639879-A 优先权日:1993-04-02 标题:Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, spect and pet imaging 发明人:MEASE RONNIE C; MAUSNER LEONARD F; SRIVASTAVA SURESH C 权利人:ASS UNIVERSITIES INC 摘要: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.
专利号:WO-9312097-A1 优先权日:1984-10-18 标 题 :Synthesis of polyazamacrocycles with more than one type of side-chain chelating groups
专利号:EP-0618910-A1 优先权日:1984-10-18 标题 :Synthesis of polyazamacrocycles with more than one type of side-chain chelating groups
专利号:US-5316757-A 优先权日:1984-10-18 标题 :Synthesis of polyazamacrocycles with more than one type of side-chain chelating groups
专利号:US-5428156-A 优先权日:1993-04-02 标题:Synthesis of macrocyclic polyaminocarboxylates and their use for preparing stable radiometal antibody immunoconjugates for therapy, spect and pet imaging