PURPOSE: To provide a new compound capable of rapidly forming a metal complex stable in vivo and useful as an agent for cancer treatment by bonding to a specific antibody, etc.
CONSTITUTION: The compound of formula I (n is 1 or 2; R1 is 1-10C alkyl or 7-16C aralkyl; R21 to R25 are H, 1-5C alkyl or 7-11C aralkyl), e.g. 1-[N- carboxymethyl-N-(p-nitrobenzyl)-aminomethyl]-2,5,8,11-tetraaza-2,5,8,11-tetrakis(carboxymethyl)cyclododecane. The compound of formula I can be produced by condensing a macrocyclic polyamine of formula II (R11 is 1-10C alkyl or 7-16C aralkyl) to an acetic acid derivative of the formula X-CH2CO2R20 (X is halogen or activated OH derivative; R20 is H, l-5C alkyl or 7-11C aralkyl) in the presence of a base. A metal complex derived from a ligand of formula I and a metallic ion is effective for the diagnosis and treatment of various diseases (especially cancer) when bonded to a specific antigen against various organism-relating substances.
TANABE MASAYASU
HASATO ATSUO
WATANABE KENZO
KIMURA EIICHI
KATO YOSHINORI
