Patent ID: 6127529
Filing Date: 2000-10-03
Classification: A61K,C07D,C07F

Abstract:
A bifuncitonal chelating 2,6-disubstituted pyridine compound having the structure where(i) n is an integer 1 or 2(ii) R.sub.1, R.sub.2 and R.sub.3 represent hydrogen, or alkyl or aralkyl groups having 1-12 carbon atoms and have an aliphatic carbon atom next to the pyridine ring and no electrons capable of delocalizing or resonating with the pyridine ring, at least two of R.sub.1, R.sub.2 and R.sub.3 being hydrogen;(iii) Z and Z' represent identical or different chelating structures, in which the chelating h eteroatom is selected from amino nitrogens and negatively charged oxygens having a free pair of electorns so that the said at least one chelating heteroatom together with the nitrogen of the pyridine ring is capable of chelating a metal ion: the bridge linking two chelating heteroatoms together providing a distance of two or three atoms between them;(iv) - - - indicates that the group X-Y is a substituent replacing one of the groups R.sub.1, R.sub.2 and R.sub.3 or replacing a hydrogen atom in the Z and/or Z' groups,(v) X-Y represents an organic group which is inert towards said chelating and which has no heteroatom closer than four atoms from a chelating heteroatom in Z or Z' and in which X is an inert and stable bridge and Y is(1) a funcitonal group selected for bromoacetamido, iodoacetamido, succinamido, pyridyldithio, mercapto, carboxyl, carboxylic ester of N-hydroxysuccinimide, p-nitrophenyl carboxylic ester, hydroxyl, aldehyde, diazonium, tosyl, mesytylyl, trexyl, phosphodiester and phosphotriester; or(2) a residue of a targeting compound participating in biospecific affinity reaction and with retained capability of participating in such reactions,said group X-Y being linked to the pyridine ring of formula II via an aliphatic carbon atom attached to said ring and providing no pi-electron system directly conjugated to said ring; or acid, ester salt and chelate forms thereof associated with at least one of said chelating heteroatoms.