C - Chemistry – Metallurgy – 12 – N
Patent
C - Chemistry, Metallurgy
12
N
C12N 9/00 (2006.01) A61K 47/48 (2006.01) A61K 51/10 (2006.01) C07D 213/53 (2006.01) C07D 213/55 (2006.01) C07D 213/61 (2006.01) C07D 213/77 (2006.01) C07D 471/04 (2006.01) C07D 471/18 (2006.01) C07H 21/00 (2006.01) C07K 14/00 (2006.01) C12N 1/00 (2006.01) C12N 5/00 (2006.01) C12N 7/01 (2006.01) A61K 43/00 (1990.01) A61K 49/02 (1990.01)
Patent
CA 2095123
2095123 9208494 PCTABS00013 A targeting radioactive immunoreagent comprises a metal radionuclide ion, a complexing agent, and an immunoreactive group covalently bonded to said complexing agent, the complexing agent having structure (A-I), wherein R represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R1 represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R2 represents hydroxy, carboxy, hydroxyalkyl, carbonyliminodiacetic acid, methyleneiminodiacetic acid, methylenethioethyleneiminodiacetic acid, hydrazinylylidenediacetic acid, or a salt of such acids, or two R2 groups, taken together, represent the atoms necessary to complete a macrocyclic ring structure containing at least one heteroatom coordinating site and at least one, preferably two alkylene groups forming part of the ring structure; R3 represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R4 represents hydrogen or a protein reactive group; n is 0 to 4, o is 0 or 1, m is 0 or 1; provided that at least one of n and m is 0 and at least one of R, R1, R3 and R4 is a protein reactive group. In a composition of matter aspect, this invention provides novel terpyridines and phenanthrolines. Preferred terpyridines have the structure (A-I) above wherein n=1, m=0 and R is a substituted phenyl containing an alkyl or alkoxy substituent and a protein reactive group. Preferred phenanthrolines have the structure (A-I) above wherein n=0, m=1 and at least one R4 is a protein reactive group. The targeting radioactive immunoreagents are particularly useful in therapeutic and diagnostic imaging compositions and methods.
Hilborn David A.
Hossain Timothy Z.
Murray Bruce J.
Toner John L.
Fetherstonhaugh & Co.
Nycomed Imaging As
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