C - Chemistry – Metallurgy – 12 – Q
Patent
C - Chemistry, Metallurgy
12
Q
C12Q 1/68 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) A61K 51/10 (2006.01) C07D 213/36 (2006.01) C07D 213/38 (2006.01) C07D 213/40 (2006.01) C07D 213/42 (2006.01) C07D 213/55 (2006.01) C07D 401/14 (2006.01) C07D 471/00 (2006.01) C07D 471/04 (2006.01) C07D 471/08 (2006.01) C07D 471/18 (2006.01) C07D 471/22 (2006.01) C07H 21/00 (2006.01) C07K 16/00 (2006.01) A61K 43/00 (1990.01)
Patent
CA 2135059
2135059 9321957 PCTABS00027 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 the structure (AI), 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, thioalkyl, formyl, carbonyliminodiacetic acid, methyleneiminodiacetic acid, methylenethioethyleneiminodiacetic acid, carboxyalkylthioalkyl, hydrazinylidenediacetic 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 another aspect, this invention provides novel terpyridines, quaterpyridines, quinqepyridines, sexipyridines and phenanthrolines having the structure (AI). Preferred terpyridines have the structure (AI) above wherein n=1, o=1, m=0, and R is a protein reactive group or a phenyl substituted with a protein reactive group. Optionally, the phenyl may also contain one or more substituents selected from alkyl and alkoxy. Preferred phenanthrolines have the structure (AI) above wherein n=0, o=1, 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.
Houssain Timothy Z.
Murray Bruce J.
Philion Richard
Saha Ashis K.
Fetherstonhaugh & Co.
Nycomed Imaging As
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