C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
167/48, 530/5.04
C07K 5/08 (2006.01) A61K 51/08 (2006.01) C07C 233/56 (2006.01) C07C 237/22 (2006.01) C07F 13/00 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01)
Patent
CA 1292084
ABSTRACT The present invention is directed to novel radiopharma- ceutical imaging agents incorporating Tc-99m as a radiolabel. In particular, the novel imaging agents disclosed herein have relatively high renal extraction efficiencies, and hence are useful for conducting renal function imaging procedures. The novel Tc-99m compounds of a present invention have the following general formula: Image wherein X is S or N; and wherein Y is -H or wherein Y is Image and where R1 is -H, -CH3, or -CH2CH3; R2 is -H, -CH2CO2H, -CH2CONH2, -CH2CH2CO2H, -CH2CH2CONH2, -CH3, -CH2CH3, CH2C6H5, or -CH2OH; and Z is -H, -CO2H, -CONH2, -SO3H, -SO2NH2, or -CONHCH2CO2H; and the Tc is Tc-99m; and water- soluble salts thereof. of the foregoing, the presently preferred Tc-99m compound of the present invention is Tc-99m-mercaptoacetylglycylglycylglycine (Tc-99m-,MAGGG). The present invention is also directed to novel chelating agents that may be reacted with Tc-99m to form the foregoing compounds. Such novel chelating agents have the following general formula. Image where X and Y have the same definitions as above, and wherein Y' is -H2 when X is N, or wherein Y' is -H, or a suitable protective group such as -COCH3, -COC6H5, -CH2NHCOCH3, -COCF3, or -COCH2OH when X is S. The present invention also provides methods for preparing and using the novel Tc-99m compounds. pat/6300-42
485220
Fritzberg Alan
Johnson Dennis L.
Kasina Sudhakar
Cassan Maclean
University Of Utah Research Foundation
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