| 摘要 |
The present invention is directed to novel radiopharmaceutical 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: wherein X is S or N; and wherein Y is -H or wherein Y is 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 watersoluble 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. 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 |
