225Ac-HEHA and related compounds, methods of synthesis and methods of use

   
   

The present invention provides an .alpha.-particle-emitting radioisotope chelation complex comprising .sup.225 Actinium (.sup.225 Ac) and 1,4,7,10,13,16-hexaazacyclohexadecane-N,N',N",N'",N"",N'""-hexaacetic acid (HEHA) (.sup.225 Ac-HEHA). Also provided is a bifunctional HEHA, and a bifunctional .sup.225 Ac-HEHA. The bifunctional HEHA and the bifunctional .sup.225 Ac-HEHA can be conjugated to a targeting agent. In view of the above, the present invention provides a method of making HEHA and methods of making a bifunctional HEHA, including a conjugate thereof. Also provided are a method of treating disease, a method of treating cancer, a method of decontaminating a sample from .sup.225 Ac, a method of decontaminating a person who has been externally contaminated with .sup.225 Ac, and a method of detoxifying a person who has internalized .sup.225 Ac.

Присытствыющий вымысел обеспечивает alpha.-castiq-ispuska4 актиний sup.225 chelation радиоизотопа сложный состоя из (ac sup.225) и кислоту 1,4,7,10,13,16-hexaazacyclohexadecane-N,N',N",N'",N"",N'""-hexaacetic (HEHA) (ac-HEHA-HEHA sup.225). Также обеспечены bifunctional HEHA, и ac-HEHA-HEHA sup.225 bifunctional. Bifunctional HEHA и ac-HEHA-HEHA sup.225 bifunctional можно проспрягать к пристреливая веществу. В виду вышеуказанного, вымысел настоящего момента обеспечивает метод делая HEHA и методы делать bifunctional HEHA, включая конъюгат thereof. Также обеспечены метод обрабатывать заболевание, метод обрабатывать рак, метод decontaminating образец от ac sup.225, метод decontaminating персона которая внешн была загрязнена с ac sup.225, и метод детоксицировать персону которая внедряла ac sup.225.

 
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