Ac-HEHA and related compounds, methods of synthesis and...

Organic compounds -- part of the class 532-570 series – Organic compounds – Radioactive metal containing

Reexamination Certificate

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C534S007000, C424S001110, C424S001650, C424S009100

Reexamination Certificate

active

06995247

ABSTRACT:
The present invention provides an α-particle-emitting radioisotope chelation complex comprising225Actinium (225Ac) and 1,4,7,10,13,16-hexaazacyclohexadecane-N,N′,N′,N′,N′,N′-hexaacetic acid (HEHA) (225Ac-HEHA). Also provided is a bifunctional HEHA, and a bifunctional225Ac-HEHA. The bifunctional HEHA and the bifunctional225Ac-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 from225Ac, a method of decontaminating a person who has been externally contaminated with225Ac, and a method of detoxifying a person who has internalized225Ac.

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patent: 03 197468 (1991-08-01), None
Beyer et al.,Nuclear Medicine&Biology24:367-372 (1997).
Beyer et al.,Isotopenpraxis26:111-114 (1990).
Deal et al.,J. Med. Chem. 42:2988-2992 (1999).

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