Tc-labeled arylpiperazine derivatives for imaging serotonin...

Details Tc-labeled arylpiperazine derivatives for imaging serotonin... Tc-labeled arylpiperazine derivatives for imaging serotonin...

2011-01-25

2011-01-25

Wax, Robert A (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

C424S001650, C546S227000, C546S228000

Reexamination Certificate

active

07875287

ABSTRACT:
The present invention relates to Tc-labeled arylpiperazine derivatives for imaging serotonin receptor and, more particularly, to arylpiperazine derivatives coupled with MAMA-disulfide, N2S2or dimethyl-N2S2chelating ligand represented by the following chemical formula (1).New arylpiperazine derivatives according to the present invention have no problem of amide hydrolysis in metabolism and have a high affinity for serotonin receptors, and can be labeled with an optimum radionuclide of technetium, thereby being usefully applied for monitoring neurodegenerative diseases or neurological diseases of a mammal.

REFERENCES:
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Hom et al.; Nuclear Medicine & Biology, vol. 24, pp. 485-498 (1997).
Advanced Organic Chemistry 4thEd. (1992); Jerry March; Ch. 10.
Machine Translation of KR 1020000051075 (2 copies).
Dirk Michalik, et al., A Short and Efficient Synthesis of N-Aryl-and-N-Heteroaryl-N′- . . . , Tetrahedron Letters, vol. 45, pp. 2057-2061, 2004.
G. Bormans, et al., Synthesis, Radio-LC-MS Analysis . . . , J. Label Compd. Radiopharm, vol. 46, pp. 575-585, 2003.
Bernard J. Cleynhens, et al., S-Trityl Protection of Bis-Amino Bis-Thiol . . . , Tetrahedron Letters, vol. 44, pp. 2597-2600, 2003.

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