28-11-2013 дата публикации
Номер: US20130317196A1
The present invention relates to a triazanonane derivative indicated by the chemical formula 1 below, or a pharmaceutically acceptable salt thereof, and a method for preparing same, and the triazanonane derivative according to the present invention forms a complex with a metal-fluoride and displays an effect of increasing the labeling efficiency up to 78-90% when labeling F-18, thus enabling use in various radioactive medicine labeling 2. The triazanonane derivative expressed by Chemical Formula 1 or pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sup': 1', '2, 'each of Rand Ris independently OH or t-butoxy;'}{'sub': '2', 'A is CHor C(═O);'}{'sub': '2', 'E is CH, C(═O) or phenyl;'}X is atom group selected from amino acid, peptide, protein, nucleic acid, vitamin, hormone, neurotransmitter, sugar, nanoparticle, microparticle, fat, fatty acid, nitroimidazole or derivatives thereof;n is integer between 0 and 10, or between 3 and 10 when E is not phenyl; andm is integer between 0 and 3.3. The triazanonane derivative expressed by Chemical Formula 1 or pharmaceutically acceptable salt thereof according to in claim 2 , whereinX may be carboxyl, hydroxyl, amine, halogen, N-hydroxysuccinimide ester, tetrafluorophenol ester, pentafluorophenol ester, maleimide, haloacetate, hydrazine, hydroxylamine, sulfhydryl, thioester, desulfide, aldehyde, isothiocyanate azide or acetylene.4. The triazanonane derivative expressed by Chemical Formula 1 or pharmaceutically acceptable salt thereof according to claim 2 , whereinX may be octreotide derivatives, bombesin, vasoactive intestinal peptide (VIP), cholecystokinin, neurotensin, EGF, VEGF, RGD, CXCR4 ligand, substance P, matrix metalloproteinase (MMP), lycin glutamate urea, or cysteine glutamate urea.5. The triazanonane derivative expressed by Chemical Formula 1 or pharmaceutically acceptable salt thereof according to claim 1 , wherein the triazanonane derivative is selected from the group consisting of:1) 4,7-bis ...
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