169237-38-1Relevant academic research and scientific papers
Alpha-emitting complexes
-
Page/Page column 37, (2017/10/18)
The present invention provides a tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand and the ion of an alpha-emitting thorium radionuclide. The invention additionally provides therapeutic methods employing such complexes, methods of their production and use, and kits and pharmaceutical compositions comprising such complexes.
RADIO-PHARMACEUTICAL COMPLEXES
-
, (2018/01/15)
The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl group, and a
RADIO-PHARMACEUTICAL COMPLEXES
-
, (2017/10/18)
The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl group, and a
An efficient chelator for complexation of thorium-227
Ramdahl, Thomas,Bonge-Hansen, Hanne T.,Ryan, Olav B.,Larsen, ?smund,Herstad, Gunnar,Sandberg, Marcel,Bjerke, Roger M.,Grant, Derek,Brevik, Ellen M.,Cuthbertson, Alan S.
supporting information, p. 4318 - 4321 (2016/08/18)
We present the synthesis and characterization of a highly efficient thorium chelator, derived from the octadentate hydroxypyridinone class of compounds. The chelator forms extremely stable complexes with fast formation rates in the presence of Th-227 (ambient temperature, 20?min). In addition, mouse biodistribution data are provided which indicate rapid hepatobiliary excretion route of the chelator which, together with low bone uptake, supports the stability of the complex in vivo. The carboxylic acid group may be readily activated for conjugation through the ?-amino groups of lysine residues in biomolecules such as antibodies. This chelator is a critical component of a new class of Targeted Thorium Conjugates (TTCs) currently under development in the field of oncology.
RADIO-PHARMACEUTICAL COMPLEXES
-
, (2016/07/05)
The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a C l-C s
ALPHA-EMITTING COMPLEXES
-
Paragraph 0207, (2013/07/25)
The present invention provides a tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand and the ion of an alpha-emitting thorium radionuclide. The invention additionally provides therapeutic methods employing such complexes, methods of their production and use, and kits and pharmaceutical compositions comprising such complexes.
3-hydroxy-2(1H)-pyridinone chelating agents
-
, (2008/06/13)
Disclosed is a series of improved metal chelating agents, which are highly effective upon both injection and oral administration; several of the most effective are of low toxicity. These chelating agents incorporate within their structure 1-hydroxy-2-pyridinone (1,2-HOPO) and 3-hydroxy-2-pyridinone (3,2-HOPO) moieties with a substituted carbamoyl group ortho to the hydroxy or oxo groups of the hydroxypyridinone ring. The electron-withdrawing carbamoyl group increases the acidity of the hydroxypyridinones. In the metal complexes of said chelating agents, the amide protons form very strong hydrogen bonds with its adjacent HOPO oxygen donor, making these complexes very stable at physiological conditions. The terminal N-substituents provides a certain degree of lipophilicity to said 3,2-HOPO, increasing oral activity. Also disclosed is a method of making the chelating agents and a method of producing a known compound, 3-hydroxy-1-alkyl-2(1H)pyridinone, used as a precursor to the chelating agent, safely and in large quantities.
Gadolinium complex of tris[(3-hydroxy-1-methyl-2-oxo-1,2-didehydropyridine-4-carboxamido)eth yl]-amine: A new class of gadolinium magnetic resonance relaxation agents
Xu,Franklin,Whisenhunt Jr.,Raymond
, p. 7245 - 7246 (2007/10/03)
Complexes of gadolinium(III) have proven to be especially effecrive MRI contrast agents; Gd3+ (S = 7/2) is unique in having the highest isotropic magnetic moment. The injection of gram quantities of potentially toxic metal cations requires that the complexes be stable to in vivo transmetalation, particularly with the competing calcium(II) ion in high concentration. while relaxivity is dependent on both the number and the rate of exchange of water molecules from the complex inner sphere. This competition between strong complexation and free water coordination sites is a challenge to MRI enhancement agent design. We report here the synthesis and characterization of Gd(III) TREN-Me-3,2-HOPO (7) {TREN-Me-3,2-HOPO = tris[(3-hydroxy-1-methyl-2-oxo-1,2- didehydropyridine-4-carboxamido)ethyl]amine}, which represents a promising new class of lanthanide compounds that meet these criteria. The hydroxypyridinonate (HOPO) monoanions are bidentate ligands that form effective multidentate sequestering agents, particularly when the HOPO ring carbon adjacent to the carbonyl or hydroxy group is functionalized and attached through an amide linkage to a suitable backbone. The geometry thus imposed promotes strong chelation of metal ions in general, and of Gd(III) in particular.
