- A convenient synthesis of 1,4,7,10,13-pentaazacyclopentadecane
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Cyclic pentamine 1 was synthesized in good yields from fragments containing two and three nitrogen atoms.
- Kovacs, Zoltan,Archer, Eric A.,Russell, Mark K.,Sherry, A. Dean
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- Synthesis of N-quaternary ammonium [3H] and [(99m)Tc]Polyazamacrocycles, potential radiotracers for cartilage imaging
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The [3H] and [(99m)Tc] synthesis of three new compounds, N-[3-(pyridinio)propyl] cyclam (NPPC), N-[3-(triethylammonium)propyl] cyclam (NTPC) and N-[3-(triethylammonium)propyl]-15ane-N5 (NTP 15-5), potential tracers for cartilage, is reported. NPPC and NTPC were labelled with tritium on the ethyl group of cyclam with a specific radioactivity of 89 MBq/mmol. The [(99m)Tc]-labelling of the three quaternary ammonium chelates was realized with a high specific activity in the range 20-25 MBq/μmol.
- Nicolas, Colette,Borel, Michele,Maurizis, Jean-Claude,Gallais, Nadine,Rapp, Maryse,Ollier, Monique,Verny, Michel,Madelmont, Jean-Claude
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- Manganese complexes of nitrogen-containing macrocyclic ligands effective as catalysts for dismutating superoxide
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The present invention is directed to low molecular weight mimics of superoxide dismutase (SOD) represented by the formula: STR1 wherein R, R', R1, R'1, R2, R'2, R3, R'3, R4, R'4, R5, R'5, R6, R'6, R7, R'7, R8, R'8, R9, and R'9 and X, Y, Z and n are as defined herein, useful as therapeutic agents for inflammatory disease states and disorders, ischemic/reperfusion injury, stroke, atherosclerosis, hypertension and all other conditions of oxidant-induced tissue damage or injury.
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- Methods of preparing manganese complexes of nitrogen-containing macrocyclic ligands
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The present invention is directed to low molecular weight mimics of superoxide dismutase (SOD) represented by the formula: STR1 wherein R, R', R1, R'1, R2, R'2, R3, R'3, R4, R'4, R5, R'5, R6, R'6, R7, R'7, R8, R'8, R9, and R'9 and X, Y, Z and n are as defined herein, useful as therapeutic agents for inflammatory disease states and disorders, ischemic/reperfusion injury, stroke, atherosclerosis, hypertension and all other conditions of oxidant-induced tissue damage or injury.
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- Cascade polymer bound chelating compounds, their chelates and conjugates, processes for their production, and pharmaceutical agents containing them
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Cascade polymers, containing complex-forming ligands, optionally at least five ions of an element of atomic numbers 21-29, 39, 42, 44 or 57-83, as well as, if desired, cations of inorganic and/or organic bases, amino acids or amino acid amides, are valuable complexing compounds and complexes for diagnostics and therapy.
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- MACROHETEROCYCLES. 15.* SYNTHESIS OF MACROCYCLIC POLYAMINES IN A BIPHASIC SYSTEM
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Macrocyclic polyamines are conveniently synthesized by condensation of bissulfonamides with ditosylates or dibromides of glycols in the biphasic system toluene(xylene)-aqueous sodium hydroxide.
- Luk'yanenko, N. G.,Basok, S. S.,Filonova, L. K.,Kulikov, N. V.,Pastushok, V. N.
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p. 346 - 349
(2007/10/02)
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- Synthesis of macrocyclic polyamines: Application to the increase of urinary excretion of copper in rats
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The properties of six chelating agents that form highly stable complexes with transition metals has been examined in a comparative study for the elimination of copper in rats. For cyclic ligands, effectiveness grows with the stability constants of their complexes with this metal. With respect to Trien L5 and Penicillamine L6, aliphalic ligands used in human therapy the 1,4,7,10,13-pentaazacyclopentadecane has proven to be more effective. After treatment by this macrocyclic polyamine, urinary excretion reached 60 times that observed in the control animals. The acute toxicity measurements in mice demonstrated that the intrinsically slightly toxic ligands are less so than their corresponding complexes. Considered in their entirety these results, with L2, permit the inference of an improvement in Wilson's disease therapy.
- Pilichowski,Borel,Meyniel
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p. 425 - 431
(2007/10/02)
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- Macrocyclic polyamines
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Macrocyclic polyamines containing 3-7 nitrogen atoms in the ring and destablized to complex formation by (1) an asymmetric ring and/or (2) provision of nitrogen atoms in excess of that required for complex formation are described. The compounds can be used to extract metal ions from solution. The metal complexes are thermally activated curing agents for epoxy resins.
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