Dipyridoxyl phosphate nmri contrast agents

Details Dipyridoxyl phosphate nmri contrast agents Dipyridoxyl phosphate nmri contrast agents

C - Chemistry, Metallurgy

07

F

167/36, 260/277.

C07F 9/58 (2006.01) A61K 49/00 (2006.01) A61K 49/06 (2006.01) C07F 13/00 (2006.01) G01R 33/28 (2006.01)

Patent

CA 1322003

-59- Abstract of the Invention N,N'-bis-(pyridoxal-5-phosphate)-alkylenediamine- N,N'-diacetic acids, N,N'-bis-(pyridoxal-5-phosphate)- 1,2-cycloalkylenediamine-N,N'-diacetic acids, and N,N'-bis-(pyridoxal-5-phosphate)-1,2-arylenediamine- N,N'-diacetic acids, the corresponding monophosphate compounds and monoacetic acid compounds, and their salts and esters form stable, highly soluble chelates with paramagnetic metal ions, and are highly effective NMRI contrast agents. Preferred contrast agents are paramagnetic ion chelates of N,N'-bis-(pyridoxal-5-phosphate)ethylene- diamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal- 5-phosphate)trans-1,2-cyclohexylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-arylened- iamine-N,N'-diacetic acid, and the soluble calcium salts thereof. Novel intermediates for forming these compounds are N,N'-bis(pyridoxal-5-phosphate)alkylenediimines, N,N'-bis(pyridoxal-5-phosphate)alkylenediamines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalkylenedi- imines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalky- lenediamines, N,N'-bis(pyridoxal-5-phosphate)-1,2-ary- lenediamines, and the corresponding monophosphate compounds.

565428

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