Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|Title:||Dipyridoxyl phosphate chelating compound intermediates useful as NMRI contrast agents|
|Abstract:||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)ethylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-cyclohexylenediamine-N,N'-diacet ic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-arylenediamine-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-cycloalkylenediimines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalkylenediamines, N,N'-bis(pyridoxal-5-phosphate)-1,2-arylenediamines, and the corresponding monophosphate compounds.|
|Inventor(s):||Rocklage; Scott M. (Saratoga, CA), Quay; Steven C. (Los Altos Hills, CA)|
|Assignee:||Salutar, Inc. (Sunnyvale, CA)|
1. An improvement in the method of performing NMR imaging with a patient, comprising administering to the patient an effective amount of a chelate of a compound of the formula I with a
metal ion having an atomic number within the range of 21 to 29, 42, 44, or 58-70: ##STR9## wherein R is hydrogen or ##STR10## R.sub.1 is hydrogen or ##STR11## with the proviso that at least one of R and R.sub.1 is other than hydrogen;
R.sub.5 and R.sub.6 are each, independently, hydroxy, alkoxy having from 1 to 18 carbons, hydroxy-substituted alkoxy having from 1 to 18 carbons, amino, or alkylamido having from 1 to 10 carbons;
R.sub.3 is alkylene having from 1 to 8 carbons, 1,2-cycloalkylene having from 5 to 8 carbons, or 1,2-arylene having from 6 to 10 carbons;
R.sub.4 is hydrogen, hydroxymethyl, alkyl having from 1 to 6 carbons, or ##STR12## each R.sub.7 is, independently, hydrogen, hydroxy-substituted alkyl having from 1 to 18 carbons; or a physiologically biocompatible inorganic or organic cation salt of said chelatable compound.
2. A method according to the formula I of claim 1 wherein each R.sub.7 is, independently, hydrogen.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.