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US 9,757,483 B2Granted
Labeled iodinated tropane formulation
AssigneeAlseres Pharmaceuticals, Inc.
InventorsChris Sterzinger, Cara Ferreira, David Leyh, Richard Thorn
Life of this patent
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Abstract
A diagnostic formulation is provided comprising a tropane having a radioactive concentration of at least 1.6 mCi/mL at least about 51 hours post creation. The diagnostic formulation optionally comprises a radiolabeled dopamine transporter (DAT) ligand useful in the diagnosis of Parkinson's disease (PS). One example of a radiolabeled dopamine transporter (DAT) ligand example is [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane.
Claims1
A product of a process comprising the steps of:
- (a) Preparing a precursor solution comprising 2β-Carbomethoxy-3β-(4-fluorophenyl)-N-(3-tributyltin-E-allyl) nortropane), ethanol, hydrogen peroxide, and a phosphate buffer;
- (b) Preparing a sodium [1231]-iodide solution comprising sodium [1231]-iodide and trifluoroacetic acid having a pH of less than about 2;
- (c) Heating a mixture of said precursor solution and said sodium [123l]-iodide solution at a temperature of about 80° C. for about 15 minutes;
- (d) Eluting said resulting product [1231]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane through a C18 preparative HPLC column with an eluent, wherein the eluent comprises about 15% (v/v) ethanol;
- and
- (e) Collecting product peak in a mixture of sodium chloride and an acetic acid buffer wherein said nortropane product is stable for at least 48 hours.
3 more elements
Dependencies are inferred from the claim text.