Substituted 2-carboxyalkyl-3(fluorophenyl)-8-(3-halopropen-2-yl) nortropanes and their use as imaging agents for neurodegenerative disorders
AssigneesOrganix, Inc., The General Hospital Corporation, President and Fellows of Harvard College, Northeastern University
InventorsDavid R. Elmaleh, Bertha K. Madras, Peter Meltzer, Robert N. Hanson
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Abstract
Disclosed are certain cocaine analogs useful for imaging of cocaine receptors and dopamine receptors. Also disclosed are analogs useful for imaging diagnostics for Parkinson's disease.
Claims4
A method of detecting parkinsonism in a human patient comprising administration to said patient of a detectably labelled compound detecting the binding of said compound to CNS tissue, said compound having the formula:
- ##STR2## wherein the following conditions are imposed on that formula:
- R is --CH.sub.3, --CH.sub.2 CH.sub.3, --CH(CH.sub.3).sub.2, --(CH.sub.2).sub.n CH.sub.3, --(CH.sub.2).sub.n C.sub.6 H.sub.4 X, --C.sub.6 H.sub.4 X, --C.sub.6 H.sub.5, --OCH.sub.3, --OCH.sub.3 CH.sub.2, --OCH (CH.sub.3).sub.2, --OC.sub.6 H.sub.5, --OC.sub.6 H.sub.4 X, --O(CH.sub.2).sub.n C.sub.6 H.sub.4 X, or --O(CH.sub.2).sub.n CH.sub.3 ;
- wherein X is --Br, --Cl, --I, --F, --OH, --OCH.sub.3, --CF.sub.3, --NO.sub.2 --NH.sub.2, --CN, --NHCOCH.sub.3, --N(CH.sub.3).sub.2, --(CH.sub.2).sub.n CH.sub.3,CHOCH.sub.3, or --C(CH.sub.3).sub.3, and n is between 0 and 6 inclusive.
A method of selectively monitoring cocaine binding regions of the central nervous system of a human patient comprising administering to the central nervous system a detectably labelled compound and detecting the binding of that compound to CNS tissue, said compound having the formula:
- ##STR3## wherein the following conditions are imposed on that formula:
- R is --CH.sub.3, --CH.sub.2 CH.sub.3, --CH(CH.sub.3).sub.2, --(CH.sub.2).sub.n CH.sub.3, --(CH.sub.2).sub.n C.sub.6 H.sub.4 X, --C.sub.6 H.sub.4 X, --C.sub.6 H.sub.5, --OCH.sub.3, --OCH.sub.3 CH.sub.2, --OCH(CH.sub.3).sub.2, --OC.sub.6 H.sub.5, --OC.sub.6 H.sub.4 X, --O(CH.sub.2).sub.n C.sub.6 H.sub.4 X, or --O(CH.sub.2).sub.n CH.sub.3 ;
- wherein X is --Br, --Cl, --I, --F, --OH, --OCH.sub.3, --CF.sub.3, --NO.sub.2 --NH.sub.2, --CN, --NHCOCH.sub.3, --N(CH.sub.3).sub.2, --(CH.sub.2).sub.n CH.sub.3,CHOCH.sub.3, or --C(CH.sub.3).sub.3, and n is between 0 and 6 inclusive.
Dependencies are inferred from the claim text.