Novel Imaging Agents for Detecting Neurological Dysfunction
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a neurological dysfunction and imaging agent technology, applied in the direction of drug compositions, isotope introduction of heterocyclic compounds, metabolic disorders, etc., can solve the problems of senile plaques and tangles, drug intervention has yet to commercialize curative therapy, and inhibit cognitive decline therapeutically ineffectively
Inactive Publication Date: 2011-02-24
SIEMENS MEDICAL SOLUTIONS USA INC
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[0010]A is N or CR1; B is N or CR2; J is N or CR3; K is N or CR4; L is N or CR5; M is N or CR6; ...
Problems solved by technology
Despite Alzheimer's disease being the fourth leading cause of death in the United States, pharmaceutical intervention has yet to commercialize a curative therapy.
Despite the usefulness of cholinesterase inhibitors, the current array of AD therapeutics can only delay full-onset AD by approximately two to three years, after which they are therapeutically ineffective in inhibiting cognitive decline.
There are several issues, however, that question the validity of imaging senile plaques and tangles.
First, the curren...
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[0148]The present invention is directed to compounds having the structural Formula I where the radicals have the meanings given above.
[0149]“Halogen” or “halo” means F, Cl, Br and I.
[0150]“Alkyl” means a saturated monovalent hydrocarbon radical having straight or branched moieties. Examples of alkyl groups include, but are not limited to, methyl, ethyl, n-propyl, isopropyl and t-butyl.
[0151]“Alkenyl” means an alkyl moieties having at least one carbon-carbon double bond wherein alkyl is as defined above. Examples of alkenyl include, but are not limited to, ethenyl and propenyl,
[0152]“Alkynyl” means alkyl moieties having at least one carbon-carbon triple bond wherein alkyl is as defined above. Examples of alkynyl groups include, but are not limited to, ethynyl and 2-propynyl,
[0153]“Alkylene” or “alkenylenyl” means a saturated, divalent hydrocarbon radicals i.e., generally present as a bridging or linking group between two other groups, having straight or branched moieties. Examples of...
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Abstract
Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease
Description
RELATED APPLICATIONS[0001]The present application is a National Stage entry of PCT / US09 / 00961, filed Feb. 17, 2009, which claims the priority of U.S. provisional application No. 60 / 066,101, filed Feb. 14, 2008. PCT / US09 / 00961 and U.S. provisional application No. 60 / 066,101 are incorporated herein by reference.BACKGROUND[0002]Alzheimer's disease (AD), a leading cause of dementia, develops in one percent of the population between the ages 65 and 69, and increasing to 40-50% in those 95 years and older. AD patients exhibit telltale clinical symptoms that include cognitive impairment and deficits in memory function. In these patients, heavy senile plaque burden found in the cerebral cortex, verified by post mortem histopathological examination, confirms the presence of AD. The mature senile plaques consist of intracellular neurofibrillary tangles (NFT) derived from filaments of hyperphosphorylated tau proteins, and extracellular β-amyloid peptides derived from enzymatic processing of am...
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Application Information
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