Thioflavin derivatives for use in antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition
AssigneeUniversity of Pittsburgh—Of the Commonwealth System of Higher Eduation
InventorsWilliam E. Klunk, Chester A. Mathis, Jr., Yanming Wang
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Abstract
This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's disease, familial Alzheimer's disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.
Claims17
A method for detecting amyloid deposits in a subject, comprising the steps of;
- (a) administering a detectable quantity of a pharmaceutical composition comprising a compound having a structure selected from the group consisting of:
- wherein the compound has at least one substituent selected from the group consisting of 131I, 125I, 123I, 76Br, 75Br, and 18F, and
- (b) detecting binding of the compound to amyloid deposits in the subject.
A method of detecting amyloid deposits in biopsy or post-mortem human or animal tissue comprising the steps of:
- (a) incubating formalin-fixed or fresh-frozen tissue with a solution of an amyloid binding compound to form labeled deposits, wherein the compound has a structure selected from the group consisting of:
- wherein the compound has at least one substituent selected from the group consisting of 131I, 125I, 76Br, 75Br, and 18F;
- and
- (b) detecting the labeled deposits.
A method of selectively binding a compound to amyloid plaques over neurofibrillary tangles in in vivo brain tissue which comprises both, wherein the compound has a structure selected from the group consisting of:
- wherein the compound has at least one substituent selected from the group consisting of 131I, 125I, 123I, 76Br, 75Br, and 18F,
- comprising administering to a subject in need an effective amount of the compound so that blood concentration of the administered compound remains below 10 nM in vivo.
Dependencies are inferred from the claim text.