The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jul. 02, 2019

Filed:

Apr. 02, 2016
Applicant:

Washington University, Saint Louis, MO (US);

Inventors:

G. S. M. Sundaram, Saint Louis, MO (US);

Jothilingam Sivapackiam, Saint Louis, MO (US);

Vijay Sharma, Wildwood, MO (US);

Assignee:

Washington University, St. Louis, MO (US);

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 51/00 (2006.01); A61M 36/14 (2006.01); A61K 51/04 (2006.01); C07F 7/18 (2006.01); C07D 417/06 (2006.01); C07D 421/06 (2006.01); C07D 277/64 (2006.01); C07D 277/66 (2006.01); C07D 293/12 (2006.01); C07B 59/00 (2006.01); G01N 33/60 (2006.01); G01N 33/68 (2006.01);
U.S. Cl.
CPC ...
A61K 51/0459 (2013.01); A61K 51/0453 (2013.01); A61K 51/0455 (2013.01); A61K 51/0465 (2013.01); C07B 59/002 (2013.01); C07D 277/64 (2013.01); C07D 277/66 (2013.01); C07D 293/12 (2013.01); C07D 417/06 (2013.01); C07D 421/06 (2013.01); C07F 7/1804 (2013.01); G01N 33/60 (2013.01); G01N 33/6893 (2013.01); G01N 33/6896 (2013.01); G01N 2333/4709 (2013.01); G01N 2800/2821 (2013.01); G01N 2800/32 (2013.01);
Abstract

Probes which target diffuse and fibrillar forms of amyloid beta (Aβ) are described. These probes demonstrate high initial brain penetration and facile clearance from non-targeted regions. The agents can be used to image amyloid quantitatively for monitoring efficacy of Aβ-modifying therapeutics and assist in premortem diagnosis of Alzheimer's disease (AD). Disclosed probes can bind Aβ aggregates of preformed Aβfibrils in vitro and can be used to image fibrillar and diffuse plaques ex vivo in brain sections. Disclosed probes can be used to determine Aβ burden in early stages of AD. These probes can be used for multimodality imaging of Aβ. F-AI-187 (1 μM) can detect Aβ plaques in brain sections of APP/PS1 mice. F-AI-187 (10 μM) can detect Aβ plaques in the frontal lobe in a brain section of a patient with confirmed AD. Some probes can be used for fluorescence imaging of plaque.


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