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:
Jan. 11, 2022

Filed:

Jul. 13, 2018
Applicants:

The Regents of the University of California, Oakland, CA (US);

University of Southern California, Los Angeles, CA (US);

Inventors:

Ichiro Nishimura, Venice, CA (US);

Akishige Hokugo, Los Angeles, CA (US);

Kenzo Morinaga, Los Angeles, CA (US);

Charles E. McKenna, Pacific Palisades, CA (US);

Boris A Kashemirov, Los Angeles, CA (US);

Eric T. Richard, Los Angeles, CA (US);

Assignees:
Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61K 49/00 (2006.01); A61K 47/54 (2017.01); A61K 47/64 (2017.01); A61K 9/00 (2006.01); A61K 38/23 (2006.01); A61K 38/29 (2006.01);
U.S. Cl.
CPC ...
A61K 49/0056 (2013.01); A61K 9/007 (2013.01); A61K 9/0014 (2013.01); A61K 9/0031 (2013.01); A61K 9/0053 (2013.01); A61K 38/23 (2013.01); A61K 38/29 (2013.01); A61K 47/548 (2017.08); A61K 47/64 (2017.08); A61K 49/0021 (2013.01);
Abstract

In certain embodiments osteoadsorptive fluorogenic substrates of cathepsin K (or other proteases) are provided. Utilizing a bisphosphonate targeting moiety, the fluorogenic substrates provide effective bone-targeted protease sensor(s). In certain embodiments the 'probes' comprise cleavable fluorophore-quencher pair linked by a cathepsin K (or other protease) peptide substrate and tethered to a bisphosphonate. Unlike existing probes that are cleared within a few days in vivo, the probes described herein (e.g., OFS-1) allow for monitoring resorption over the course of longer time periods with a single dose.


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