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:
Feb. 02, 2016

Filed:

Oct. 21, 2011
Applicants:

Benjamin Cravatt, La Jolla, CA (US);

Daniel Nomura, San Diego, CA (US);

Jae W. Chang, La Jolla, CA (US);

Inventors:

Benjamin Cravatt, La Jolla, CA (US);

Daniel Nomura, San Diego, CA (US);

Jae W. Chang, La Jolla, CA (US);

Assignee:

The Scripps Research Institute, La Jolla, CA (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07C 69/017 (2006.01); C07D 409/12 (2006.01); C07C 271/44 (2006.01); C07C 271/46 (2006.01); C07C 271/48 (2006.01); C07D 207/327 (2006.01); C07D 307/86 (2006.01); C07D 317/16 (2006.01); C07D 403/12 (2006.01); C07D 405/12 (2006.01); C07D 207/337 (2006.01); C07D 307/87 (2006.01); C07D 333/24 (2006.01);
U.S. Cl.
CPC ...
C07D 409/12 (2013.01); C07C 69/017 (2013.01); C07C 271/44 (2013.01); C07C 271/46 (2013.01); C07C 271/48 (2013.01); C07D 207/327 (2013.01); C07D 207/337 (2013.01); C07D 307/86 (2013.01); C07D 307/87 (2013.01); C07D 317/16 (2013.01); C07D 333/24 (2013.01); C07D 403/12 (2013.01); C07D 405/12 (2013.01);
Abstract

Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar ICvalues. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.


Find Patent Forward Citations

Loading…