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:
Apr. 24, 2018

Filed:

Dec. 04, 2013
Applicants:

The Board of Trustees of the University of Illinois, Urbana, IL (US);

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

Inventors:

Wei Zhu, Urbana, IL (US);

Steffen Lindert, San Diego, CA (US);

Yonghui Zhang, Beijing, CN;

William Sinko, La Jolla, CA (US);

Kai Li, Urbana, IL (US);

James Andrew McCammon, La Jolla, CA (US);

Eric Oldfield, Champaign, IL (US);

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07H 15/26 (2006.01); A61K 31/4178 (2006.01); A61K 31/506 (2006.01); A61K 31/551 (2006.01); A61K 31/7034 (2006.01); C07H 15/203 (2006.01); A61K 31/167 (2006.01); A61K 31/4439 (2006.01); C07D 233/24 (2006.01); C07D 239/06 (2006.01); C07D 239/28 (2006.01); C07D 243/04 (2006.01); C07D 209/08 (2006.01); A61K 31/43 (2006.01); A61K 31/7056 (2006.01);
U.S. Cl.
CPC ...
C07H 15/26 (2013.01); A61K 31/167 (2013.01); A61K 31/4178 (2013.01); A61K 31/43 (2013.01); A61K 31/4439 (2013.01); A61K 31/506 (2013.01); A61K 31/551 (2013.01); A61K 31/7034 (2013.01); A61K 31/7056 (2013.01); C07D 209/08 (2013.01); C07D 233/24 (2013.01); C07D 239/06 (2013.01); C07D 239/28 (2013.01); C07D 243/04 (2013.01); C07H 15/203 (2013.01);
Abstract

With the rise in resistance to antibiotics such as methicillin, there is a need for new drugs. The invention provides small molecules that inhibit cellular drug targets such as UPPS and FPPS by interacting with binding pockets, thereby preventing enzyme function. Compounds described herein are also active against(MIC90˜0.25 μg/mL), can potently synergize with methicillin (fractional inhibitory concentration index=0.25), and are protective in a mouse infection model. The invention therefore provides numerous compounds for anti-bacterial treatments and for restoring sensitivity to drugs such as methicillin, using combination therapies.


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