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:
Mar. 03, 2020

Filed:

Jul. 10, 2015
Applicant:

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

Inventor:

Dale L. Boger, La Jolla, CA (US);

Assignee:

THE SCRIPPS RESEARCH INSTITUTE, La Jolla, CA (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 38/00 (2006.01); C07K 9/00 (2006.01);
U.S. Cl.
CPC ...
C07K 9/008 (2013.01); A61K 38/00 (2013.01);
Abstract

The total synthesis and evaluation of key analogs of vancomycin containing single atom changes in the binding pocket are disclosed as well as their peripherally modified, N-(hydrophobe-substituted) derivatives exemplified by a N-4-(4'-chlorobiphenyl)-methyl derivative and their pharmaceutically acceptable salts are disclosed. Their evaluation indicates the combined pocket and peripherally modified analogs exhibit a remarkable spectrum of antimicrobial activity and truly impressive potencies against both vancomycin-sensitive and -resistant bacteria, and likely benefit from two independent and synergistic mechanisms of action. A pharmaceutical composition containing a contemplated compound or its pharmaceutically acceptable salt is disclosed, as is a method of treating a bacterial infection in a mammal by administering an antibacterial amount of a contemplated compound or its salt as above to an infected mammal in need of treatment.


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