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:
Aug. 02, 2022

Filed:

Oct. 02, 2018
Applicant:

University of Notre Dame Du Lac, South Bend, IN (US);

Inventors:

Marvin J. Miller, South Bend, IN (US);

Serena Carosso, South Bend, IN (US);

Rui Liu, South Bend, IN (US);

Patricia Miller, South Bend, IN (US);

Assignee:

University of Notre Dame du Lac, South Bend, IN (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61K 31/427 (2006.01); A61P 31/04 (2006.01); A61K 31/431 (2006.01); A61K 38/12 (2006.01);
U.S. Cl.
CPC ...
A61K 31/427 (2013.01); A61P 31/04 (2018.01); A61K 31/431 (2013.01); A61K 38/12 (2013.01);
Abstract

Bromine induced lactamization of vinyl acetohydroxamates facilitated syntheses of monocyclic β-lactams suitable for incorporation of a thiomethyl and extended functionality at the C(4) position. Elaboration of the resulting substituted N-hydroxy-2-azetidinones allowed incorporation of functionalized α-amino substituents appropriate for enhancement of antibiotic activity. Evaluation of antibacterial activity against a panel of Gram-positive and Gram-negative bacteria revealed structure-activity-relationships (SAR) and identification of potent new monobactam antibiotics. The corresponding bis-catechol conjugate, 42, has excellent activity against Gram-negative bacteria including carbapenemase and carbacephalosporinase producing strains ofwhich have been listed by the WHO as being of critical concern worldwide.


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