Oxford University Innovation Limited

Isis Innovation Limited

Michael Arnold McDonough

Christopher Joseph Schofield

Jürgen Brem

Peter John Ratcliffe

Philip Stephen Jones

Matthew Edward Cockman

Angus John Morrison

Kirsty Sarah Hewitson

Sander S Van Berkel

Nicolas Joseph Jean Granatino

Norma Masson

Anna M Rydzik

Joanne Hewitt

Andrew Pannifer

The present invention relates to certain compounds, in particular, indole derivatives that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection.

Inhibitors of metallo-beta-lactamases

A compound which is a thienolate of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R, R, Ring A1, n and Ring A2 are as defined herein, are found to be useful in inhibiting metallo-beta-lactamase and therefore in potentiating the activity of beta lactamase antibiotics. The compound can be used alone or in combination with a rhodanine of formula (II) or a pharmaceutically acceptable salt thereof: (II) wherein R, Ring A1, n, Ring A2, L and Ring B are as defined herein. Treatment or prevention of bacterial infection in combination with beta-lactam antibiotic agents is also provided. 

Beta lactamase inhibitors

The present invention comprises a method for assaying oxygenase activity the method comprising monitoring oxygenase activity of Mina53.

Mina53 assays

A method of identifying an agent which modulates 2-oxoglutarate dependent oxygenase activity, the method comprising contacting a 2-oxoglutarate dependent oxygenase and a test agent in the presence of a substrate comprising one or more ankyrin repeat, or fragment thereof, in conditions under which the substrate is hydroxylated in the absence of the test agent; and determining hydroxylation of the substrate.

Assays for identifying modulators of the hydroxylation of ankyrin repeat proteins by 2-oxoglutarate dependent oxygenase and methods of using the same

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Oxford, United Kingdom

Michael Arnold McDonough