Methylgene, Inc.

Methylgere, Inc.

Jubrail Rahil

Jeffrey M Besterman

Arkadii Vaisburg

Rex Pratt

Daniel Delorme

Milton L Hammond

Helen Y Chen

Stephane Raeppel

Kevin D Dykstra

Michael Mannion

Katherine Young

Frederic Gaudette

Jeffrey Donald Hermes

Qiang Tan

Seongkon Kim

Nafsika Georgopapadakou

Nancy Z Zhou

Frank Dininno

This invention provides novel &#x3b2;-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of &#x3b2;-lactamases and synergize the antibacterial effects of &#x3b2;-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the &#x3b2;-lactam antibiotics as a result of the presence of the &#x3b2;-lactamases.

Inhibitors of beta-lactamase

The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &#x3b2;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &#x3b2;-lactamase inhibitors presently available, and which do not require a &#x3b2;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Inhibitors of &#x3b2;-lactamase

The invention provides novel &#x3b2;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &#x3b2;-lactamase inhibitors presently available, and which do not possess a &#x3b2;-lactam pharmacophore. These new inhibitors are fully synthetic, allowing ready access to a wide variety of structurally related analogs. Certain embodiments of these new inhibitors also bind bacterial DD-peptidases, thus potentially acting both as &#x3b2;-lactamase inhibitors and as antibiotics.

Acyl phosphonate inhibitors of &#x3b2;-lactamases

Sulfonamidomethyl phosphonate inhibitors of &#x3b2;-lactamase

The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &#x3b2;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &#x3b2;-lactamase inhibitors presently available, and which do not require a &#x3b2;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not possess &bgr;-lactam pharmacophore. These new inhibitors are fully synthetic, allowing ready access to a wide variety of structurally related analogs. Certain embodiments of these new inhibitors also bind bacterial DD-peptidases, thus potentially acting both as &bgr;-lactamase inhibitors and as antibiotics.

&bgr;-lactamase and DD-peptidase inhibitors

The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not possess a &bgr;-lactam pharmacophore. These new inhibitors are fully synthetic, allowing ready access to a wide variety of structurally related analogs. Certain embodiments of these new inhibitors also bind bacterial DD-peptidases, thus potentially acting both as &bgr;-lactamase inhibitors and as antibiotics.

Acyl phosphonate inhibitors of &bgr;-lactamases

The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

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Montreal, Canada

Jubrail Rahil