β-lactamase and DD-peptidase inhibitors
AssigneeMethylGene Inc.
InventorsJeffrey M. Besterman, Jubrail Rahil, Rex Pratt
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Abstract
The invention provides novel β-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic β-lactamase inhibitors presently available, and which do not possess β-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 β-lactamase inhibitors and as antibiotics.
Claims6
A β-lactamase inhibitor of Formula I
- or a salt thereof;
- wherein X is Ph, C(O)Ph, or Me;
- Y is Z or OZ;
- and Z is Ph, C(O)Ph, Me, or PO3C(O)Ph.
A pharmaceutical composition comprising a β-lactamase inhibitor of Formula I:
- or a salt thereof;
- wherein X is alkyl, alkenyl, alkynyl, aryl, aralkyl, or heterocyclic radical;
- Y is Z or OZ;
- and Z is alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, heterocyclic radical, phosphonyl, or X;
- provided, however, that when Y is Z, then Z is not phosphonyl;
- and further provided that when Y is Z and Z is methyl, then X is not methyl;
- and
- a pharmaceutically acceptable carrier, excipient, or diluent.
A pharmaceutical composition comprising a β-lactamase inhibitor of Formula I
- or a salt thereof
- wherein X is Ph, C(O)Ph, or Me, and Z;
- Y is Z or OZ;
- and Z is Ph, C(O)Ph, Me, or PO3C(O)Ph;
- and
- a pharmaceutically acceptable carrier, excipient, or diluent.
A pharmaceutical composition comprising a β-lactamase inhibitor of Formula II
- wherein Y is O or alkylene, and X is a fused carbocyclic, heterocyclic, aromatic, heteroaromatic ring or phenylene, wherein the fused carbocyclic, heterocyclic, aromatic, heteroaromatic ring or phenylene, may be optionally substituted.
Dependencies are inferred from the claim text.