Novel compounds - Patents

Novel compounds

Agent: Swanson & Bratschun L.L.C. - Highlands Ranch, CO, US
Inventors: Deiter Wolfgang Hamprecht, Richard Lewis Jarvest
Applicaton #: 20060287360
Class: 514314000 (USPTO)
12/21/06
Novel NH-substituted fused triazoles are inhibitors of the bacterial enzyme S aureus methionyl t RNA synthetase and are of use in treating bacterial infections.
[0001] The present invention relates to novel NH-substituted fused triazoles which are inhibitors of methionyl t-RNA synthetase (MRS), processes for their preparation and their use in therapy as anti-bacterial agents.
[0002] t-RNA synthetases are involved in protein biosynthesis so that inhibition thereof may be expected to lead to a cessation of cell growth. Thus, for instance, the compound mupirocin, produced by the organism Pseudomonas fluorescens, is an anti-bacterial agent and is used as the active ingredient in the product Bactroban, marketed by SmithKline Beecham. Mupirocin has been shown to be an inhibitor of the isoleucyl t-RNA synthetase. Each t-RNA synthetase represents a separate target for drug discovery. t-RNA synthetase inhibitors which are selective for bacterial cells over mammalian cells are of considerable therapeutic interest as they have the potential to be used as anti-bacterial agents.
[0003] The sequence of the t-RNA synthetase genes in organisms such as S aureus have recently been determined, see for instance European Patent application no 97300317.1 (SmithKline Beecham, S aureus MRS), thereby assisting the process of identifying inhibitors.
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