By Donald Zuhn --
Ulysses Pharmaceuticals announced today that the U.S. Patent and Trademark Office has issued U.S. Patent No. 7,410,974, which is directed to a class of compounds that exhibit antibiotic activity against a wide spectrum of microorganisms, including organisms that are resistant to multiple antibiotic families (the so-called "superbugs"). According to Ulysses Pharmaceuticals' statement, the nitrofuran antibiotics of the '974 patent are "designed to make the development of [drug] resistance almost impossible, because of their exquisite potency, rapid killing of bacteria and multiple mechanisms of action." The Sherbrooke, Quebec-based biotech company, which focuses on the discovery and development of novel antibiotics for empiric monotherapy (i.e., before the causative bacteria are identified) to control resistant bacterial infections, noted that the '974 patent was the first patent to issue from a series of applications covering the company’s technology for combating drug resistant bacteria. The '974 patent is also the company's first U.S. patent; Ulysses Pharmaceuticals is named as an assignee on two U.S. patent application publications.
According to the '974 patent:
The general structural feature of the [disclosed] compounds is a nitrofuran linked to the 2 position of a quinazoline directly or via a vinyl group. It is believed that the nitrofuran is essential for antimicrobial activity while the quinazoline in particular as substituted, e.g., with an halogen and/or a methylpiperazino group, improves potency, expands the spectrum of activity (e.g., activity against E. coli, S. aureus, Salmonella, Mycobacterium, anaerobic bacteria and microorganisms that are resistant to multiple antibiotics), provides a bactericidal (lethal) activity (i.e., as opposed to a bacteriostatic growth-inhibitory activity), provides in vivo activity, and improves solubility.
The '974 patent issued from U.S. Application No. 10/567,660, filed August 6, 2004, which is a national stage application of International Application No. PCT/CA2004/001466, which claims the benefit of U.S. Provisional Application No. 60/493,336, filed Aug. 8, 2003. Independent claim 1 of the '974 patent recites:
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