Antibiotic and non-antibiotic tetracycline patents: 2002 – 2007

Abstract

Background: Infectious diseases in all populations are increasing in frequency and severity as the problem of antibiotic resistance continues to emerge. As other antibiotics become ineffective, it is up to researchers worldwide to create new and more potent compounds to thwart such diseases. Objective: This review presents the recent efforts and patent portfolios of those groups actively engaged in tetracycline research. Methods: The tetracyclines, once studied thoroughly shortly after their discovery > 50 years ago, have been neglected as new sources of scaffolds suitable for producing more potent compounds until recently, where several companies and research institutions have described newer and more potent analogs via semisynthesis or by total synthesis. Furthermore, other useful therapeutic properties of the tetracyclines have also been discovered, primarily as observations from their use as clinical antibiotic agents, in the areas of inflammation, neurodegeneration and diseases characterized by tissue degradation. Results and conclusions: The recent patents pertaining to the synthesis and biological properties indicate that the tetracyclines are undergoing a renaissance as their activities are being revised against prokaryotic organisms and against mammalian disease states related to inflammation.

Keywords::

• aminomethylcyclines
• antiparasite agents
• calpain inhibitors
• convergent tetracycline synthesis
• matrix metalloproteases
• oxazoles
• PTK0796
• resistant bacteria
• semisynthesis
• tetracycline prodrugs
• tetracyclines
• tigecycline
• total synthesis
• transition metal reactions