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Novel synthetic route provides for huge array of newchemical entities, whilst the original route had little scope to produce such compounds.
About
Overview Overview Mecamylamine (Inversine ®) is a general nicotinic acetylcholine receptor (nAChR) antagonist drug that was previously used to treat high blood pressure prior to the discovery and clinical use of beta-blockers. More recently mecamylamine (MA) has been reinvestigated as an antiaddiction agent and to treat conditions such as depression, ADHD, Tourette’s syndrome amongst others by action at nicotinic acetylcholine receptors. Despite such potential over numerous disease states only limited SAR information is available. Researchers at Trinity College Dublin have devised a novel synthetic route facilitating the preparation of a library of MA derivatives that are inaccessible by prior art synthetic methods. The novel and inventive compounds prepared by the method of the present invention may find utility in the treatment of any condition responsive to the antagonism of nicotinic acetylcholine receptors. Advantages Novel synthetic route provides for huge array of new chemical entities, whilst the original route had little scope to produce such compounds. MA has an excellent biological profile, good absorption, pharmacokinetics and crosses the blood-brain-barrier and millions of doses have been employed in humans. Offers potential new therapeutics for addiction and/or depression along with other CNS issues/disorders for example Tourette’s Syndrome and ADHD The analogues have been prepared with the aim of providing a more efficacious treatment with reduced sideeffects. Technology and Patent Status Preliminary testing of the first library is extremely positive. The novel compounds are at worst comparable to MA however, one compound is a considerably more potent antagonist of the alpha-4- beta-2 nicotinic acetylcholine receptor than the lead compound MA. Preliminary electrophysiological testing of the initial compound library has shown that most compounds have similar or slightly improved activity with respect to MA itself but one compound in particular is a significantly more potent antagonist than MA. A priority patent application has been filed with the EPO. Applications Treatment of a condition responsive to antagonism of a nicotinic acetylcholine receptor; Treatment of substance addiction, aiding smoking cessation; Treatment of depression The Opportunity These high-growth-potential compounds have been developed from their inception to be suitable for clinical development and commercialisation. Trinity College Dublin are offering an opportunity to collaborate and/or licence the technology for further development.