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New medical use of triazine derivatives

Patent number WO2008/007149 (New medical use of triazine derivatives) and WO2009/0900431 (Cyclic triazo and diazo sodium channel blockers) are representative of a portfolio of filed and territory (UK, US, EU, Australia, Israel, China) granted patents. The patents cover compounds which are novel inventions, discovered and generated by the University of Greenwich (School of Science) spin out company: CenTRion Therapeutics Limited. The novel patented compounds are principally triazine analogues (but also representative pyrimidines and pyrazines) of the triazine anti-epileptic agent Lamotrigine (Lamictal), marketed by GSK. Lamotrigine is a substituted phenyl triazine. A principal inventor (Leach) of the novel CenTRion analogues played a key role in the original discovery and development of Lamotrigine for the treatment of adult and paediatric epilepsy.

WO2008/007149 is an invention where the general formula is a phenyl triazine and R1 substitution on a triazine nitrogen is alkyl, alkenyl, alkynyl or cycloalkyl . R2-R6 (phenyl ring) are selected from hydrogen, halogen , alkyl, alkenyl, alkynyl or alkoxy, or other substituents. WO2009/090431is an invention where substitution on R1 triazine nitrogen is alkyl, alkenyl, alkynyl or cycloalkyl. R2-R6 (phenyl ring) are selected from hydrogen, halogen, alkyl, alkenyl, alkynyl or alkoxy (all optionally substituted by one or more of halogen, hydroxy and aryl), amino, mono- or di-substituted amino, alkenyloxy, acyl, acyloxy, cyano, nitro, aryl and alkylthio groups or any adjacent two of R2-R6 are linked to form a (-CH=CH-CH=CH-) group.

The compounds protected by patents WO2008/007149 and WO2009/0900431 are orally active voltage gated sodium channel (VGSC) blockers. These VGSCs have a recognized role in the cause and symptoms of numerous disease states, including epilepsy, multiple sclerosis, neuropathic pain, stroke and other cerebral traumas and brain degenerative disorders. As such VGSCs are Pharma industry drug targets. Some triazine compounds within the above patents are also anti-folates, inhibiting mammalian dihydrofolate reductase, and thus may be useful for mammalian cancers.