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PENTAFLUOROSULFANYL ANALOGS OF MEFLOQUINE, METHODS OF MAKING AND METHODS OF USING SAME
The present invention relates to new mefloquine derivatives and therapeutic compositions comprising one or more mefloquine derivatives. Mefloquine derivatives of the invention have at least one pentafluorosulfanyl moiety substitution at the 6 or 7 or 8 position. Certain mefloquine derivatives further include a quinoline methonal moiety substitution at the 4 position. These compositions are useful in the reduction, treatment, or prevention of malaria, microbial, parasitic, protozoan, bacterial, and fungal diseases and conditions. Advantageously, compositions of the invention are less able to cross the blood-brain barrier than mefloquine and as a result produce fewer adverse side effects to the central nervous system as compared to mefloquine.
Publication/Issued No.:WO 2010/144102
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Inventor(s):DOW, G.; MILNER, E.; WIPF, P.; GEIB, S.; MO, T.