| abstract |
The present invention relates to phenoxymethyl piperidinenderivatives, and pharmaceutically acceptable salts and N -oxidesnthereof, which are sodium channel blockers, and thus exhibit usefulnpharmacological properties, including utility for the treatment ofnneuropathic pain conditions. n represented by formula I:n nwhere:n R 1 is hydrogen,n(C1-4)alkyl, -(CH 2 ) m cycloalkyl,n-(CH 2 ) m NR 7 R 8 , orn-(CH 2 ) m NR 7 SO 2 R 9 ; m is 1 to 3; R 7 and R 8 are independently hydrogen orn(C1-4)alkyl; and R 9 is (C1-4)alkyl; R 2 ,R 3 ,R 5 , and R 6 arenindependently hydrogen, (C1-4)alkyl, or halogen; R 4 is hydrogen, (C1-4)alkyl, hydroxy, alkyloxy, fluoroalkyloxy,nhalogen, or phenyl or mono- or di-substituted phenyl, the substituentsnselected from alkyloxy, amino, nitro or acetylamino; nprovided that when R 1 is hydrogen at least two ofnR 2 ,R 3 ,R 4 ,R 5 , and R 6 arenother than hydrogen; and further provided that when R 1 isnmethyl and R 2 ,R 3 ,R 5 and R 6 arenhydrogen, R 4 is other than fluoro; nor a pharmaceutically acceptable salt or N -oxide thereof, as annindividual isomer or as a racemic or non-racemic mixture of isomers. |