TRIAZOLS REPLACED WITH BIARILO AS BLOCKERS OF SODIUM CHANNELS.

摘要

A pharmaceutical composition comprising a therapeutically effective amount of a compound represented by Formulas (I) or (II): (See formulas) or a pharmaceutically acceptable salt thereof, wherein R 1 is (a) H; (b) C1-C6 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C3-C6 cycloalkyl or C1-C4 alkylene- [C3-C6 cycloalkyl], any of which is optionally substituted with one or more of the following substituents : F, CF3, OH, O-C1-C4 alkyl, S (O) 0-2-C1-C4 alkyl, O-CONR a R b, NR a R b, N (R a) CONR a R b, COO -C1-C4 alkyl, COOH, CN, CONR a R b, SO3NR a R b, N (R a) SO2NR a R b, -C (= NH) NH2, tetrazolyl, triazolyl, imidazolyl, oxazolyl, oxadiazolyl, isoxazolyl, thiazolyl, furyl, thienyl, pyrazolyl, pyrrolyl, pyridyl, pyrimidinyl, pyrazinyl, phenyl, piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl; (c) -C0-C4 alkylene-C1-C4 perfluoroalkyl; (d) NO2; (e) NR a R b, -N (COR a) R b, -N (SO2R a) R b, -N (R a) SO2R a, -N (OR a) CONR a R b, -N (R a) CON (R a) 2 or -N (R a) SO2N (R a) 2; (f) -CH (OR a) R a, -C (OR b) CF3, -CH (NHR b) R a, -C (= O) R a, C (= O) CF3, -SOCH3, -SO2CH3 , COOR a, CN, CONR a R b, -COCONR a R b, -SO2NR a R b, -CH2O-SO2NR a R b, SO2N (R a) OR a, -C (= NH) NH2, -CR 2 = NOR a, CH = CHCONR a R b; (g) -CONR a (CH2) 0 - 2C (R a) (R b) (CH2) 0 - 2CONR a R b; (h) tetrazolyl, tetrazolinonyl, triazolyl, triazolinonyl, imidazolyl, imidazolonyl, oxazolyl, oxadiazolyl, isoxazolyl, thiazolyl, furyl, thienyl, pyrazolyl, pyrazolonyl, pyrrolyl, pyridyl, pyrimidinyl, pyrazinyl or phenyl, whichever one of which is substituted with any of the 1, -3 independent substituents selected from i) F, Cl, Br, I, ii) -CN, iii) -NO2, iv) -C (= O) R a, v) C1-C6 alkyl, vi) -OR a, vii) -NR a R b, viii) -C0-C4-CO-OR alkylene a, ix) - (C0-C4 alkylene) -NH-CO-OR a, x) - (C0-C4 alkylene) -CO- NR a R b, xi) -S (O) 0-2R a, xii) -SO2NR a R b, xiii) -NHSO2R a, xiv) -C1-C4-perfluoroalkyl and xv) -O-C1-C4-perfluoroalkyl; (i) -C (R a) = C (R b) -COOR a or -C (R a) = C (R b) -CONR a R b; (j) (See formula) (k) piperidin-1-yl, morpholin-4-yl, pyrrolidin-1-yl, piperazin-1-yl or 4-substituted piperazin-1-yl, any of which is optionally substituted with 1-3 substituents selected from i) -CN, ii) -C (= O) (R a), iii) C1-C6 alkyl, iv) -OR a, v) -NR to R b, vi) -alkylene C0-C4-CO-OR a, vii) - (C0-C4 alkylene) -NH-CO-OR a, viii) - (C0-C4 alkylene) -CON (R a) (R b), ix) -SR a, x) -S (O) 0 - 2R a, xi) -SO2N (R a) (R b), xii) -NR a SO2R a, xiii) -C1-C4-1-perfluoroalkyl-O-perfluoroalkyl C1 -C4; R a is ...