| abstract |
The compound of formula I; or optically active isomer thereof, wherein R 1 is selected from the group consisting of (a) linear or branched chain C 1-6 alkyl or C 2-5 alkenyl optionally substituted with substituents selected from the group consisting of hydroxy, C 1-4 alkoxy, C 1-4 alkylthio , and halogen; R is hydrogen; R 2 is selected from the group consisting of (a) linear or branched chain C 1-6 alkyl or C 3-6 alkenyl optionally substituted with substituents selected from the group consisting of halogen, C 1-4 alkoxy, and NR 4 R 5 (b) C3-7cycloalkylmethyl optionally substituted with substituents selected from the group consisting of amino, (C1-4alkyl) NH-, di (C1-4alkyl) N-, C1-4alkylC (= O) NH-, and C1- (C) linear or branched chain C 1-6 alkyl-C (= O) -A; (d) -B-naphthyl; (e) D and E are each independently a direct bond, linear or branched chain C 1-6 alkyl, C 2-6 alkenyl, or C 3-7 cycloalkyl; Z is selected from the group consisting of hydrogen, C 1-4 alkyl, C 1-4 alkoxy, halogen, cyano , hydroxy, -OCHF2, -OCF3, -CF3, and -CHF2; X and Y are each independently selected from the group consisting of hydrogen, hydroxy. halogen, (halogen) 3C-, (halogen) 2CH-, C1-4alkylS-, C1-4alkylS (O) -, C1-4alkylSO2-, nitro, F3S-, and cyano; -OR6; -NR4R5; -NR7C (= O) R8; -NR7C (= O) OR8; -NHSO2 C 1-4 alkyl; -C (= O) W wherein W is selected from the group consisting of hydroxy, C1-4alkyl, C1-4alkoxy, phenoxy, and -NR4R5; -OC (= O) C 1-4 alkyl; -phenyl wherein said phenyl is optionally substituted with cyano. halogen, C1-4alkoxy, C1-4alkylS-, CH3C (= O), C1-4alkylS (O) -, or C1-4alkylSO2-; and a heterocyclic group wherein said heterocyclic group is selected from the group consisting of furanyl, thiofuranyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl. pyridinyl, pyrimidinyl. oxadiazolyl, oxazolyl, isoxazolyl, thiadiazolyl, and thiazolyl. wherein said heterocyclic group is optionally substituted with substituents selected from the group consisting of cyano, halogen, C1-4alkyl, (halogen) C1-4alkyl, and CO2 C1-4alkyl; (f) -B- (heterocycle), wherein said heterocycle selected from the group consisting of furanyl, thiofuranyl. pyrrolyl, imidazolyl, pyrazolyl. triazolyl, tetrazolyl, pyridinyl, pyrimidinyl, oxadiazolyl, oxazolyl, isoxazolyl, thiadiazolyl and thiazolyl, wherein said heterocycle is optionally substituted with substituents selected from the group consisting of cyano, halogen, (C1-4alkyl), amino C1-4alkyl, CO2 C1-4alkyl (C1-4alkyl) NH-, di (C1-4alkyl) N-, morpholin-4-yl, thiomorpholin-4-yl, pyrrolidin-1-yl, piperidin-1-yl, piperazin-1-yl, and 4- (C1-6alkyl) piperazin-1-yl; (g) -B- (piperidin-4-yl), wherein said piperidin-4-yl is optionally substituted with substituents selected from the group consisting of linear or branch-chain C1 -6alkyl, CH2C (= O) phenyl, phenyl and phenylmethyl where C1-6alkyl and f |