Patent ID: 6399631
Filing Date: 2002-06-04
Classification: C07D

Abstract:
A compound of formula wherein X, Y, and Z are independently selected from (a) hydrogen; (b) halogen; (c) hydroxy; (d) nitro; (e) cyano; (f) C1-C6 alkyl; (g) C1-C6 alkoxy; (h) â€”NR7R8; (i) â€”CH2NR7R8; (j) â€”CH2OR7; (k) â€”C(O)NR7R8; (l) C1-C6 alkylaryl; and R1 is C1-C5 alkyl, alkylaryl, alkenyl, (cycloalkyl)alkyl, or mono or C1-C6 polyfluoroalkyl; and A is NR2COR3 or NR2SO2R3 wherein; R2 is hydrogen, C1-C3 alkyl, C1-C3 alkylaryl, C1-C3 alkenyl, C2-C4 alkynyl, or C1-C3 polyfluoroalkyl; R3 is selected from C1-C6 mono or polyfluoroalkyl, C1-C6 alkyl, excluding CH3, C3-C8 cycloalkyl, C2-C6 alkenyl, C5-C8 cycloalkenyl, C2-C6 alkynyl, or C4-C8 cycloazaalkyl; wherein C1-C6 alkyl, C3-C8 cycloalkyl, C2-C6 alkenyl, C5-C8 cycloalkenyl, C2-C6 alkynyl, or C4-C8 cycloazaalkyl can be independently substituted with one to three substituents selected from the group consisting of F, Br, Cl, aryl, aryloxy, NR4R5, (C1-C6)alkoxy, NO2, OH, ON, COOH, and C1-C6 alkylthio, R4 and R5 are selected independently from H, C1-C6 alkyl, C2-C6 alkenyl, C3-C6 cycloalkyl, C5-C8 cycloalkenyl, C2-C6 alkynyl, aryl, alkylaryl, R7 and R8 are independently selected from C1-C6 alkyl; C2-C6 alkenyl; C2-C6 alkynyl or aryl and optical and geometric or tautomeric isomers thereof; and nontoxic pharmacologically acceptable acid addition salts, N-oxides, esters, and quaternary ammonium salts thereof, with provisos that:when X, Y and Z are hydrogen and A is NR2SO2R3, wherein R2 is hydrogen and R3 is perfluoroalkyl, R1 is not C1-C5 alkyl; and when only one of either X or Y is â€”CH2OR7, then A is not acylamido.