Patent IL-106927-A (IL)
Title: Sulfonamide derivatives and pharmaceutical compositions containing the same
IPC: C07D231/14
Filed: 1993-09-06
Abstract: Aspartyl protease inhibitor compounds of the formula 5 ט" ז בטבת התשס" א - January 11, 2001 wherein: A is selected from the group consisting of H; Het*; -R1-Het; -R1-C1-C6 alkyl, which may be optionally substituted with one or more groups selected from the group consisting of hydroxy, C1-C4 alkoxy, Het, -O-Het, -NR2-CO-N(R2) (R2) and -CO-N(R2)(R2); and -R1-C2-C6 alkenyl, which may be optionally substituted with one or more groups selected from the group consisting of hydroxy, C1-C4 alkoxy, Het, -O-Het, -NR2-CO-N(R2)(R2) and -CO-N(R2)(R2); each R1 is independently selected from the group consisting of -C(O)-, -S(O)2-, -C(O)-C(O)-, -O- C(O)-, -O-S(O)2, -NR2-S(O)2-, -NR2-C(O)- and -NR2-C(O)- C(O)-; each Het is independently selected from the group consisting of C3-C7 cycloalkyl; C5-C7 cycloalkenyl; C6-C10 aryl; and 5-7 membered saturated or unsaturated heterocycle, containing one or more heteroatoms selected from N, N(R2), O, S and S(O)n, wherein said heterocycle may optionally be benzofused; and wherein any member of said Het may be optionally substituted with one or more substituents selected from the group consisting of oxo, -OR2, -R2, -N(R2)(R2), -R2-ON, -CN, -CO2R2, -C(O)-N(R2)(R2), -S(O)2-N(R2)(R2), -N(R2)-C(O) -R2, -C(O)-R2, -S(O)n-R2, -OCF3, -S(O)n- Ar, methylenedioxy, -N(R2) - S(O)2 (R2), halo, -CF3, -NO2, Ar and -O-Ar*; each R2 is independently selected from the group consisting of H and C1-C3 alkyl optionally substituted with Ar; with the proviso that when R2 is C1-C3 alkyl substituted with Ar, said Ar may not be substituted with an Ar-containing moiety; B, when present, is -N(R2) -C(R3) (R3) -C(O)-**; x is 0 or 1; 6 ט" ז בטבת התשס" א - January 11, 2001 each R3 is independently selected from the group consisting of H, Het, C1-C6 alkyl, C2-C6 alkenyl, C3-C6 cycloalkyl and C5-C6 cycloalkenyl, wherein any member of said R3, except H, may be optionally substituted with one or more substituents selected from the group consisting of -OR2, -C(O) -NH-R2, -S(O)n- N(R2) (R2), Het, -CN, -SR2, -CO2R2, NR2-C(O)-R2; each n is independently 1 or 2; D and D' are independently selected from the group consisting of Ar; C1-C4 alkyl, which may be optionally substituted with one or more groups selected from C3-C6 cycloalkyl, -OR2, -R3, -O-Ar and Ar; C2-C4 alkenyl, which may be optionally substituted with one or more groups selected from the group consisting of C3-C6 cycloalkyl, -OR2, -R3, -O-Ar and Ar; C3-C6 cycloalkyl, which may be optionaly substituted with or fused with Ar; and C5-C6 cycloalkenyl, which may be optionally substituted with or fused with Ar; each Ar is independently selected from the group consisting of phenyl; 3-6 membered carbocyclic ring and 5-6 membered heterocyclic ring containing one or more heteroatoms selected from O, N, S, S(O)n and N(R2)*, wherein said carboyclic or heterocylic ring may be saturated or unsaturated and optionally substituted with one or more groups selected from the group consisting of oxo, -OR2, -R2, -N(R2)- C(O) -R2, C1-C3 alkyl substituted with -OH and optionally substituted with Ar, -CN, -CO2R2, -C(O) -N(R2)R2) (R2), halo and -CF3; E is selected from the group consisting of Het; O-Het; Het-Het; -O-R3; -NR2R3; C1-C6 alkyl, which may be optionally substituted with one or more groups selected from the group consisting of R4 and Het; C2-C6 alkenyl, which may be optionally substituted with one or more groups selected from the group consisting of R4 and Het; C3-C6 saturated carbocycle, which may optionally be substituted with one or more groups selected from the group consisting or R4 and Het; and C5-C6 unsaturated carbocycle, which may optionally be substituted with one or more groups selected from the group consisting of R4 and Het; and each R4 is independently selected from the group consisting of -OR2, -C(O)-NHR2, -S(O)2-NHR2, halo, -NR2-C(O)-R2 and -CN.