A compound of the formula
- and pharmaceutically acceptable salts thereof, wherein:
- R is hydrogen, C1-C6 alkyl, —(CH2)n(C3-C7 cycloalkyl) wherein n is 0 to 2, (C1-C6 alkoxy)C1-C6 alkyl, C2-C6 alkenyl, or —(Z′)b(Z″)c(C6-C10 aryl) wherein b and c are independently 0 or 1, Z′ is C1-C6 alkylene or C2-C6 alkenylene, and Z″ is O, S, SO2, or NR9, and wherein said alkyl, alkenyl, alkoxalkyl, and aryl moieties of said R groups are optionally substituted by one or more substituents independently selected from halo, hydroxy, C1-C5 alkyl, C2-C5 alkenyl, C1-C5 alkoxy, C3-C6 cycloalkoxy, trifluoromethyl, nitro, CO2R9, C(O)NR9R10, NR9R10 and SO2NR9R10;
- R1 is hydrogen, C1-C7 alkyl, C2-C3 alkenyl, phenyl, C3-C7 cycloalkyl, or (C3-C7 cycloalkyl)C1-C2 alkyl, wherein said alkyl, alkenyl and phenyl R1 groups are optionally substituted with up to 3 substituents independently selected from the group consisting of methyl, ethyl, trifluoromethyl, and halo,
- R2a and R2b are independently selected from the group consisting essentially of hydrogen and hereinafter recited substituents, provided that one, but not both of R2a and R2b must be independently selected as hydrogen, wherein said substituents are selected from:
- wherein the dashed lines in formulas (Ia) and (Ib) independently and optionally represent a single or double bond, provided that in formula (Ia) both dashed lines cannot both represent double bonds at the same time;
- m is 0 to 4;
- R3 is H, halo, cyano, C2-C4 alkynyl optionally mono substituted by phenyl;
- C1-C4 alkyl optionally substituted by one or more halogens;
- —CH2NHC(O)C(O)NH2, cyclopropyl optionally substituted by R11, R17, CH2OR9, NR8R10, CH2NR9R10, (CO2R9, C(O)N8R10, C(O)CR11, C(Z)H or CH═CR11R11;
- provided that R3 is absent when the dashed line In formula (Ia) attached to the ring carbon atom to which R3 is attached represents a double bond;
- R4 is H, R6, C(Y)R14, CO2R14, C(Y)NR17R14, CN, C(NR17)NR17R14, C(NOR9)R14, C(O)NR9NR9C(O)R9, C(O)NR8NR17R14, C(NOR14)R9, C(NR9)NR17R14, C(NR14)NR9R10, C(NCN)NR17R14, C(NCN)S(C1-C4 alkyl), CR9R10OR14, CR9R10SR14, CR9R10S(O)nR15 wherein n is 0 to 2, CR8R10NR14R17, CR9R10NR17SO2R15, CR9R10NR17C(Y)R14, CR9R10NR17CO2R15, CR8R10NR17C(Y)NR17R14, CR9R10NR17C(NCN)NR17R14, CR9R10NR17C(CR9NO2)S(C1-C4 alkyl), CR9R10CO2R16;
- CR9R10C(Y)NR17R14, CR9R10C(NR17)NR17R14, CR9R10CN, CR9R10C(NOR10)R14, CR9R10C(NOR14)R10, CR8R10NR17C(NR17)S(C1-C4 alkyl), CR9R10NR17C(NR17)NR17R14, CR9R10NR17C(O)C(O)NR17R14, or CR9R10NR17C(O)C(O)OR14;
- R5 is R8, OR8, CH2OR9, cyano, C(O)R9, CO2R9, C(O)NR9R10, or NR9R10, provided that R5 is absent when the dashed line in formula (Ia) represents a double bond;
- or R4 and R5 are taken together to form —O;
- or R5 is hydrogen and R4 is OR14, SR14, S(O)nR16 wherein n is 0 to 2, SO2NR17R14, NR17R14, NR14C(O)R9, NR17C(Y)R14, NR17C(O)OR15, NR17C(Y)NR17R14, NR17SO2NR17R14, NR17C(NCN)NR17R14, NR17SO2R15, NR17C(CR9NO2)NR17R14, NR17C(NCN)S(C1-C4 alkyl), NR17C(CR9NO7)S(C1-C4 alkyl), NR17C(NR17)NR17R14, NR17C(O)C(O)NR17R14, or NR17C(O)C(O)OR14;
- R6 is independently selected from methyl and ethyl optionally substituted by one or more halogens;
- R11 is independently fluoro or R10;
- R12 is C1-C6 alkyl, C2-C3 alkenyl, C3-C7 cycloalkyl, (C3-C7 cycloalkyl)C1-C2 alkyl, C6-C10 aryl, or C3-C9 heterocyclyl, wherein said R12 groups are optionally substituted with up to 3 substituents independently selected from the group consisting of methyl, ethyl, trifluoromethyl, and halo;
- R13 is hydrogen or R12;
- R14 is hydrogen or R15;
- R15 is C1-C6 alkyl or —(CR9R10)nR16 wherein n is 0 to 2 and R10 and said C1-C9 alkyl are optionally substituted by one or more substituents independently selected from halo, nitro, cyano, NR10R17, C(O)R9, OR9, C(O)NR10R17, OC(O)NR10N17, NR17C(O)NR17R10, NR17C(O)R10, NR17C(O)O(C1-C4 alkyl), C(NR17)NR17R10, C(NCN)NR17R10, C(NCN)S(C1-C4 alkyl), NR17C(NCN)S(C1-C4 alkyl), NR17C(NON)NR17R10, NR17SO2(C1-C4 alkyl), S(O)n(C1-C4 alkyl) wherein n is 0 to 2, NR17C(O)C(O)NR17R10, NR17C(O)C(o)R17, or C1-C2 alkyl optionally substituted with one to three flourines;
- R16 is C3-C7 cycloalkyl;
- R17 is OR8 or R10;
- R18 is H, C(Y)R14, CO2R14, C(Y)NR17R14, CN, C(NR17)NR17R14, C(NOR9)R14, C(O)NR9NR9C(O)R8, C(O)NR8NR17R14, C(NOR14)R9, C(NR9)NR17R14, C(NR14)NR9R10, C(NCN)NR17R14, C(NCN)S(C1-C4 alkyl), CR8R10OR14, CR9R10SR14, CR9R10S(O)nR15 wherein n is 0 to 2, CR9R10NR14R17, CR9R10NR17SO2R15, CR9R10NR17C(Y)R14, CR9R10NR17CO2R15, CR9R10NR17C(Y)NR17R14, or CR9R10NR17C(NCN)NR17R14, or CR9R10NR17C(CR5NO2)S(C1-C4 alkyl);
- R19 is —C(O)R14, —C(O)NR9R14, —S(O)2R15, or —S(O)2NR9R14,
- Y is O or S;
- and,
- Z is O, NR17, NCN, C(—CN)2, CR9CN, CR9NO2, CR9CO2R9, CR9C(O)NR9R10, C(—CN)CO2(C1-C4 alkyl) or C(CN)C(O)NR9R10.