| 主权项 |
1. A compound having the formula:wherein:
R3 is each m is independently 0, 1, or 2; n is 0, 1, 2, or 3, each s is independently 0, 1, 2, or 3; each X is independently selected from the group consisting of O, S, S(O), SO2, CH2, CHR5, and C(R5)2; provided that when m is 0, X is selected from the group consisting of CH2, CHR5, and C(R5)2; each R5 is independently selected from the group consisting of 5-membered heteroaryl, halo substituted 5-membered heteroaryl, thioalkyl, thioaryl, SCH3, SCF3, sulfoxide alkyl, sulfoxide aryl, S(O)CH3, S(O)CF3, sulfone alkyl, sulfone aryl, S(O)2CH3, S(O)2CF3, haloalkyl, CF3, N3, and CN, with the proviso that —C(R5)2 can be —C(O), each R′ is is independently H, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C2-6 alkenyl, C2-6 alkenyl, C3-6 cycloalkyl, aryl, heteroaryl, alkylaryl, arylalkyl, or if two R′ reside on the same nitrogen atom, they can come together to form a C3-6 alkyl ring containing none or one heteroatom independently selected from the group consisting of N, O, and S; wherein the R′ groups can be substituted with one or more hydroxyalkyl, aminoalkyl, and alkoxyalkyl substituents, with the proviso that C(R5)2 cannot be C(alkoxy)2, C(OH)2, C(alkoxy)(OH), or C(halo)(OH), and with the further proviso that C(R5)2 can also be C(═O), each R6 is independently selected from the group consisting of —C(O)—, —C(S)— and —C(NRz)—; each R10 and R11 are independently selected from the group consisting of H, alkylcarboxy amino, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkyl, alkylcarbonyl, alkylcarbonylalkyl, alkylamino, alkylguanasyl, alkylaryl, aryl, arylalkenyl, arylalkoxy, arylalkyl, aryloxyalkyl, cycloalkyl, cycloakylamino, (cycloalkyl)alkenyl, (cycloalkyl)alkyl, cycloalkyloxyalkyl, haloalkyl, alkylheterocyclyl, heterocyclyl, heterocyclylalkenyl, heterocyclylalkoxy, heterocyclylalkyl, heterocyclyloxyalkyl, and hydroxyalkyl, wherein the groups can be substituted with one or more hydroxyaryl, aminoalkyl, and alkoxyalkyl substituents; each R12 and R16 are independently selected from the group consisting of hydrogen, R13—C(O)—, R13—C(S)—, and R′; Each R′ is as defined above; each R13 is independently selected from the group consisting of alkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkyl, alkylcarbonylalkyl, aryl, arylalkenyl, arylalkoxy, arylalkyl, aryloxyalkyl, cycloalkyl, (cycloalkyl)alkenyl, (cycloalkyl)alkyl, cycloalkyloxyalkyl, haloalkyl, heterocyclyl, heterocyclylalkenyl, heterocyclylalkoxy, heterocyclylalkyl, heterocyclyloxyalkyl, hydroxyalkyl, and —N(R′)2, wherein each R′ is as defined above; R14 and R14′ are independently selected from the group consisting of halogen CF3, hydroxy, C1-6 alkoxy, aryl, 5-membered heteroaryl, lower C1-6 alkyl or halo substituted aryl, aryl or halo substituted 5-membered heteroaryl, cyano, C2-6 alkynyl alkoxyalkyl, alkoxycarbonylalkyl, alkyl, arylalkoxycarbonyl, carboxy, haloalkyl, heterocyclylalkyl, hydroxyalkyl; and R15 and R15′ are independently selected from the group consisting of hydrogen, C2-6 alkoxy C3-6 alkoxyalkyl alkoxycarbonyl, carbonylalkyl, carbonyl aryl, alkyl, heterocyclylalkyl, and C2-6 hydroxyalkyl, and pharmaceutically acceptable salts and prodrugs thereof, Z is selected from the group consisting of C1-6 alkyl, alkenyl, heterocyclyl, aryl, heteroaryl, halo, —OR′, —NR′R″, —CF3, —CN, —NO2, —C2R′, —SR′, —N3, —C(═O)NR′R″, —NR′C(═O) R″, —C(═O)R′, —C(═O)OR′, —OC(═O)R′, —OC(═O)NR′R″, —NR′C(═O)O R″, —SO2R′, —SO2NR′R″, and —NR′SO2R″, where R′ and R″ are individually hydrogen, C1-6 alkyl, cycloalkyl, heterocyclyl, aryl, or arylalkyl, and j is an integer of from 0 to 3, wherein the compounds can be in the form of the R- or S-configuration, or a mixture thereof, with the proviso that at least one of R14 and R14′ is halogen. |
