| CPC C07D 487/04 (2013.01) [C07D 403/14 (2013.01); C07D 471/04 (2013.01); C07D 471/14 (2013.01); C07F 9/6561 (2013.01)] | 28 Claims |
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1. A compound of Formula (I) or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or tautomer thereof,
 wherein
R1 is hydrogen or a prodrug moiety;
R2 is selected from the group consisting of hydrogen, halo, cyano, nitro, C1-3 alkyl, halo (C1-3) alkyl, halo (C1-3) alkoxy, —S(O) R7, —SO2R7, —C(O) NR7R8, —NR7C(O) R8, —CO2R7, wherein C1-3 alkyl, halo (C1-3) alkyl, and halo (C1-3) alkoxy is optionally substituted by hydroxyl or —NR7R8;
R3 is a 5- or 6-membered heteroaryl optionally substituted by C1-3 alkyl, —C(O) R8 or a prodrug moiety;
each R4, R5 and R6 is independently-L-Y;
each L is independently selected from a bond, —(CRaRb)n—, —O—, —(CRaRb)nO—, —O (CRaRb)n—, or —(CRaRb)nO(CRaRb)m—;
wherein each n or m is independently 1, 2 or 3;
each Ra and Rb is independently selected from hydrogen, halo and methyl;
each Y is independently selected from the group consisting of hydrogen, halo, hydroxyl, cyano, C1-4 alkyl, C1-4 alkoxy, C3-7cycloalkyl, C2-4 alkenyl, C1-4 thioalkyl, C1-6 hydroxyalkyl, C1-4 cyanoalkyl, halo (C1-4) alkyl, halo (C2-4) alkenyl, —NR9R10, —C(O) NR9R10, —CO2R10, —C(O) R10, —SO2R10, —OSO2R10, —S(O) R10, —SO2NR9R10, —N(R10) SO2R10, —CF2CH2OR10, phenyl, 5- or 6-membered heteroaryl, and 4- to 10-membered heterocycloalkyl ring containing one, two or three heteroatoms independently selected from N, O and S, wherein the C3-7cycloalkyl, phenyl, heteroaryl and heterocycloalkyl groups are optionally substituted with one, two or three substituents independently selected from halo, hydroxyl, —C(O) R10, oxo, C1-4 alkyl, halo (C1-4) alkyl and C1-4 hydroxyalkyl; or
R4 and R5 taken together with the carbon atoms to which they are attached form a 5- to 8-membered monocyclic or bicyclic ring which optionally contains one or two heteroatoms independently selected from N, O and S, wherein the ring is optionally substituted with one, two or three substituents independently selected from halo, C1-4 alkyl, oxo, —C(O) R10 and —SO2R10;
R7 and R8 are independently selected from hydrogen and C1-4 alkyl;
R9 is independently selected from the group consisting of hydrogen, C1-4 alkyl, —C(O) C1-4 alkyl and halo (C1-4) alkyl; and
R10 is independently selected from hydrogen and C1-6 alkyl; or
wherein R9 and R10 taken together with the nitrogen atom to which they are attached form a 5- to 8-membered heterocycloalkyl ring containing one or two heteroatoms independently selected from N, O and S, wherein the heterocycloalkyl is optionally substituted with oxo;
wherein each prodrug moiety is independently selected from the group consisting of —CH(Rc)O—P(O)(ORd) (ORe), —CH(Rc)O—C(O)—C1-6 alkylene-O—P(O)(ORd) (ORe), —CH(Rc)O—C(O)—C1-6 alkylene-P(O)(ORd) (ORe), —CH(Rc)O—C(O)—C1-6 alkylene-CO2H, —CH(Rc)O—C(O) Rd, —CH(Rc)O—C(O)O—C1-6 alkylene-CO2H, —CH(Rc)O—C(O)—C1-6 alkylene-NRdRe, —CH(Rc)O—C(O)O—C1-6 alkylene-NRdRe, —C(O) Rd, —CH(Rc)O—C(O)—C1-6 alkylene-heterocycloalkyl, —CH(Rc)O—C(O)—C1-6 alkylene-heterocycloalkyl and —CRdRe—O—(C(O)—NRd-heteroarylene-CH2O—C(O)—CH2—NRdRe, wherein each heterocycloalkyl is 4- to 6-membered and contains one or two heteroatoms independently selected from N, O and S, and each heteroarylene is 5- or 6-membered and contains one or two heteroatoms independently selected from N, O and S;
wherein Rc is independently selected from hydrogen and methyl; and
Rd and Re are each independently hydrogen or C1-6 alkyl.
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