主权项 |
1. A compound having the structure:or any pharmaceutically-acceptable salt thereof, wherein:
X1 is C or N;
Z is —C═C—, —C—C—, —O—C—C—, —C—O—C—, —C—C—O—, —C═N—, —N═C—, —C—N—, —N—C—, —S(═O)2—C—C—, —C—S(═O)2—C—, —C—C—S(═O)2—, —S(═O)2—N—C—, —N—S(═O)2—C—, —C—S(═O)2—N—, —C—N—S(═O)2—, —C═C—C(═O)— and —C(═O)—C═C—; any of which are substituted by 0, 1, 2, 3 or 4 substituents selected from halo, nitro, cyano, C1-4alk, OC1-4alk, OC1-4haloalk, NHC1-4alk, N(C1-4alk)C1-4alk and C1-4haloalk; and additionally substituted by 0 or 1 saturated or partially saturated 3-, 4-, 5- or 6-membered spiro rings containing 0, 1 or 2 heteroatoms selected from N, O and S, the spiro ring being substituted by 0, 1, 2 or 3 substituents independently selected from halo, C1-6alk and C1-4haloalk; n is 0, 1, 2 or 3; R1 is a saturated, partially-saturated or unsaturated 5-, 6- or 7-membered monocyclic or 8-, 9-, 10- or 11-membered bicyclic ring containing 0, 1, 2, 3 or 4 atoms selected from N, O and S, but containing no more than one O or S atom, substituted by 0, 1, 2 or 3 substituents independently selected from halo, C1-6alk, C1-4haloalk, cyano, nitro, —C(═O)Ra, —C(═O)ORa, —C(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Ra, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O)2Ra, —OC2-6alkNRaRa, —OC2-6alkORa, —SRa, —S(═O)Ra, —S(═O)2Ra, —S(═O)2NRaRa, —S(═O)2N(Ra)C(═O)Ra, —S(═O)2N(Ra)C(═O)ORa, —S(═O)2N(Ra)C(═O)NRaRa, —NRaRa, —N(Ra)C(═O)Ra, —N(Ra)C(═O)ORa, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S(═O)2Ra, —N(Ra)S(═O)2NRaRa, —NRaC2-6alkNRaRa and —NRaC2-6alkORa, wherein the available carbon atoms of the ring are additionally substituted by 0, 1 or 2 oxo or thioxo groups; R2 is selected from H, halo, C1-6alk, C1-4haloalk, cyano, nitro, —C(═O)Ra, —C(═O)ORa, —C(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Ra, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O2)Ra, —OC2-6alkNRaRa, —OC2-6alkORa, —SRa—S(═O)Ra, —S(═O)2Ra, —S(═O)2NRaRa, —S(═O)2N(Ra)C(═O)Ra, —S(═O)2N(Ra)C(═O)ORa, —S(═O)2N(Ra)C(═O)NRaRa, —NRaRa, —N(Ra)C(═O)Ra, —N(Ra)C(═O)ORa, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S(═O)2Ra, —N(Ra)S(═O)2NRaRa, —NRaC2-6alkNRaRa and —NRaC2-6alkORa; R3 is selected from saturated, partially-saturated or unsaturated 5-, 6- or 7-membered monocyclic or 8-, 9-, 10- or 11-membered bicyclic ring containing 0, 1, 2, 3 or 4 atoms selected from N, O and S, but containing no more than one O or S, wherein the available carbon atoms of the ring are substituted by 0, 1 or 2 oxo or thioxo groups, wherein the ring is additionally substituted by 0, 1, 2 or 3 substituents independently selected from halo, C1-6alk, C1-4haloalk, cyano, nitro, —C(═O)Ra, —C(═O)ORa, —C(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Ra, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O)2Ra, —OC2-6alkNRaRa, —OC2-6alkORa, —SRa, —S(═O)Ra, —S(═O)2Ra, —S(═O)2NRaRa, —S(═O)2N(Ra)C(═O)Ra, —S(═O)2N(Ra)C(═O)ORa, —S(═O)2N(Ra)C(═O)NRaRa, —NRaRa, —N(Ra)C(═O)Ra, —N(Ra)C(═O)ORa, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S(═O)2Ra, —N(Ra)S(═O)2NRaRa, —NRaC2-6alkNRaRa and —NRaC2-6alkORa; or R3 is selected from halo, C1-6alk, C1-4haloalk, cyano, nitro, —C(═O)Ra, —C(═O)ORa, —C(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Ra, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O)2Ra, —OC2-6alkNRaRa, —OC2-6alkORa, —SRa, —S(═O)Ra, —S(═O)2Ra, —S(═O)2NRaRa, —S(═O)2N(Ra)C(═O)Ra, —S(═O)2N(Ra)C(═O)ORa, —S(═O)2N(Ra)C(═O)NRaRa, —NRaRa, —N(Ra)C(═O)Ra, —N(Ra)C(═O)ORa, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S(═O)2Ra, —N(Ra)S(═O)2NRaRa, —NRaC2-6alkNRaRa and —NRaC2-6alkORa; R4 is, independently, in each instance, H, halo, nitro, cyano, C1-4alk, OC1-4alk, OC1-4haloalk, NHC1-4alk, N(C1-4alk)C1-4alk, C1-4haloalk, or an unsaturated 5-, 6- or 7-membered monocyclic ring containing 0, 1, 2, 3 or 4 atoms selected from N, O and S, but containing no more than one O or S, substituted by 0, 1, 2 or 3 substituents selected from halo, C1-4alk, C1-3haloalk, —OC1-4alk, —NH2, —NHC1-4alk, —N(C1-4alk)C1-4alk; R5 is, independently, in each instance, H, halo, nitro, cyano, C1-4alk, OC1-4alk, OC1-4haloalk, NHC1-4alk, N(C1-4alk)C1-4alk or C1-4haloalk; R6 is selected from halo, cyano, OH, OC1-4alk, C1-4alk, C1-3haloalk, OC1-4alk, NH2, NHC1-4alk, N(C1-4alk)C1-4alk; Ra is independently, at each instance, H or Rb; and Rb is independently, at each instance, phenyl, benzyl or C1-6alk, the phenyl, benzyl and C1-6alk being substituted by 0, 1, 2 or 3 substituents selected from halo, C1-4alk, C1-3haloalk, —OC1-4alk, —NH2, —NHC1-4alk, —N(C1-4alk)C1-4alk. |