主权项 |
1. A compound having the structure:or any pharmaceutically-acceptable salt thereof, wherein:
X1 is C(R9) or N; Y is N(R11), O or S; n is 0, 1, 2 or 3; R1 is a direct bonded or —O-linked saturated, partially-saturated or 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, wherein the available carbon atoms of the ring are substituted by 0, 1 or 2 oxo or thioxo groups, wherein the ring is substituted by 0 or 1 R2 substituents, and the ring is additionally substituted by 0, 1, 2 or 3 substituents independently selected from halo, nitro, cyano, C1-4alkyl, OC1-4alkyl, OC1-4haloalkyl, NHC1-4alkyl, N(C1-4alkyl)C1-4alkyl and C1-4haloalkyl; R2 is selected from halo, C1-4haloalkyl, cyano, nitro, —C(═O)Ra, —C(═O)ORa, —(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Ra, —OC(═O)NRaRa, —OC(═O)N(Ra)S(═O)2Ra, —OC2-6alkylNRaRa, —OC2-6alkylORa, —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, —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, —NRaC2-6alkylNRaRa and —NRaC2-6alkylORa; or R2 is selected from C1-6alkyl, phenyl, benzyl, heteroaryl, heterocycle, —(C1-3alkyl)heteroaryl, —(C1-3,alkyl)heterocycle, —O(C1-3alkyl)heteroaryl, —O(C1-3alkyl)heterocycle, —NRa(C1-3alkyl)heteroaryl, —NRa(C1-3alkyl)heterocycle, —(C1-3alkyl)phenyl, —O(C1-3alkyl)phenyl and —NRa(C1-3alkyl)phenyl all of which are substituted by 0, 1, 2 or 3 substituents selected from C1-4haloalkyl, OC1-4alkyl, Br, Cl, F, I and C1-4alkyl; R3 is selected from H, halo, C1-4haloalkyl, cyano, nitro, —C(═O)Ra, —C(═O)ORa, —C(═O)NRaRa, —C(═NRa)NRaRa, —ORa, —OC(═O)Ra, —OC(═)NRaRa, —OC(═O)N(Ra)S(═O)2Ra, —OC2-6alkylNRaRa, —OC2-6alkylORa, —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, —NRaC2-6alkylNRaRa, —NRaC2-6alkylORa, C1-6alkyl, phenyl, benzyl, heteroaryl and heterocycle, wherein the C1-6alkyl, phenyl, benzyl, heteroaryl and heterocycle are additionally substituted by 0, 1, 2 or 3 substituents selected from C1-6haloalkyl, OC1-6alkyl, Br, Cl, F, I and C1-6alkyl; R4 is, independently, in each instance, halo, nitro, cyano, C1-4alkyl, OC1-4alkyl, OC1-4haloalkyl, NHC1-4alkyl, N(C1-4alkyl)C1-4alkyl or C1-4haloalkyl; R5 is, independently, in each instance, H, halo, C1-6alkyl, C1-4haloalkyl, or C1-6alkyl substituted by 1, 2 or 3 substituents selected from halo, cyano, OH, OC1-4alkyl, C1-3haloalkyl, OC1-4alkyl, NH2, NHC1-4alkyl, N(C1-4alkyl)C1-4alkyl; or both R5 groups together with the carbon atom to which they are attached form a C3-6cycloalkyl substituted by 0, 1, 2 or 3 substituents selected from halo, cyano, OH, OC1-4alkyl, C1-4alkyl, C1-3haloalkyl, OC1-4alkyl, NH2, NHC1-4alkyl, N(C1-4alkyl)C1-4alkyl; R6 is selected from H, halo, C1-6alkyl, C1-4haloalkyl, cyano, nitro, —C(═O)Ra, —C(═O)ORa, —C(═O)NRaRa, —C(═NRa)NRaRa, —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, R7 is selected from H, halo, C1-6alkyl, C1-4haloalkyl, cyano, nitro, —C(═O)Ra, —C(═O)ORa, —C(═O)NRaRa, —C(═NRa)NRaRa, —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; R8 is selected from H, C1-6haloalkyl, Br, Cl, F, I, ORa, NRaRa, C1-6alkyl, phenyl, benzyl, heteroaryl and heterocycle, wherein the C1-6alkyl, phenyl, benzyl, heteroaryl and heterocycle are additionally substituted by 0, 1, 2 or 3 substituents selected from C1-6haloalkyl, OC1-6alkyl, Br, Cl, F, I and C1-6alkyl; R9 is selected from H, halo, C1-4haloalkyl, 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, —OC2-6alkylNRaRa, —OC2-6alkylORa, —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, —NRaRa, —NRaC2-6alkylORa, C1-6alkyl, phenyl, benzyl, heteroaryl and heterocycle, wherein the C1-6alkyl, phenyl, benzyl, heteroaryl and heterocycle are additionally substituted by 0, 1, 2 or 3 substituents selected from halo, C1-4haloalkyl, 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, —OC2-6alkylNRaRa, —OC2-6alkylORa, —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, —NRaC2-6alkylNRaRa, —NRaC2-6alkylORa; or R9 is a saturated, partially-saturated or 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, wherein the available carbon atoms of the ring are substituted by 0, 1 or 2 oxo or thioxo groups, wherein the ring is substituted by 0, 1, 2, 3 or 4 substituents selected from halo, C1-4haloalkyl, 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, —OC2-6alkylNRaRa, —OC2-6alkylORa, —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, NRaC2-6alkylNRaRa and —NRaC2-6alkylORa; R10 is H, C1-3alkyl, C1-3haloalkyl, cyano, nitro, CO2Ra, C(═O)NRaRa, —C(═NRa)NRaRa, —S(═O)2N(Ra)C(═O)Ra, —S(═O)2N(Ra)C(═O)ORa, —S(═O)2N(Ra)C(═O)NRaRa, S(═O)Ra, S(═O)2Ra or S(═O)2NRaRa; R11 is H or C1-4alkyl; Ra is independently, at each instance, H or Rb; and Rb is independently, at each instance, phenyl, benzyl or C1-6alkyl, the phenyl, benzyl and C1-6alkyl being substituted by 0, 1, 2 or 3 substituents selected from halo, C1-4, C1-3haloalkyl, —OC1-4alkyl, —NH2, —NHC1-4alkyl, —N(C1-4alkyl)C1-4alkyl. |