| 主权项 |
1. At least one compound of formula 1: and/or at least one pharmaceutically acceptable salt thereof wherein X is N, Y is selected from —O—, —S—, and —N(R7)— and R1 is selected from aryl and heteroaryl, each of which is optionally substituted with one or more groups selected from halo, —CF3, —CF2H, cycloalkyl, —C(O)R11, —C(O)OR11, —CN, —C(O)NR13R14, —NR13R14, —NR13C(O)R11, —NR13S(O)nR12, —NR13S(O)nNR13R14, —NR13C(O)OR12, —NR13C(O)NR13R14, —NO2, —S(O)nR12, —S(O)nNR13R14, heterocycle, heteroaryl, aryl, alkenyl, alkynyl, lower alkyl, lower alkyl substituted with hydroxy, lower alkyl substituted with lower alkoxy, lower alkyl substituted with —NR13R14, and lower alkyl substituted with heterocycle; or X is N, Y is absent and R1 is a fused bicyclic heteroaryl optionally substituted with one or more groups selected from halo, —CF3, —CF2H, cycloalkyl, —C(O)R11, —C(O)OR11, —CN, —C(O)NR13R14, —NR13R14, —NR13C(O)R11, —NR13S(O)nR12, —NR13S(O)nNR13R14, —NR13C(O)OR12, —NR13C(O)NR13R14, —NO2, —S(O)nR12, —S(O)nNR13R14, heterocycle, heteroaryl, aryl, alkenyl, alkynyl, lower alkyl, lower alkyl substituted with hydroxy, lower alkyl substituted with lower alkoxy, lower alkyl substituted with —NR13R14, and lower alkyl substituted with heterocycle; or X is C(R6), Y is selected from —O—, —S—, and —N(R7)— or Y is absent, and R1 is heteroaryl optionally substituted with one or more groups selected from halo, —CF3, —CF2H, cycloalkyl, —C(O)R11, —C(O)OR11, —CN, —C(O)NR13R14, —NR13R14, —NR13C(O)R11, —NR13S(O)nR12, —NR13S(O)nNR13R14, —NR13C(O)OR12, —NR13C(O)NR13R14, —NO2, —S(O)nR12, —S(O)nNR13R14, heterocycle, heteroaryl, aryl, alkenyl, alkynyl, lower alkyl, lower alkyl substituted with hydroxy, lower alkyl substituted with lower alkoxy, lower alkyl substituted with —NR13R14 and lower alkyl substituted with heterocycle; R2 and R3 are independently selected from hydrogen, and alkyl, or R2 and R3, together with the carbon to which they are attached, form a ring chosen from 3- to 7-membered cycloalkyl and 3- to 7-membered heterocycle; R4 is selected from halo, alkyl, cycloalkyl, heterocycle, aryl and heteroaryl, each of which, except for halo, is optionally substituted with one or more groups selected from
lower alkyl optionally substituted with one or more groups selected from hydroxy, lower alkoxy, cyano, halo, —C(O)OR11, —C(O)NR13R14, —NR13R14, —OC(O)R11, —NR13C(O)R11, —NR13S(O)nR12, —NR13S(O)nNR13R13R14, —NR13C(O)OR12, and —NR13C(O)NR13R14,lower alkoxy optionally substituted with one or more groups selected from halo, hydroxy, and lower alkoxy,cycloalkoxy optionally substituted with one or more groups selected from halo, hydroxy, and lower alkoxy,heterocycloalkoxy optionally substituted with one or more groups selected from halo, hydroxy, and lower alkoxy,heterocycle optionally substituted with one or more groups selected from lower alkyl, halo, hydroxy, and lower alkoxy,heteroaryloxy optionally substituted with one or more groups selected from lower alkyl, halo, hydroxy, and lower alkoxy,aryl optionally substituted with one or more groups selected from lower alkyl, halo, hydroxy, and lower alkoxy,heteroaryl optionally substituted with one or more groups selected from lower alkyl, halo, hydroxy, and lower alkoxy,halo, cyano, —C(O)R11, —C(O)OR11, —NR13R14, —NR13C(O)R11, —NR13S(O)nR12, —NR13S(O)nNR13R14, —NR13C(O)OR12, —NR13C(O)NR13R14, —C(O)NR13R14, —S(O)nR12, and —S(O)nNR13R14; R5 is selected from hydrogen, halo, OH, NH2, CF3, —CF2H, alkyl, alkenyl, and alkynyl; R6 is selected from hydrogen, —OH, —NH2, —NHC(O)R11, halo and alkyl; R7 is selected from hydrogen and lower alkyl; each n is independently 0, 1, or 2; R11, R12, R13, and R14 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocycle, each of which except for hydrogen, is optionally substituted with one or more groups selected from halo, lower alkyl, hydroxy, and lower alkoxy, or R13 and R14, with the nitrogen to which they are attached, combine to form a heterocycle ring, which is optionally substituted with one or more groups selected from halo, lower alkyl, hydroxy, and lower alkoxy and further optionally includes one or two additional heteroatoms in the heterocycle ring wherein the one or two additional heteroatoms are selected from —O—, —S—, and —N(R15)—; and R15 is selected from hydrogen, lower alkyl, —C(O)R11, —C(O)OR11, —C(O)NR13R14, —S(O)nR12, and —S(O)nNR13R14; provided that
R1 is not optionally substituted phenyl or optionally substituted 4-pyridinyl;when X is N, R2 is hydrogen or methyl, R3 and R5 are hydrogen, and Y is absent, then R1 is not quinolin-6-yl, 7-fluoroquinolin-6-yl, 3-quinazolin-6-yl, 2-3-dihydro-benzofuran-5-yl, or 2,3-dihydro-benzo[1,4]dioxin-6-yl; andwhen X is N, R2, R3 and R5 are hydrogen, and Y is —O— or —N(R7)—, and R1 is quinolin-6-yl, 7-fluoroquinolin-6-yl, 3-quinazolin-6-yl, 2-3-dihydro-benzofuran-5-yl, or 2,3-dihydro-benzo[1,4]dioxin-6-yl, then R4 is optionally substituted heteroaryl. |
