| 主权项 |
1. A compound having the structure of Formula I:wherein:
X1 is CH or N; X2 is CR1a, NR1b or S; X3 is C or N;
wherein,X1, X2 and X3 are arranged in such a way to form a heteroaromatic ring system, andR1a is hydrogen, halo, haloalkyl, cyano, C1-6 alkyl, C1-6 alkoxy, C3-6 cycloalkoxy, C3-12 cycloalkyl, C2-12 heterocyclyl, C6-12 aryl, C2-12 heteroaryl, or —N(R20)(R22),
wherein the C1-6 alkyl, C3-12 cycloalkyl, C2-12heterocyclyl, C6-12 aryl, or C2-12 heteroaryl moieties may be optionally substituted with one, two, or three substituents independently selected from fluoro, CFH2, CF2H, CF3, C1-6 alkyl, C1-6 alkoxy, C3-6 cycloalkoxy, C3-12 cycloalkyl, and —N(R20)(R22),R1b is hydrogen, haloalkyl, C1-6 alkyl, C3-12 cycloalkyl, C2-12 heterocyclyl, C6-12 aryl, or C2-12 heteroaryl,
wherein the C1-6 alkyl, C3-12 cycloalkyl, C2-12 heterocyclyl, C6-12 aryl, or C2-12 heteroaryl moieties may be optionally substituted with one, two, or three substituents independently selected from fluoro, CFH2, CF2H, CF3, and C1-6 alkyl, C1-6 alkoxy, C3-6 cycloalkoxy, C3-12 cycloalkyl, and —N(R20)(R22); provided that either (a) or (b) applies:
a) when X3 is N then X2 is CR1a, orb) when X2 is S then X1 is CH and X3 is C; Y is O or NH; R2 is hydrogen, C1-6 alkyl, C3-12 cycloalkyl, C2-12 heterocyclyl, C1-6 alkoxy, or —N(R20)(R22);
wherein the C1-6 alkyl, C3-12 cycloalkyl, C2-12 heterocyclyl, or C1-6 alkoxy moieties may be optionally substituted with one, two, or three substituents independently selected from fluoro, CFH2, CF2H, CF3, C1-6 alkyl, and C1-6 alkoxy; each R3 and R4 is independently hydrogen, C1-6 alkyl, C3-8 cycloalkyl, C2-8 heterocyclyl, and C2-6 alkenyl,
wherein the C1-6 alkyl, C3-8 cycloalkyl, C2-8 heterocyclyl, and C2-6 alkenyl moieties may be optionally substituted with one, two, or three substituents independently selected from halogen, C1-6 alkyl, C3-6 cycloalkyl, C6-12 aryl, C2-8 heterocyclyl, C2-12 heteroaryl, —OR20, or —N(R20)(R22); R5 is monocyclic or bicyclic C6-12 aryl, monocyclic or bicyclic C3-12 cycloalkyl, monocyclic or bicyclic C2-8 heterocyclyl, or monocyclic or bicyclic C2-12 heteroaryl having one, two, three, or four heteroatoms individually selected from 0, N, and S;
wherein the monocyclic or bicyclic C6-12 aryl, monocyclic or bicyclic C3-12 cycloalkyl, monocyclic or bicyclic C2-8 heterocyclyl, or monocyclic or bicyclic C2-12 heteroaryl moiety may be optionally substituted with one, two, or three substituents independently selected from the group consisting of C1-6 alkyl, C2-6 alkynyl, C1-6 alkoxy, halo, —NO2, —CFH2, —CF3, —CF2H, —OCF3, C3-6 cycloalkyl, C2-8 heterocyclyl, C6-12 aryl, C2-12 heteroaryl, —S(O)2R20, —S(O)2—N(R20)(R22), —N(R20)(R22), —N(R20)—S(O)2—R20, —N(R20)—C(O)—R22, —C(O)—R20, —C(O)—OR20, —C(O)—N(R20)(R22), —CN, oxo, and —O—R20;
wherein the C1-6 alkyl, C2-6 alkynyl, C1-6 alkoxy, C3-8 cycloalkyl, C2-8 heterocyclyl, C6-12 aryl, or C2-12 heteroaryl moiety may be optionally further substituted with one, two, or three substituents independently selected from the group consisting of halo, —NO2, —CFH2, —CF3, —CF2H, —OCF3, C1-6 alkyl, C3-6 cycloalkyl, C6-12 aryl, C2-8 heterocyclyl, C2-6 heteroaryl, —N(R20)(R22), —C(O)—R20, —C(O)—OR20, —C(O)_N(R20)(R22), —CN, —S(O)2R20, —S(O)2—N(R20)(R22), —S(O)2—R20—N(R20)(R22), oxo, and —O—R20;
wherein the C1-6 alkyl, C3-6 cycloalkyl, C2-8 heterocyclyl, C6-12 aryl, and C2-6 heteroaryl may be further optionally substituted with one, two, or three substituents independently selected from the group consisting of C1-6 alkyl, C3-6 cycloalkyl, C6-12 aryl, C2-6 heteroaryl, C2-8 heterocyclyl, halo, —NO2, —CFH2, —CF2H, —CF3, —OCF3, —N(R20)(R22), —C(O)R20, —C(O)—OR20, —C(O)—N(R20)(R22), —CN, —S(O)2—R20, —S(O)2—N(R20)(R22), —S(O)2—R20—N(R20)(R22), oxo, and —O—R20; and each R20 and R22 is independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-8 heterocyclyl, C6-12 aryl, or C2-12 heteroaryl;
wherein each C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-8 heterocyclyl, C6-12 aryl and C2-12 heteroaryl are optionally substituted with one, two or three substituents independently selected from the group consisting of hydroxyl, halo, C1-6 alkyl, acylamino, oxo, —NO2, —S(O)2R26, —CN, C1-6 alkoxy, C3-6 cycloalkoxy, —CFH2, —CF3, —CF2H, —OCF3, —OCH2CF3, —C(O)—NH2, C6-12 aryl, C3-6 cycloalkyl, C2-8 heterocyclyl, and C2-6 heteroaryl; and
wherein R26 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-8 heterocyclyl, C6-12 aryl, C2-6 heteroaryl, acylamino, NH2, —CFH2, —CF3, —CF2H;or a pharmaceutically acceptable salt, ester, stereoisomer, mixture of stereoisomers or tautomer thereof. |
