| 主权项 |
1. A compound of Formula 1 or a pharmaceutically acceptable salt therefore, wherein: G1 is selected from N and CR7; G2 is selected from C═O and CH2; Ar is C6-14 aryl; m is 0, 1, 2, 3, or 4; n is 0, 1, 2 or 3; each R1 is independently selected from cyano, halo, hydroxy, nitro, oxo, optionally substituted C1-6 alkyl, optionally substituted C1-4 alkoxy, optionally substituted C2-4 alkenyl, optionally substituted C2-4 alkynyl, optionally substituted C3-8 cycloalkyl, optionally substituted C3-6 heterocyclyl, optionally substituted C6-14 aryl, optionally substituted C6-14 aryloxy, optionally substituted C1-10 heteroaryl, optionally substituted C1-10 heteroaryloxy, —C(O)OR4, —OC(O)R4, —N(R4)R5, —NHC(O)N(R8)R9, —S(O)2R6, —S(O)2N(R4)R5, —C(O)N(R8)R9, —NHC(O)OR10, —NHS(O)2NHR8, —NHS(O)2R6, —NHC(O) NHN(R8)R9, —NHC(S)N(R8)R9, —NHC(═NR11)N(R8)R9, —NHC(SR12)N(R8)R9, and —NHC(═NR11)OR13; R2 is selected from hydrogen, cyano, halo, hydroxy, nitro, optionally substituted C1-6 alkyl, optionally substituted C1-4 alkoxy, optionally substituted C2-4 alkenyl, optionally substituted C2-4 alkynyl, optionally substituted C3-6 heterocyclyl, optionally substituted C6-14 aryl, optionally substituted C6-14 aryloxy, optionally substituted C1-10 heteroaryl, —C(O)OR4, —OC(O)R4, —N(R4)R5, and —S(O)2R6; R3 is selected from hydrogen, optionally substituted C1-6 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted C3-6 heterocyclyl, optionally substituted C6-14 aryl, optionally substituted C1-10 heteroaryl, —(CH2)N(R4)R5, —(CH2)C(O)N(R4)R5, and —S(O)2R6; each R4 and R5 is independently selected from hydrogen, optionally substituted C1-6 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted phenyl, optionally substituted C3-6 heterocyclyl, and optionally substituted C1-10 heteroaryl; each R6 is independently selected from optionally substituted C1-6 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted phenyl, optionally substituted C3-6 heterocyclyl, and optionally substituted C1-10 heteroaryl; R7 is selected from hydrogen, cyano, halo, hydroxy, nitro, optionally substituted C1-4 alkyl, optionally substituted C1-4 alkoxy, —C(O)OR4, —C(O)N(R4)R5, —N(R4)R5, —NHC(O)R4, —NHC(O)N(R4)R5, —OC(O)N(R4)R5, —NHC(O)OR6, —S(O)2R6, —NHS(O)2R6, and —S(O)2N(R4)R5; each R8 and R9 is independently selected from hydrogen, optionally substituted C1-6 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted C6-14 aryl, optionally substituted C3-6 heterocyclyl, and optionally substituted C1-10 heteroaryl; each R10 is independently selected from optionally substituted C1-6 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted C6-14 aryl, optionally substituted C3-6 heterocyclyl, and optionally substituted C1-10 heteroaryl; each R11 is independently selected from hydrogen, cyano, nitro, optionally substituted C1-6 alkyl, optionally substituted C1-4 alkoxy, optionally substituted C3-8 cycloalkyl, optionally substituted C3-6 heterocyclyl, optionally substituted C6-14 aryl, and optionally substituted C1-10 heteroaryl; each R12 is independently selected from optionally substituted C1-6 alkyl and optionally substituted phenyl; each R13 is independently selected from optionally substituted C1-6 alkyl, optionally substituted C3-8 cycloalkyl, and optionally substituted C6-14 aryl; each R14 and R15 is independently selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, optionally substituted phenyl, C3-6 heterocyclyl, and C1-10 heteroaryl; and each R16 is independently selected from C1-6 alkyl, C3-8 cycloalkyl, optionally substituted phenyl, C3-6 heterocyclyl, and C1-10 heteroaryl; wherein: each optionally substituted C1-6 alkyl is independently substituted with from 0 to 7 substituents independently selected from cyano, halo, hydroxy, oxo, optionally substituted C1-4 alkyl, C1-4 alkoxy, C2-4 alkenyl, optionally substituted C3-8 cycloalkyl, optionally substituted C3-6 heterocyclyl, optionally substituted C1-10 heteroaryl, optionally substituted phenyl, optionally substituted C6-14 aryloxy, —SR14, —C(O)OR14, —N(R14)R15, —C(O)N(R14)R15, and —S(O)2R16; each optionally substituted C1-4 alkoxy is independently substituted with from 0 to 6 substituents independently selected from cyano, halo, hydroxy, oxo, C2-4 alkenyl, C1-4 alkoxy, optionally substituted C3-8 cycloalkyl, optionally substituted C1-10 heteroaryl, optionally substituted phenyl, —C(O)N(R14)R15, and —C(O)OR14; each optionally substituted C2-4 alkenyl is independently substituted with from 0 to 3 substituents independently selected from cyano, halo, hydroxy, oxo, C1-4 alkoxy, C3-8 cycloalkyl, optionally substituted C1-10 heteroaryl, optionally substituted phenyl, —C(O)N(R14)R15, and —C(O)OR14; each optionally substituted C2-4 alkynyl is independently substituted with from 0 to 3 substituents independently selected from cyano, halo, hydroxy, oxo, C1-4 alkoxy, C3-8 cycloalkyl, optionally substituted C1-10 heteroaryl, optionally substituted phenyl, —C(O)N(R14)R15, and —C(O)OR14; each optionally substituted C3-8 cycloalkyl is independently substituted with from 0 to 6 substituents independently selected from cyano, halo, hydroxy, nitro, oxo, optionally substituted C1-4 alkyl, C1-4 alkoxy, C2-4 alkenyl, C3-8 cycloalkyl, C3-8 cycloalkoxy, optionally substituted C1-10 heteroaryl, optionally substituted phenyl, —C(O)N(R14)R15, —C(O)N(R14)R15, —N(R14)R15, —NHC(O)R14, —NHC(O)OR14, and —C(O)OR14; each optionally substituted C1-10 heteroaryl is independently substituted with from 0 to 5 substituents independently selected from cyano, halo, hydroxy, oxo, nitro, optionally substituted C1-4 alkyl, C1-4 alkoxy, C3-8 cycloalkyl, optionally substituted C3-6 heterocyclyl, C1-10 heteroaryl, optionally substituted phenyl, —C(O)N(R14)R15, —N(R14)R15, —C(O)N(R14)R15, —OC(O)NR14R15, —NHC(O)OR16, —NHS(O)2R16, —S(O)2N(R14)R15, —NHC(O)N(R14)R15, —C(O)OR14, and —S(O)2R16; each optionally substituted C1-10 heteroaryloxy is independently substituted with from 0 to 5 substituents independently selected from cyano, halo, hydroxy, nitro, oxo, optionally substituted C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, optionally substituted phenyl, and —S(O)2R16; each optionally substituted C3-6 heterocyclyl is independently substituted with from 0 to 4 substituents independently selected from cyano, halo, hydroxy, nitro, oxo, optionally substituted C1-4 alkyl, optionally substituted C1-4 alkoxy, C2-4 alkenyl, optionally substituted C3-8 cycloalkyl, C3-8 cycloalkoxy, C3-6 heterocyclyl, C1-10 heteroaryl, optionally substituted phenyl, —C(O)N(R14)R15, —C(O)N(R14)R15, —N(R14)R15, and —C(O)OR14; each optionally substituted C1-4 alkyl is independently substituted with from 0 to 5 substituents independently selected from cyano, halo, hydroxy, nitro, oxo, optionally substituted C1-4 alkoxy, C2-4 alkenyl, C3-8 cycloalkyl, C3-8 cycloalkoxy, C3-6 heterocyclyl, C1-10 heteroaryl, phenyl, —SR14, —C(O)N(R14)R15, —N(R14)R15, —C(O)OR14, and —S(O)2R16; each optionally substituted C6-14 aryl is independently substituted with from 0 to 5 substituents independently selected from cyano, halo, hydroxy, nitro, oxo, optionally substituted C1-4 alkyl, C1-4 alkoxy, C2-4 alkenyl, C1-10 heteroaryl, trifluoromethyl, trifluoromethoxy, —N(R14)R15, —C(O)N(R14)R15, —OC(O)N(R14)R15, —NHC(O)OR16, —NHS(O)2R16, —S(O)2N(R14)R15, —NHC(O)N(R14)R15, —C(O)OR14, and —S(O)2R16; each optionally substituted C6-14 aryloxy is independently substituted with from 0 to 5 substituents independently selected from cyano, halo, hydroxy, nitro, oxo, optionally substituted C1-4 alkyl, C1-4 alkoxy, C2-4 alkenyl, trifluoromethyl, trifluoromethoxy, —N(R14)R15, —C(O)N(R14)R15, —OC(O)N(R14)R15, —NHC(O)OR16, —NHS(O)2R16, —S(O)2N(R14)R15, —NHC(O)N(R14)R15, —C(O)OR14, and —S(O)2R16; each optionally substituted phenyl is independently substituted with from 0 to 5 substituents independently selected from cyano, halo, hydroxy, nitro, optionally substituted C1-4 alkyl, C1-4 alkoxy, C2-4 alkenyl, C1-10 heteroaryl, trifluoromethyl, trifluoromethoxy, —N(R14)R15, —C(O)N(R14)R15, —OC(O)N(R14)R15, —NHC(O)OR16, —NHS(O)2R16, —S(O)2N(R14)R15, —NHC(O)N(R14)R15, —C(O)OR14, and —S(O)2R16; each of the aforementioned heteroaryl and heteroaryloxy moieties has independently one to four ring heteroatoms independently selected from N, O, and S, and each of the aforementioned heterocyclyl moieties is independently saturated or partially unsaturated and has one or two ring heteroatoms independently selected from N, O, and S; and provided the compound of Formula 1 is not: 1-methyl-3-(4-(6-oxo-5-(tetrahydro-2H-pyran-4-yl)-5,6,6a,7,9,10-hexahydro-[1,4]oxazino[3,4-h]pteridin-2-yl)phenyl)urea. |
