| 主权项 |
1. A compound, or a pharmaceutically acceptable salt, hydrate or solvate thereof, of Formula (I): wherein: R1 is chosen from mono- and bicyclic aryl and heteroaryl, wherein R1 may be optionally substituted with one or more R3 substituents; R2 is chosen from heterocycloalkyl, aryl, and heteroaryl, each of which is substituted with one R4 substituent, and any of which may be further optionally substituted with one or more R8 substituents, or alternatively R2 is NR12R13; each R3 is independently chosen from hydrogen, hydroxyl, cyano, C1-6alkyl, hydroxyC1-4alkyl, C1-6alkoxyalkyl, arylC1-6alkyl, arylC1-6alkoxy, heteroarylC1-6alkyl, heteroarylC1-6alkoxy, aryloxyC1-6alkyl, heteroaryloxyC1-6alkyl, aryloxyC1-6alkyl, heteroaryloxyC1-6alkyl, cyclopropylC1-4alkyl, cyclopropylC1-4alkoxy, cyclopropoxyC1-4alkyl, C1-4alkylamino, C1-4alkylarylamino, C1-4alkylheteroarylamino, di(C1-4alkyl)amino, —C(O)NR6R6′, C1-4alkanoyl, —C(O)aryl, —C(O)heteroaryl, —C(O)NHaryl, —C(O)NHheteroaryl, trifluoromethyl, and halo, wherein aryl and heteroaryl may be optionally substituted with R9; R4 is chosen from NR5R6, —(CH2)nCR7═CR9C(O)CH3, —(CH2)nCR7═CR9C(O)NR7R7′, and —(CH2)nC7═CR9CN; R5 is chosen from cyano, —C(O)CF3, —C(O)CH═CH2, —C(O)CR7═CH2, —C(O)CH═CHR7, —C(O)CR7═CHR7, —C(O)CH═CR7R7′, —C(O)CH═CHCH2R8, —C(O)CH═CHC(O)CH2R8, —COC(CN)═CHR6, —C(O)(C(O)NH2)═CHR6, C(O)alkynylR7, —S(O)2CH═CH2, —(CH2)mCR7═CR9C(O)CH3, —(CH2)mCR7═CR9C(O)NR7R7′, and —(CH2)mCR7═CR9CN; R6 and R6′ are each independently chosen from hydrogen, C1-4alkyl, C3-7cycloalkylalkyl, and phenylC1-4alkyl; R7 and R7′ are each independently chosen from hydrogen, cyano, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkoxyalkyl, C3-7cycloalkyl, C3-7heterocycloalkyl, C3-7heterocycloalkylalkyl, (NR6R6′)C1-4alkyl, aryl, and heteroaryl, wherein aryl and heteroaryl may be optionally substituted with one or more R9; R8 is chosen from hydrogen, halo, cyano, C1-4alkyl, arylC1-4alkyl, heteroarylC1-4alkyl, C3-7cycloalkyl, hydroxyC1-6alkyl, heterocycloalkylC1-4alkyl, C3-7heterocycloalkyl, hydroxyl, C1-4alkoxy, C3-7cycloalkoxy, C3-7cycloalkoxyalkyl, heteroaryloxy, aryloxy, (NR6R6′)alkyl, arylalkoxy, C1-4alkoxyC1-4alkyl, amino, C1-4alkylamino, di(C1-4alkyl)amino, trifluoromethyl, aryl, and heteroaryl, wherein alkyl, heterocycloalkyl, aryl and heteroaryl may be optionally substituted with one or more R9; R9 is chosen from hydrogen, halo, hydroxyl, C1-4 alkyl, cyano, trifluoromethyl, alkanoyl, amino, amido, and aryl; R10 is chosen from hydrogen, C1-4alkyl, C1-4alkoxy, halo, trifluoromethyl, and cyano; R11 is chosen from hydrogen, C1-4alkyl, C3-7cycloalkylalkyl, heterocycloalkylalkyl, arylC1-4alkyl, and heteroarylC1-4alkyl, wherein aryl and heteroaryl may be optionally substituted with one or more R9; R12 is a nitrogen-containing C3-7heterocycloalkyl, wherein said nitrogen is further substituted by R5; R13 is chosen from hydrogen, C1-4alkyl, and C3-7cycloalkylalkyl; X is N or CR11; m is an integer chosen from 1, 2 and 3; and n is an integer chosen from 0, 1, 2, and 3. |
