| 主权项 |
1. A compound of Formula (I): wherein: E is O or is absent; R is (a) an 8-, 9-, or 10-membered bicyclic heteroaryl comprising one heteroatom selected from N, S, and O, and one, two, or three additional N atoms, wherein said bicyclic heteroaryl is unsubstituted or is substituted with one or more substituents selected from the group consisting of deuterium, amino, alkylamino, dialkylamino, alkyl, halo, cyano, haloalkyl, hydroxy, hydroxyalkyl, and alkoxy, and wherein one or more N atoms of said bicyclic heteroaryl is optionally an N-oxide; or (b) a five- or six-membered nitrogen-linked heterocycloalkyl ring fused to a phenyl or monocyclic six-membered heteroaryl, wherein said phenyl or heteroaryl is unsubstituted or is substituted with one or more substituents selected from the group consisting of deuterium, amino, alkylamino, dialkylamino, alkyl, halo, cyano, haloalkyl, hydroxy, hydroxyalkyl, and alkoxy; R1 is (I) a saturated, monocyclic heterocycloalkyl, which is unsubstituted or substituted with one or more substituents RX;
wherein each RX substituent is independently selected from the group consisting of: deuterium, halo, hydroxy, cyano, —NRaRb, -alkylenyl-NRaRb, oxo, alkyl, hydroxyalkyl, cyanoalkyl, haloalkyl, alkoxy, haloalkoxy, alkoxyalkyl-, —S-alkyl, alkenyl, alkynyl, aryl, arylalkyl-, aryloxy-, arylalkoxy-, cycloalkyl, cycloalkoxy, (cycloalkyl)alkyl-, heterocycloalkyl, (heterocycloalkyl)alkyl-, (heterocycloalkyl)alkoxy-, —C(O)alkyl, —CO2alkyl, —CO2H, —C(O)cycloalkyl, —C(O)aryl, —C(O)heterocycloalkyl, —S(O)-alkyl, —SO2-alkyl, —SO2-aryl, —SO2-(haloalkyl), —CONH2, C(O)NH(alkyl), —C(O)NH(haloalkyl), —C(O)N(alkyl)2, —C(O)NH(cycloalkyl), heteroaryl, (heteroaryl)alkyl-, —N(Rc)—C(O)-alkyl, —N(Rc)—C(O)-aryl, —N(Rc)—CO2-alkyl, —SO2NH2, —SO2NH(alkyl), —SO2N(alkyl)2, —SO2NH(cycloalkyl), and —N(H)(SO2alkyl), or two adjacent RX substituents taken together form a phenyl ring,
wherein each of said cycloalkyl, heterocycloalkyl, aryl, heteroaryl, and phenyl substituents within RX is independently unsubstituted or substituted with one or more substituents selected from the group consisting of alkyl, halo, hydroxy, cyano, alkoxy, amino, —NHCO2alkyl, —C(O)alkyl, and —CO2alkyl;wherein Ra and Rb are each independently H, alkyl, alkoxy, alkoxyalkyl, cyanoalkyl, or haloalkyl; andRc is H or alkyl; or (2) a saturated, bicyclic or tricyclic, nitrogen-linked heterocycloalkyl, wherein said heterocycloalkyl comprises a fused, bridged, or spiro bicyclic system, and said heterocycloalkyl is unsubstituted or substituted with one or more substituents independently selected from the group consisting of: alkyl, halo, haloalkyl, hydroxy, hydroxyalkyl, alkoxy, cyano, cyanoalkyl, oxo, —NRdRe, -alkylenyl-NRdRe, —C(O)alkyl, —CO2alkyl, and —SO2alkyl;
wherein Rd is H or alkyl; andRc is H, alkyl, haloalkyl, —C(O)alkyl, —CO2alkyl, or —SO2alkyl; and R2 and R3 are each independently H or deuterium; or a pharmaceutically acceptable salt thereof, with the proviso that the compound of Formula I is not one of the following compounds: |
