主权项 |
1. A compound of Formula I: wherein: 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 five- or 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; and R1 is H, —(C1-4alkylene)0-1C(O)Ra, —(C1-4alkylene)0-1CO2Ra, —(C1-4alkylene)0-1S(O)Ra, —(C1-4alkylene)0-1SO2Ra, —C(O)NH(Ra), —C(O)N(Ra)2, or —C(O)C(O)NH(Ra);
wherein each Ra is independently(1) alkyl, unsubstituted or substituted with one or more Rm substituents,
wherein each Rm is independently selected from the group consisting of hydroxy, —NRbRc, alkoxy, cyano, halo, —C(O)alkyl, —CO2alkyl, —CONRbRc, —S(O)alkyl, —SO2alkyl, —SO2NRbRc, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, phenoxy, and —O-alkyl-OH;
wherein Rb is H or alkyl;Rc is H, alkyl, alkoxyalkyl, haloalkyl, —C(O)alkyl, —CO2alkyl, —SO2alkyl, —C(O)NH2, or C(O)H; andeach aryl, heteroaryl, cycloalkyl, and heterocycloalkyl group within Rm is unsubstituted or substituted with one or more substituents independently selected from the group consisting of alkyl, haloalkyl, hydroxy, —NRbRc, alkoxy, haloalkoxy, cyano, halo, oxo, —C(O)alkyl, —CO2alkyl, —C(O)— heterocycloalkyl, —CONRbRc, —S(O)alkyl, —SO2alkyl, —SO2-haloalkyl, —SO2NRbRc, aryl, heteroaryl, cycloalkyl, and heterocycloalkyl; wherein each alkyl or alkoxy is unsubstituted or substituted with —NRbRc, heterocycloalkyl, heteroaryl, or —C(O)alkyl; and each aryl, heteroaryl, cycloalkyl, and heterocycloalkyl is unsubstituted or substituted with alkyl, halo, or —C(O)alkyl;(2) phenyl, cycloalkyl, heteroaryl, or heterocycloalkyl, each unsubstituted or substituted with one or more substituents selected from the group consisting of alkyl, haloalkyl, hydroxy, —NRbRc, alkoxy, haloalkoxy, cyano, halo, oxo, —C(O)alkyl, —CO2alkyl, —C(O)-heterocycloalkyl, —CONRbRc, —S(O)alkyl, —SO2alkyl, —SO2-haloalkyl, —SO2NRbRc, aryl, heteroaryl, cycloalkyl, and heterocycloalkyl;
wherein each alkyl or alkoxy is unsubstituted or substituted with —NRbRc, heterocycloalkyl, heteroaryl, or —C(O)alkyl; andeach aryl, heteroaryl, cycloalkyl, and heterocycloalkyl is unsubstituted or substituted with alkyl, halo, or —C(O)alkyl; or(3) —NRxRy,
where Rx is H or alkyl; andRy is H, alkyl, alkoxyalkyl, haloalkyl, —C(O)alkyl, —CO2alkyl, or —SO2alkyl; R2 and R3 are each independently H or deuterium; and n is 1 or 2; or a stereoisomer thereof, or a pharmaceutically acceptable salt of such a compound or stereoisomer. |