| 主权项 |
1. A compound of Formula (I): wherein: A is CH or N; E is O or is absent; R is (a) a bicyclic heteroaryl comprising one or more heteroatom ring members independently selected from N, S or O, 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 ring members 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 heteroaryl, wherein said phenyl or heteroaryl is unsubstituted or is substituted with one or more substituent selected from the group consisting of deuterium, amino, alkylamino, dialkylamino, alkyl, halo, cyano, haloalkyl, hydroxy, hydroxyalkyl, and alkoxy; R1 is (1) Rm or -alkylenyl-Rm, where Rm is cycloalkyl, heterocycloalkyl, phenyl, or monocyclic heteroaryl;
wherein each of said cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl is unsubstituted or is substituted with one or more substituents Rx;
wherein each Rx substituent is independently selected from the group consisting of: deuterium, halo, hydroxy, hydroxyalkyl, cyano, —NRaRb, -alkylenyl-NRaRb, oxo, alkyl, cyanoalkyl, haloalkyl, alkoxy, —S-alkyl, haloalkoxy, alkoxyalkyl-, alkenyl, alkynyl, —C(O)alkyl, —C(O)alkyl-O-alkyl, —CO2alkyl, —CO2H, —CONH2, C(O)NH(alkyl), —C(O)NH(haloalkyl), —C(O)N(alkyl)2, —C(O)NH(cycloalkyl), arylalkyl-, arylalkoxy-, aryloxy-, cycloalkyl, cycloalkyloxy, (cycloalkyl)alkyl, heterocycloalkyl, aryl, (heterocycloalkyl)alkyl-, (heterocycloalkyl)alkoxy-, —C(O)cycloalkyl, —C(O)heterocycloalkyl, heteroaryl, (heteroaryl)alkyl-, —S(O)— alkyl, —SO2-alkyl, —SO2-aryl, —SO2-fluoroalkyl, —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 on a phenyl or heteroaryl Rm groups taken together form methylenedioxy,
wherein each of said cycloalkyl, heterocycloalkyl, aryl, and heteroaryl within Rx is unsubstituted or is substituted with one or more substituents independently selected from the group consisting of deuterium, alkyl, halo, hydroxy, cyano, alkoxy, amino, —C(O)alkyl, and —CO2alkyl;wherein Ra and Rb are each independently H, alkyl, alkoxy, alkoxyalkyl, cyanoalkyl, or haloalkyl; andRc is H, alkyl or arylalkyl-;(2) alkyl unsubstituted or substituted with one or more substituents selected from the group consisting of deuterium, halo, hydroxy, cyano, alkoxy, haloalkoxy, —NRsRt, —C(O)alkyl, CO2alkyl, —CO2H, —CONRsRt, —SOalkyl, —SO2alkyl, and —SO2NRsRt;
where Rs and Rt are each independently H, alkyl, alkoxyalkyl, haloalkyl, —C(O)alkyl, or —CO2alkyl; or(3) —N(Rn)Ro,
wherein Rn is H, Rm, -alkylenyl-Rm, hydroxyalkyl, cyanoalkyl, alkoxyalkyl, haloalkyl, —CONRhRi, or —C(O)Rj;
where Rm is as defined in (1) above;Rh and Ri are each independently H or alkyl, or Rh and Ri taken together with the nitrogen to which they are attached form a monocyclic heterocycloalkyl; andRj is an alkyl unsubstituted or substituted with one or more substituents selected from the group consisting of: deuterium, halo, amino, hydroxy, alkoxy, cycloalkyl, heteroaryl, phenyl, and heterocycloalkyl; or a cycloalkyl, heterocycloalkyl, phenyl, or heteroaryl, each unsubstituted or substituted with one or more substituents selected from the group consisting of: deuterium, alkyl, halo, amino, hydroxy, and alkoxy; andRo is H or Rj; R2 and R3 are each independently selected from the group consisting of H and deuterium; wherein the compound of Formula I is not 1H-pyrrolo[3,2-c]pyridine-2-carboxylic acid (5-benzenesulfonyl-pyridin-2-ylmethyl)-amide; or a pharmaceutically acceptable salt thereof. |
