IRE-1alpha Inhibitors

摘要

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

主权项

1. A compound or a pharmaceutically acceptable salt thereof, wherein the compound is a compound of structural formula (A): wherein:
R1 is hydrogen, halogen, or a 5- or 6-membered heterocyclic containing one or two heteroatoms independently selected from nitrogen, oxygen, and sulfur;R2 is hydrogen,phenyl, or a 5- or 6-membered heterocyclic containing 1 or 2 heteroatoms independently selected from nitrogen, oxygen, and sulfur, wherein the heterocyclic is optionally benzofused and wherein the heterocyclic is optionally substituted by 1, 2, or 3 substituents independently selected fromC1-C3 linear or branched alkyl,C1-C3 phenylalkyl, C1-C3 alkoxyphenylalkyl, R3 is hydrogen, halogen, —NO2, C1-C3 linear or branched alkoxy, C1-C3 linear or branched hydroxyl alkyl,and
Q is a five- or six-membered heterocycle.