Abstract: The present disclosure provides compounds having Stimulator of Interferon Genes (STING) agonistic bioactivity that can be used in the treatment of tumors in patients afflicted therewith. The compounds are a compound of formula (I) or formula (II): wherein the substituents are as defined herein. Ring A is a bicyclic fully aromatic or partially reduced heteroaryl ring system comprising 3, 4, or 5 N atoms, substituted with 0, 1, 2, 3,or 4 substituents as defined herein. Compounds for practice of a method of the present disclosure can be delivered via oral delivery for systemic exposure, as well as delivered intratumorally. Antitumor therapy using a compound of formula (I) can further comprise administration of an effective dose of an immune-checkpoint targeting drug.

Abstract: The invention provides compounds having STimulator of INterferon Genes (STING) agonistic bioactivity that can be used in the treatment of tumors inpatients afflicted therewith. The compounds are of formula (IA), formula (I), and formula (II): wherein the various substituents are as defined herein. Ring A is a 5- or 6-membered heteroaryl comprising 1, 2, or 3 N atoms, unsubstituted or substituted with 1, 2, or 3 groups as defined herein. Compounds for practice of a method of the invention can be delivered via oral delivery for systemic exposure, as well as delivered intratumorally. Antitumor therapy using a compound of formula (I) can further comprise administration of an effective dose of an immunecheckpoint targeting drug.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activation of steroid hormone nuclear receptors.

Abstract: Bisaryloxime ethers and bisarylhydroazones are shown to be effective for inhibiting formation of amyloid fibrils of transthyretin.

Abstract: Dibenzofuran-4,6-dicarboxylic acid core structures having an aromatic substituent appended onto the at the C1 position using three different types of linkages are disclosed herein and shown to afford exceptional amyloidogenesis inhibitors that display increased affinity and greatly increased binding selectivity to TTR over all the other plasma proteins, relative to lead compound 1. It is further disclosed herein that these compounds function by imposing kinetic stabilization on the TTR tetramer.

Abstract: Bisaryloxime ethers and bisarylhydroazones are shown to be effective for inhibiting formation of amyloid fibrils of transthyretin.

Abstract: Bisaryloxime ethers and bisarylhydroazones are shown to be effective for inhibiting formation of amyloid fibrils of transthyretin.