The present disclosure provides compounds that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

There is provided a compound of formula VIIa,

##STR00001##

wherein Q.sup.x represents C(O)OC.sub.1-4 alkyl, or a salt or protected derivative thereof, and other compounds that are useful in the preparation of compounds that have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I):

##STR00001##

including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

The present disclosure generally relates to methods of synthesizing compounds useful as modulators of hepatitis B virus core protein assembly as well as novel synthetic intermediates. The methods disclosed may be used in the manufacture of compounds which may have allosteric effector properties against hepatitis B virus (HBV) core protein (Cp), a protein found as a dimer, a multimer, and as the protein shell of the HBV core. As one example, provided herein is a process for preparing compounds which may be useful for treating viral infections, such as hepatitis B.

The present disclosure relates to compositions comprising N-substituted-dioxocyclobutenylamino-3-hydroxy-picoliamide compounds or a pharmaceutically acceptable salt or hydrate thereof, methods of preparing said compositions, and uses thereof. The compositions may be useful in the treatment of conditions ameliorated by inhibition of CC chemokine receptor 6.

Disclosed herein are compounds for treating conditions related to oxidative stress/damage among other causes, with pharmaceutically accepted salts hydrate, solvate, optical isomer, or combination thereof, comprising lipophilic cation moieties linked to heterocyclics compounds of formula (I) and formula (8); ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may be selected from the group consisting of ##STR00002##
wherein X, Y, and Z are selected from the group consisting of H, methyl, ethyl, propyl, butyl, substituted or unsubstituted aryl, and heteroaryls; n is an integer selected from 0-18, and E is a phosphorous or nitrogen atom.

Disclosed are substituted heterocyclic compounds and proteolysis-targeting chimeric molecules (PROTACs). The substituted heterocycles disclosed herein are shown to be useful in inhibiting c-MYC. The disclosed PROTACs are shown to induce degradation of c-MYC protein. The substituted heterocyclic compounds and proteolysis-targeting chimeric molecules (PROTACs) disclosed, herein may be utilized as therapeutics for treating cancer and cell proliferative disorders.