Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):

##STR00001##

and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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.

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): ##STR00001##
and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

The present invention relates to a compound represented by the formula (E) which is useful for treating or preventing melanoma.

##STR00001##

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.

Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step.

The present invention provides a phosphorus-containing compound characterized by being a compound represented by the following structure:

##STR00001## the compound is a novel immune cell migration inhibitor. The compound has good hydrophilicity and can be developed into eye drops. The compound has a strong inhibitory ability to immune cell migration and can relieve the symptoms of most dry-eye patients.

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.

In one aspect, the invention relates to compounds having the formula XII:

##STR00001##

where R.sup.a, R.sup.b, R.sup.2, R.sup.7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

The novel bisphosphonic acid ester derivatives represented by the following formula (1):
YCy(NH).sub.m(CH.sub.2).sub.nC(X)(PO(OR.sup.1)(OR.sup.2)).sub.2(1)
wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.