The presently-disclosed subject matter generally relates to antimicrobial compounds, compositions, methods of making and methods of use thereof. The presently-disclosed subject matter further relates to compounds, compositions and methods for the control of Porphyromonas gingivalis.

Disclosed are compounds of Formula (I):

##STR00001##

or a salt thereof, wherein: X is CR.sub.4 or N; R.sub.1, R.sub.2, R.sub.3, R.sub.4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), 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.

Disclosed are compounds of Formula (I):

##STR00001##

or a salt thereof, wherein: X is CR.sub.4 or N; R.sub.1, R.sub.2, R.sub.3, R.sub.4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), 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 provides novel compounds of formula (I) that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, fibrotic diseases, or cholestatic diseases.

##STR00001##

A binding pair for chromatographic separation or purification of a molecule of interest, where one binding member of the pair is an isomerizable organic molecule and the other binding member of the pair is an isomer-specific affinity agent bound to a molecule of interest. The binding pair associates and disassociates upon exposure to a binding agent, such as using light, decreased intensity of light, darkness, heat, stress, ions, an isomerizable affinity agent, change in pH, or a combination thereof.

A binding pair for chromatographic separation or purification of a molecule of interest, where one binding member of the pair is an isomerizable organic molecule and the other binding member of the pair is an isomer-specific affinity agent bound to a molecule of interest. The binding pair associates and disassociates upon exposure to a binding agent, such as using light, decreased intensity of light, darkness, heat, stress, ions, an isomerizable affinity agent, change in pH, or a combination thereof.

Cyclooxygenase inhibitors include compounds of the formula: ##STR00001##
where R represents phenyl, nitrophenyl, 2-nitrophenyl, 3-nitrophenyl, 4-nitrophenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 3,4-dimethoxyphenyl, 2-methoxyphenyl, 4-hydroxyphenyl, dimethylaminophenyl, 3-methoxyphenyl, 4-ethoxyphenyl, 2,4,5-trimethoxyphenyl, 3,4,5-trimethoxyphenyl, 2,4,6-trimethoxyphenyl, and 2,4-dimethoxyphenyl, 3-hydroxyphenyl, 4-dimethylaminophenyl, or 2,3,4-trimethoxyphenyl.

Cyclooxygenase inhibitors include compounds of the formula: ##STR00001##
where R represents phenyl, nitrophenyl, 2-nitrophenyl, 3-nitrophenyl, 4-nitrophenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 3,4-dimethoxyphenyl, 2-methoxyphenyl, 4-hydroxyphenyl, dimethylaminophenyl, 3-methoxyphenyl, 4-ethoxyphenyl, 2,4,5-trimethoxyphenyl, 3,4,5-trimethoxyphenyl, 2,4,6-trimethoxyphenyl, and 2,4-dimethoxyphenyl, 3-hydroxyphenyl, 4-dimethylaminophenyl, or 2,3,4-trimethoxyphenyl.

The invention relates to an industrial scale process for the preparation of a compound of general formula (I): (Formula (I)) wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein. The process comprises reacting compounds of general formulae (II) and (III): (formulae (II), (III)) in the presence of a Lewis acid followed by a reduction with triethylsilane.

##STR00001##

The present disclosure relates to compounds that bind to at least one of ACAT1/2 and OXCT1/2 and inhibit mitochondrial ATP production, referred to herein as mitoketoscins. Methods of screening compounds for mitochondrial inhibition and anti-cancer properties are disclosed. Also described are methods of using mitoketoscins to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitoketoscins to provide anti-aging benefits. Specific mitoketoscin compounds are also disclosed.