C07D295/16

Spirocyclic EBI2 modulators

Provided herein are small molecule Epstein-Barr virus-induced G-protein coupled receptor 2 (EBI2) modulator compounds, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds. In some embodiments, EBI2 is a therapeutic target for the treatment of diseases or conditions such as, but not limited to, autoimmune diseases or conditions, cancer, and cardiovascular disease.

Spirocyclic EBI2 modulators

Provided herein are small molecule Epstein-Barr virus-induced G-protein coupled receptor 2 (EBI2) modulator compounds, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds. In some embodiments, EBI2 is a therapeutic target for the treatment of diseases or conditions such as, but not limited to, autoimmune diseases or conditions, cancer, and cardiovascular disease.

Anthelmintic compounds and compositions and method of using thereof

The present invention relates to novel anthelmintic compounds of formula (I) below: ##STR00001##
wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5, X.sub.6, X.sub.7 and X.sub.8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.

Anthelmintic compounds and compositions and method of using thereof

The present invention relates to novel anthelmintic compounds of formula (I) below: ##STR00001##
wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5, X.sub.6, X.sub.7 and X.sub.8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.

Cyanopyridine Derivatives as Liver X Receptor Beta Agonists, Compositions, and Their Use

In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X- receptor (LXR) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

##STR00001##

Cyanopyridine Derivatives as Liver X Receptor Beta Agonists, Compositions, and Their Use

In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X- receptor (LXR) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

##STR00001##

TRIAZOLE AGONISTS OF THE APJ RECEPTOR

Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures:

##STR00001##

where the definitions of the variables are provided herein.

TRIAZOLE AGONISTS OF THE APJ RECEPTOR

Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures:

##STR00001##

where the definitions of the variables are provided herein.

Thermoresponsive polyesters
10106514 · 2018-10-23 · ·

A thermoresponsive polyester comprising units derived from an amide functional diol compound having a first amide group having a nitrogen atom and a carbonyl group; a second amide group tethered directly or indirectly through an organic group at the carbonyl group of the first amide group; and two organic groups terminated with a hydroxyl group attached to the nitrogen atom of the first amide group. The thermoresponsive polyesters exhibit a lower critical solution temperature at which they undergo a thermally induced reversible hydrophobicity change. This hydrophobicity change may involve the formation of coacervates of the thermoresponsive polyesters which can then coalesce into a precipitated polymer rich phase.

Thermoresponsive polyesters
10106514 · 2018-10-23 · ·

A thermoresponsive polyester comprising units derived from an amide functional diol compound having a first amide group having a nitrogen atom and a carbonyl group; a second amide group tethered directly or indirectly through an organic group at the carbonyl group of the first amide group; and two organic groups terminated with a hydroxyl group attached to the nitrogen atom of the first amide group. The thermoresponsive polyesters exhibit a lower critical solution temperature at which they undergo a thermally induced reversible hydrophobicity change. This hydrophobicity change may involve the formation of coacervates of the thermoresponsive polyesters which can then coalesce into a precipitated polymer rich phase.