1,7-diaryl-1,6-heptadiene-3,5-dione derivatives, methods for the production and use thereof.

Compounds, pharmaceutically acceptable salts, and pharmaceutical compositions thereof are disclosed that are useful for inhibition of the biological activity of CCL2, as well as methods of treatment for diseases involving the biological activity of CCL2.

The present invention relates to compounds that modify low density lipoprotein receptor (LDLR) expression. The compounds have the structural formula I shown below:

##STR00001##

wherein m, R.sub.1, n, R.sub.2 and R.sub.3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with elevated levels of low density lipoprotein cholesterol (LDL-C).

The present invention relates to compounds that modify low density lipoprotein receptor (LDLR) expression. The compounds have the structural formula I shown below:

##STR00001##

wherein m, R.sub.1, n, R.sub.2 and R.sub.3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with elevated levels of low density lipoprotein cholesterol (LDL-C).

1,7-diaryl-1,6-heptadiene-3,5-dione derivatives, methods for the production and use thereof.

1,7-diaryl-1,6-heptadiene-3,5-dione derivatives, methods for the production and use thereof.

Cationic pillar[n]arenes, e.g., positively charged poly-ammonium, poly-phosphonium and poly-imidazolium pillar[5-6]arene derivatives are capable of inhibiting or preventing biofilm formation, and facilitating existing biofilm decomposition. A composition for inhibiting or disrupting biofilm, e.g., bacterial or fungal biofilm, formation, or reducing biofilm, can include a pharmaceutically acceptable carrier, and a cationic pillar[n]ene.

The present invention provides cationic pillar[n]arenes, e.g., positively charged poly-ammonium, poly-phosphonium and poly-imidazolium pillar[5-6]arene derivatives, capable of inhibiting or preventing biofilm formation, and facilitating existing biofilm decomposition; as well as compositions thereof and methods of use.

Methods are provided herein for the treatment of ophthalmic diseases or conditions such as an ophthalmic disease or disorder associated with diabetes in a patient. Also provided herein are methods of treating retinopathy of prematurity in a patient. Further, provided herein are methods for treating wet age-related macular degeneration in a patient. The methods comprise administration of compounds disclosed herein to a patient in need thereof that inhibit or slow one or more signs or symptoms of such conditions.

Methods are provided herein for the treatment of ophthalmic diseases or conditions such as an ophthalmic disease or disorder associated with diabetes in a patient. Also provided herein are methods of treating retinopathy of prematurity in a patient. Further, provided herein are methods for treating wet age-related macular degeneration in a patient. The methods comprise administration of compounds disclosed herein to a patient in need thereof that inhibit or slow one or more signs or symptoms of such conditions.