The present invention relates to compounds of formula (Ia) and the use thereof as inhibitors of P. aeruginosa virulence factor LasB. Formula (Ia). These compounds are useful in the treatment of bacterial infections, especially caused by P. aeruginosa.

##STR00001##

The invention relates to prodrug compounds of formula I: ##STR00001##
wherein R.sup.2, R.sup.3, R.sup.5, R.sup.7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.

The invention relates to prodrug compounds of formula I: ##STR00001##
wherein R.sup.2, R.sup.3, R.sup.5, R.sup.7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.

This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.

This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.

Some embodiments of the present disclosure relate to polymerizable compounds that comprise biocidal activity and/or the potential for increased biocidal activity and that comprise at least one hydrophobic portion and at least one hydrophilic portion. Together the hydrophobic portion and the hydrophilic portion of the compounds may provide the polymerizable compounds with one or more surfactant-like properties. The polymerizable compounds can be incorporated into polymer coating formulations. The polymer coating formulations can be used to coat one or more surfaces of a substrate. The coating formulation can provide biocidal activity and/or the potential for increased biocidal activity to the coated substrate-surface.

Some embodiments of the present disclosure relate to polymerizable compounds that comprise biocidal activity and/or the potential for increased biocidal activity and that comprise at least one hydrophobic portion and at least one hydrophilic portion. Together the hydrophobic portion and the hydrophilic portion of the compounds may provide the polymerizable compounds with one or more surfactant-like properties. The polymerizable compounds can be incorporated into polymer coating formulations. The polymer coating formulations can be used to coat one or more surfaces of a substrate. The coating formulation can provide biocidal activity and/or the potential for increased biocidal activity to the coated substrate-surface.

The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.

Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.

Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.