C07F9/59

Kinase inhibitors

There are provided compounds of formula I, ##STR00001##
wherein R.sup.1A to R.sup.1E, R.sup.2 to R.sup.4, R.sup.5a, L and X.sup.1 to X.sup.3 have meanings given in the description, which compounds have anti-inflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Kinase inhibitors

There are provided compounds of formula I, ##STR00001##
wherein R.sup.1A to R.sup.1E, R.sup.2 to R.sup.4, R.sup.5a, L and X.sup.1 to X.sup.3 have meanings given in the description, which compounds have anti-inflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

PRODRUGS OF PYRIDONE AMIDES USEFUL AS MODULATORS OF SODIUM CHANNELS

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.

PRODRUGS OF PYRIDONE AMIDES USEFUL AS MODULATORS OF SODIUM CHANNELS

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.

Prodrugs of phenolic TRPV1 agonists

Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity.

Prodrugs of phenolic TRPV1 agonists

Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity.

Gold(III) complex, a conjugate of the gold(III) complex, a pharmaceutical composition comprising the gold(III) complex and uses and a process for preparing the gold(III) complex

A gold(III) complex, a conjugate of the gold(iII) complex, a pharmaceutical composition comprising the gold(III) complex and uses and a process for preparing the gold(III) complex. The complex comprises a group of (S{circumflex over ()}C)-cyclometallated gold(III) complexes containing a 1,1-dithio ligand, which exhibit antibacterial activity against multiresistant microorganisms or against biofilm activity or biofilm disruption. The gold(III) complex has efficacy against a variety of microorganisms and low toxicity.

Gold(III) complex, a conjugate of the gold(III) complex, a pharmaceutical composition comprising the gold(III) complex and uses and a process for preparing the gold(III) complex

A gold(III) complex, a conjugate of the gold(iII) complex, a pharmaceutical composition comprising the gold(III) complex and uses and a process for preparing the gold(III) complex. The complex comprises a group of (S{circumflex over ()}C)-cyclometallated gold(III) complexes containing a 1,1-dithio ligand, which exhibit antibacterial activity against multiresistant microorganisms or against biofilm activity or biofilm disruption. The gold(III) complex has efficacy against a variety of microorganisms and low toxicity.

POLYMERIZABLE COMPOUNDS WITH ONE OR MORE SURFACTANT-LIKE PROPERTIES

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.

POLYMERIZABLE COMPOUNDS WITH ONE OR MORE SURFACTANT-LIKE PROPERTIES

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.