Jeffrey Laskin - Piscataway NJ, US Diane Heck - Rumson NJ, US Karine Fabio - Bethlehem PA, US C. Jeffrey Lacey - Bethlehem PA, US Sherri Young - Bethlehem PA, US Pramod Mohanta - Bethlehem PA, US Christophe Guillon - Bethlehem PA, US Ned Heindel - Easton PA, US
A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X═C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.
Augmenting Moieties For Anti-Inflammatory Compounds
Augmented or synergized anti-inflammatory constructs are disclosed including terpenes covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids, amino acids and polyamines; and anti-inflammatory molecules covalently conjugated with specific amino acids. For the latter, further conjugation with a choline bioisostere further augments the anti-inflammatory activity.