Novel dipyrazoles acting as glutamate modulators

in Expert Opinion on Therapeutic Patents (2007), 17(12), 1489-1493

Knowing the potential therapeutic interest of AMPA potentiation, patents have been published for 15 years relating the discovery of novel compounds able to allosterically bind to the AMPA receptors and ... [more ▼]

Knowing the potential therapeutic interest of AMPA potentiation, patents have been published for 15 years relating the discovery of novel compounds able to allosterically bind to the AMPA receptors and leading to a potentiation of the AMPA signals. Besides this classical approach, a new target for the medicinal chemist has been defined due to the recent findings describing the modulation of AMPA receptors by neuronal proteins, and has led to the design of dipyrazole compounds by Aventis. These new dipyrazole derivatives may be considered as `indirect AMPApams', constituting a new pharmacological class. Based on their in vitro activity, it is probable that these compounds could be of therapeutic value for the treatment of cognitive disorders, schizophrenia or depression. [less ▲]

Update on GPIIb/IIIa antagonists

in Expert Opinion on Therapeutic Patents (2003), 13

The inhibition of metalloproteinases to treat osteoarthritis: reality and new perspectives

in Expert Opinion on Therapeutic Patents (2002), 12(1), 29-43

The objective of this paper is to analyse the potential therapeutic action of MMP inhibitors in the management of osteoarthritis (OA), based on a critical review of the literature. The role played by ... [more ▼]

The objective of this paper is to analyse the potential therapeutic action of MMP inhibitors in the management of osteoarthritis (OA), based on a critical review of the literature. The role played by metalloproteinases (MPs) in the pathophysiology of osteoarthritis is discussed, as well as their regulation by tissular inhibitors, activators and cytokines. The evidences that commonly used drugs for treating osteoarthritis are also active on MPs synthesis is also reported. Finally, this paper provides an analysis of the recent patents published with promising therapeutic potential and gives new perspectives for anti-MPs therapy. [less ▲]

Latest discoveries in prostaglandin receptor modulators

in Expert Opinion on Therapeutic Patents (2002), 12