Novel prostaglandin receptor modulators: a patent review (2002 - 2012) - part I: non-EP receptor modulators

Prostaglandins and their G-protein coupled receptors play numerous physiological and pathophysiological roles especially in inflammation and its resolution. The variety of physiological effects mediated by prostanoids makes prostanoid receptors valuable drug targets and the research on prostaglandin receptor modulators is intensive. Prostaglandin receptor targeting drugs might be beneficial for the treatment of inflammatory, allergic, respiratory and cardiovascular disorders as well as treatment of pain but several novel fields of use such as cancer and ophthalmic diseases have also been found apart from these classical indications.

Evaluation of the patent activity over the last decade (2002 - 2012) illustrates many potent and selective modulators of the distinct prostanoid receptors and some novel methods for their use besides the classical indications. By now, some prostaglandin receptor antagonists already have reached clinical development.

Though the structural diversity of compounds targeting prostanoid receptors is not really large, several highly potent agents with favorable properties have been developed. The clinical potential of FP, IP, TP and DP modulators remains to be investigated, while first very promising clinical results are available as far as CRTH2 is concerned.