Novel prostaglandin receptor modulators--part II: EP receptor modulators; a patent review (2002 - 2012)

Expert Opin Ther Pat. 2013 Feb;23(2):233-67. doi: 10.1517/13543776.2013.744822. Epub 2013 Jan 4.

Abstract

Introduction: Prostaglandins and their G-protein-coupled receptors play numerous physiological and pathophysiological roles, especially in inflammation and its resolution. The variety of effects mediated by prostanoids makes prostanoid receptors valuable drug targets and the research on prostaglandin receptor modulators is intensive. The physiological and pathophysiological effects of prostaglandin E(2) are especially complex and numerous. The four subtypes of EP receptor have gained a lot of industrial and academic interest, in particular EP(2) and EP(4) for various indications.

Areas covered: Evaluation of the patent activity over the last decade (2002 - 2012) illustrates several potent compounds targeting the distinct prostaglandin E(2) receptors. Many novel methods for the use of EP receptor modulators have been developed, in addition to the classical indications for agents modulating the arachidonic acid cascade such as pain and inflammation.

Expert opinion: Several EP targeting agents with good potency and selectivity have been developed but their pharmacological use and utility has not yet been satisfactorily investigated. More research is necessary, and clinical use of these agents might therefore take some more time.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Dinoprostone / metabolism
  • Drug Design*
  • Humans
  • Molecular Structure
  • Patents as Topic*
  • Receptors, Prostaglandin E / drug effects*
  • Receptors, Prostaglandin E / metabolism
  • Receptors, Prostaglandin E, EP1 Subtype / drug effects
  • Receptors, Prostaglandin E, EP1 Subtype / metabolism
  • Receptors, Prostaglandin E, EP2 Subtype / drug effects
  • Receptors, Prostaglandin E, EP2 Subtype / metabolism
  • Receptors, Prostaglandin E, EP3 Subtype / drug effects
  • Receptors, Prostaglandin E, EP3 Subtype / metabolism
  • Receptors, Prostaglandin E, EP4 Subtype / drug effects
  • Receptors, Prostaglandin E, EP4 Subtype / metabolism
  • Signal Transduction / drug effects
  • Structure-Activity Relationship

Substances

  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP1 Subtype
  • Receptors, Prostaglandin E, EP2 Subtype
  • Receptors, Prostaglandin E, EP3 Subtype
  • Receptors, Prostaglandin E, EP4 Subtype
  • Dinoprostone