title: CXCR2 modulators: a patent review (2009 - 2013).
abstract: BACKGROUND
  Small-molecule antagonists of CXC chemokine receptor 2 (CXCR2) have attracted a considerable amount of attention due to the key central role that this receptor plays in inflammatory conditions. Recently, several CXCR2 receptor antagonists have demonstrated promising proof of activity in early pulmonary clinical trials, which has stimulated additional efforts to identify new CXCR2 receptor antagonists.
  
  
  METHODS
  During the period 2009 - 2013, there were numerous patent publications from various companies claiming the discovery of novel CXCR2 receptor antagonists. Herein, an interpretation of these new patent publications combined with emerging disclosures from the peer-reviewed literature during this time frame is given. This review highlights the preferred or representative compounds from the patent applications along with relevant biological characterization.
  
  
  CONCLUSIONS
  Many of the new CXCR2 receptor antagonists described in this review represent closely related analogs to previously disclosed clinical candidates. With the recent discontinuation of several CXCR2 receptor antagonists in the clinic, additional clinical trial information for CXCR2 receptor antagonists, both past and present, will determine the long-term therapeutic potential of these compounds for the treatment of a variety of inflammatory disorders.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories , 126 E. Lincoln Ave, RY800-D101, Rahway, NJ 07065-0900 , USA +1 732 594 1733 ; +1 732 594 9490 ; michael.dwyer@merck.com.
authors.forename: Michael P
authors.initials: MP
authors.lastname: Dwyer
authors.forename: Younong
authors.initials: Y
authors.lastname: Yu
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D004345:Drug Industry; D006801:Humans; D010330:Patents as Topic; D023063:Receptors, Interleukin-8B / Q000037:antagonists & inhibitors* / Q000187:drug effects
chemical_list: D000893:Anti-Inflammatory Agents; D023063:Receptors, Interleukin-8B