Progress in the development of histamine H receptor antagonists/inverse agonists: a patent review (2013-2017).

INTRODUCTION

Since years, ligands blocking histamine H receptor (HR) activity (antagonists/inverse agonists) are interesting targets in the search for new cures for CNS disorders. Intensive works done by academic and pharmaceutical company researchers have led to many potent and selective HR antagonists/inverse agonists. Some of them have reached to clinical trials.

AREAS COVERED

Patent applications from January 2013 to September 2017 and the most important topics connected with HR field are analysed. Espacenet, Patentscope, Pubmed, GoogleScholar or Cochrane Library online databases were principially used to collect all the materials.

EXPERT OPINION

The research interest in histamine HR field is still high although the number of patent applications has decreased during the past 4 years (around 20 publications). Complexity of histamine HR biology e.g. many isoforms, constitutive activity, heteromerization with other receptors (dopamine D, D, adenosine A) and pharmacology make not easy realization and evaluation of therapeutic potential of anti-HR ligands. First results from clinical trials have verified potential utility of histamine HR antagonist/inverse agonists in some diseases. However, more studies are necessary for better understanding of an involvement of the histaminergic system in CNS-related disorders and helping more ligands approach to clinical trials and the market. Lists of abbreviations: hAChEI - human acetylcholinesterase inhibitor; hBuChEI - human butyrylcholinesterase inhibitor; hMAO - human monoamine oxidase; MAO - monoamine oxidase.