The renoprotective potential of endothelin receptor antagonists

Intensive research, stemming from experimental and clinical findings, has been carried out in the last few years into a possible role for endothelin (ET) in the mediation of acute and chronic renal dysfunction. So far, a number of pre-clinical studies have been performed with ET antagonists. These were aimed at exploring the possibility that modulation of ET synthesis or activity at the receptor level could ameliorate the renal haemodynamic and/or structural damage associated with various nephropathies. This review will cover patenting activity concerning endothelin-converting enzyme (ECE) inhibitors, either presently in pre-clinical development or that have appeared recently in patent literature. Special emphasis will be placed on the more significant developments and patent applications concerning selective and unselective ET receptor antagonists, and the few compounds for which in vivo pre-clinical data are already available will be identified and separated from those that have only been tested in vitro.