Johnson & Johnson Pharmaceutical Research & Development, LLC 3210 Merryfield Row, San Diego, CA 92121, USA. bsavall@its.jnj.com
Abstract:
This report discloses the development of a series of tricyclic histamine H(4) receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H(4) receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model.