Bioavailable pyrrolo-benzo-1,4-diazines as Nav1.7 sodium channel blockers for the treatment of pain

A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. Compound 33 displayed oral anti-nociceptive efficacy in both rat CFA pain model (100 mpk oral dosing) and SNL neuropathic pain model (EC50 75 μM).