Novel Kv1.3 blockers for immunosuppression: WO2012155199

Expert Opin Ther Pat. 2013 Nov;23(11):1511-6. doi: 10.1517/13543776.2013.831072. Epub 2013 Aug 23.

Abstract

A recent patent application from Bionomics/Merck Serono describes novel compounds as blockers of the voltage-gated Kv1.3 ion channel. The blockade of this channel shows great promise as a new therapeutic target for the treatment of autoimmune disorders such as multiple sclerosis, psoriasis, diabetes and rheumatoid arthritis. The generic claim of this patent refers to a new chemotype of Kv1.3 blockers based on an amide core with potent IC50's which are potentially within the nanomolar range. This article briefly reviews the chemistry and biology found in the patent and compares it with previous discoveries in the field.

Publication types

  • Review

MeSH terms

  • Animals
  • Autoimmune Diseases / drug therapy
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Humans
  • Immunosuppressive Agents / chemistry
  • Immunosuppressive Agents / pharmacology*
  • Immunosuppressive Agents / therapeutic use
  • Kv1.3 Potassium Channel / antagonists & inhibitors*
  • Patents as Topic
  • Potassium Channel Blockers / chemistry
  • Potassium Channel Blockers / pharmacology*
  • Potassium Channel Blockers / therapeutic use

Substances

  • Immunosuppressive Agents
  • Kv1.3 Potassium Channel
  • Potassium Channel Blockers