Spiro azepane-oxazolidinones as Kv1.3 potassium channel blockers: WO2010066840.
This article evaluates a patent application from Solvay Pharmaceuticals, which claims spiro azepane-oxazolidinones as novel blockers of the voltage-gated potassium channel Kv1.3 for the treatment of diabetes, psoriasis, obesity, transplant rejection and T-cell mediated autoimmune diseases such as rheumatoid arthritis and MS. The patent describes a new chemotype of Kv1.3 blockers and thus illustrates the growing interest of the pharmaceutical industry in Kv1.3 as a target of immunosuppression and metabolic disorders. This article briefly summarizes the chemistry and biological data provided in the patent and then compares the new compounds to Kv1.3 blockers previously disclosed by both academia and pharmaceutical companies.
University of California, Department of Pharmacology, Davis, Davis, CA 95616, USA. hwulff@ucdavis.edu
Heike
H
Wulff
D000818:Animals; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D051664:Kv1.3 Potassium Channel / Q000037:antagonists & inhibitors*; D023303:Oxazolidinones / Q000494:pharmacology*; D010330:Patents as Topic; D026902:Potassium Channel Blockers / Q000494:pharmacology*; D013141:Spiro Compounds / Q000494:pharmacology; D013601:T-Lymphocytes / Q000187:drug effects / Q000276:immunology
D051664:Kv1.3 Potassium Channel; D023303:Oxazolidinones; D026902:Potassium Channel Blockers; D013141:Spiro Compounds