Novel Kv1.3 blockers for immunosuppression: WO2012155199

被引：2
|
作者：
William Nguyen [1 ]
机构：
[1] Scripps Res Inst, Dept Mol Therapeut, Jupiter, FL USA
来源：
EXPERT OPINION ON THERAPEUTIC PATENTS | 2013年 / 23卷 / 11期
关键词：
autoimmune disorder; Kv1.3; MS; potassium channel; psoriasis; rheumatoid arthritis; GATED POTASSIUM CHANNEL; MEMORY T-CELLS; AUTOIMMUNE ENCEPHALOMYELITIS; MULTIPLE-SCLEROSIS; ION-CHANNEL; K+ CHANNELS; DERIVATIVES; IMMUNOMODULATION; KHELLINONE; ACTIVATION;
D O I：
10.1517/13543776.2013.831072
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
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收藏
页码：1511 / 1516
页数：6
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