JNJ-26990990(JNJ-26990990) - 药物靶点：N-type calcium channel x Sodium channels_在研适应症：癫痫_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

N-type calcium channel x Sodium channels

作用机制

N-type calcium channel抑制剂(Calcium channel inhibitor N-types inhibitors)、钠通道阻滞剂

治疗领域

神经系统疾病

在研适应症

癫痫

非在研适应症-

原研机构

Johnson & Johnson

在研机构

Johnson & Johnson

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C9H10N2O2S2

InChIKeyAWSKBQNOSRREEY-UHFFFAOYSA-N

CAS号877316-38-6

关联

100 项与 JNJ-26990990 相关的临床结果

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100 项与 JNJ-26990990 相关的转化医学

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100 项与 JNJ-26990990 相关的专利（医药）

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2

项与 JNJ-26990990 相关的文献（医药）

2009-12-10·Journal of Medicinal Chemistry1区 · 医学

Novel, Broad-Spectrum Anticonvulsants Containing a Sulfamide Group: Advancement of N-((Benzo[b]thien-3-yl)methyl)sulfamide (JNJ-26990990) into Human Clinical Studies

1区 · 医学

Article

作者: Parker, Michael H. ; Qin, Ning ; Milewski, Michael E. ; Malatynska, Ewa ; Lubin, Mary Lou ; Cuyckens, Filip ; Smith-Swintosky, Virginia L. ; Klein, Brian ; Leclercq, Laurent ; White, H. Steve ; Brenneman, Douglas ; Liu, Yi ; Maryanoff, Bruce E. ; Reitz, Allen B. ; Herb, Mark ; Iannucci, Robert ; Finley, Michael F. A. ; McComsey, David F. ; Huang, Yifang

In seeking broad-spectrum anticonvulsants to treat epilepsy and other neurological disorders, we synthesized and tested a group of sulfamide derivatives (4a-k, 5), which led to the clinical development of 4a (JNJ-26990990). This compound exhibited excellent anticonvulsant activity in rodents against audiogenic, electrically induced, and chemically induced seizures, with very weak inhibition of human carbonic anhydrase-II (IC(50) = 110 microM). The pharmacological profile for 4a supports its potential in the treatment of multiple forms of epilepsy, including pharmacoresistant variants. Mechanistically, 4a inhibited voltage-gated Na(+) channels and N-type Ca(2+) channels but was not effective as a K(+) channel opener. The pharmacokinetics and metabolic properties of 4a are discussed.

Organic & Biomolecular Chemistry3区 · 化学

The anticonvulsant sulfamide JNJ-26990990 and its S,S-dioxide analog strongly inhibit carbonic anhydrases: solution and X-ray crystallographic studies

3区 · 化学

Article

作者: Alterio, Vincenzo ; Winum, Jean-Yves ; De Simone, Giuseppina ; Riccio, Vincenzo ; Carta, Fabrizio ; Di Fiore, Anna ; Supuran, Claudiu T.

Inhibition and X-ray crystallographic data for the binding of JNJ-26990990 and itsS,S-dioxide analog to hCAs have been reported.

100 项与 JNJ-26990990 相关的药物交易

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