Histone H1 inhibitors( Neurocrine Biosciences, Inc.)(Histone H1 inhibitors( Neurocrine Biosciences, Inc.)) - 药物靶点：组蛋白H1_在研适应症：睡眠异常_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

组蛋白H1

作用方式

抑制剂

作用机制

组蛋白H1抑制剂

治疗领域

神经系统疾病

在研适应症

睡眠异常

非在研适应症-

原研机构

Neurocrine Biosciences, Inc.

在研机构

Neurocrine Biosciences, Inc.

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-

关联

100 项与 Histone H1 inhibitors( Neurocrine Biosciences, Inc.) 相关的临床结果

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100 项与 Histone H1 inhibitors( Neurocrine Biosciences, Inc.) 相关的转化医学

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100 项与 Histone H1 inhibitors( Neurocrine Biosciences, Inc.) 相关的专利（医药）

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1

项与 Histone H1 inhibitors( Neurocrine Biosciences, Inc.) 相关的文献（医药）

2009-09-10·Journal of Medicinal Chemistry1区 · 医学

Characterization of Novel Selective H₁-Antihistamines for Clinical Evaluation in the Treatment of Insomnia

1区 · 医学

Article

作者: Crowe, Paul D. ; Malany, Siobhan ; Madan, Ajay ; Jovic, Florence ; Yu, Jinghua ; Petroski, Robert E. ; Tucci, Fabio ; Gross, Raymond S. ; Wang, Hua ; Sacaan, Aida ; Moree, Wilna J. ; O’Brien, Zhihong ; Hernandez, Lisa M. ; Li, Bin-Feng ; Bradbury, Margaret J. ; Marinkovic, Dragan ; Coon, Timothy ; Hoare, Samuel R. J. ; Zamani-Kord, Said ; Beaton, Graham ; Wen, Jianyun

Analogues of the known H(1)-antihistamine R-dimethindene were profiled as potential agents for the treatment of insomnia. Several highly selective compounds were efficacious in rodent sleep models. On the basis of overall profile, indene 1d and benzothiophene 2a had pharmacokinetic properties suitable for evaluation in night time dosing. Compound 2a did not show an in vivo cardiovascular effect from weak hERG channel inhibition.

100 项与 Histone H1 inhibitors( Neurocrine Biosciences, Inc.) 相关的药物交易

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