TASP-0428980(TASP-0428980) - 药物靶点：Orexin receptor_在研适应症：入睡和睡眠障碍_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

Orexin receptor

作用方式

拮抗剂

作用机制

食欲素受体拮抗剂

治疗领域

神经系统疾病

在研适应症

入睡和睡眠障碍

非在研适应症-

原研机构

Taisho Pharmaceutical Co., Ltd.

在研机构

Taisho Pharmaceutical Co., Ltd.

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 TASP-0428980 相关的临床结果

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100 项与 TASP-0428980 相关的转化医学

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100 项与 TASP-0428980 相关的专利（医药）

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1

项与 TASP-0428980 相关的文献（医药）

2015-03-01·Bioorganic & Medicinal Chemistry3区 · 医学

Discovery and in vitro and in vivo profiles of N-ethyl-N-[2-[3-(5-fluoro-2-pyridinyl)-1H-pyrazol-1-yl]ethyl]-2-(2H-1,2,3-triazol-2-yl)-benzamide as a novel class of dual orexin receptor antagonist

3区 · 医学

Article

作者: Araki, Yuko ; Nishikawa-Shimono, Rie ; Futamura, Aya ; Kambe, Daiji ; Tokura, Seiken ; Suzuki, Ryo ; Kawamoto, Hiroshi ; Nozawa, Dai ; Ohtake, Norikazu ; Ohmichi, Mari ; Abe, Masahito ; Hattori, Nobutaka ; Aoki, Takeshi ; Ohta, Hiroshi

Orexins play an important role in sleep/wake regulation, and orexin receptor antagonists are a focus of novel therapy for the treatment of insomnia. We identified 27e (TASP0428980) as a potent dual orexin receptor antagonist through the systematic modification of our original designed lead A. We demonstrated the potent sleep-promoting effects of 27e at ip dose of 3mg/kg in a rat polysomnogram study. 27e exhibited relatively short half-life profiles in rats and dogs. Furthermore, accumulating evidence regarding ADME profiles indicates that the predicted human half-life of 27e should be 1.2-1.4h. These data indicated that 27e has a short-acting hypnotic property, suggesting that 27e might be useful for treating primary insomnia while exhibiting a low risk of next-day residual somnolence. Thus, 27e and its related compounds should be further evaluated to enable advancement to clinical trials.

100 项与 TASP-0428980 相关的药物交易

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