首页> 外国专利> Pro-drugs of riluzole and their method of use for the treatment of amyotrophic lateral sclerosis

Pro-drugs of riluzole and their method of use for the treatment of amyotrophic lateral sclerosis

机译:利鲁唑的前药及其用于治疗肌萎缩性侧索硬化症的方法

摘要

Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.
机译:本发明的药物组合物包括取代的利鲁唑前药,其可通过利鲁唑的释放用于治疗肌萎缩性侧索硬化症(ALS)和相关疾病,尤其是避免初次通过Cyp 1A2促进肝代谢的患者之间的差异。利鲁唑的前药对肝脏代谢具有增强的稳定性,并通过口服给药进入全身循环,然后通过酶促或常规生物物理释放过程裂解以在血浆中释放利鲁唑。本发明进一步包括用于治疗疾病状态的利鲁唑前药,其可以通过从前药中释放利鲁唑来用利鲁唑来治疗。

著录项

  • 公开/公告号US10357497B2

    专利类型

  • 公开/公告日2019-07-23

    原文格式PDF

  • 申请/专利权人 BIOHAVEN PHARMACEUTICAL HOLDING COMPANY LIMITED;

    申请/专利号US201314410647

  • 发明设计人 ALLEN B. REITZ;GARRY R. SMITH;

    申请日2013-06-24

  • 分类号A61K31/541;A61K31/428;A61K31/4439;A61K31/454;A61K31/4725;A61K31/496;A61K31/5377;

  • 国家 US

  • 入库时间 2022-08-21 12:16:08

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