(Z)-N-[(1,1-dioxothiolan-3-yl)methyl]-3-[3-[3-methyl-5-(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]prop-2-enamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: (Z)-N-[(1,1-dioxothiolan-3-yl)methyl]-3-[3-[3-methyl-5-(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]prop-2-enamide
• 化学式: C₁₈H₁₉F₃N₄O₃S
• 分子量: 428.4
• InChiKey: CNBPONARDOXWAG-RQOWECAXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  102
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• HYDRAZIDE CONTAINING NUCLEAR TRANSPORT MODULATORS AND USES THEREOF
  申请人：Karyopharm Therapeutics, Inc.

  公开号：US20140235653A1

  公开（公告）日：2014-08-21

  The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.

  本发明通常涉及核运输调节剂，例如CRM1抑制剂，更具体地涉及由结构式I表示的化合物或其药学上可接受的盐，其中变量和备选变量的值如本文所定义和描述的那样。本发明还包括合成和使用结构式I的化合物，或其药学上可接受的盐或组合物，例如在治疗、调节和/或预防与CRM1活性相关的生理状况中使用。
• Hydrazide Containing Nuclear Transport Modulators and Uses Thereof
  申请人：Karyopharm Therapeutics Inc.

  公开号：US20160304472A1

  公开（公告）日：2016-10-20

  The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
• METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF BETA-THALASSEMIAS
  申请人：INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE)

  公开号：US20170020847A1

  公开（公告）日：2017-01-26

  The present invention relates to methods and pharmaceutical compositions for the treatment of beta-thalassemias. In particular, the present invention relates to an XPO1 inhibitor for use in a method for treating beta-thalassemia in a subject in need thereof.
• METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF MYELODYSPLASTIC SYNDROMES
  申请人：INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE)

  公开号：US20170100378A1

  公开（公告）日：2017-04-13

  The present invention provides methods and pharmaceutical compositions designed to intervene in this defective process and to promote or restore erythrocyte maturation in individuals suffering from a myelodysplastic syndrome. The methods involve maintaining the activity of GATA-1 by preventing sequestration of Hsp70 in the cytoplasm. Accordingly, it is an object of this invention to provide methods of restoring or increasing erythrocyte maturation in a subject suffering from a myelodysplastic syndrome by preventing proteolytic inactivation of GATA-1. In some embodiments, preventing is achieved by administering to the subject a compound that inhibits the XPO1 nuclear transporter.
• US8999996B2
  申请人：——

  公开号：US8999996B2

  公开（公告）日：2015-04-07