1-[5-(2,5-Difluorophenyl)spiro[1,3,4-thiadiazole-2,7'-bicyclo[4.2.0]octa-1,3,5-triene]-3-yl]-4-(dimethylamino)butan-1-one | 1146208-96-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: 1-[5-(2,5-Difluorophenyl)spiro[1,3,4-thiadiazole-2,7'-bicyclo[4.2.0]octa-1,3,5-triene]-3-yl]-4-(dimethylamino)butan-1-one
• CAS: 1146208-96-9
• 化学式: C₂₁H₂₁F₂N₃OS
• 分子量: 401.48
• InChiKey: LVVNIHMNFJQODU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  61.2
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• [EN] SPIRO-CONDENSED 1, 3, 4-THIADIAZOLE DERIVATIVES FOR INHIBITING KSP KINESIN ACTIVITY<br/>[FR] DÉRIVÉS DE 1,3,4-THIADIAZOLE SPIRO-CONDENSÉS POUR INHIBER L'ACTIVITÉ DE LA KINÉSINE KSP
  申请人：SCHERING CORP

  公开号：WO2009052288A1

  公开（公告）日：2009-04-23

  The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity. Formula I [Chemical formula should be inserted here as it appears on abstract in paper form.]

  本发明涉及以下式（I）的化合物（其中X、R1、R2、R3、p、E、环A和环B的定义如本文所述）。本发明还涉及包括这些化合物的组合物（包括药学上可接受的组合物），单独或与一个或多个额外治疗剂的组合物，并且涉及它们在抑制KSP动力蛋白活性以及治疗与KSP动力蛋白活性相关的细胞增殖性疾病或紊乱的用途的方法。Formula I [化学式应按照纸质形式中的摘要插入在此处。]
• Sequential Administration of Chemotherapeutic Agents for Treatment of Cancer
  申请人：Wang Yaolin

  公开号：US20110129456A1

  公开（公告）日：2011-06-02

  The present invention relates to the sequential administration of a cytotoxic agent followed by an IGF1R antagonist (e.g., an antibody) for the treatment of hyperproliferative disorders including cancer.

  本发明涉及采用细胞毒性药物后接IGF1R拮抗剂（例如抗体）的顺序治疗高增殖性疾病，包括癌症。
• SPIRO-CONDENSED 1, 3, 4-THIADIAZOLE DERIVATIVES FOR INHIBITING KSP KINESIN ACTIVITY
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2220061B1

  公开（公告）日：2016-02-17
• COMPOUNDS FOR INHIBITING KSP KINESIN ACTIVITY
  申请人：Siddiqui M. Arshad

  公开号：US20110123435A1

  公开（公告）日：2011-05-26

  The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity. Formula I
• US8796460B2
  申请人：——

  公开号：US8796460B2

  公开（公告）日：2014-08-05