(S)-3-[8-[(二甲基氨基)甲基]-6,7,8,9-四氢吡啶并[1,2-a]吲哚-10-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮 | 151342-35-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 中文名称: (S)-3-[8-[(二甲基氨基)甲基]-6,7,8,9-四氢吡啶并[1,2-a]吲哚-10-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮
• 中文别名: (S)-3-[8-[(二甲基氨基)甲基]-6,7,8,9-四氢吡啶并[1,2-A]吲哚-1-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮；(S)-3-[8-[(二甲基氨基)甲基]-6,7,8,9-四氢吡啶并[1,2-A]吲哚-10-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮
• 英文名称: (S)-3-(8-(Dimethylaminomethyl)-6,7,8,9-tetrahydropyrido(1,2-a)indol-10-yl)-4-(1-methyl-3-indolyl)-1H-pyrrole-2,5-dione hydrochloride
• 英文别名: 3-[(8S)-8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-methylindol-3-yl)pyrrole-2,5-dione
• CAS: 151342-35-7
• 化学式: C₂₈H₂₈N₄O₂
• 分子量: 452.5
• InChiKey: FXGHOAZJQNLNFD-KRWDZBQOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  34
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  59.3
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS
  申请人：BROWN Dennis M.

  公开号：US20160045502A1

  公开（公告）日：2016-02-18

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to mustard-based alkylating agents such as uracil mustard and analogs, derivatives, or prodrugs thereof, including 6-methyluracil mustard and 6-ethyluracil mustard.

  本发明描述了一种改善先前受到治疗性能不佳限制的治疗剂的治疗效果的方法和组合物，通过改善单药疗法的功效或减少副作用。这种方法和组合物特别适用于芥子碱基烷基化剂，例如尿嘧啶芥和其类似物、衍生物或前药，包括6-甲基尿嘧啶芥和6-乙基尿嘧啶芥。
• Combinations comprising staurosporines
  申请人：Novartis AG

  公开号：EP2305265A1

  公开（公告）日：2011-04-06

  The present invention relates to a method of treating myelodysplastic syndromes, lymphomas and leukemias, and also solid tumors with a pharmaceutical combination of a FLT-3 kinase inhibitor and a histone deacetylase inhibitor (HDAI). It also relates to the use of a pharmaceutical combination of a histone deacetylase inhibitor and a FLT-3 kinase inhibitor for the treatment of the diseases or malignancies mentioned above and the use of such a pharmaceutical composition for the manufacture of a medicament for the treatment of these diseases or malignancies

  本发明涉及一种用FLT-3激酶抑制剂和组蛋白去乙酰化酶抑制剂（HDAI）的药物组合治疗骨髓增生异常综合征、淋巴瘤和白血病以及实体瘤的方法。它还涉及组蛋白去乙酰化酶抑制剂和FLT-3激酶抑制剂的药物组合物治疗上述疾病或恶性肿瘤的用途，以及用这种药物组合物制造治疗这些疾病或恶性肿瘤的药物的用途
• METHOD FOR SUPPRESSING DIFFERENTIATION OF PLURIPOTENT STEM CELLS
  申请人：Kaneka Corporation

  公开号：EP4105319A1

  公开（公告）日：2022-12-21

  Pluripotent stem cells are suspension-cultured with the undifferentiated state thereof maintained. In suspension culture of pluripotent stem cells, the undifferentiated state is maintained by the presence of a PKC inhibitor, especially, a PKCβ inhibitor, and a tankyrase inhibitor (TNKS inhibitor).

  多能干细胞是在保持未分化状态下进行悬浮培养的。在多能干细胞的悬浮培养过程中，PKC 抑制剂（尤其是 PKCβ 抑制剂）和罐酸酶抑制剂（TNKS 抑制剂）的存在可维持多能干细胞的未分化状态。
• Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo
  申请人：Brown Dennis M.

  公开号：US10383847B2

  公开（公告）日：2019-08-20

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutically active agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to therapeutically active agents selected from the group consisting of: (i) indirubin; (ii) an analog of indirubin; (iii) a derivative of indirubin or of an analog of indirubin; and (iv) a pharmaceutical composition comprising indirubin, an analog of indirubin, or a derivative of indirubin or of an analog of indirubin, especially meisoindigo. In particular, the therapeutically active agents selected from the group consisting of: (i) indirubin; (ii) an analog of indirubin; (iii) a derivative of indirubin or of an analog of indirubin; and (iv) a pharmaceutical composition comprising indirubin, an analog of indirubin, or a derivative of indirubin or of an analog of indirubin, especially meisoindigo, are effective Nek9 inhibitors. The active agent, such as meisoindigo, can act as a Nek9 inhibitor. The active agent can be used together with Nek9 inhibitors or agents that inhibit the expression of Nek9.

  本发明描述了通过提高单一疗法的疗效或减少副作用来提高以前受次优治疗性能限制的治疗活性制剂的疗效的方法和组合物。这种方法和组合物特别适用于选自以下组别的治疗活性剂：(i) 靛红素；(ii) 靛红素的类似物；(iii) 靛红素或靛红素类似物的衍生物；(iv) 包含靛红素、靛红素类似物或靛红素或靛红素类似物衍生物的药物组合物，特别是甲异靛。特别是，选自以下组别的治疗活性剂是有效的 Nek9 抑制剂：(i) 靛红素；(ii) 靛红素的类似物；(iii) 靛红素的衍生物或靛红素的类似物；以及 (iv) 由靛红素、靛红素的类似物或靛红素的衍生物或靛红素的类似物，特别是 meisoindigo 组成的药物组合物。活性剂，如 meisoindigo，可作为 Nek9 抑制剂。活性剂可与 Nek9 抑制剂或抑制 Nek9 表达的制剂一起使用。
• Use of dianhydrogalactitol and analogs and derivatives thereof to treat recurrent malignant glioma or progressive secondary brain tumor
  申请人：DelMar Pharmaceuticals, Inc.

  公开号：US11026914B2

  公开（公告）日：2021-06-08

  Methods and compositions suitable for the treatment of malignancies such as recurrent glioma and progressive secondary brain tumor are disclosed. These methods employ a hexitol derivative such as dianhydrogalactitol, a derivative or analog of dianhydrogalactitol, diacetyldianhydrogalactitol, or a derivative or analog of diacetyldianhydrogalactitol. The compositions can include such hexitol derivatives.

  本发明公开了适用于治疗复发性胶质瘤和进行性继发性脑瘤等恶性肿瘤的方法和组合物。这些方法采用己糖醇衍生物，如二氢半乳糖醇、二氢半乳糖醇的衍生物或类似物、二乙酰二氢半乳糖醇或二乙酰二氢半乳糖醇的衍生物或类似物。组合物可以包括此类己糖醇衍生物。