SZL-P1-41

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: SZL-P1-41
• 英文别名: Skp2-C25；3-(benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one；3-(1,3-benzothiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)chromen-4-one
• 化学式: C₂₄H₂₄N₂O₃S
• mdl: MFCD00711481
• 分子量: 420.532
• InChiKey: JKIXLEKBXHMXTN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  90.9
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-(2,4-dihydroxy-5-ethylphenacyl)benzothiazole 在 哌啶 作用下， 以 1,4-二氧六环 、 吡啶 为溶剂， 反应 7.0h， 生成 SZL-P1-41
  参考文献：
  名称：

  Chemistry of the hetero analogs of isoflavones. 22. Mannich reaction in the benzimidazole and benzothiazole analogs of isoflavones

  摘要：

  DOI：

  10.1007/bf02311328

文献信息

• [EN] ANTI-CANCER COMPOUNDS<br/>[FR] COMPOSÉS ANTI-CANCEREUX
  申请人：UNIV TEXAS

  公开号：WO2015010032A1

  公开（公告）日：2015-01-22

  Provided are methods and compositions for the treatment of diseases such as cancer. In certain aspects, compounds which can inhibit Skp2 are provided. Specifically chromenone derivatives are disclosed that have the capability toward reducing differentiation of pluripotent, multipotent or totipotent cells and thus have therapeutic utility in the treatment of a proliferative disease such as cancer.

  提供了治疗癌症等疾病的方法和组合物。在某些方面，提供了可以抑制Skp2的化合物。具体地，披碱酮衍生物被揭示具有减少多能、多潜能或全能细胞分化的能力，因此在治疗癌症等增生性疾病中具有治疗效用。
• METHOD FOR DETERMINING PARP INHIBITOR RESPONSIVENESS AND IMPROVING PARP INHIBITOR THERAPY
  申请人：Universität Zürich

  公开号：EP3822637A1

  公开（公告）日：2021-05-19

  The invention relates to a method for determining the responsiveness of a patient's tumour disease to treatment by administration of a PARP inhibitor. The method comprising the steps of determining a level of TRIP12 protein and/or a level of an mRNA encoding TRIP12 protein, or the presence of a TRIP12 mutation, and comparing the TRIP12 expression level and/or the TRIP12 activity level with a threshold value, and assigning to said tumour disease a likelihood of responsiveness. The invention further relates to a PARP inhibitor for use in treatment of a tumour disease associated with a level of TRIP12 expression lower than a threshold, or to a PARP inhibitor for use in treatment of a tumour disease administered concomitant with or after administration of an ubiquitin ligase inhibitor and/or a nucleic acid agent capable of decreasing or inhibiting or blocking TRIP12 expression.

  本发明涉及一种确定患者肿瘤疾病对给予 PARP 抑制剂治疗的反应性的方法。该方法包括以下步骤：确定TRIP12蛋白的水平和/或编码TRIP12蛋白的mRNA的水平，或TRIP12突变的存在，以及将TRIP12表达水平和/或TRIP12活性水平与阈值进行比较，并给所述肿瘤疾病分配反应性的可能性。 本发明进一步涉及一种用于治疗与TRIP12表达水平低于阈值相关的肿瘤疾病的PARP抑制剂，或涉及一种用于治疗肿瘤疾病的PARP抑制剂，该PARP抑制剂与泛素连接酶抑制剂和/或能够降低或抑制或阻断TRIP12表达的核酸制剂同时给药或在给药后给药。
• Modulators of toll-like receptors for the treatment of HIV
  申请人：Gilead Sciences, Inc.

  公开号：US11116774B2

  公开（公告）日：2021-09-14

  Provided are methods, uses, pharmaceutical regimens, pharmaceutical compositions, and kits comprising modulators of TLR7, including those of Formula II: and pharmaceutically acceptable salts thereof, useful in treating HIV infections.

  本发明提供以下方法、用途、药物方案、药物组合物和试剂盒，其中包含TLR7的调节剂，包括公式II中的化合物及其药学上可接受的盐，所述化合物在治疗HIV感染中有用。
• MODULATORS OF TOLL-LIKE RECEPTORS FOR THE TREATMENT OF HIV
  申请人：Gilead Sciences, Inc.

  公开号：US20160008374A1

  公开（公告）日：2016-01-14

  Provided are methods, uses, pharmaceutical regimens, pharmaceutical compositions, and kits comprising modulators of TLR7, including those of Formula II: and pharmaceutically acceptable salts thereof, useful in treating HIV infections.
• ANTI-CANCER COMPOUNDS
  申请人：BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

  公开号：US20160145250A1

  公开（公告）日：2016-05-26

  Provided are methods and compositions for the treatment of diseases such as cancer. In certain aspects, compounds which can inhibit Skp2 are provided. Specifically chromenone derivatives are disclosed that have the capability toward reducing differentiation of pluripotent, multipotent or totipotent cells and thus have therapeutic utility in the treatment of a proliferative disease such as cancer.