3,5-Diethyl-4-propan-2-yl-1,2-oxazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3,5-Diethyl-4-propan-2-yl-1,2-oxazole
• 英文别名: 3,5-diethyl-4-propan-2-yl-1,2-oxazole
• 化学式: C₁₀H₁₇NO
• 分子量: 167.25
• InChiKey: ASEGAJUSUVEFQI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  26
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• AZETIDINE DERIVATIVES AS FXR (NR1H4) MODULATORS
  申请人：Gilead Sciences, Inc.

  公开号：EP3730487A1

  公开（公告）日：2020-10-28

  The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

  本公开一般涉及与 NR1H4 受体 (FXR) 结合并作为 FXR 激动剂的化合物。本公开进一步涉及化合物在制备通过所述化合物结合所述核受体治疗疾病和/或病症的药物中的用途，以及所述化合物的合成工艺。
• 9H-pyrimido [4,5-b]indoles and related analogs as BET bromodomain inhibitors
  申请人：THE REGENTS OF THE UNIVERSITY OF MICHIGAN

  公开号：US10253044B2

  公开（公告）日：2019-04-09

  The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.

  本公开提供了由式 I 表示的取代的 9H-嘧啶并[4,5-b]吲哚和 5H-嘧啶并[4,3-b]吲哚及相关类似物： 及其药学上可接受的盐、水合物和溶液，其中 R1a、A、B1、B2、G、X1、Y1、Y2 和 Y3 如说明书中所定义。本公开还涉及使用式 I 的化合物治疗对抑制 BET 溴链有反应的病症或紊乱。本公开的化合物特别适用于治疗癌症。
• Methods and compositions for inhibition of bromodomain-containing proteins
  申请人：ConverGene LLC

  公开号：US10266536B2

  公开（公告）日：2019-04-23

  The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

  本发明涉及与含溴结构域蛋白质结合或以其他方式调节其活性的化合物、制备这些化合物的工艺、含有这些化合物的药物组合物，以及使用这些化合物治疗各种病症和疾病的方法。
• 9H-pyrimido [4,5-B] indoles as BET bromodomain inhibitors
  申请人：THE REGENTS OF THE UNIVERSITY OF MICHIGAN

  公开号：US10307407B2

  公开（公告）日：2019-06-04

  The present disclosure provides substituted 9H-pyrimido [4,5-b] indoles and 5H-pyrido [4,3-b] indoles and related analogs represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, W, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates.

  本公开提供了由式 I 代表的取代的 9H-嘧啶基[4,5-b]吲哚和 5H-嘧啶基[4,3-b]吲哚及相关类似物及其药学上可接受的盐、水合物和溶剂，其中 R1a、W、B1、B2、G、X1、Y1、Y2 和 Y3 如说明书中所定义。本公开还涉及使用式 I 的化合物治疗对 BET 溴链抑制有反应的病症或紊乱，如癌症。本公开还涉及式 I 化合物作为合成中间体的用途。
• BET bromodomain inhibitors and therapeutic methods using the same
  申请人：THE REGENTS OF THE UNIVERSITY OF MICHIGAN

  公开号：US10391175B2

  公开（公告）日：2019-08-27

  Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.

  本研究公开了 BET 溴基链抑制剂和含有这些抑制剂的组合物。此外，还公开了将 BET 溴基链抑制剂用于治疗 BET 溴基链抑制可带来益处的疾病和病症（如癌症）的方法。