1,4-Diisopropyl-2-hydroxymethyl-piperazin | 91336-78-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1,4-Diisopropyl-2-hydroxymethyl-piperazin
• 英文别名: (1,4-diisopropyl-piperazin-2-yl)-methanol；[1,4-Di(propan-2-yl)piperazin-2-yl]methanol
• CAS: 91336-78-6
• 化学式: C₁₁H₂₄N₂O
• 分子量: 200.324
• InChiKey: WJGBCXNHBWTXGK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  26.7
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• KRAS G12C INHIBITORS AND METHODS OF USING THE SAME
  申请人：AMGEN INC.

  公开号：US20180177767A1

  公开（公告）日：2018-06-28

  Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

  本文提供了KRAS G12C抑制剂，其组成，以及使用方法。这些抑制剂对治疗多种疾病有用，包括胰腺癌、结直肠癌和肺癌。
• [EN] (R) -GLUTARIMIDE CRBN LIGANDS AND METHODS OF USE<br/>[FR] LIGANDS DE (R)-GLUTARIMIDE CRBN ET PROCÉDÉS D'UTILISATION
  申请人：BEIGENE LTD

  公开号：WO2022268052A1

  公开（公告）日：2022-12-29

  Disclosed herein are compounds for binding and modulating the activity of cereblon (CRBN), and methods of use. The present invention also provides compounds that can be used as synthetic intermediates in the preparation of bifunctional compounds for use in targeted protein degradation. The present compounds are thus useful for the treatment or prophylaxis tumors and cancer.

  本文披露了用于结合和调节小脑素（CRBN）活性的化合物，以及使用方法。本发明还提供了可用作合成双功能化合物的中间体的化合物，用于靶向蛋白质降解。因此，本化合物对于治疗或预防肿瘤和癌症是有用的。
• BENZOISOTHIAZOLE, ISOTHIAZOLO[3,4-B]PYRIDINE, QUINAZOLINE, PHTHALAZINE, PYRIDO[2,3-D]PYRIDAZINE AND PYRIDO[2,3-D]PYRIMIDINE DERIVATIVES AS KRAS G12C INHIBITORS FOR TREATING LUNG, PANCREATIC OR COLORECTAL CANCER
  申请人：Amgen Inc.

  公开号：EP4001269A1

  公开（公告）日：2022-05-25

  Provided herein are compounds of formulae (I), (II), (III), (III´), (IV), (IV´) and (V): as KRAS G12C inhibitors for use in treating cancer, such as e.g. pancreatic, colorectal and lung cancer. Preferred compounds are e.g. benzoisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives. An exemplary compound is e.g. 1-(4-(6-(2-bromo-5-hydroxyphenyl)-5-chloro-7-fluorobenzo[c]isothiazol-3-yl)piperazin-1-yl)prop-2-en-1-one (example 1-1):

  这里提供的是式 (I)、(II)、(III)、(III´)、(IV)、(IV´) 和 (V) 的化合物： 作为 KRAS G12C 抑制剂用于治疗癌症，如胰腺癌、结直肠癌和肺癌。 首选化合物为苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物等。 例如，1-(4-(6-(2-溴-5-羟基苯基)-5-氯-7-氟苯并[c]异噻唑-3-基)哌嗪-1-基)丙-2-烯-1-酮（例 1-1）就是一种示例性化合物：
• KRAS G12C inhibitors and methods of using the same
  申请人：Amgen Inc.

  公开号：US10519146B2

  公开（公告）日：2019-12-31

  Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

  本文提供了 KRAS G12C 抑制剂、其组合物以及使用方法。这些抑制剂可用于治疗多种疾病，包括胰腺癌、结直肠癌和肺癌。
• BENZISOTHIAZOLE, ISOTHIAZOLO[3,4-B]PYRIDINE, QUINAZOLINE, PHTHALAZINE, PYRIDO[2,3-D]PYRIDAZINE AND PYRIDO[2,3-D]PYRIMIDINE DERIVATIVES AS KRAS G12C INHIBITORS FOR TREATING LUNG, PANCREATIC OR COLORECTAL CANCER
  申请人：Amgen Inc.

  公开号：EP3558955B1

  公开（公告）日：2021-08-11