2-Dimethylaminomethyl-4-methyl-pent-1-en-3-one | 63707-93-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-Dimethylaminomethyl-4-methyl-pent-1-en-3-one
• 英文别名: 2-[(Dimethylamino)methyl]-4-methylpent-1-en-3-one
• CAS: 63707-93-7
• 化学式: C₉H₁₇NO
• 分子量: 155.24
• InChiKey: ANPJVKNZIQYETQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  11
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] PYRAZOLO AND TRIAZOLO BICYCLIC COMPOUNDS AS JAK KINASE INHIBITORS<br/>[FR] COMPOSÉS BICYCLIQUES PYRAZOLO ET TRIAZOLO UTILISÉS EN TANT QU'INHIBITEURS DE KINASE JAK
  申请人：THERAVANCE BIOPHARMA R&D IP LLC

  公开号：WO2019027960A1

  公开（公告）日：2019-02-07

  The invention provides compounds of formula (I) or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.

  这项发明提供了式（I）的化合物或其药用可接受的盐，其中变量在规范中定义，这些化合物是JAK激酶的抑制剂，特别是JAK3。该发明还提供了结晶形式，包含这些化合物的药物组合物，使用这些化合物治疗胃肠道和其他炎症性疾病的方法，以及用于制备这些化合物的工艺和中间体。
• 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。
• 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：
• Pyrazolo and triazolo bicyclic compounds as JAK kinase inhibitors
  申请人：THERAVANCE BIOPHARMA R&D IP, LLC

  公开号：US10392368B2

  公开（公告）日：2019-08-27

  The invention provides compounds of formula (I): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.

  本发明提供了式 (I) 的化合物： 或其药学上可接受的盐，其中变量在说明书中定义，是 JAK 激酶，特别是 JAK3 的抑制剂。本发明还提供了结晶形式、包含此类化合物的药物组合物、使用此类化合物治疗胃肠道疾病和其他炎症性疾病的方法，以及制备此类化合物的有用工艺和中间体。
• KRAS G12C inhibitors and methods of using the same
  申请人：AMGEN INC.

  公开号：US11285135B2

  公开（公告）日：2022-03-29

  Provided herein are methods of treating cancer with KRAS G12C inhibitors of Formula I and compositions of the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

  本文提供了用式 I 的 KRAS G12C 抑制剂及其组合物治疗癌症的方法。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。