2-(4-(adamantan-1-yl)phenoxy)-1-(piperazin-1-yl)ethanone | 1429054-64-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 2-(4-(adamantan-1-yl)phenoxy)-1-(piperazin-1-yl)ethanone
• 英文别名: 2-(4-(Adamantan-1-yl)phenoxy)-1-(piperazin-1-yl)ethanone；2-[4-(1-adamantyl)phenoxy]-1-piperazin-1-ylethanone
• CAS: 1429054-64-7
• 化学式: C₂₂H₃₀N₂O₂
• 分子量: 354.492
• InChiKey: IFTBVJALBVQCAA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.68
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(4-(adamantan-1-yl)phenoxy)-1-(piperazin-1-yl)ethanone 在 potassium carbonate 、 caesium carbonate 、 三氟乙酸 、 potassium iodide 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 、 丙酮 为溶剂， 反应 39.0h， 生成
  参考文献：
  名称：

  使用炔烃偶联的光亲和探针鉴定HIF-1抑制剂IDF-11774的靶标

  摘要：

  我们开发了一种缺氧诱导因子-1（HIF-1）抑制剂IDF-11774，作为癌症治疗的临床候选药物。为了了解IDF-11774的作用机理，我们尝试使用生物偶联探针分离IDF-11774的靶蛋白。设计并合成了包含点击偶联和光亲和标记位点的多功能化学探针。对蛋白质进行荧光和光亲和性标记后，进行二维电泳（2DE）以分离IDF-11774的特定分子靶标。热激蛋白（HSP）70被鉴定为IDF-11774的目标蛋白。我们发现IDF-11774通过结合其变构口袋而不是其核苷酸结合域（NBD）中的ATP结合位点来抑制HSP70伴侣活性。而且，IDF-11774降低了耗氧率（OCR）和ATP的产生，从而增加了细胞内的氧气张力。该结果表明IDF-11774对HSP70分子伴侣活性的抑制抑制了HIF-1α的重折叠并刺激了HIF-1α的降解。综上所述，这些发现表明，IDF-11774衍生的化学探针成功鉴定了IDF-

  DOI：

  10.1021/acs.bioconjchem.6b00305
• 作为产物：
  描述：

  (4-金刚烷-1-基苯氧基)乙酸 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 、 三氟乙酸 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 生成 2-(4-(adamantan-1-yl)phenoxy)-1-(piperazin-1-yl)ethanone
  参考文献：
  名称：

  使用炔烃偶联的光亲和探针鉴定HIF-1抑制剂IDF-11774的靶标

  摘要：

  我们开发了一种缺氧诱导因子-1（HIF-1）抑制剂IDF-11774，作为癌症治疗的临床候选药物。为了了解IDF-11774的作用机理，我们尝试使用生物偶联探针分离IDF-11774的靶蛋白。设计并合成了包含点击偶联和光亲和标记位点的多功能化学探针。对蛋白质进行荧光和光亲和性标记后，进行二维电泳（2DE）以分离IDF-11774的特定分子靶标。热激蛋白（HSP）70被鉴定为IDF-11774的目标蛋白。我们发现IDF-11774通过结合其变构口袋而不是其核苷酸结合域（NBD）中的ATP结合位点来抑制HSP70伴侣活性。而且，IDF-11774降低了耗氧率（OCR）和ATP的产生，从而增加了细胞内的氧气张力。该结果表明IDF-11774对HSP70分子伴侣活性的抑制抑制了HIF-1α的重折叠并刺激了HIF-1α的降解。综上所述，这些发现表明，IDF-11774衍生的化学探针成功鉴定了IDF-

  DOI：

  10.1021/acs.bioconjchem.6b00305

文献信息

• NOVEL COMPOUNDS AS HIF-1ALPHAINHIBITORS AND MANUFACTURING PROCESS THEREOF
  申请人：KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY

  公开号：US20140228357A1

  公开（公告）日：2014-08-14

  The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

  本发明涉及作为HIF-1α抑制剂的新化合物，其制造工艺以及药物组合物。根据本发明的化合物具有对HIF-1α的抑制活性，可用作治疗预防和/或治疗各种实体癌症，如结肠癌、肝癌、胃癌和乳腺癌。此外，根据本发明的化合物在治疗由HIF-1α介导的VEGFA表达加重的糖尿病视网膜病变和类风湿性关节炎方面具有用处。
• [EN] NOVEL COMPOUNDS AS HIF-1alphaINHIBITORS AND MANUFACTURING PROCESS THEREOF<br/>[FR] NOUVEAUX COMPOSÉS EN TANT QU'INHIBITEURS DU HIF-1Alpha, ET LEUR PROCÉDÉ DE FABRICATION
  申请人：UNIV DONGGUK IND ACAD COOP

  公开号：WO2013048164A1

  公开（公告）日：2013-04-04

  The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

  本发明涉及作为HIF-1α抑制剂的新化合物，其制造工艺以及药物组合物。根据本发明的化合物具有针对HIF-1α的抑制活性，可用作治疗预防和/或治疗各种实体癌症，如结肠癌、肝癌、胃癌和乳腺癌。此外，根据本发明的化合物在治疗由HIF-1α介导的VEGFA表达加重的糖尿病视网膜病变和类风湿性关节炎方面具有用处。
• 진공 및 실린더 통합 제어용 모듈
  申请人：TPC Mechatronics Corp (주) 티피씨 메카트로닉스(119980005717) Corp. No ▼ 110111-0245575BRN ▼109-81-14912

  公开号：KR20180002361U

  公开（公告）日：2018-08-03

  본 고안은 진공 및 실린더 통합 제어용 모듈에 관한 것으로, 보다 상세하게는 진공 제어 및 실린더 구동을 하나의 베이스블럭으로 통합하여 제어하고, 공급포트 또한 외부압력 공급포트, 외부진공 공급포트 2개만으로도 통합 제어가 가능한 진공 및 실린더 통합 제어용 모듈에 관한 것이다. 본 고안에 따른 진공 및 실린더 통합 제어용 모듈은, 일면 상에 진공 제어용 밸브 및 실린더 구동용 밸브가 각각 적어도 하나 이상 결합되는 베이스블록과; 상기 베이스블록의 일측에 구비되어 외부의 압축공기원과 접속되는 단일의 외부압력 공급포트와; 상기 베이스블록의 일측에 구비되어 외부의 진공원과 접속되는 단일의 외부진공 공급포트를; 포함하되, 상기 외부압력 공급포트는 상기 베이스블록의 내부에서 분기되어 상기 진공 제어용 밸브에 진공파괴유로 및 파일럿유로로 연결되고, 상기 실린더 구동용 밸브에 압축공기유로로 연결되며, 상기 외부진공 공급포트는 상기 베이스블록의 내부에서 상기 진공 제어용 밸브에 진공유로로 연결된 것을 특징으로 한다.

  这个概念涉及到用于真空和气缸集成控制的模块，更详细地说，是将真空控制和气缸驱动集成到一个基础模块中进行控制，同时还可以通过仅使用两个外部供应口，即外部压力供应口和外部真空供应口，实现集成控制。根据这个概念，用于真空和气缸集成控制的模块包括：至少一个真空控制阀和至少一个气缸驱动阀各自连接的基础模块；一个连接到外部压缩空气源的单一外部压力供应口位于基础模块的一侧；一个连接到外部真空源的单一外部真空供应口位于基础模块的一侧；其中，外部压力供应口在基础模块内部分支连接到真空控制阀的真空破坏流体和导向流体，并连接到气缸驱动阀的压缩空气流体，而外部真空供应口在基础模块内部连接到真空控制阀的真空流体。
• NOVEL COMPOUNDS AS HIF-1 ALPHA INHIBITORS AND MANUFACTURING PROCESS THEREOF
  申请人：DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION

  公开号：US20160193215A1

  公开（公告）日：2016-07-07

  The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

  本发明涉及一种新型化合物作为HIF-1α抑制剂，其制造过程以及制药组合物。本发明的化合物具有对HIF-1α的抑制活性，可用于治疗和/或预防各种实体癌症，如结肠癌、肝癌、胃癌和乳腺癌。此外，本发明的化合物对于由HIF-1α介导的VEGFA表达加剧的糖尿病视网膜病变和类风湿性关节炎的治疗也很有用。
• Compounds as HIF-1alphainhibitors and manufacturing process thereof
  申请人：DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION

  公开号：US09315507B2

  公开（公告）日：2016-04-19

  The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

  本发明涉及一种新型化合物作为HIF-1α抑制剂，其制备方法和制备的药物组合物。本发明的化合物具有对HIF-1α的抑制活性，可用于治疗预防和/或治疗各种实体肿瘤，如结肠癌、肝癌、胃癌和乳腺癌。此外，本发明的化合物对于由HIF-1α介导的VEGFA表达加重的糖尿病视网膜病变和类风湿性关节炎的治疗也是有用的。