1,7-二氮杂螺[3.5]壬烷 | 25408-26-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 1,7-二氮杂螺[3.5]壬烷
• 英文名称: 1,7-diazaspiro[3.5]nonane
• 英文别名: 1,7-diazaspiro[3.5]nonan
• CAS: 25408-26-8
• 化学式: C₇H₁₄N₂
• mdl: MFCD13180579
• 分子量: 126.202
• InChiKey: NHJZLTUVYSLGRQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  24.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  [1-[(3R,5R)-4-(4-chlorophenyl)sulfonyl-5-(cyclopropylmethyl)morpholin-3-yl]cyclopropyl] carbonochloridate 、 1,7-二氮杂螺[3.5]壬烷 以 二氯甲烷 为溶剂， 生成 1-((3R,5R)-4-(4-chlorophenylsulfonyl)-5-(cyclopropylmethyl)morpholin-3-yl)cyclopropyl1,7-diazaspiro[3.5]nonane-7-carboxylate
  参考文献：
  名称：

  Design, synthesis, and structure–activity relationship studies of N-arylsulfonyl morpholines as γ-secretase inhibitors

  摘要：

  Design and synthesis of cis-2,6-disubstituted N-arylsulfonyl morpholines as novel gamma-secretase inhibitors for the potential treatment of Alzheimer's disease (AD) is reported. Several different small alkyl groups are installed on the left-hand side to lower the CYP3A4 liability while maintaining excellent in vitro potency. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.09.028

文献信息

• IMIDAZO[1',2':1,6]PYRIDO[2,3-D]PYRIMIDINE COMPOUND AS PROTEIN KINASE INHIBITOR
  申请人：SHENGKE PHARMACEUTICALS (JIANGSU) LTD.

  公开号：US20200270251A1

  公开（公告）日：2020-08-27

  Provided is an imidazo[1′;2′:1,6]pyrido[2,3-d]pyrimidine compound of general formula (I). The compound can be used in treating a cell proliferative disorder and is a cyclin-dependent kinase (CDK) inhibitor with broad-spectrum and strong activity.

  提供的是一种通式为(I)的咪唑[1′;2′:1,6]吡啶[2,3-d]嘧啶化合物。该化合物可用于治疗细胞增殖紊乱，是一种具有广谱和强活性的周期蛋白依赖性激酶（CDK）抑制剂。
• Synthesis of biaryl ketones and biaryl diketones via carbonylative Suzuki-Miyaura coupling reactions catalyzed by bridged bis(N-heterocyclic carbene)palladium(II) catalysts
  申请人：King Fahd University of Petroleum & Minerals

  公开号：US11192912B1

  公开（公告）日：2021-12-07

  This disclosure relates to bridged bis(N-heterocyclic carbene)palladium(II) complexes, methods of preparing the complexes, and methods of using the complexes in Suzuki-Miyaura coupling reactions.

  这项披露涉及到桥联的双(N-杂环卡宾)钯(II)配合物，制备这些配合物的方法，以及在Suzuki-Miyaura偶联反应中使用这些配合物的方法。
• [EN] SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1<br/>[FR] PYRIDINES SUBSTITUÉES EN TANT QU'INHIBITEURS DE DNMT1
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2017216726A1

  公开（公告）日：2017-12-21

  The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

  该发明涉及取代吡啶衍生物。具体而言，该发明涉及符合以下式（Iar）的化合物：（Iar）其中Yar、X1ar、X2ar、R1ar、R2ar、R3ar、R4ar和R5ar如本文所定义；或其药学上可接受的盐或前药。该发明的化合物是DNMT1的选择性抑制剂，可用于治疗癌症、癌前综合征、β血红蛋白病、镰状细胞病、镰状细胞贫血、β地中海贫血以及与DNMT1抑制相关的疾病。因此，该发明进一步涉及包含该发明化合物的药物组合物。该发明还进一步涉及使用该发明化合物或包含该发明化合物的药物组合物抑制DNMT1活性和治疗相关疾病的方法。
• [EN] SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS<br/>[FR] COMPOSÉS SUBSTITUÉS DE PYRAZOLO[1,5-A]PYRIDINES COMME INHIBITEURS DE LA KINASE RET
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2017011776A1

  公开（公告）日：2017-01-19

  Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

  本文提供了一般式I的化合物及其立体异构体和药用可接受的盐或溶剂，其中A、B、D、E、X1、X2、X3和X4的含义如规范中所述，这些化合物是RET激酶的抑制剂，可用于治疗和预防可以用RET激酶抑制剂治疗的疾病，包括由RET激酶介导的疾病或紊乱。
• [EN] SHP2 INHIBITORS<br/>[FR] INHIBITEURS DE SHP2
  申请人：IRBM S P A

  公开号：WO2021028362A1

  公开（公告）日：2021-02-18

  The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase, having the general Formula (I).

  本发明涉及一种能够抑制SHP2磷酸酶活性的新化合物，其具有一般式(I)。