1-Methoxy-3-(4-methylpiperazin-1-yl)propan-2-ol

• 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-Methoxy-3-(4-methylpiperazin-1-yl)propan-2-ol
• 化学式: C₉H₂₀N₂O₂
• 分子量: 188.27
• InChiKey: CTAMULLCRARZHS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  35.9
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [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] SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS<br/>[FR] COMPOSÉS DE PYRAZOLO[1,5-A]PYRAZINE SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS DE LA KINASE RET
  申请人：ANDREWS STEVEN W

  公开号：WO2018136661A1

  公开（公告）日：2018-07-26

  Provided herein are compounds of the 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Formula I的化合物及其立体异构体和药学上可接受的盐或溶剂，其中A、B、D、E、X1、X2、X3和X4在规范中给出的含义，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] SYNTHESIS AND USE OF AMINO LIPIDS<br/>[FR] SYNTHÈSE ET UTILISATION DE LIPIDES AMINÉS
  申请人：INCELLA GMBH

  公开号：WO2016005318A1

  公开（公告）日：2016-01-14

  The present invention provides novel amino lipids and a method for synthesizing these compounds. According to the invention, the amino lipids have a structure of the following formula (I) wherein Z is either hydrogen or -X1 R1, R1 and R2 are the same or different and independently C6-C24 alkyl, C6-C24 alkenyl, C6-C24 alkynyl, or C6-C24 acyl, which can be optionally substituted with a C1-C6 hydrocarbyl group, X1 and X2 are the same or different, either S or S=O or S(=O)2, Y is either (II) or heterocycles of the formula (III) or (IV) wherein k and I are integers from 0 to 2, R3 and R4 are either the same or different and independently C1-C12 alkyl, C1-C12 alkenyl, or C1-C12 alkynyl, wherein alkyl, alkenyl or alkynyl may be optionally substituted with a C1-C6 hydrocarbyl group, or R3 and R4 optionally join to form, together with the nitrogen atom to which they are bound, an optionally substituted N-heterocyclic ring of 3 to 10 atoms comprising 1 to 7 nitrogen atoms, or R3 and R4 are the same or different alkyl amines; R5 and R6 are either absent or is hydrogen or C1-C12 alkyl to provide a quaternary amine, R7 is either hydrogen or C1-C12 alkyl, m is an integer from 1 to 12, n is an integer from 1 to 12, and p is an integer from 1 to 3, wherein preferably Y = N for p = 2 or 3.

  本发明提供了新型氨基脂质和合成这些化合物的方法。根据本发明，氨基脂质具有以下式（I）的结构，其中Z为氢或-X1 R1，R1和R2相同或不同，独立为C6-C24烷基，C6-C24烯基，C6-C24炔基或C6-C24酰基，可选择地取代为C1-C6烃基团，X1和X2相同或不同，为S或S=O或S(=O)2，Y为（II）或式（III）或（IV）的杂环，其中k和l为0至2的整数，R3和R4相同或不同，独立为C1-C12烷基，C1-C12烯基或C1-C12炔基，其中烷基，烯基或炔基可选择地取代为C1-C6烃基团，或R3和R4可选择地结合，与它们所结合的氮原子一起形成，可选择地取代的含有1至7个氮原子的3至10个原子的N-杂环，或R3和R4为相同或不同的烷基胺；R5和R6要么不存在，要么为氢或C1-C12烷基以提供季铵盐，R7要么为氢，要么为C1-C12烷基，m为1至12的整数，n为1至12的整数，p为1至3的整数，其中最好是Y = N，当p = 2或3时。
• [EN] RAPIDLY ACCELERATING FIBROSARCOMA PROTEIN DEGRADING COMPOUNDS AND ASSOCIATED METHODS OF USE<br/>[FR] COMPOSÉS DE DÉGRADATION DE PROTÉINE DE FIBROSARCOME RAPIDEMENT ACCÉLÉRÉ ET LEURS PROCÉDÉS D'UTILISATION
  申请人：ARVINAS OPERATIONS INC

  公开号：WO2022047145A1

  公开（公告）日：2022-03-03

  Bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (Raf, such as c-Raf, A-Raf, and/or B-Raf), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds Raf, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

  本文描述了作为快速加速纤维肉瘤（Raf，如c-Raf、A-Raf和/或B-Raf）调节剂的双功能化合物。具体来说，本公开的异双功能化合物在一端含有结合到cereblon E3泛素连接酶的部分，另一端含有结合Raf的部分，使目标蛋白质靠近泛素连接酶以实现目标蛋白质的降解（和抑制）。本公开的异双功能化合物表现出与目标蛋白质的降解/抑制相关的广泛的药理活性。由于目标蛋白质异常调节导致的疾病或疾病可以通过本公开的化合物和组合物进行治疗或预防。
• Tetrahydrocarbazoles as Active Agents for Inhibiting VEGF Production by Translational Control
  申请人：Lennox William

  公开号：US20090042866A1

  公开（公告）日：2009-02-12

  The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.

  本发明涉及用于抑制血管生成的方法、化合物和组合物。更具体地说，本发明涉及用于抑制VEGF产生的方法、化合物和组合物。