3-fluoro-5-propan-2-yl-1H-pyrazole

• 分子结构分类: 有机化合物 - 有机卤素化合物 - 芳基卤化物
• 英文名称: 3-fluoro-5-propan-2-yl-1H-pyrazole
• 化学式: C₆H₉FN₂
• 分子量: 128.15
• InChiKey: IXEFNQZQECPQAW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  28.7
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] MAP4K4 INHIBITORS<br/>[FR] INHIBITEURS DE MAP4K4
  申请人：IMPERIAL INNOVATIONS LTD

  公开号：WO2019073253A1

  公开（公告）日：2019-04-18

  This invention relates to pyrrolopyrimidine comprising compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these pyrrolopyrimidine comprising compounds, for example in a method of treatment. There are also provided processes for producing compounds of the present invention and method of their use. In particular, the present invention relates to compounds of formula (I).

  这项发明涉及含有吡咯吡嘧啶的化合物，这些化合物可能作为丝裂原活化蛋白激酶激酶激酶激酶-4（MAP4K4）的抑制剂而有用。该发明还涉及利用这些含有吡咯吡嘧啶的化合物，例如在治疗方法中的使用。还提供了生产本发明化合物的方法以及它们的使用方法。具体而言，本发明涉及式（I）的化合物。
• [EN] DNA-PK INHIBITING COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS DE L'ADN-PK
  申请人：PROVINCIAL HEALTH SERVICES AUTHORITY

  公开号：WO2021050059A1

  公开（公告）日：2021-03-18

  The present disclosure relates to DNA-PK inhibiting compounds and prodrugs thereof that are useful in the treatment of diseases, including cancer. In particular, the compounds sensitise cancers to therapies such as chemotherapy and radiotherapy.

  本公开涉及DNA-PK抑制化合物及其前药，它们可用于治疗包括癌症在内的疾病。特别是，这些化合物能够增强癌症对化疗和放疗等疗法的敏感性。
• [EN] LYSYL OXIDASE INHIBITORS<br/>[FR] INHIBITEURS DE LA LYSYLE OXYDASE
  申请人：THE INSTITUTE OF CANCER RES ROYAL CANCER HOSPITAL

  公开号：WO2019073251A1

  公开（公告）日：2019-04-18

  This invention relates to compounds useful as lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family member (LOXL1, LOXL2, LOXL3, LOXL4) inhibitors. In addition there are contemplated pharmaceutical compositions comprising the compounds and the use of the compounds in the treatment of conditions mediated by LOX and LOXL, for example cancer. In particular a LOX inhibitor such as the present compounds may be for use in the treatment of a cancer associated with EGFR. The present invention also contemplates the identification of biomarkers that predict responsiveness to a LOX inhibitor.

  这项发明涉及作为赖氨酸氧化酶（LOX）和赖氨酸氧化酶类（LOXL）家族成员（LOXL1、LOXL2、LOXL3、LOXL4）抑制剂有用的化合物。此外，还考虑了包括这些化合物的药物组合物以及利用这些化合物治疗由LOX和LOXL介导的疾病，例如癌症。特别是像目前的这些化合物这样的LOX抑制剂可能用于治疗与EGFR相关的癌症。本发明还考虑了预测对LOX抑制剂响应性的生物标志物的鉴定。
• [EN] FACTOR XIIA INHIBITORS<br/>[FR] INHIBITEURS DU FACTEUR XIIA
  申请人：UNIV LEEDS INNOVATIONS LTD

  公开号：WO2019186164A1

  公开（公告）日：2019-10-03

  This invention relates to compoundsof formula (I)and methods of treatment using the compounds. The invention also relates to processes and methods for producing the compounds of the invention. The compounds of the invention are modulators of Factor XII (e.g. Factor XIIa). In particular, the compounds are inhibitors of Factor XIIa and may be useful as anticoagulants.

  本发明涉及公式(I)的化合物以及使用这些化合物进行治疗的方法。该发明还涉及用于生产该发明化合物的过程和方法。该发明化合物是凝血因子XII（例如凝血因子XIIa）的调节剂。具体来说，这些化合物是凝血因子XIIa的抑制剂，可能作为抗凝血剂有用。
• [EN] BETA-AMINO-ALPHA-HYDROXYALKYLPHENYL DERIVATIVES AND THEIR USE FOR CANCER TREATMENT<br/>[FR] DÉRIVÉS DE BÊTA-AMINO-ALPHA-HYDROXYALKYLPHÉNYLE ET LEUR UTILISATION POUR LE TRAITEMENT DU CANCER
  申请人：RISING TIDE FOUND

  公开号：WO2019234228A1

  公开（公告）日：2019-12-12

  This invention relates to compounds that disrupt cell function, such as the disruption of cell metabolism in particular cancer cell metabolism, that are useful as cancer therapies. The compounds comprise (β-amino-α-hydroxyalkyl)phenyl derivatives having a phosphonium cation tethered to the (β-amino-α-hydroxyalkyl)phenyl amine.

  这项发明涉及破坏细胞功能的化合物，例如特定癌细胞代谢的干扰，这些化合物可用作癌症治疗。这些化合物包括将磷酸铵阳离子系在(β-氨基-α-羟基烷基)苯胺上的(β-氨基-α-羟基烷基)苯衍生物。