8,8-difluoro-1,3-diazaspiro[4.5]decane-2,4-dione | 1393823-97-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: 8,8-difluoro-1,3-diazaspiro[4.5]decane-2,4-dione
• CAS: 1393823-97-6
• 化学式: C₈H₁₀F₂N₂O₂
• 分子量: 204.176
• InChiKey: GQPPHCKZCKRZOI-UHFFFAOYSA-N

物化性质

• 密度：
  1.41±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  8,8-difluoro-1,3-diazaspiro[4.5]decane-2,4-dione 在 水 、 potassium hydroxide 作用下， 以4.3 g的产率得到1-氨基-4,4-二氟环己基羧酸
  参考文献：
  名称：

  SUBSTITUTED 3-(BIPHENYL-3-YL)-8,8-DIFLUORO-4-HYDROXY-1-AZASPIRO[4.5]DEC-3-EN-2-ONES FOR THERAPY

  摘要：

  该发明涉及用于治疗目的的取代3-(联苯基-3-基)-8,8-二氟-4-羟基-1-氮杂螺[4.5]癸-3-烯-2-酮（Ia）的化合物，以及药物组合物和它们在治疗中的使用，特别是用于预防和治疗肿瘤疾病。该发明还涉及新化合物（I）的化合物，其中W、X、Y、Z、A、B、D和G具有上述给定的含义，以及用于它们的制备的多种过程和中间体，以及它们作为杀虫剂和/或除草剂和/或杀菌剂的用途。该发明还涉及选择性除草剂组合物，首先包括卤素取代的螺环酮醇，其次包括一种提高作物植物兼容性的化合物。本发明还涉及通过向作物保护组合物中添加铵盐或磷铵盐以及可选的渗透剂，从而提高作物保护组合物的作用，特别是卤素取代的螺环酮醇，以及它们的生产过程和在作物保护中作为杀虫剂和/或杀菌剂和/或用于预防不受欢迎的植物生长的应用。

  公开号：

  US20140011853A1
• 作为产物：
  描述：

  8,8-二氟-1,4-二噁螺[4.5]癸烷 在 盐酸 、 potassium cyanide 作用下， 以 水 为溶剂， 反应 3.0h， 生成 8,8-difluoro-1,3-diazaspiro[4.5]decane-2,4-dione
  参考文献：
  名称：

  1-氨基-4,4-二氟环己烷羧酸作为药物发现的有前途的组成部分：设计，合成和表征

  摘要：

  1-氨基-4,4-二氟环己烷羧酸已被设计为药理学上相关的1-氨基环己烷羧酸的氟化类似物。由市售材料分三步进行合成，总产率为22％。已经研究了氟原子对氨基酸的构象，亲脂性，酸性和荧光性质的影响。建议了所得化合物的各种实际应用。

  DOI：

  10.1016/j.tet.2013.03.072

文献信息

• [EN] AZASPIRO DERIVATIVES AS TRPM8 ANTAGONISTS<br/>[FR] DÉRIVÉS AZASPIRO EN TANT QU'ANTAGONISTES DE TRPM8
  申请人：RAQUALIA PHARMA INC

  公开号：WO2015136947A1

  公开（公告）日：2015-09-17

  The present invention relates to azaspiro derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.

  本发明涉及式(I)的氮杂环螺环衍生物或其药用可接受盐或前药，其制备方法，含有它们的药物组合物以及它们在治疗通过TRPM8受体介导的各种疾病中的应用。
• SUBSTITUTED 3-(BIPHENYL-3-YL)-8,8-DIFLUORO-4-HYDROXY-1-AZASPIRO[4.5]DEC-3-EN-2-ONES FOR THERAPY AND HALOGEN-SUBSTITUTED SPIROCYCLIC KETOENOLS
  申请人：Bretschneider Thomas

  公开号：US20140045696A1

  公开（公告）日：2014-02-13

  The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selective herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, halogen-substituted spirocyclic ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as pesticides and/or fungicides and/or for preventing unwanted plant growth. The invention also relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones of the formula (Ia) for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumor disorders.

  本发明涉及公式（I）的新化合物，其中W，X，Y，Z，A，B，D和G具有上述给定的含义，以及其制备的多种过程和中间体，以及它们作为杀虫剂和/或除草剂和/或杀菌剂的用途。本发明还涉及选择性除草剂组合物，其包括第一，卤代螺环酮烯醇，第二，作物植物相容性改良化合物。本发明还涉及通过向相应的组合物添加铵盐或膦盐和可选的渗透剂，从而提高特别是卤代螺环酮烯醇的作物保护组合物的作用的方法，以及生产它们的过程和它们在作物保护中作为杀虫剂和/或杀菌剂和/或防止不良植物生长的应用。本发明还涉及公式（Ia）的取代3-（联苯基-3-基）-8,8-二氟-4-羟基-1-氮杂螺[4.5]癸-3-烯-2-酮，用于治疗目的，以及制药组合物和它们在治疗中的用途，特别是用于肿瘤疾病的预防和治疗。
• Substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones for therapy and halogen-substituted spirocyclic ketoenols
  申请人：Bretschneider Thomas

  公开号：US08946124B2

  公开（公告）日：2015-02-03

  The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selective herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, halogen-substituted spirocyclic ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as pesticides and/or fungicides and/or for preventing unwanted plant growth. The invention also relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones of the formula (Ia) for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumor disorders.

  该发明涉及式(I)的新化合物，其中W、X、Y、Z、A、B、D和G具有上述给定的含义，以及它们的制备的多种过程和中间体，以及它们作为杀虫剂和/或除草剂和/或杀菌剂的用途。该发明还涉及选择性除草剂组合物，包括第一，卤代螺环酮烯醇，第二，改善作物植株相容性的化合物。本发明还涉及通过向相应的组合物添加铵盐或磷酸盐和可选的渗透剂，增强以卤代螺环酮烯醇为特征的作物保护组合物的作用的方法，以及生产它们的过程和它们在作物保护中作为杀虫剂和/或杀菌剂和/或预防不良植物生长的用途。该发明还涉及式(Ia)的取代3-(联苯基-3-基)-8,8-二氟-4-羟基-1-氮杂螺[4.5]癸-3-烯-2-酮，用于治疗目的，以及药物组合物和它们在治疗中的用途，特别是用于预防和治疗肿瘤疾病。
• Substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones for therapy
  申请人：Liu Ningshu

  公开号：US09000026B2

  公开（公告）日：2015-04-07

  The invention relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones of the formula (Ia) for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumor disorders. The invention also relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selectively herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, halogen-substituted spirocyclic ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as pesticides and/or fungicides and/or for preventing unwanted plant growth.

  该发明涉及用于治疗目的的取代3-(联苯基-3-基)-8,8-二氟-4-羟基-1-氮杂螺[4.5]癸-3-烯-2-酮(Ia式)、药物组合物及其在治疗中的使用，特别是用于预防和治疗肿瘤疾病。该发明还涉及公式(I)中的新化合物，其中W、X、Y、Z、A、B、D和G具有上述所述的含义，以及其制备的多种过程和中间体，以及它们作为杀虫剂和/或除草剂和/或杀菌剂的用途。该发明还涉及选择性除草剂组合物，包括第一，卤代螺环酮醇，第二，提高作物植物相容性的化合物。本发明还涉及通过向相应组合物添加铵盐或膦盐和可选的渗透剂来提高作物保护组合物的作用，特别是卤代螺环酮醇的作用，以及生产它们的过程及其在作物保护中作为杀虫剂和/或杀菌剂和/或防止植物不良生长的用途。
• Azaspiro derivatives as TRPM8 antagonists
  申请人：RaQualia Pharma Inc.

  公开号：US10093678B2

  公开（公告）日：2018-10-09

  The present invention relates to azaspiro derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.

  本发明涉及式（I）的氮杂螺衍生物或其药学上可接受的盐或其原药、其制备工艺、含有它们的药物组合物以及它们在治疗通过 TRPM8 受体介导的各种疾病中的用途。