(R)-4,4-difluoro-3-methylpiperidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (R)-4,4-difluoro-3-methylpiperidine
• 英文别名: (3R)-4,4-difluoro-3-methylpiperidine
• 化学式: C₆H₁₁F₂N
• 分子量: 135.157
• InChiKey: ZNUSFHANDPUSAD-RXMQYKEDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (R)-4,4-difluoro-3-methylpiperidine 、 2-(6-(ethylamino)-4-(2-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)pyridin-2-yl)-3-oxo-7-(trifluoromethyl)isoindoline-5-carbaldehyde 在 三乙酰氧基硼氢化钠 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 以4.5 mg的产率得到(R)-6-((4,4-difluoro-3-methylpiperidin-1-yl)methyl)-2-(6-(ethylamino)-4-(2-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)pyridin-2-yl)-4-(trifluoromethyl)isoindolin-1-one
  参考文献：
  名称：

  [EN] CBL-B MODULATORS AND USES THEREOF
  [FR] MODULATEURS DE CBL-B ET LEURS UTILISATIONS

  摘要：

  本发明提供了化合物、其组合物以及使用它们的方法，用于抑制Cbl-b和治疗Cbl-b介导的疾病。

  公开号：

  WO2022217276A1

文献信息

• Substituted benzyl-triazole compounds for Cbl-b inhibition, and further uses thereof
  申请人：Nurix Therapeutics, Inc.

  公开号：US11401267B2

  公开（公告）日：2022-08-02

  Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.

  本发明公开了用于抑制泛素蛋白酶体途径中的 E3 酶 Cbl-b 的化合物、组合物和方法。这些化合物、组合物和方法可用于调节免疫系统，治疗免疫系统可调节的疾病，以及体内、体外或体外细胞的治疗。还公开了包含 Cbl-b 抑制剂和癌症疫苗的药物组合物，以及使用 Cbl-b 抑制剂和癌症疫苗治疗癌症的方法；以及包含 Cbl-b 抑制剂和溶瘤病毒的药物组合物，以及使用 Cbl-b 抑制剂和溶瘤病毒治疗癌症的方法。
• SUBSTITUTED BENZYL-TRIAZOLE COMPOUNDS FOR CBL-B INHIBITION, AND FURTHER USES THEREOF
  申请人：Nurix Therapeutics, Inc.

  公开号：EP3990117A1

  公开（公告）日：2022-05-04
• [EN] 3-SUBSTITUTED PIPERIDINE COMPOUNDS FOR CBL-B INHIBITION, AND USE OF A CBL-B INHIBITOR IN COMBINATION WITH A CANCER VACCINE AND/OR ONCOLYTIC VIRUS<br/>[FR] COMPOSÉS DE PIPÉRIDINE SUBSTITUÉS EN POSITION 3 POUR L'INHIBITION DE CBL-B, ET UTILISATION D'UN INHIBITEUR DE CBL-B EN COMBINAISON AVEC UN VACCIN CONTRE LE CANCER ET/OU UN VIRUS ONCOLYTIQUE
  申请人：NURIX THERAPEUTICS INC

  公开号：WO2020210508A1

  公开（公告）日：2020-10-15

  Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.
• [EN] SUBSTITUTED BENZYL-TRIAZOLE COMPOUNDS FOR CBL-B INHIBITION, AND FURTHER USES THEREOF<br/>[FR] COMPOSÉS BENZYL-TRIAZOLES SUBSTITUÉS POUR L'INHIBITION DE CBL-B ET AUTRES UTILISATIONS DE CES COMPOSÉS
  申请人：NURIX THERAPEUTICS INC

  公开号：WO2020264398A1

  公开（公告）日：2020-12-30

  Compounds of formula (I), compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.