4-Propan-2-yl-1-oxa-4,9-diazaspiro[5.5]undecane

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂螺癸烷衍生物
• 英文名称: 4-Propan-2-yl-1-oxa-4,9-diazaspiro[5.5]undecane
• 英文别名: 4-propan-2-yl-1-oxa-4,9-diazaspiro[5.5]undecane
• 化学式: C₁₁H₂₂N₂O
• 分子量: 198.31
• InChiKey: ZFXQLMTUVSCNFB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  24.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• PYRIDAZINYL THIAZOLECARBOXAMIDE COMPOUND
  申请人：Astellas Pharma Inc.

  公开号：EP4083038A1

  公开（公告）日：2022-11-02

  A compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer having resistance to anti-PD-1 antibody / anti-PD-Ll antibody therapy is provided. The present inventors have conducted studies on a compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer having resistance to anti-PD-1 antibody / anti-PD-Ll antibody therapy, and found that a pyridazinyl-thiazolecarboxamide compound has DGK ξ (DGKzeta) inhibitory effect, leading to completion of the present invention. The pyridazinyl-thiazolecarboxamide compound of the present invention has DGK ξ inhibitory effect, and can be used as a therapeutic agent for treatment of cancer related to activation of immune cells or cancer having resistance to anti-PD-1 antibody / anti-PD-Ll antibody therapy.

  本发明提供了一种可作为药物组合物活性成分的化合物，该药物组合物可用于治疗与免疫细胞活化相关的癌症或对抗癌多肽-1 抗体/抗癌多肽-Ll 抗体治疗具有抗药性的癌症。 本发明人对一种可作为药物组合物活性成分的化合物进行了研究，该药物组合物可用于治疗与免疫细胞活化相关的癌症或对抗朴-PD-1抗体/抗朴-PD-Ll抗体治疗具有抗药性的癌症，并发现一种哒嗪基噻唑甲酰胺化合物具有DGKξ（DGKzeta）抑制作用，从而完成了本发明。本发明的哒嗪基噻唑甲酰胺化合物具有DGKξ抑制作用，可作为治疗剂用于治疗与免疫细胞活化相关的癌症或抗PD-1抗体/抗PD-Ll抗体治疗耐药的癌症。
• GCN2 inhibitors and uses thereof
  申请人：Merck Patent GmbH

  公开号：US10988477B2

  公开（公告）日：2021-04-27

  The present invention provides compounds inhibiting General amino acid Control Non-derepressible 2 kinase (“GCN2”), compositions thereof, and methods of using the same for treating various disorders, such as cancer.

  本发明提供了抑制通用氨基酸控制非去势 2 激酶（"GCN2"）的化合物、其组合物及其用于治疗各种疾病（如癌症）的方法。
• GCN2 INHIBITORS AND USES THEREOF
  申请人：Merck Patent GmbH

  公开号：US20190233425A1

  公开（公告）日：2019-08-01

  The present invention provides compounds, compositions thereof, and methods of using the same.
• TRIAZOLOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF
  申请人：Genentech, Inc.

  公开号：US20190233441A1

  公开（公告）日：2019-08-01

  Compounds of Formula 0, Formula I and Formula II and methods of use as Janus kinase inhibitors are described herein.
• BIFUNCTIONAL DEGRADERS AND THEIR METHODS OF USE
  申请人：NOVARTIS AG

  公开号：US20220387602A1

  公开（公告）日：2022-12-08

  Described herein are bifunctional degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of conditions, diseases, and disorders mediated by various target proteins.