(R)-3-(叔丁基)吗啉 | 1286768-66-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 中文名称: (R)-3-(叔丁基)吗啉
• 英文名称: (R)-3-(tert-butyl)morpholine
• 英文别名: (3R)-3-tert-butylmorpholine
• CAS: 1286768-66-8
• 化学式: C₈H₁₇NO
• 分子量: 143.23
• InChiKey: YGBCOMFKPPSDAN-ZETCQYMHSA-N

物化性质

• 沸点：
  189.0±15.0 °C(Predicted)
• 密度：
  0.896±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Pro-drugs of riluzole and their method of use for the treatment of amyotrophic lateral sclerosis
  申请人：Biohaven Pharmaceutical Holding Company Limited

  公开号：US10357497B2

  公开（公告）日：2019-07-23

  Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.

  本发明的药物组合物包括通过释放利鲁唑治疗肌萎缩性脊髓侧索硬化症（ALS）和相关疾病的取代利鲁唑原药，特别是避免了由Cyp 1A2促进的肝脏代谢中患者与患者之间的首过差异。利鲁唑原药对肝脏代谢的稳定性增强，通过口服进入全身循环，然后通过酶或一般生物物理释放过程裂解，在血浆中释放利鲁唑。本发明还包括可用于治疗疾病的利鲁唑原药，这些疾病可以通过利鲁唑原药释放利鲁唑来治疗。
• Prodrugs of riluzole and their method of use
  申请人：Biohaven Pharmaceutical Holding Company Ltd.

  公开号：US10844026B2

  公开（公告）日：2020-11-24

  Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

  本发明的药物组合物包括取代的利鲁唑原药，可通过释放利鲁唑治疗癌症，包括黑色素瘤、乳腺癌、脑癌和前列腺癌。利鲁唑原药对肝脏代谢的稳定性增强，通过口服进入全身循环，然后通过酶或一般生物物理释放过程裂解，在血浆中释放利鲁唑。
• Macrocyclic compounds for treatment of medical disorders
  申请人：Achillion Pharmaceuticals, Inc.

  公开号：US11053253B2

  公开（公告）日：2021-07-06

  Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

  本发明提供了大环补体因子 D 抑制剂、药物组合物及其用途以及制造工艺。所提供的化合物包括式I、式II、式III、式IV、式V、式VI、式VII和式VIII或其药学上可接受的盐、原药、同位素类似物、N-氧化物或分离异构体，可选药学上可接受的组合物。本文所述的抑制剂以因子 D 为靶点，抑制或调节补体级联。
• Degraders and Degrons for targeted protein degradation
  申请人：C4 Therapeutics, Inc.

  公开号：US11524949B2

  公开（公告）日：2022-12-13

  Pharmaceutical Degraders and Degrons for use in therapeutic applications are described herein.

  本文介绍了用于治疗的药物降解剂和降解器。
• 3-SUBSTITUTED 1,3,4-OXADIAZOLE AND THIADIAZOLE COMPOUNDS AS IMMUNOMODULATORS
  申请人：AURIGENE DISCOVERY TECHNOLOGIES LIMITED

  公开号：US20180044305A1

  公开（公告）日：2018-02-15

  The present invention relates to 3-substituted 1,3,4-oxadiazole and thiadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.