(5S)-8-[3-cyanobenzoyl]-3-[(1R)-1-phenylethyl]-1-oxa-3,8-diazaspiro[4.6]undecan-2-one | 1229520-25-5

• 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: (5S)-8-[3-cyanobenzoyl]-3-[(1R)-1-phenylethyl]-1-oxa-3,8-diazaspiro[4.6]undecan-2-one
• 英文别名: 3-[(5S)-2-oxo-3-[(1R)-1-phenylethyl]-1-oxa-3,9-diazaspiro[4.6]undecane-9-carbonyl]benzonitrile
• CAS: 1229520-25-5
• 化学式: C₂₄H₂₅N₃O₃
• 分子量: 403.481
• InChiKey: IJLAKLCXGHCORN-KOSHJBKYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  73.6
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] SPIRO AZEPANE-OXAZOLIDINONES AS Kv1.3 POTASSIUM CHANNEL BLOCKERS<br/>[FR] SPIRO-AZÉPANE-OXAZOLIDINONES AU TITRE D'AGENTS BLOQUANTS DU CANAL POTASSIQUE KV1.3
  申请人：SOLVAY PHARM BV

  公开号：WO2010066840A1

  公开（公告）日：2010-06-17

  This invention concerns spiro azepane-oxazolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein the symbols have the meanings given in the specification.

  这项发明涉及螺环氮杂环己烷-噁唑烷酮作为电压门控Kv1.3钾通道阻滞剂，含有这些化合物的药物组合物，制备这些化合物的方法，制备用于它们的合成的新型中间体的方法，以及制备组合物的方法。该发明还涉及这些化合物和组合物的用途，特别是它们在向患者施用以在治疗糖尿病、牛皮癣、肥胖、移植排斥和炎症性神经病，包括T细胞介导的自身免疫疾病，如类风湿性关节炎和多发性硬化症中实现治疗效果的用途。这些化合物的化学式为(1)：其中符号的含义如规范中所述。
• SPIRO AZEPANE-OXAZOLIDINONES AS Kv1.3 POTASSIUM CHANNEL BLOCKERS
  申请人：Smid Pieter

  公开号：US20110237569A1

  公开（公告）日：2011-09-29

  This invention concerns Spiro azepane-ox-azolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein R 1 , R 2 , (R 3 ) n , and (R 4 ) m have the meanings given in the specification.

  本发明涉及螺环氧氮杂环己烷酮作为电压门控Kv1.3钾通道阻滞剂，包含这些化合物的制药组合物，制备这些化合物的方法，制备有用于它们的合成的新型中间体的方法，以及制备组合物的方法。本发明还涉及这些化合物和组合物的用途，特别是它们在向患者施用以在治疗糖尿病、银屑病、肥胖症、移植排斥和炎症性神经病变，包括T细胞介导的自身免疫疾病，如类风湿性关节炎和多发性硬化症中实现治疗效果的用途。这些化合物的化学式为(1)：其中R1、R2、(R3)n和(R4)m的含义如规范中所给出。
• US8575148B2
  申请人：——

  公开号：US8575148B2

  公开（公告）日：2013-11-05