4-[5-(1,5-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-7-yl)-1H-pyrrol-2-yl]benzoic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: 4-[5-(1,5-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-7-yl)-1H-pyrrol-2-yl]benzoic acid
• 化学式: C₂₃H₂₄N₂O₂
• 分子量: 360.4
• InChiKey: WMQGHSGUSBZNAN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  27
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  56.3
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• RETINOIC ACID AGONISTS AS PREVENTIVE AND THERAPEUTIC AGENTS FOR NEPHRITIS
  申请人：Eisai Co., Ltd.

  公开号：EP1025857A1

  公开（公告）日：2000-08-09

  Therapeutic or preventive agents for system lupus erythematosus, glomerulonephritis, lupus nephritis, idiopathic thrombocytopenic purpura or autoimmune anemia, which can be substituted for conventional steroid preparations or immunosuppressive agents. The active ingredients of the therapeutic or preventive agents are agonists for retinoic acid receptors, particularly retinoic receptor, subtype α (i.e., RAR α), and examples of the agonists include (1) carboxylic acid derivatives bearing fused rings as represented by general formula (I) wherein rings L and M are fused with each other, and are each independently an optionally substituted aromatic hydrocarbon ring or an optimally substituted heterocycle; rings A and B are each independently an optionally substituted aromatic hydrocarbon ring or a heterocycle; and D is optionally protected carboxyl, and (2) 4-[(3,5-bistrimethylsilylphenyl)carbonyl]amino}benzoic acid and 42-[5-(3-methoxymethyl-5,6,7,8-tetrahydro-5,5,8,8,-tetramethylnaphthalen-2-yl)-pyrrolyl]}benzoic acid.

  治疗或预防系统性红斑狼疮、肾小球肾炎、狼疮性肾炎、特发性血小板减少性紫癜或自身免疫性贫血的药物，可替代传统的类固醇制剂或免疫抑制剂。治疗剂或预防剂的有效成分是视黄酸受体激动剂，特别是视黄酸受体α亚型（即 RAR α、RAR β 和 RAR β 例子）、RAR α）的激动剂，激动剂的例子包括 (1) 如通式（I）所示的带有融合环的羧酸衍生物，其中环 L 和 M 相互融合，且各自独立地为任选取代的芳香烃环或最佳取代的杂环；(2) 4-[(3,5-二甲基硅基苯基)羰基]氨基}苯甲酸和 42-[5-(3-甲氧基甲基-5,6,7,8-四氢-5,5,8,8,-四甲基萘-2-基)-吡咯基]}苯甲酸。
• US6355669B1
  申请人：——

  公开号：US6355669B1

  公开（公告）日：2002-03-12