1H-Indole-3-acetic acid, 1-((4-chlorophenyl)methyl)-2-methyl-5-(2-quinolinylmethoxy)- | 135872-94-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1H-Indole-3-acetic acid, 1-((4-chlorophenyl)methyl)-2-methyl-5-(2-quinolinylmethoxy)-
• 英文别名: 2-[1-[(4-chlorophenyl)methyl]-2-methyl-5-(quinolin-2-ylmethoxy)indol-3-yl]acetic acid
• CAS: 135872-94-5
• 化学式: C₂₈H₂₃ClN₂O₃
• 分子量: 470.9
• InChiKey: UVEUKSMEMNIKBS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  64.4
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• COMPOSITIONS AND TREATMENTS COMPRISING 5-LIPOXYGENASE-ACTIVATING PROTEIN INHIBITORS AND NITRIC OXIDE MODULATORS
  申请人：Hutchinson John H.

  公开号：US20100068301A1

  公开（公告）日：2010-03-18

  Disclosed herein are compositions and compounds that combine an inhibitor of 5 -lipoxygenase activating protein (FLAP) and a modulator of NO levels in a mammal. The NO modulator can be an agent that induces the production of NO in a mammal, or can be an agent that itself produces NO in the mammal. Further disclosed herein are strategies for synthesizing such compounds, and methods for testing whether the combination compounds and compositions provide a desired benefit. Also disclosed herein are pharmaceutical compositions and formulations that combine a FLAP inhibitor and an NO modulator. Further described herein are methods for using such compositions and compounds for the treatment of diseases, conditions, and disorders in a mammal, including a human. Such treatment methods include the separate administration of a FLAP inhibitor and a NO modulator to the mammal, and the simultaneous administration of a FLAP inhibitor and a NO modulator to the mammal.

  本文揭示了一种将5-脂氧合酶激活蛋白（FLAP）抑制剂和哺乳动物中NO水平调节剂结合的组合物和化合物。NO调节剂可以是在哺乳动物中诱导NO产生的药物，也可以是在哺乳动物中自身产生NO的药物。本文还揭示了合成这种化合物的策略，以及测试组合化合物和组合物是否提供所需益处的方法。本文还揭示了将FLAP抑制剂和NO调节剂结合的制药组合物和配方。本文还进一步描述了使用这些组合物和化合物治疗哺乳动物（包括人类）的疾病、状况和障碍的方法。这种治疗方法包括将FLAP抑制剂和NO调节剂分别给哺乳动物，以及同时给哺乳动物FLAP抑制剂和NO调节剂。
• SUBSTITUTED INDOLE-, INDENE-, PYRANOINDOLE- AND TETRAHYDROCARBAZOLE- ALKANOIC ACID DERIVATIVES AS INHIBITORS OF PLA 2? AND LIPOXYGENASE
  申请人：AMERICAN HOME PRODUCTS CORPORATION

  公开号：EP0502106A1

  公开（公告）日：1992-09-09
• COMPOSITIONS FOR TREATMENT OF CHRONIC INFLAMMATORY DISEASES
  申请人：SHAPIRO, Howard, K.

  公开号：EP0759750A1

  公开（公告）日：1997-03-05
• EP0759750A4
  申请人：——

  公开号：EP0759750A4

  公开（公告）日：1998-05-27
• Compositions and method for treatment of chronic inflammatory diseases
  申请人：Shapiro K. Howard

  公开号：US20050090553A1

  公开（公告）日：2005-04-28

  This invention defines novel compositions that can be used for clinical treatment of a class of chronic inflammatory diseases. Increased generation of carbonyl substances, namely aldehydes and ketones, occurs at sites of chronic inflammation and is common to the etiologies of all of the clinical disorders addressed herein. Such carbonyl substances are cytotoxic and additionally serve to perpetuate and disseminate the inflammatory process. This invention defines use of compositions, the orally administered required primary agents of which are primary amine derivatives of benzoic acid capable of covalently reacting with the carbonyl substances. p-Aminobenzoic acid (or PABA) is an example of the required primary agent of the present invention. PABA has a small molecular weight, is water soluble, has a primary amine group which reacts with carbonyl-containing substances and is tolerated by the body in relatively high dosages for extended periods. The method of the present invention includes administration of a composition comprising: (1) an orally consumed therapeutically effective amount of at least one required primary agent; (2) at least one required previously known medicament co-agent recognized as effective to treat a chronic inflammatory disease addressed herein administered to the mammalian subject via the oral route, other systemic routes of administration or via the topical route; and (3) optionally one or more additional orally consumed co-agent selected from the group consisting of antioxidants, vitamins, metabolites at risk of depletion, sulfhydryl co-agents, co-agents which may facilitate glutathione activity and nonabsorbable primary amine polymeric co-agents, so as to produce an additive or synergistic physiological effect of an anti-inflammatory nature.