5-Nitro-3-hydroxychinolin | 41068-81-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 5-Nitro-3-hydroxychinolin
• 英文别名: 5-nitro-quinolin-3-ol；3-Hydroxy-5-nitroquinoline；5-Nitroquinolin-3-ol
• CAS: 41068-81-9
• 化学式: C₉H₆N₂O₃
• 分子量: 190.158
• InChiKey: SISRQKHBPIZTNW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  78.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-Nitro-3-hydroxychinolin 、 碘甲烷 在 sodium hydride 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 2.0h， 生成 3-methoxy-5-nitroquinoline
  参考文献：
  名称：

  [EN] TETRAHYDRO-QUINOLINYLUREA DERIVATIVES AS VRL ANTAGONISTS
  [FR] DERIVES DE TETRAHYDRO-QUINOLINYLUREE

  摘要：

  公开号：

  WO2005044802A3
• 作为产物：
  描述：

  3-羟基喹啉 在 硫酸 、 硝酸 作用下， 反应 2.0h， 生成 5-Nitro-3-hydroxychinolin
  参考文献：
  名称：

  [EN] TETRAHYDRO-QUINOLINYLUREA DERIVATIVES AS VRL ANTAGONISTS
  [FR] DERIVES DE TETRAHYDRO-QUINOLINYLUREE

  摘要：

  公开号：

  WO2005044802A3

文献信息

• Tetrahydro-Quinolinylurea Derivatives
  申请人：Bouchon Axel

  公开号：US20070213363A1

  公开（公告）日：2007-09-13

  This invention relates to tetrahydro-quinolinylurea derivatives and salts thereof which are useful as active ingredi- ents of pharmaceutical preparations. The tetrahydro-quinolinylurea derivative of the present invention has vanilloid receptor (VR I) C antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR 1 activity, in particular for =the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pul- monary (or airways) disease (COPD).

  本发明涉及四氢喹啉基脲衍生物及其盐，它们是制备药物制剂的有效成分。本发明的四氢喹啉基脲衍生物具有vanilloid受体（VR I）C拮抗活性，并可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗泌尿系统疾病或障碍，如膀胱平滑肌过度活动（过度活动膀胱）、尿失禁、神经源性膀胱平滑肌过度活动（膀胱过度弯曲）、特发性膀胱平滑肌过度活动（膀胱不稳定）、良性前列腺增生和下尿路症状；慢性疼痛、神经性疼痛、术后疼痛、类风湿关节炎疼痛、神经痛、神经病、疼痛、神经损伤、缺血、神经变性、中风和哮喘等炎症性疾病以及慢性阻塞性肺（或气道）疾病（COPD）。
• Inhibitors of prenyl-protein transferase
  申请人：Merck & Co., Inc.

  公开号：US06441017B1

  公开（公告）日：2002-08-27

  The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

  本发明涉及一种宏环化合物，其抑制戊二烯蛋白转移酶（FTase）和致癌基因蛋白Ras的戊二烯化。本发明还涉及含有本发明化合物的化疗组合物以及抑制戊二烯蛋白转移酶和致癌基因蛋白Ras的方法。
• Tetrahydro-quinolinylurea derivatives
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：US07683076B2

  公开（公告）日：2010-03-23

  This invention relates to tetrahydro-quinolinylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-quinolinylurea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

  本发明涉及四氢喹啉基脲衍生物及其盐，其可作为制药制剂的活性成分。本发明的四氢喹啉基脲衍生物具有vanilloid受体（VR1）拮抗活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗泌尿系统疾病或障碍，如膀胱过度活动（过度活跃的膀胱），尿失禁，神经源性膀胱过度活动（膀胱过度弯曲），特发性膀胱过度活动（膀胱不稳定性），良性前列腺增生症和下尿路症状；慢性疼痛，神经病性疼痛，术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，疼痛，神经损伤，缺血，神经退行性疾病，中风，以及哮喘和慢性阻塞性肺（或气道）疾病（COPD）等炎症性疾病。
• INHIBITORS OF PRENYL-PROTEIN TRANSFERASE
  申请人：Merck & Co., Inc.

  公开号：EP1214326A1

  公开（公告）日：2002-06-19
• TETRAHYDRO-QUINOLINYLUREA DERIVATIVES
  申请人：Bayer HealthCare AG

  公开号：EP1685112A2

  公开（公告）日：2006-08-02