8-amino-7-chloro-2-naphthol | 497151-49-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 8-amino-7-chloro-2-naphthol
• 英文别名: 8-Amino-7-chloronaphthalen-2-ol
• CAS: 497151-49-2
• 化学式: C₁₀H₈ClNO
• 分子量: 193.633
• InChiKey: HSUVVEOSEDYFSO-UHFFFAOYSA-N

物化性质

• 沸点：
  388.7±27.0 °C(Predicted)
• 密度：
  1.421±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  13
• 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：
  46.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  8-amino-7-chloro-2-naphthol 、 甲胺 在 乙酸乙酯 、 水 、 magnesium sulfate 作用下， 以 水 为溶剂， 反应 24.0h， 以to give N-(8-amino-7-chloro-2-naphthyl)-N-methylamine (16.1 mg, 7.7% yield)的产率得到N-(8-amino-7-chloro-2-naphthyl)-N-methylamine
  参考文献：
  名称：

  Amine derivatives

  摘要：

  本发明揭示了一种具有vanilloid receptor 1（VR1）拮抗活性的胺衍生物、其互变异构体或立体异构体形式或其盐。该胺衍生物具有优异的VR1拮抗活性，适用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁、过度活动膀胱、慢性疼痛、神经痛、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、失禁和/或炎症性疾病。

  公开号：

  US20040259875A1
• 作为产物：
  描述：

  1-氨基-7-萘酚 在 N-氯代丁二酰亚胺 作用下， 以 四氢呋喃 为溶剂， 反应 16.0h， 以69%的产率得到8-amino-7-chloro-2-naphthol
  参考文献：
  名称：

  Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence

  摘要：

  We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced clearance, improved potency and is active in rat cystometry models of urinary incontinence after intravenous administration. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.04.013

文献信息

• [EN] NAPHTHYLUREA AND NAPHTHYLACETAMIDE DERIVATIVES AS VANILLOID RECEPTOR 1 (VR1) ANTAGONISTS<br/>[FR] DERIVES AMINES
  申请人：BAYER AG

  公开号：WO2003014064A1

  公开（公告）日：2003-02-20

  Naphthylurea and naphthylacetamide derivatives of formula (I) which have vanilloid receptor 1 (VR1) antagonistic activity are disclosed, formula (I) wherein Y represents formula (II) and formula (III) and the variables Q, X, R6, R7, R8, R8a, R9, R10 and R11 are as defined in the claims. The compounds are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.

  本文披露了公式(I)的萘基脲和萘基乙酰胺衍生物，其具有vanilloid受体1（VR1）拮抗活性，其中公式(I)中Y代表公式(II)和公式(III)，而变量Q、X、R6、R7、R8、R8a、R9、R10和R11如权利要求中所定义。这些化合物可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁、过度活动膀胱、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、失禁和/或炎症性疾病。
• Ether derivative
  申请人：Okuzumi Tatsuya

  公开号：US20060270693A1

  公开（公告）日：2006-11-30

  The present invention relates to an ether derivative represented by the formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof wherein each symbol is as defined in the description, and an ether derivative represented by the formula (III), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof wherein each symbol is as defined in the description; a pharmaceutical composition containing the ether derivative; and a package containing the pharmaceutical composition and a description of use thereof. A pharmaceutical composition of the present invention, which contains this compound of the present invention has a superior anti-inflammatory and analgesic activity and is useful as various pharmaceutical agents such as an anti-inflammatory agent, an analgesic, a therapeutic agent for inflammatory bowel disease, a therapeutic agent for pollakiuria and/or incontinentia, a therapeutic agent for asthma and the like.

  本发明涉及一种以式(I)表示的醚衍生物，其药学上可接受的盐、水合物或溶剂化物，其中每个符号如描述中所定义的，并且一种以式(III)表示的醚衍生物，其药学上可接受的盐、水合物或溶剂化物，其中每个符号如描述中所定义的；一种含有该醚衍生物的制药组合物；以及一个包含该制药组合物及其使用说明的包装。本发明的制药组合物，包含该化合物具有优异的抗炎和镇痛活性，并且可用作各种药物剂型，如抗炎剂、镇痛剂、治疗炎症性肠病的治疗剂、治疗排尿过频和/或失禁的治疗剂、治疗哮喘等。
• ETHER DERIVATIVE
  申请人：Ajinomoto Co., Inc.

  公开号：EP1679296A1

  公开（公告）日：2006-07-12

  The present invention relates to an ether derivative represented by the formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof wherein each symbol is as defined in the description, and an ether derivative represented by the formula (III), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof wherein each symbol is as defined in the description; a pharmaceutical composition containing the ether derivative; and a package containing the pharmaceutical composition and a description of use thereof. A pharmaceutical composition of the present invention, which contains this compound of the present invention has a superior anti-inflammatory and analgesic activity and is useful as various pharmaceutical agents such as an anti-inflammatory agent, an analgesic, a therapeutic agent for inflammatory bowel disease, a therapeutic agent for pollakiuria and/or incontinentia, a therapeutic agent for asthma and the like.

  本发明涉及一种由式（I）表示的醚衍生物、其药学上可接受的盐、其水合物或其溶液 其中各符号如描述中所定义，以及由式（III）表示的醚衍生物、其药学上可接受的盐、其水合物或其溶物 其中各符号在说明中定义；含有醚衍生物的药物组合物；以及含有药物组合物及其使用说明的包装。含有本发明化合物的本发明药物组合物具有优异的抗炎和镇痛活性，可用作各种药物制剂，如抗炎剂、镇痛剂、炎症性肠病治疗剂、花粉尿症和/或失禁治疗剂、哮喘治疗剂等。
• NAPHTHYLUREA AND NAPHTHYLACETAMIDE DERIVATIVES AS VANILLOID RECEPTOR 1 (VR1) ANTAGONISTS
  申请人：Bayer HealthCare AG

  公开号：EP1414788A1

  公开（公告）日：2004-05-06
• US7728005B2
  申请人：——

  公开号：US7728005B2

  公开（公告）日：2010-06-01