3-dimethylaminomethyl-8-ethoxy-7-methoxy-2-oxo-1,2-dihydroquinoline | 282089-54-7

• 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: 3-dimethylaminomethyl-8-ethoxy-7-methoxy-2-oxo-1,2-dihydroquinoline
• 英文别名: 3-[(dimethylamino)methyl]-8-ethoxy-7-methoxy-1H-quinolin-2-one
• CAS: 282089-54-7
• 化学式: C₁₅H₂₀N₂O₃
• 分子量: 276.335
• InChiKey: SQVWIAWYHKKQEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  50.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-dimethylaminomethyl-8-ethoxy-7-methoxy-2-oxo-1,2-dihydroquinoline 、 8-butoxy-3-aminomethyl-7-methoxy-2-oxo-1,2-dihydroquinoline 、 异氰酸对氟苯基酯 在 三乙胺 作用下， 以 甲醇 、 氯仿 为溶剂， 以86%的产率得到N-[(8-butoxy-7-methoxy-2-oxo-1,2-dihydroquinoline-3-yl)methyl]-N'-(4-fluorophenyl)urea
  参考文献：
  名称：

  2-oxoquinoline compounds and medicinal uses thereof

  摘要：

  通用公式为[I]的2-氧喹啉化合物或其药用可接受的盐：（其中公式中的每个符号如描述中确定），及其药用。本发明的化合物[I]及其药用可接受的盐选择性作用于大麻素受体，特别是外周型大麻素受体，对中枢神经系统的副作用较少，具有很强的免疫抑制作用、抗炎作用或抗过敏作用。因此，这些化合物可用作大麻素受体（特别是外周型大麻素受体）调节剂、免疫抑制剂、抗炎剂和抗过敏剂。

  公开号：

  US06509352B1

文献信息

• 2-oxoquinoline compounds and pharmaceutical uses thereof
  申请人：——

  公开号：US20030191069A1

  公开（公告）日：2003-10-09

  A 2-oxoquinoline compound or its pharmaceutically acceptable salt of general formula [I]: 1 (wherein each symbol in the formula is as determined in the description), and its pharmaceutical use. The compound [I] of the present invention and its pharmaceutically acceptable salts selectively act on cannabinoid receptors, particularly on peripheral type cannabinoid receptors, and have fewer side effects on the central nervous system, having great immunosuppressive action, anti-inflammatory action or antiallergic action. Therefore, these compounds are useful as cannabinoid receptors (particularly peripheral type cannabinoid receptors) modulator, immunosuppressants, anti-inflammatory agents, and antiallergic agents.

  一种2-氧基喹啉化合物或其药学上可接受的盐，其通式为[I]:1（其中公式中的每个符号如说明中所确定的那样），以及其医药用途。本发明的化合物[I]及其药学上可接受的盐，能够选择性地作用于大麻素受体，特别是外周型大麻素受体，并且对中枢神经系统的副作用较少，具有很强的免疫抑制作用、抗炎作用或抗过敏作用。因此，这些化合物可用作大麻素受体（特别是外周型大麻素受体）调节剂、免疫抑制剂、抗炎剂和抗过敏剂。
• 2-OXOQUINOLINE COMPOUNDS AND MEDICINAL USES THEREOF
  申请人：Japan Tobacco Inc.

  公开号：EP1142877A1

  公开（公告）日：2001-10-10

  A 2-oxoquinoline compound or its pharmaceutically acceptable salt of general formula [I]: (wherein each symbol in the formula is as determined in the description), and its pharmaceutical use. The compound [I] of the present invention and its pharmaceutically acceptable salts selectively act on cannabinoid receptors, particularly on peripheral type cannabinoid receptors, and have fewer side effects on the central nervous system, having great immunosuppressive action, anti-inflammatory action or antiallergic action. Therefore, these compounds are useful as cannabinoid receptors (particularly peripheral type cannabinoid receptors) modulator, immunosuppressants, anti-inflammatory agents, and antiallergic agents.

  通式[I]的 2-氧代喹啉化合物或其药学上可接受的盐： (其中式中各符号由说明中确定）及其药物用途。 本发明的化合物[I]及其药学上可接受的盐选择性地作用于大麻素受体，特别是外周型大麻素受体，对中枢神经系统的副作用较小，具有很好的免疫抑制作用、抗炎作用或抗过敏作用。因此，这些化合物可用作大麻素受体（特别是外周型大麻素受体）调节剂、免疫抑制剂、抗炎剂和抗过敏剂。
• Antipruritics
  申请人：SHIONOGI & CO., LTD.

  公开号：EP2130820A1

  公开（公告）日：2009-12-09

  The present invention relates to the use of a compound having an agonistic activity to the cannabinoid receptor, a prodrug, a pharmaceutically acceptable salt or solvate thereof for the preparation of an antipruritic, wherein the compound having an agonistic activity to the cannabinoid receptor is a compound selected from (R,S)-4,4,4-trifluoro-1-butane sulfonic acid-3-(2-hydroxymethyl-indanyl-4-oxy)-phenylester; (S)-1-(4,4,4-trifluoro-1-butane sulfonic acid-3-(2-hydroxymethyl-indanyl-4-oxy)phenyl ester; and (R)-1-(4,4,4-trifluoro-1-butane sulfonic acid-3-(2-hydroxymethyl-indanyl-4-oxy)phenyl ester.

  本发明涉及一种对大麻素受体具有激动活性的化合物、其原药、药学上可接受的盐或溶液用于制备止痒剂的用途，其中对大麻素受体具有激动活性的化合物是选自以下各项的化合物 (R,S)-4,4,4-三氟-1-丁烷磺酸-3-(2-羟甲基-茚满-4-氧基)-苯酯； (S)-1-(4,4,4-三氟-1-丁烷磺酸-3-(2-羟甲基-茚满-4-氧基)苯基酯；和 (R)-1-(4,4,4-三氟-1-丁烷磺酸-3-(2-羟甲基-茚满-4-氧基)苯基酯。
• Therapeutic agent for allergic disease
  申请人：Japan Tobacco Inc.

  公开号：US20030232855A1

  公开（公告）日：2003-12-18

  In accordance with the invention, a therapeutic agent of allergic disease is provided, which contains a cannabinoid receptor-regulating substance, particularly a regulating substance selectively acting on peripheral cell type cannabinoid receptor, specifically N-(benzo[1,3]dioxol-5-ylmethyl)-7-methoxy-2-oxo-8-pentyloxy-1,2-dihydroquinoline-3-carboxamide or a pharmaceutically acceptable salt thereof; and the therapeutic agent of the invention shows effects on intractable allergic disease, for example asthma and atopic dermatitis.

  根据本发明，提供了一种治疗过敏性疾病的药物，其中含有一种大麻素受体调节物质，特别是一种选择性作用于外周细胞型大麻素受体的调节物质，具体为N-(苯并&lsqb；1,3]二氧戊环-5-基甲基）-7-甲氧基-2-氧代-8-戊氧基-1,2-二氢喹啉-3-甲酰胺或其药学上可接受的盐；本发明的治疗剂对难治性过敏性疾病，例如哮喘和特应性皮炎有疗效。
• US6509352B1
  申请人：——

  公开号：US6509352B1

  公开（公告）日：2003-01-21