(5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-thione

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-thione
• 英文别名: (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline-2(1H)-thione；3-(Methylamino)-1,3-diazatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-triene-2-thione；3-(methylamino)-1,3-diazatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-triene-2-thione
• 化学式: C₁₁H₁₃N₃S
• 分子量: 219.31
• InChiKey: ATTASLXRNQYFQW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  50.6
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  diphosphorus pentasulfide 、 (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]-quinolin-2(1h)-one 在 sodium hydroxide 作用下， 以 吡啶 为溶剂， 生成 (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-thione
  参考文献：
  名称：

  (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline-2(1H)-thione

  摘要：

  本发明是一种新型药物代理，（5R）-5-（甲胺基）-5,6-二氢-4H-咪唑并且其药用可接受的盐。

  公开号：

  US20020137763A1

文献信息

• Novel pharmaceutical compounds
  申请人：Tung Roger

  公开号：US20070037815A1

  公开（公告）日：2007-02-15

  The present invention relates to derivatives of tadalafil, substituted with fluorine on the methylene carbon atom situated between the oxygens of the benzodioxol ring, and optionally further substituted with deuterium atoms in place of normally abundant hydrogen, and 13 C in place of normally abundant 12 C. These compounds are selective PDE5 inhibitors and possess advantageous biopharmaceutical and pharmacokinetic properties. The invention further provides compositions comprising these compounds and methods of treating diseases and conditions that are responsive to PDE5 inhibition, alone and in combination with additional agents.

  本发明涉及替代他达拉非的衍生物，在苯并二氧杂环戊二烷环的氧原子之间的亚甲基碳原子上取代氟，并且可选地进一步用氘原子取代正常丰富的氢，以及用13C取代正常丰富的12C。这些化合物是选择性的PDE5抑制剂，并具有有利的生物制药和药代动力学性质。该发明还提供了包含这些化合物的组合物和治疗对PDE5抑制有响应的疾病和症状的方法，单独或与其他药物联合使用。
• Use of heterocyclic amine-type compounds as neuroprotective agents
  申请人：——

  公开号：US20040142937A1

  公开（公告）日：2004-07-22

  The present invention provides the use of heterocyclic amine-type compounds to prevent or reduce neuronal damages in patients afflicted with or susceptible to disease states or conditions known to result in or cause neuronal damage.

  本发明提供了利用杂环胺类化合物来预防或减少患有或易受患有已知会导致或引起神经元损伤的疾病状态或病况的患者中的神经元损伤。
• (5R)-5-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline-2(1H)-thione
  申请人：Pharmacia & Upjohn Company

  公开号：US20040266812A1

  公开（公告）日：2004-12-30

  The present invention is a novel pharmaceutical agent, (5R)-5-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline-2(1H)-thione 1 and pharmaceutically acceptable salts thereof.

  本发明是一种新型药物制剂，(5R)-5-(甲基氨基)-5,6-二氢-4H-咪唑[4,5,1-ij]喹啉-2(1H)-硫醇及其药学上可接受的盐。
• (5R)-5-(methyamino)-5, 6-dihydro-4H-imidazo[4,5,1,-ij]quinoline-2(1H)-thione
  申请人：——

  公开号：US20040029909A1

  公开（公告）日：2004-02-12

  The present invention is a novel pharmaceutical agent, (5R)-5-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline-2(1H)-thione 1 and pharmaceutically acceptable salts thereof.

  本发明是一种新型药物代理，(5R)-5-(甲基氨基)-5,6-二氢-4H-咪唑[4,5,1-ij]喹啉-2(1H)-硫醇及其药学上可接受的盐。
• (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline-2(1H)-thione and method of preparation thereof
  申请人：McCall B. Robert

  公开号：US20060040929A1

  公开（公告）日：2006-02-23

  The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually mating amount is from about 0.003 thru 0.2 mg/kg/dose. The present invention also provides a novel pharmaceutical agent, (5R)-5 -(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline-2(1H)-thione and pharmaceutically acceptable salts thereof.

  本发明涉及使用公式（A）化合物治疗人类的性障碍和诱导非人哺乳动物交配的方法，其中性治疗剂量范围为每人/次约0.2到8毫克，性交配剂量范围为每千克体重/次约0.003到0.2毫克。本发明还提供了一种新型药物，即（5R）-5-（甲基氨基）-5,6-二氢-4H-咪唑并[4,5,1-ij]喹啉-2（1H）-硫醇及其药学上可接受的盐。