2-ethoxycarbonylmethyl-4-(4-chlorobenzylsulfinyl)-8-methylimidazo[1,5-d][1.2.4]triazine-1(2H)-one | 179316-92-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-ethoxycarbonylmethyl-4-(4-chlorobenzylsulfinyl)-8-methylimidazo[1,5-d][1.2.4]triazine-1(2H)-one
• 英文别名: 2-ethoxycarbonylmethyl-4-(4-chlorobenzylsulfinyl)-8-methylimidazo[1,5-d] [1,2,4]triazin-1(2H)-one；Ethyl 2-[4-[(4-chlorophenyl)methylsulfinyl]-8-methyl-1-oxoimidazo[1,5-d][1,2,4]triazin-2-yl]acetate
• CAS: 179316-92-8
• 化学式: C₁₇H₁₇ClN₄O₄S
• 分子量: 408.865
• InChiKey: HYKZDIWCKMSDJC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  27
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  113
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  4-(4-chlorobenzylthio)-2-ethoxycarbonylmethyl-8-methyl imidazo[1,5-d][1.2.4]triazine-1(2H)-one 以91%的产率得到2-ethoxycarbonylmethyl-4-(4-chlorobenzylsulfinyl)-8-methylimidazo[1,5-d][1.2.4]triazine-1(2H)-one
  参考文献：
  名称：

  Triazine derivative, chymase activity inhibitor and nitric oxide production inhibitor

  摘要：

  本发明提供了新颖的三嗪衍生物，可以抑制钳形酶活性和一氧化氮产生。这些三嗪衍生物通过抑制钳形酶活性对预防和治疗支气管哮喘、过敏性鼻炎和荨麻疹具有用处，并且通过抑制一氧化氮产生对预防和治疗心脏病和脑血管疾病、缺血性心脏病、感染性休克、疼痛、风湿热、关节炎、哮喘、免疫功能缺陷、病毒或非病毒感染、自身免疫疾病和癌症具有用处。

  公开号：

  EP0713876A1

文献信息

• PREVENTIVES OR REMEDIES FOR EYE CIRCULATORY FAILURE
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP1112749A2

  公开（公告）日：2001-07-04

  The conventional pharmaootherapy for diseases caused by a disturbance of ocular circulation, inclusive of glaucoma, comprises oral administration of steroids and other drugs and/or topical administration of β -adrenergic antagonists but these therapeutic regimens are invariably not effective enough but rather entail adverse reactions characteristic of the respective drugs used. This invention is characterized in that a chymase inhibitor is used for the prevention or treatment of diseases caused by a disturbance of ocular circulation and enables positive prophylaxis or therapy with reduced risks for side effects.

  传统的药物疗法用于治疗眼循环障碍引起的疾病，包括青光眼，包括口服类固醇和其他药物和/或局部使用β-肾上腺素能拮抗剂，但这些治疗方案总是不够有效，反而会引起所用药物特有的不良反应。 本发明的特点在于，糜蛋白酶抑制剂可用于预防或治疗由眼部循环障碍引起的疾病，并能在降低副作用风险的同时进行积极的预防或治疗。
• TENSION-RELIEVING AGENTS FOR CILIARY MUSCLE
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP1224945A1

  公开（公告）日：2002-07-24

  Use of a chymase inhibitor in preventing and treating nearsightedness caused by the continuous tension of ciliary muscles makes it possible to achieve exact preventive and therapeutic effects with little side effects.

  使用糜蛋白酶抑制剂来预防和治疗因睫状肌持续紧张而引起的近视，可以达到确切的预防和治疗效果，而且副作用很小。
• Prophylactic or threapeutic composition for ocular circulation disorders
  申请人：——

  公开号：US20040086537A1

  公开（公告）日：2004-05-06

  The conventional pharmacotherapy for diseases caused by a disturbance of ocular circulation, inclusive of glaucoma, comprises oral administration of steroids and other drugs and/or topical administration of &bgr;-adrenergic antagonists but these therapeutic regimens are invariably not effective enough but rather entail adverse reactions characteristic of the respective drugs used. This invention is characterized in that a chymase inhibitor is used for the prevention or treatment of diseases caused by a disturbance of ocular circulation and enables positive prophylaxis or therapy with reduced risks for side effects.

  对眼部循环障碍引起的疾病（包括青光眼）的传统药物治疗包括口服类固醇和其他药物和/或局部使用肾上腺素能拮抗剂，但这些治疗方案总是不够有效，反而会引起所用药物特有的不良反应。 本发明的特点在于，糜蛋白酶抑制剂可用于预防或治疗由眼部循环障碍引起的疾病，并能在降低副作用风险的情况下进行积极的预防或治疗。
• Methods and Compositions for the Treatment of Hypertension and Gastrointestinal Disorders
  申请人：Talley John Jeffrey

  公开号：US20090054319A1

  公开（公告）日：2009-02-26

  The use of guanylin potentiating agents for treating various disorders, including hypertension as well as IBS and other gastrointestinal disorders and conditions (e.g., gastrointestinal motility disorders, chronic intestinal pseudo-obstruction, colonic pseudo-obstruction, Crohn's disease, duodenogastric reflux, dyspepsia, functional dyspepsia, nonulcer dyspepsia, a functional gastrointestinal disorder, functional heartburn, gastroesophageal reflux disease (GERD), gastroparesis, inflammatory bowel disease, irritable bowel syndrome, post-operative ileus, ulcerative colitis, chronic constipation, and disorders and conditions associated with constipation is described.
• [EN] METHODS AND COMPOSITIONS FOR THE TREATMENT OF HYPERTENSION AND GASTROINTESTINAL DISORDERS<br/>[FR] METHODES ET COMPOSITIONS POUR LE TRAITEMENT DE L'HYPERTENSION ET DE TROUBLES GASTRO-INTESTINAUX
  申请人：MICROBIA INC

  公开号：WO2006102069A2

  公开（公告）日：2006-09-28

  [EN] The use of guanylin potentiating agents for treating various disorders, including hypertension as well as IBS and other gastrointestinal disorders and conditions (e.g., gastrointestinal motility disorders, chronic intestinal pseudo-obstruction, colonic pseudo-obstruction, Crohn's disease, duodenogastric reflux, dyspepsia, functional dyspepsia, nonulcer dyspepsia, a functional gastrointestinal disorder, functional heartburn, gastroesophageal reflux disease (GERD), gastroparesis, inflammatory bowel disease, irritable bowel syndrome, post-operative ileus, ulcerative colitis, chronic constipation, and disorders and conditions associated with constipation is described.
  [FR] L'invention porte sur l'utilisation d'agents potentialiseurs pour traiter différents troubles dont le syndrome du côlon irritable et d'autres troubles et états gastro-intestinaux tels que: les troubles de la motilité gastro-intestinale, la pseudo obstruction intestinale, la pseudo obstruction du côlon, la maladie de Crohn, le reflux duodénogastrique, la dyspepsie, la dyspepsie fonctionnelle, la dyspepsie non ulcéreuse, les troubles gastro-intestinaux fonctionnels, la pyrosis fonctionnelle, le reflux gastrooesophagien, la gastroparésie, l'inflammation de l'intestin, le syndrome de l'intestin irritable, l'occlusion intestinale post opératoire, la rectocolite hémorragique, la constipation chronique, et des troubles et états associés à la constipation.