2-(5-benzylaminosulfonylamino-6-oxo-2-phenyl-1,6-dihydropyrimidin-1-yl)-N-[2,3-dioxo-1-phenylmethyl-6-(2-pyridyloxy)]hexylacetamide | 504425-58-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(5-benzylaminosulfonylamino-6-oxo-2-phenyl-1,6-dihydropyrimidin-1-yl)-N-[2,3-dioxo-1-phenylmethyl-6-(2-pyridyloxy)]hexylacetamide
• 英文别名: 2-(5-Benzylaminosulfonylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-{2,3-dioxo-1-phenylmethyl-6-(2-pyridyloxy)}hexylacetamide；2-[5-(benzylsulfamoylamino)-6-oxo-2-phenylpyrimidin-1-yl]-N-(3,4-dioxo-1-phenyl-7-pyridin-2-yloxyheptan-2-yl)acetamide
• CAS: 504425-58-5
• 化学式: C₃₇H₃₆N₆O₇S
• 分子量: 708.795
• InChiKey: YMOIJESROGPDLS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  51
• 可旋转键数：
  18
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  185
• 氢给体数：
  3
• 氢受体数：
  11

文献信息

• Novel remedies or preventives for angiostenosis
  申请人：——

  公开号：US20040019068A1

  公开（公告）日：2004-01-29

  The present invention relates to a therapeutic or prophylactic agent for an angiostenosis comprising as an active ingredient a compound having a pyrimidone skeleton and having chymase inhibiting activity, for example, a compound having a structure represented by the following Formula (II) 1 and having high selective chymase inhibiting activity or a pharmacologically acceptable salt thereof.

  本发明涉及一种治疗或预防血管狭窄的药物或预防剂，其活性成分为具有嘧啶酮骨架并具有chymase抑制活性的化合物，例如，具有以下式（II）1表示的结构并具有高选择性chymase抑制活性或其药理学上可接受的盐。
• NOVEL ACETAMIDE DERIVATIVES AND PROTEASE INHIBITORS
  申请人：NIPPON KAYAKU KABUSHIKI KAISHA

  公开号：EP0936216A1

  公开（公告）日：1999-08-18

  The present invention relates to novel acetamide derivatives having a substituted heterocyclic group and consecutive dicarbonyl structures, for example 1-pyrimidinylacetamide compounds, 1-pyrazinylacetamide compounds, 1-triazinylacetamide compounds etc., and these compounds have inhibitory activity on chymotrypsin type proteases and are useful as inhibitors for said enzymes, particularly as chymase inhibitors. The novel acetamide derivatives of the present invention are shown in formula (I) below: wherein R0 is substituted or unsubstituted phenyl; R1 is aryl, heteroaryl or aliphatic lower alkyl which may be substituted or unsubstituted; R2 is substituted or unsustituted alkyl, arylalkyl, or heteroarylalkyl; R3 is hydrogen; acyl group; sulfonyl group; isocyanate group; thiourea; or hydrogen, a lower alkyl or a substituted lower alkyl; aryl (1-7C) alkyl, heteroaryl (1-7C) alkyl, aryl and heteroaryl; X and Y independently represent a nitrogen atom or a carbon atom; and Z is a polymethylene group wherein a hydrogen atom in the polymethylene may be replaced.

  本发明涉及具有取代杂环基团和连续二羰基结构的新型乙酰胺衍生物，例如1-嘧啶基乙酰胺化合物、1-吡嗪基乙酰胺化合物、1-三嗪基乙酰胺化合物等，这些化合物对糜蛋白酶型蛋白酶具有抑制活性，可用作上述酶的抑制剂，特别是糜蛋白酶抑制剂。本发明的新型乙酰胺衍生物如下式(I)所示： 其中 R0 是取代或未取代的苯基；R1 是芳基、杂芳基或可取代或未取代的脂肪族低级烷基；R2 是取代或未取代的烷基、芳烷基或杂芳基；R3 是氢；酰基；磺酰基；异氰酸酯基；硫脲；或氢、低级烷基或取代的低级烷基；芳基（1-7C）烷基、杂芳基（1-7C）烷基、芳基和杂芳基； X 和 Y 独立地代表一个氮原子或一个碳原子；Z 是一个聚亚甲基，其中聚亚甲基中的一个氢原子可被取代。
• 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.