利马扎封 | 99593-25-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 利马扎封
• 中文别名: 5-[[(氨基乙酰基)氨基]甲基]-1-[4-氯-2-(2-氯苯甲酰基)苯基]-N,N-二甲基-1H.1,2,4-三唑-3-甲酰胺
• 英文名称: 2',5-dichloro-2-(3-dimethylcarbamoyl-5-glycylaminomethyl-1H-1,2,4-triazol-1-yl)benzophenone
• 英文别名: 1-[4-chloro-2-(2-chloro-benzoyl)-phenyl]-5-(glycylamino-methyl)-1H-[1,2,4]triazole-3-carboxylic acid dimethylamide；rilmazafone；5-[[(2-aminoacetyl)amino]methyl]-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1,2,4-triazole-3-carboxamide
• CAS: 99593-25-6
• 化学式: C₂₁H₂₀Cl₂N₆O₃
• 分子量: 475.334
• InChiKey: KYHFRCPLIGODFH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  123
• 氢给体数：
  2
• 氢受体数：
  6

制备方法与用途

Rilmazafone是一种苯二氮卓类ω配体，具有镇静和催眠的作用。

反应信息

• 作为反应物：
  描述：

  利马扎封 生成 8-chloro-6-(2-chlorophenyl)-N-(hydroxymethyl)-4H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide
  参考文献：
  名称：

  KOIKE, M.;NORIKURA, R.;FUTAGUCHI, S.;YAMAGUCHI, T.;SUGENO, K.;IWATANI, K.+, DRUG METAB. AND DISPOSIT. BIOL. FATE CHEM., 15,(1987) N 3, 426-428

  摘要：

  DOI：
• 作为产物：
  描述：

  ethyl (2E)-2-amino-2-[[4-chloro-2-(2-chlorobenzoyl)phenyl]hydrazinylidene]acetate 在 一水合肼 作用下， 以 甲醇 、 乙醇 为溶剂， 反应 102.5h， 生成 利马扎封
  参考文献：
  名称：

  合成和生物活性（3,5-二取代-1- ħ -1,2,4-三唑-1-基）二苯甲酮衍生物†

  摘要：

  描述了（5-酰基氨基甲基-3-氨基甲酰基-1 H -1,2,4-三唑-1-基）二苯甲酮衍生物4a-i，14a-d，15a-d，16a-c的合成。关键中间体1-苯甲酰基苯基偶氮-1-氨基乙酰胺7的酰化，然后在酸存在下环化，得到1 H -1,2,4-三唑衍生物。对这些化合物的中枢神经系统（CNS）活性进行了评估。当口服时，这些化合物中的一些在小鼠抗戊烯四唑和旋转脚架试验中表现出高活性。

  DOI：

  10.1002/jhet.5570190621

文献信息

• Nitrosated and nitrosylated diuretic compounds, compositions and methods of use
  申请人：Garvey S. David

  公开号：US20050059655A1

  公开（公告）日：2005-03-17

  The invention describes novel nitrosated and/or nitrosylated diuretic compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated diuretic compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one diuretic compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; and (l) treating nephropathy.

  该发明描述了新颖的亚硝基化和/或亚硝酰化利尿化合物或其药用盐，以及包含至少一种亚硝基化和/或亚硝酰化利尿化合物的新型组合物，以及可选地至少一种一氧化氮供体和/或至少一种治疗剂。该发明还提供了包含该发明中至少一种利尿化合物的新型组合物和试剂盒，该利尿化合物可选择地亚硝基化和/或亚硝酰化，并且可选地至少一种一氧化氮供体化合物和/或至少一种治疗剂。该发明还提供了用于(a)治疗由于过多水分和/或电解贮留引起的疾病；(b)治疗心血管疾病；(c)治疗肾血管疾病；(d)治疗糖尿病；(e)治疗由氧化应激引起的疾病；(f)治疗内皮功能障碍；(g)治疗由内皮功能障碍引起的疾病；(h)治疗肝硬化；(j)治疗子痫前期；(k)治疗骨质疏松症；和(l)治疗肾病的方法。
• Nitric Oxide Releasing Prodrugs of Therapeutic Agents
  申请人：SATYAM Apparao

  公开号：US20110263526A1

  公开（公告）日：2011-10-27

  The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

  本发明涉及已知药物或治疗剂的一氧化氮释放前药，其在此处表示为式(I)的化合物，其中药物或治疗剂包含一个或多个功能基团，独立地选自羧酸、氨基、羟基和巯基。该发明还涉及制备一氧化氮释放前药（式(I)的化合物）的方法，含有它们的药物组合物以及使用这些前药的方法。
• [EN] BENZIMIDAZOLE DERIVATIVES AS MCH RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS DE BENZIMIDAZOLE COMME ANTAGONISTES DU RÉCEPTEUR MCH
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2013105676A1

  公开（公告）日：2013-07-18

  The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula (I) wherein each symbol as defined in the specification, or a salt thereof.

  本发明提供了一种具有黑色素浓集激素受体拮抗作用并且用作预防或治疗肥胖等疾病的芳香环化合物。本发明涉及一种由式(I)表示的化合物，其中每个符号如规范中定义的，或其盐。
• [EN] HETEROCYCLIC COMPOUND<br/>[FR] COMPOSÉ HÉTÉROCYCLIQUE
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2015005489A1

  公开（公告）日：2015-01-15

  Provided is a compound having a melanin-concentrating hormone receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of obesity and the like. A compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

  提供的是一种具有黑色素浓缩激素受体拮抗作用的化合物，可用作预防或治疗肥胖等疾病的药物。该化合物由以下式（I）表示：其中每个符号如规范中定义，或其盐。
• Nitric oxide enhancing diuretic compounds, compositions and methods of use
  申请人：Garvey S. David

  公开号：US20060189603A1

  公开（公告）日：2006-08-24

  The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia. The nitric oxide enhancing diuretic compounds comprise at least one nitric oxide enhancing group linked to the diuretic compound through one or more sites such as carbon, oxygen and/or nitrogen via a bond or moiety that cannot be hydrolyzed.

  该发明描述了包含至少一种增强一氧化氮利尿化合物或其药用盐的新型组合物和试剂盒，以及可选地，至少一种增强一氧化氮化合物和/或至少一种治疗剂的试剂盒。该发明还提供了以下方法：(a)治疗由过多水分和/或电解贮留引起的症状；(b)治疗心血管疾病；(c)治疗肾血管疾病；(d)治疗糖尿病；(e)治疗由氧化应激引起的疾病；(f)治疗内皮功能障碍；(g)治疗由内皮功能障碍引起的疾病；(h)治疗肝硬化；(j)治疗子痫前期；(k)治疗骨质疏松症；(l)治疗肾病；(m)治疗外周血管疾病；(n)治疗门静脉高压；(o)治疗中枢神经系统疾病；(p)治疗代谢综合征；(q)治疗性功能障碍；以及(r)高脂血症。增强一氧化氮利尿化合物包括至少一种增强一氧化氮基团，通过碳、氧和/或氮等一个或多个位点与利尿化合物连接，连接通过不能水解的键或基团。