莫那匹尔马来酸盐 | 103379-03-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并硫平类
• 中文名称: 莫那匹尔马来酸盐
• 英文名称: Monatepil maleate
• 英文别名: 11-<<4-<4-(4-fluorophenyl)-1-piperazinyl>butyryl>amino>-6,11-dihydrodibenzothiepin maleate；11-({4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl}amino)-6,11-dihydrodibenzo[b,e]thiepin maleate；(Z)-but-2-enedioic acid;N-(6,11-dihydrobenzo[c][1]benzothiepin-11-yl)-4-[4-(4-fluorophenyl)piperazin-1-yl]butanamide
• CAS: 103379-03-9
• 化学式: C₄H₄O₄*C₂₈H₃₀FN₃OS
• 分子量: 591.703
• InChiKey: ZDZXCYHMVFLGMT-BTJKTKAUSA-N

物化性质

• 熔点：
  149-150°

计算性质

• 辛醇/水分配系数(LogP)：
  4.95
• 重原子数：
  42
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  136
• 氢给体数：
  3
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  1-哌嗪丁酰胺,N-(6,11-二氢二苯并[b,e]噻庚英-11-基)-4-(4-氟苯基)- 以96的产率得到莫那匹尔马来酸盐
  参考文献：
  名称：

  Calcium antagonist piperazine derivatives, and compositions therefor

  摘要：

  分子式为：##STR1## 其中A表示烷基；Y--Z表示##STR2## --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, 或 ##STR3## R.sub.1和R.sub.2分别表示取代基；R.sub.3表示氢原子、烷基或烷氧基；R.sub.4表示苯基、苯基烷基、苯基烯基、二苯甲基、萘基、噻唑基、可选取代吡啶基、可选取代嘧啶基、喹啉基、苯甲酰基烷基、苯甲酰基、呋喃基、硫代苯甲酰基、苯氧羰基、苯氧磺酰基或苯基磺酰基；a为2或3，b和c分别为1或2，d为0至2的整数，但苯基、苯基基团和萘基可以选择性地被取代，以及其药学上可接受的盐，其制备方法和包含其的制药组合物。该化合物及其盐具有强大的钙拮抗作用，可用于预防和治疗高血压和/或缺血性心脏病。

  公开号：

  US04749703A1

文献信息

• Combinations of lipid modulating agents and substituted azetidinones and treatments for vascular conditions
  申请人：Graziano P. Michael

  公开号：US20050096307A1

  公开（公告）日：2005-05-05

  The present invention provides compositions, therapeutic combinations and methods including: (a) at least one lipid modulating agent; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols or 5α-stanols.

  本发明提供了包括以下内容的组合物、治疗组合和方法：(a)至少一种脂质调节剂；和(b)至少一种取代的噁唑烷酮或取代的β-内酰胺甾醇吸收抑制剂，可用于治疗血管疾病、糖尿病、肥胖以及降低血浆中甾醇或5α-甾烷醇的水平。
• Combinations of substituted azetidinones and CB1 antagonists
  申请人：Veltri P. Enrico

  公开号：US20060069080A1

  公开（公告）日：2006-03-30

  The present invention provides compositions, therapeutic combinations and methods including: (a) at least one selective CB 1 antagonist; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity, metabolic syndrome and lowering plasma levels of sterols or 5α-stanols.

  本发明提供了包括以下内容的组合物、治疗组合和方法：(a)至少一种选择性CB1拮抗剂；和(b)至少一种取代的氮杂环丁烷或取代的β-内酰胺甾醇吸收抑制剂，可用于治疗血管疾病、糖尿病、肥胖、代谢综合征以及降低血浆中的甾醇或5α-甾烷醇水平。
• [EN] DIPHENYLAZETIDINONE DERIVATES PROCESSING CHOLESTEROL ABSORPTION INHIBITORY ACTIVITY<br/>[FR] DERIVES DIPHENYLAZETIDINONE PRESENTANT UNE ACTIVITE D'INHIBITION D'ABSORPTION DU CHOLESTEROL
  申请人：ASTRAZENECA AB

  公开号：WO2005061451A1

  公开（公告）日：2005-07-07

  Compounds of formula (XV): [Chemical formula should be inserted here. Please see paper copy] (XV) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.

  公式（XV）的化合物：[应在此处插入化学公式。请参见纸质副本]（XV）（其中变量组如内部定义）药物可接受的盐、溶剂化物、这些盐的溶剂化物和前药及其用作治疗高脂血症的胆固醇吸收抑制剂。还描述了它们的制造过程和含有它们的药物组合物。
• [EN] SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS<br/>[FR] PIPÉRAZINES SUBSTITUÉES EN TANT QU'ANTAGONISTES DE CB1
  申请人：SCHERING CORP

  公开号：WO2009005645A1

  公开（公告）日：2009-01-08

  Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.

  化合物式(I)或其药用可接受的盐、溶剂合物或酯，可用于治疗由CB1受体介导的疾病或症状，如代谢综合征和肥胖症、神经炎症性疾病、认知障碍和精神病、成瘾（例如戒烟）、胃肠道疾病和心血管疾病。
• Hydroxylated nebivolol metabolites
  申请人：O'Donnell P. John

  公开号：US20070014733A1

  公开（公告）日：2007-01-18

  Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

  羟基化奈必洛尔代谢物在急性给药后以浓度依赖性方式增加人内皮细胞制剂的一氧化氮释放。此外，羟基化奈必洛尔代谢物，包括但不限于4-羟基-6,6'-二氟代-、4-羟基-5-苯酚-6,6'-二氟代-和4-羟基-8-苯并-6,6'-二氟代-，在慢性给药后能够增加人内皮细胞的一氧化氮释放能力。本发明提供了羟基化奈必洛尔代谢物和包含奈必洛尔和/或至少一种羟基化奈必洛尔代谢物和/或至少一种用于治疗心血管疾病的附加化合物的组合物，以及可药用的盐。此外，本发明还提供了通过给药至少一种能够释放治疗有效量的一氧化氮到受血管疾病影响的靶向部位的羟基化奈必洛尔代谢物来治疗和/或预防血管疾病的方法。本发明还涉及通过给药至少一种羟基化奈必洛尔代谢物来治疗和/或预防偏头痛。本发明还可以与治疗代谢综合征障碍的其他治疗联合使用，或作为单一治疗。