福米诺苯 | 18053-31-1

• 物质功能分类: 原料药 - 呼吸系统用药 - 镇咳药
• 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: 福米诺苯
• 中文别名: N-[3-氯-2-[[甲基-(2-吗啉-4-基-2-氧代乙基)氨基]甲基]苯基]苯甲酰胺；胺酰苯吗琳
• 英文名称: fominoben
• 英文别名: 2-Benzoylamino-6-chlor-N-methyl-N-morpholinocarbonylmethyl-benzylamin；4-[N-(2-benzoylamino-6-chloro-benzyl)-N-methyl-glycyl]-morpholine；N-[3-chloro-2-[[methyl-(2-morpholin-4-yl-2-oxoethyl)amino]methyl]phenyl]benzamide
• CAS: 18053-31-1
• 化学式: C₂₁H₂₄ClN₃O₃
• mdl: MFCD00866851
• 分子量: 401.893
• InChiKey: KSNNEUZOAFRTDS-UHFFFAOYSA-N

物化性质

• 熔点：
  122.5-123°
• 保留指数：
  3210

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  61.9
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] DEUTERATED MORPHINE DERIVATIVES<br/>[FR] DÉRIVÉS DE MORPHINE DEUTÉRÉS
  申请人：SZEGEDI TUDOMÁNYEGYETEM

  公开号：WO2014170704A1

  公开（公告）日：2014-10-23

  The invention relates to new morphine derivatives deuterated at the 7,8-position of the morphine ring, furthermore to a process for the preparation thereof, and to pharmaceutical compositions comprising them. The new deuterated morphine derivatives show high and selective μ-opioid receptor binding activity leading to the benefit of higher analgesic activity at lower dosages inducing thereby reduced adverse effects compared to the hydrogenated derivatives. The compounds of the invention are useful for example in the treatment of pain or can be used as antitussive agents with a reduced risk of the possibility of drug abuse.

  这项发明涉及新的吗啡衍生物，其在吗啡环的7,8-位置被氘代取，此外还涉及其制备方法以及包含它们的药物组合物。这些新的氘代吗啡衍生物显示出高度和选择性的μ-阿片受体结合活性，从而在较低剂量下产生更高的镇痛活性，因此与氢化衍生物相比，减少了不良反应。该发明的化合物可用于例如治疗疼痛，或可用作镇咳剂，具有较低的药物滥用可能性。
• 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。
• 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] METAL NANOPARTICLE SURFACE LIGAND REPLACEMENT METHOD<br/>[FR] PROCÉDÉ DE REMPLACEMENT DE LIGAND DE SURFACE DE NANOPARTICULE MÉTALLIQUE
  申请人：UNIV WIEN BODENKULTUR

  公开号：WO2018091666A1

  公开（公告）日：2018-05-24

  The invention relates to a method of producing inorganic nanoparticles with a polar surface, a) providing an inorganic nanoparticle with a coordinated organic ligand to the nanoparticles surface, b) providing a replacement salt comprising a replacement ion and a counterion, c) treating the inorganic nanoparticle with the coordinated organic ligand with the replacement salt in the presence of a chelating agent that complexes the counterion, thereby increasing the replacements ion's reactivity and replacing the organic ligand on the nanoparticle surface by the replacement ion which results in an inorganic nanoparticle with a polar surface; and a kit.

  这项发明涉及一种制备具有极性表面的无机纳米颗粒的方法，a)提供具有配位有机配体的无机纳米颗粒至纳米颗粒表面，b)提供包括替代离子和对离子的替代盐，c)在存在络合剂的情况下，用替代盐处理具有配位有机配体的无机纳米颗粒，络合剂络合对离子，从而增加替代离子的反应性并通过替代离子替换纳米颗粒表面上的有机配体，从而得到具有极性表面的无机纳米颗粒；以及一个试剂盒。
• [EN] PROCESS FOR THE PREPARATION OF A POLYUNSATURATED KETONE COMPOUND<br/>[FR] PROCÉDÉ POUR LA PRÉPARATION D'UN COMPOSÉ POLYINSATURÉ DE CÉTONE
  申请人：AVEXXIN AS

  公开号：WO2015011206A1

  公开（公告）日：2015-01-29

  The invention relates to the manufacture of certain polyunsaturated compounds employing a particular application of the Mitsonobu reaction in the presence of at least one anti-oxidant. We have found a method of making a pharmaceutically-acccptable polyunsaturated ester or thioester compound directly, which can ultimately be converted to the advantageous ketone compounds, in which unwanted oxidation and cis/trans isomerization are substantially reduced or eliminated using particular Mitsonobu chemistry.

  这项发明涉及在至少一种抗氧化剂存在的情况下，利用Mitsonobu反应的特定应用制造某些多不饱和化合物。我们发现了一种直接制造药用可接受的多不饱和酯或硫酯化合物的方法，最终可以转化为有利的酮化合物，其中使用特定的Mitsonobu化学方法大大减少或消除了不需要的氧化和題/反式异构化。