1,4-二氢-2,6-二甲基-4-(2-硝基苯基)-3,5-吡啶二羧酸二甲酯盐酸盐(1:1)

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 1,4-二氢-2,6-二甲基-4-(2-硝基苯基)-3,5-吡啶二羧酸二甲酯盐酸盐(1:1)
• 英文名称: dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;hydron;chloride
• 化学式: C17H19ClN2O6
• 分子量: 382.8
• InChiKey: ISQGFMPRCDAJRT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Processes of manufacturing substituted-1,4-dihydropyridines, improved aqueous solutions thereof, and processes of manufacturing the solutions
  申请人：Jobdevairakkam Christopher N.

  公开号：US20080125595A1

  公开（公告）日：2008-05-29

  A process of preparing a stable parenteral solution of a 1,4-dihydropyridine salt, such as nicardipine hydrochloride, in an acidic aqueous medium. The presence of L-arginine in the solution enhances the solubility of the salt, which is poorly soluble in water. An aqueous, injectable isotonic solution at pH about 3.5-3.6 consists essentially of nicardipine hydrochloride, L-arginine, and a sugar alcohol. An improved single pot manufacturing process for obtaining unsymmetrical 1,4-dihydropyridines by using more than one mole equivalent of aldehyde with respect to the other reactants (amino crotonate and acetoacetate ester). The reaction can be conducted in a solvent present at 20 times the amount of any one component. A process for changing one polymorph of nicardipine hydrochloride (Form A) into another (Form B), and a separate process for the reverse (Form B into Form A).

  一种制备1,4-二氢吡啶盐（如盐酸尼卡地平）的稳定无菌溶液的工艺，该工艺在酸性水介质中进行。溶液中存在L-精氨酸，可增强盐的溶解度，而盐在水中溶解度较差。该无菌溶液为水溶性、注射用的等渗溶液，pH值约为3.5-3.6，主要由盐酸尼卡地平、L-精氨酸和糖醇组成。 一种改进的单锅制造工艺，用于通过使用超过其他反应物（氨基丙烯酸酯和乙酰乙酸酯）的摩尔当量的醛类来获得非对称的1,4-二氢吡啶。该反应可以在溶剂中进行，溶剂的量为任何一个组分的20倍。 一种将尼卡地平盐酸的一种多晶形式（A型）转变为另一种多晶形式（B型）的工艺，以及将B型转变为A型的单独工艺。
• pH-mediated drug delivery system
  申请人：Merck & Co., Inc.

  公开号：EP0197504A2

  公开（公告）日：1986-10-15

  57 A transdermal delivery system suitable for administering a weakly acidic or basic drug is described which comprises a substantially impermeable backing member, a drug reservoir comprising the drug, a hydroxylated solvent and a buffering agent, and a membrane selectively permeable to the unionized form of the drug and substantially impermeable to the ionized form of the drug and the buffer salts.

  57 描述了一种适用于施用弱酸性或弱碱性药物的透皮给药系统，该系统包括一个基本不透水的衬垫部件，一个由药物、羟化溶剂和缓冲剂组成的药物贮存器，以及一个可选择性渗透药物结合形式、基本不渗透药物离子化形式和缓冲盐的膜。
• REMEDY FOR ANXIETY NEUROSIS
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：EP0846465A1

  公开（公告）日：1998-06-10

  N-(2-Hydroxyethyl)nicotinamide nitrate or its salt prevents or ameliorates anxiety neurosis or panic disorder, or the following anxiety. This compound or its salt has few side effects and exhibits immediate action.

  硝酸 N-(2-羟乙基)烟酰胺或其盐类可预防或改善焦虑性神经症或恐慌症或以下焦虑症。这种化合物或其盐几乎没有副作用，而且能立即发挥作用。
• MUCOSAL PREPARATION CONTAINING PHYSIOLOGICALLY ACTIVE PEPTIDE
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：EP0845265A1

  公开（公告）日：1998-06-03

  A preparation for transmucosal administration admixed with at least absorption promotor and vasodilator in physiologically active peptide is provided. Absorption of the physiologically active peptide can be increased by combining the peptide with absorption promotor and a compound having vasodilating activity. Accordingly auto-administration can be performed by the patients without pain of injection. It is useful for long term administration of physiologically active peptide.

  本研究提供了一种用于经粘膜给药的制剂，其中至少掺入了生理活性肽的吸收促进剂和血管扩张剂。通过将生理活性肽与吸收促进剂和具有血管扩张活性的化合物结合，可增加生理活性肽的吸收。因此，患者可以在没有注射痛苦的情况下进行自动给药。这对长期服用具有生理活性的多肽非常有用。
• Anti-adhesion barrier comprising carboxymethylcellulose and gellan gum
  申请人：Amitie Co., Ltd.

  公开号：EP1323436A1

  公开（公告）日：2003-07-02

  Anti-adhesion barrier compositions for preventing adhesion between tissues at an surgical lesion comprising sodium carboxymethyl cellulose and gellan gum in a weight ratio of 1 : (0.2 to 5), preferably 1 : (0.8 to 1.25). The compositions may further contain from 0.2 to 5 parts by weight of one or more of interleukine-10, hyaluronate, heparin, nifedipine HCl, phosphatidylcholine, medroxyprogestone acetate, L-arginine, nitric oxide, polyvinylalcohol (PVA), protein inhibitor and dextran per 1 part by weight of the sodium carboxymethyl cellulose and/or from 0.02 to 0.06 parts by weight of an antibiotic substance per 1 part by weight of the sodium carboxymethyl cellulose.

  用于防止手术病灶处组织间粘连的抗粘连屏障组合物，由羧甲基纤维素钠和结冷胶组成，重量比为 1 : (0.2 至 5)，最好是 1 : (0.8 至 1.25)。按每 1 份羧甲基纤维素钠的重量计，组合物还可含有 0.2 至 5 份（按重量计）白细胞介素-10、透明质酸、肝素、盐酸硝苯地平、磷脂酰胆碱、醋酸甲羟孕酮、L-精氨酸、一氧化氮、聚乙烯醇（PVA）、蛋白质抑制剂和葡聚糖中的一种或多种，和/或 0.02 至 0.06 份（按重量计）羧甲基纤维素钠。或每 1 份（重量）羧甲基纤维素钠含 0.02 至 0.06 份（重量）抗生素物质。