Dihydroergocornine mesylate | 14271-04-6

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 麦角林及其衍生物
• 英文名称: Dihydroergocornine mesylate
• 英文别名: dihydroergocomine；12'-hydroxy-2',5'α-diisopropyl-(10α)-9,10-dihydro-ergotamane-18,3',6'-trione; methanesulfonate；12'-Hydroxy-2',5'α-diisopropyl-(10α)-9,10-dihydro-ergotaman-18,3',6'-trion; Methansulfonat；dihydroergocornine methansulfonic acid；dihydroergocornine methanesulfonate；Hydergine；(6aR,9R,10aR)-N-[(1S,2S,4R,7S)-2-hydroxy-5,8-dioxo-4,7-di(propan-2-yl)-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-4-yl]-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline-9-carboxamide;methanesulfonic acid
• CAS: 14271-04-6；29261-94-7
• 化学式: CH₄O₃S*C₃₁H₄₁N₅O₅
• 分子量: 659.804
• InChiKey: UOOWRCRLTSXSAV-GSZJWLEYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.63
• 重原子数：
  46
• 可旋转键数：
  4
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.66
• 拓扑面积：
  181
• 氢给体数：
  4
• 氢受体数：
  9

文献信息

• Ophthalmic ointments for the treatment of glaucoma, comprising ergot alkaloids
  申请人：LEK, tovarna farmacevtskih in kemicnih izdelkov, n.sol.o.

  公开号：EP0342396A1

  公开（公告）日：1989-11-23

  There are described a novel stable ophthalmic ointment for the treatment of increased intraocular pressure in glaucoma patients, comprising a therapeutically effective amount of a peptidic ergot alkaloid of the formula wherein R₁ is hydrogen or halogen, R₂ is hydrogen or alkyl having 1 to 4 carbon atoms, and (i) R₃ is isopropyl, sec. butyl or isobutyl, R₄ is methyl, ethyl or isopropyl, and R₅ is hydrogen and R₆ is hydrogen or methoxy or R₅ and R₆ together are a single bond, or (ii) R₃ is benzyl, R₄ is methyl, R₅ is hydrogen and R₆ is hydrogen or methoxy, in the form of free base or in the form of a pharmaceutically acceptable acid addition salt, in a concentration between 0.005 and 0.05 % by weight in a topically applicable ophthal­mic pharmaceutically acceptable carrier and other excipients, the use thereof in a method for the treatment of increased intraocular pressure in glaucoma patients and a process for preparing the same.

  描述了一种用于治疗青光眼患者眼压升高的新型稳定眼膏，其中含有治疗有效量的肽麦角生物碱，其式为 其中 R₁ 是氢或卤素、 R₂ 是氢或具有 1 至 4 个碳原子的烷基，以及 (i) R₃ 是异丙基、仲丁基或异丁基、 R₄ 是甲基、乙基或异丙基，以及 R₅ 是氢，R₆ 是氢或甲氧基，或 R₅ 和 R₆ 合在一起是单键，或 (ii) R₃ 是苄基，R₄ 是甲基，R₅ 是氢，R₆ 是氢或甲氧基、 以游离碱的形式或以药学上可接受的酸加成盐的形式，在局部适用的眼科药学上可接受的载体和其他赋形剂中的浓度在 0.005 和 0.05 %（重量百分比）之间，将其用于治疗青光眼患者眼压升高的方法和制备方法。
• Preparation of biodegradable microparticles containing a biologically active agent
  申请人：Alkermes Controlled Therapeutics Inc. II

  公开号：EP0998917A1

  公开（公告）日：2000-05-10

  A process for preparing biodegradable microparticles comprising a biodegradable polymeric binder and a biologically active agent. A first phase, comprising the active agent and the polymer, and a second phase are pumped through a static mixer into a quench liquid to form microparticles containing the active agent. Preferably, a blend of at least two substantially non-toxic solvents, free of halogenated hydrocarbons, is used to dissolve or disperse the agent and dissolve the polymer.

  一种制备可生物降解微粒的工艺，包括一种可生物降解聚合物粘合剂和一种生物活性剂。由活性剂和聚合物组成的第一阶段和第二阶段通过静态混合器泵入淬火液，形成含有活性剂的微颗粒。最好使用至少两种基本无毒、不含卤代烃的溶剂混合物来溶解或分散活性剂并溶解聚合物。
• Microparticles
  申请人：Alkermes Controlled Therapeutics Inc. II

  公开号：EP1210942A2

  公开（公告）日：2002-06-05

  The invention provides a particulate material comprising microparticles of a biodegradable biocompatible polymeric matrix containing an active agent and an organic solvent, said organic solvent being present in said microparticles at 2% or less of the total weight of said microparticles.

  本发明提供了一种微粒材料，它由含有活性剂和有机溶剂的可生物降解的生物相容性聚合物基质微粒组成，所述有机溶剂在所述微粒中的含量不超过所述微粒总重量的 2%。
• Apparatus and method for preparing microparticles
  申请人：——

  公开号：US20010031801A1

  公开（公告）日：2001-10-18

  Apparatus and method for preparing microparticles. An emulsion is formed by combining two phases in a static mixing assembly. The static mixing assembly preferably includes a preblending static mixer and a manifold. The emulsion flows out of the static mixing assembly into a quench liquid whereby droplets of the emulsion form microparticles. The residence time of the emulsion in the static mixing assembly is controlled to obtain a predetermined particle size distribution of the resulting microparticles.

  制备微粒的装置和方法。在静态混合组件中将两相混合形成乳液。静态混合组件最好包括一个预混合静态混合器和一个歧管。乳液从静态混合组件流出，进入骤冷液，乳液液滴在骤冷液中形成微粒。控制乳液在静态混合组件中的停留时间，以获得所得微粒的预定粒度分布。
• Preparation of biodegradable, biocompatible microparticles containing a biologically active agent
  申请人：——

  公开号：US20020146457A1

  公开（公告）日：2002-10-10

  A method for preparing biodegradable, biocompatible microparticles. A first phase is prepared that includes a biodegradable, biocompatible polymer, an active agent, and a solvent. A second phase is prepared. The first and second phases are combined to form an emulsion in which the first phase is discontinuous and the second phase is continuous. The discontinuous first phase is separated from the continuous second phase. The residual level of solvent in the discontinuous first phase is reduced to less than about 2% by weight.

  一种制备可生物降解的生物相容性微粒的方法。制备第一阶段，其中包括可生物降解的生物相容性聚合物、活性剂和溶剂。制备第二相。第一相和第二相结合形成乳液，其中第一相是不连续的，第二相是连续的。将不连续的第一相从连续的第二相中分离出来。非连续第一相中溶剂的残留量按重量计降至约 2% 以下。