(4R)-Isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate

• 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
• 英文名称: (4R)-Isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate
• 英文别名: isopropyl 2-methoxyethyl 4-(2-chloro-3-cyanophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate；rac-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate；(Rac)-MEM 1003；3-O-(2-methoxyethyl) 5-O-propan-2-yl 4-(2-chloro-3-cyanophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
• 化学式: C₂₂H₂₅ClN₂O₅
• 分子量: 432.904
• InChiKey: GTIKSQYSAKETQA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  30
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  97.6
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  (-)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyanophenyl)-2,6-dimethylpyridine-3,5-dicarboxylate 以 甲醇 为溶剂， 生成 (4R)-Isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate
  参考文献：
  名称：

  Process for the preparation of optically active ortho-substituted

  摘要：

  该发明涉及一种通过氧化和随后还原其对映异构体制备光学活性的邻取代的4-芳基或杂芳基-1,4-二氢吡啶的过程。

  公开号：

  US05708177A1

文献信息

• Pyrrolidine compounds and process of preparing
  申请人：Bayer Aktiengesellschaft

  公开号：US05700948A1

  公开（公告）日：1997-12-23

  This invention relates to benzolididene compounds of the formula ##STR1## in which R.sup.2 represents the radical ##STR2## in which R.sup.4 and R.sup.5 are identical or different and denote halogen, cyano, ethinyl, trifluoromethoxy, methylthio, nitro, trifluoromethyl or straight-chain or branched alkyl, alkenyl, alkinyl or alkoxy having up to 4 carbon atoms, and one of the substituents optionally represents hydrogen, or a salt thereof.

  这项发明涉及化学式为##STR1##的苯并二亚胺化合物，其中R.sup.2代表基团##STR2##，其中R.sup.4和R.sup.5相同或不同，表示卤素、氰基、乙炔基、三氟甲氧基、甲硫基、硝基、三氟甲基或直链或支链烷基、烯基、炔基或烷氧基，碳原子数最多为4个，并且其中的一个取代基可以是氢，或其盐。
• Isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,
  申请人：Bayer Aktiengesellschaft

  公开号：US05665740A1

  公开（公告）日：1997-09-09

  The present invention relates to the new compound rac-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)1,4 -dihydro-2,6-dimethylpyridine-3,5-dicarboxylate and its pure enantiomers, processes for their preparation and their use as medicaments, in particular for the treatment of cerebral and neuronal disorders, and a new intermediate for their preparation.

  本发明涉及一种新化合物 rac-异丙基-2-甲氧基乙基-4-(2-氯-3-氰基苯基)1,4-二氢-2,6-二甲基吡啶-3,5-二羧酸酯及其纯对映体，其制备过程以及它们作为药物的用途，特别是用于治疗脑和神经系统疾病，并提供了一种新的制备它们的中间体。
• Compositions and methods of treatment using L-type calcium channel blockers and cholinesterase inhibitors
  申请人：Memory Pharmaceuticals Corporation

  公开号：EP1952824A1

  公开（公告）日：2008-08-06

  The present invention relates to compositions at least one L-type calcium channel blocker, particularly the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, in combination with at least one cholinesterase inhibitor, particularly donepezil, and uses thereof in methods of treatment.

  本发明涉及至少一种L型钙通道阻滞剂，特别是化合物(+)-2-甲氧基乙基4-(2-氯-3-氰基苯基)-1,4-二氢-2,6-二甲基吡啶-3,5-二甲酸异丙酯，与至少一种胆碱酯酶抑制剂，特别是多奈哌齐的组合物及其在治疗方法中的用途。
• Transdermal delivery systems with pharmacokinetics bioequivalent to oral delivery
  申请人：Corium International, Inc.

  公开号：US10016372B2

  公开（公告）日：2018-07-10

  A method for delivering a therapeutic agent to a subject from a transdermal delivery system is described, where the therapeutic agent (i) has a half-life in the blood when delivered orally of greater than about 48 hours and (ii) is for the treatment of a chronic condition. The transdermal delivery system achieves transdermal delivery of the therapeutic agent at steady state that is bioequivalent to administration of the therapeutic agent orally, wherein bioequivalency is established by (a) a 90% confidence interval of the relative mean Cmax and AUC of the therapeutic agent administered from the transdermal delivery system and via oral delivery between 0.70 and 1.43 or between 0.80 and 1.25, or (b) a 90% confidence interval of the ratios for AUC and Cmax of the therapeutic agent administered from the transdermal delivery system and via oral delivery between 0.70 and 1.43 or between 0.80 and 1.25.

  描述了一种通过透皮给药系统向受试者提供治疗剂的方法，其中治疗剂(i) 口服时在血液中的半衰期大于约 48 小时，(ii) 用于治疗慢性疾病。透皮给药系统在稳态时实现治疗剂的透皮给药，其生物等效性与口服给药相等，其中生物等效性的确定标准是：(a)透皮给药系统给药和口服给药的治疗剂相对平均 Cmax 和 AUC 的 90%置信区间在 0.70和1.43之间或0.80和1.25之间，或(b)透皮给药系统给药和通过口服给药的治疗剂的AUC和Cmax的比率的90%置信区间在0.70和1.43之间或0.80和1.25之间。
• Memantine transdermal delivery systems
  申请人：Corium, Inc.

  公开号：US10945968B2

  公开（公告）日：2021-03-16

  Transdermal delivery systems for the systemic delivery of memantine are described, wherein the system comprises a drug reservoir layer and an adhesive layer, optionally together with one or more intermediate and/or supporting layers, wherein the drug reservoir layer comprises an acrylate polymer or copolymer, a permeation enhancer, a carrier, and memantine base generated in situ by reaction of a memantine salt and an alkaline salt. Compositions and kits comprising the various components, e.g., drug reservoir and/or adhesive compositions are described. Methods relating to treatment of CNS disorders, e.g., Alzheimer's disease and/or dementia, using the aforementioned transdermal delivery devices and/or compositions are also described.

  描述了用于全身给药美金刚烷的透皮给药系统，其中该系统包括储药层和粘合剂层，可选择与一个或多个中间层和/或支撑层一起使用，其中储药层包括丙烯酸酯聚合物或共聚物、渗透促进剂、载体和通过美金刚烷盐和碱性盐反应就地生成的美金刚烷碱。本文介绍了包含各种成分的组合物和试剂盒，例如药物储层和/或粘合剂组合物。还介绍了使用上述透皮给药装置和/或组合物治疗中枢神经系统疾病（如阿尔茨海默病和/或痴呆症）的方法。