(3α,14β)14,15-dihydro-20,21-dinoreburnamenin-14-ol | 68779-67-9

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吲哚萘啶生物碱
• 英文名称: (3α,14β)14,15-dihydro-20,21-dinoreburnamenin-14-ol
• 英文别名: Vindeburnolum；(15R,17R,19S)-1,11-diazapentacyclo[9.6.2.02,7.08,18.015,19]nonadeca-2,4,6,8(18)-tetraen-17-ol
• CAS: 68779-67-9
• 化学式: C₁₇H₂₀N₂O
• 分子量: 268.359
• InChiKey: KOIGYXJOGRVNIS-LYRGGWFBSA-N

物化性质

• 沸点：
  482.5±45.0 °C(Predicted)
• 密度：
  1.46±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  20
• 可旋转键数：
  0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  28.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  (3α,14α)-14,15-dihydro-20,21-dinoreburnamenin-14-ol 、 盐酸 生成 (3α,14β)14,15-dihydro-20,21-dinoreburnamenin-14-ol
  参考文献：
  名称：

  AKTOGU, NURGUM;CLEMENCE, FRANCOIS;OBERLANDER, CLAUDE

  摘要：

  DOI：

文献信息

• Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol, and applications thereof
  申请人：Ciapetti Paola

  公开号：US20070088046A1

  公开（公告）日：2007-04-19

  The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical —AR′ wherein A represents a heteroatom and R′ represents a group selected from the group comprising linear or branched C 1 -C 6 alkyl radicals, C 2 -C 6 alkenyls, C 2 -C 6 alkynyls, arylalkyls; esters comprising the formula —R 1 — CO—O—R 2 ; amides comprising the formula —R 3 —CO—NZY, wherein Y and Z together can form a cycloalkyl radical or a heterocyclic radical, optionally substituted by one or more alkyl radicals; a radical selected from the group comprising alkyl radicals, alkenyls or alkynyls, substituted by at least one amine with formula —NZY; or one of the pharmaceutically-acceptable salts thereof, including the isomers, enantiomers and diastereoisomers thereof and mixtures thereof. The invention also relates to the use of the novel derivatives for the preparation of a pharmaceutical composition which is intended, in particular, for the treatment and/or prevention of depression, sleep-wake cycle disorders and symptomatic frontal disorders in cognitive components among humans.

  该发明涉及14,15-二氢20,21-二诺雷布鲁美宁-14-醇的新衍生物，其化学式为（I），其中R代表一个基团-AR′，其中A代表一个杂原子，R′代表从包括线性或支链C1-C6烷基基团、C2-C6烯基、C2-C6炔基、芳基烷基的基团中选取的一个基团；酯类包括化学式-R1—CO—O—R2；酰胺类包括化学式-R3—CO—NZY，其中Y和Z共同形成一个环烷基基团或一个杂环基团，可以选择地被一个或多个烷基基团取代；从包括被至少一个胺基（化学式为—NZY）取代的烷基、烯基或炔基基团中选取的一个基团；或者其药学上可接受的盐，包括其异构体、对映异构体和立体异构体以及它们的混合物。该发明还涉及利用这些新化合物制备药物组合物，该组合物特别用于治疗和/或预防人类中的抑郁症、睡眠-清醒周期紊乱和认知成分中的症状性额叶紊乱。
• Use of 14,15-dihydro-20,21-dinoreburnamenin-14-ol for the treatment and/or prevention of serious depression and sleep/waking cycle disorders
  申请人：Pujol Jean-Francois

  公开号：US20070155769A1

  公开（公告）日：2007-07-05

  The invention relates to a novel therapeutic use of 14,15-dihydro-20,21-dinoreburnamenin-14-ol for the treatment of serious depression in humans, particularly for the treatment of a patients resistant to conventional anti-depressant treatments and for treatment of sleep/waking cycle disorders.

  该发明涉及使用14,15-二氢-20,21-二去氧热巴曼宁-14-醇的新型治疗用途，用于治疗人类严重抑郁症，特别是用于治疗对传统抗抑郁治疗方法有抵抗性的患者以及治疗睡眠/清醒周期障碍。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• Treatment of synucleinopathies
  申请人：Deutsches Zentrum für Neurodegenerative Erkrankungen e. V. (DZNE)

  公开号：US10918628B2

  公开（公告）日：2021-02-16

  A modulator of PDE1A and/or PDE1C can be used as a medicament, in particular in the prevention or treatment of synucleinopathies, such as multiple system atrophy, dementia with Lewy bodies, Parkinson's disease, pure autonomic failure, rapid eye movement sleep behavior disorder, inherited synucleinopathies caused by mutations or multiplications of the SNCA gene, or synucleinopathies caused by mutations in other genes including, but not limited to, GBA, LRRK2 and PARK2.

  PDE1A 和/或 PDE1C 的调节剂可用作药物，特别是用于预防或治疗突触核蛋白病，如多发性系统萎缩症、路易体痴呆症、帕金森病、纯自律神经衰竭、快速眼动睡眠行为障碍、由 SNCA 基因突变或增殖引起的遗传性突触核蛋白病，或由其他基因突变引起的突触核蛋白病，包括但不限于 GBA、LRRK2 和 PARK2。
• Therapeutic formulations for the treatment of beta-amyloid related diseases
  申请人：Gervais Francine

  公开号：US20050031651A1

  公开（公告）日：2005-02-10

  This invention relates to methods and pharmaceutical compositions for treating amyloid-β related diseases, including Alzheimer's disease. The invention, for example, includes a method of concomitant therapeutic treatment of a subject, comprising administering an effective amount of a first agent and a second agent, wherein said first agent treats an amyloid-β disease, neurodegeneration, or cellular toxicity; and said second agent is a therapeutic drug or nutritive supplement.

  本发明涉及治疗淀粉样蛋白-β相关疾病（包括阿尔茨海默病）的方法和药物组合物。例如，本发明包括一种同时治疗受试者的方法，包括施用有效量的第一种药剂和第二种药剂，其中所述第一种药剂治疗淀粉样蛋白-β疾病、神经变性或细胞毒性；所述第二种药剂是治疗药物或营养补充剂。