(+)-N-methylphysostigmine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: (+)-N-methylphysostigmine
• 英文别名: [(3aS,8bR)-3,4,8b-trimethyl-2,3a-dihydro-1H-pyrrolo[2,3-b]indol-7-yl] N,N-dimethylcarbamate
• 化学式: C₁₆H₂₃N₃O₂
• 分子量: 289.378
• InChiKey: IUHMWLMDASQDJQ-GOEBONIOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  36
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  (+)-esermethole 在 吡啶 、 三溴化硼 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 生成 (+)-N-methylphysostigmine
  参考文献：
  名称：

  Yu, Qian-Sheng; Brossi, Arnold, Heterocycles, 1988, vol. 27, # 3, p. 745 - 750

  摘要：

  DOI：

文献信息

• [EN] TARGETED DRUG DELIVERY THROUGH AFFINITY BASED LINKERS<br/>[FR] ADMINISTRATION CIBLÉE D'UN MÉDICAMENT FAISANT APPEL À DES COUPLEURS FONDÉS SUR L'AFFINITÉ
  申请人：INVICTUS ONCOLOGY PVT LTD

  公开号：WO2015148126A1

  公开（公告）日：2015-10-01

  The current invention discloses targeted drug delivery conjugates comprising a targeting moiety linked to a drug via a molecule having an affinity for the targeting moiety. Typically, the conjugate comprises a targeting ligand and a molecule of interest, e.g., a therapeutic agent. The targeting ligand and the molecule of interest are linked to each other via an affinity ligand. The affinity ligand is further covalently or non-covalently linked to a drug or therapeutic agent. The drug can be modified to make it more soluble and so that it cleaves from the linking molecule at the target site.

  当前的发明揭示了包括通过具有与靶向基团亲和力的分子连接到药物的靶向药物传递共轭物。通常，该共轭物包括一个靶向配体和一个感兴趣的分子，例如，一个治疗剂。靶向配体和感兴趣的分子通过一个亲和配体相互连接。该亲和配体进一步以共价或非共价方式连接到药物或治疗剂。药物可以被修改以使其更溶解，并使其在靶点处从连接分子中解离。
• Biodegradable ocular implants and methods for treating ocular conditions
  申请人：Burkstrand J. Michael

  公开号：US20080089923A1

  公开（公告）日：2008-04-17

  Biodegradable ocular implants are described. The ocular implants include a bioactive agent that can be released within the eye to treat an ocular condition or indication. The implants can be used for the administration of a bioactive agent over prolonged periods of time. In some aspects the implants are formed of a matrix of natural biodegradable polysaccharides.

  可降解眼部植入物被描述。这些眼部植入物包括可以在眼内释放的生物活性剂，用于治疗眼部疾病或症状。这些植入物可用于在较长时间内给药生物活性剂。在某些方面，这些植入物由天然可降解多糖的基质形成。
• Latent stabilization of bioactive agents releasable from implantable medical articles
  申请人：Burkstrand Michael J.

  公开号：US20080154241A1

  公开（公告）日：2008-06-26

  Implantable medical articles comprising natural biodegradable polysaccharides are described. The polysaccharides can provide desirable release properties, and can also be degraded into products that can act as an excipient in the presence of the bioactive agent. In some aspects, the articles are ocular implants formed of a matrix of natural biodegradable polysaccharides. These ocular implants include a bioactive agent that can be released within the eye to treat an ocular condition or indication.

  描述了包含天然可生物降解多糖的可植入医疗器械。这些多糖可以提供理想的释放特性，并且在生物活性剂存在的情况下也可以降解为可作为赋形剂的产物。在某些方面，这些器械是由天然可生物降解多糖构成的眼部植入物。这些眼部植入物包括可以在眼内释放的生物活性剂，用于治疗眼部疾病或症状。
• CELL DELIVERY COMPOSITIONS
  申请人：——

  公开号：US20010006817A1

  公开（公告）日：2001-07-05

  The present invention provides improved cell delivery compositions. In particular, the invention provides biocompatible endosomolytic agents. In a preferred embodiment, the endosomolytic agents are also biodegradable and can be broken down within cells into components that the cells can either reuse or dispose of. Preferred endosomolytic agents include cationic polymers, particularly those comprised of biomolecules, such as histidine, polyhistidine, polylysine or any combination thereof. Other exemplary endosomolytic agents include, but are not limited to, other imidazole containing compounds such as vinylimidazole and histamine. More particularly preferred are those agents having multiple proton acceptor sites and acting as a “proton sponge”, disrupting the endosome by osmolytic action. In preferred embodiments, the endosomolytic agent comprises a plurality of proton acceptor sites having pKas within the range of 4 to 7, which endosomal lysing component is polycationic at pH 4. The present invention also contemplates the use of these endosomolytic agents as delivery agents by complexation with the desired compound to be delivered. Thus, the present invention also acts as a cell delivery system comprising an endosomolytic agent, a delivery agent, and a compound to be delivered.

  本发明提供了改进的细胞递送组合物。具体而言，本发明提供了生物相容的内体溶解剂。在一个优选实施例中，内体溶解剂也是可生物降解的，可以在细胞内分解为细胞可以重新利用或处置的组分。优选的内体溶解剂包括阳离子聚合物，特别是由生物分子组成的聚组氨酸，如组氨酸、多组氨酸、多赖氨酸或二者的任意组合。其他示例性的内体溶解剂包括但不限于其他含咪唑醇基的化合物，如乙烯咪唑和组胺。更具体优选的是那些具有多个质子受体位点并作为“质子海绵”起作用的剂，通过渗透调节作用破坏内体。在优选实施例中，内体溶解剂包括具有pKa在4到7范围内的多个质子受体位点的内体溶解组分，在pH 4时为多阳离子性的。本发明还考虑了将这些内体溶解剂作为递送剂通过与要递送的化合物结合的复合物的使用。因此，本发明还作为一个细胞递送系统，包括一个内体溶解剂、一个递送剂和一个要递送的化合物。
• Agents useful for reducing amyloid precursor protein and treating demantia and methods of use thereof
  申请人：——

  公开号：US20040138282A1

  公开（公告）日：2004-07-15

  The present invention provides compounds and methods of administering compounds to a subject taht can reduce &bgr;APP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce &bgr;APP production and that is not tocix in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease &bgr;APP production.

  本发明提供了化合物和给予这些化合物给受试者的方法，可以减少βAPP的产生，并且在广泛剂量范围内不具有毒性。本发明还提供了非碳酸酯化合物和给予这些化合物给受试者的方法，可以减少βAPP的产生，并且在广泛剂量范围内不具有毒性。已经发现无论是混合物还是对映纯的非碳酸酯化合物都可以用于降低βAPP的产生。