(4R,4aR,7S,7aR,12bS)-3-prop-2-enyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol;hydron;chloride

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吗啡烷
• 英文名称: (4R,4aR,7S,7aR,12bS)-3-prop-2-enyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol;hydron;chloride
• 化学式: C19H22ClNO3
• 分子量: 347.8
• InChiKey: NAHATSPWSULUAA-ZQGPYOJVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.18
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  52.9
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• 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。
• BIODEGRADABLE STEALTH POLYMERIC PARTICLES FABRICATED USING THE MACROMONOMER APPROACH BY FREE RADICAL DISPERSION POLYMERIZATION
  申请人：AKALA Emmanuel

  公开号：US20120129797A1

  公开（公告）日：2012-05-24

  The present invention is directed to a crosslinked or non-crosslinked polymer particle, wherein the crosslinked polymer particle comprises a copolymer of poly(alklyene glycol-graft-lactate) that is crosslinked by at least one hydrolysable monmer. Another embodiment of the present invention is a polymer particle comprising a crosslinked polymer particle that is a product of starting materials comprising (a) a hydrophilic monomer, (b) a hydrophobic monomer, and (c) a hydrolysable crosslinking agent. Another embodiment of the present invention is a polymer particle comprising, a crosslinked copolymer comprises structures represented by Formulas (I), (II), and (III), where Formulas (I), (II) and (III) are defined in the specification. Yet other embodiments of the present invention include a method of preparing a methacrylate terminated macromonomer, a method of preparing a crosslinking agent, and a method of preparing a therapeutic agent loaded nanosphere by dispersion polymerization.

  本发明涉及交联或非交联聚合物颗粒，其中交联聚合物颗粒包括聚（烷基二醇接枝乳酸酯）共聚物，该共聚物由至少一种可水解单体交联。本发明的另一实施例是聚合物颗粒，包括由起始材料制成的交联聚合物颗粒，该起始材料包括（a）亲水性单体，（b）疏水性单体和（c）可水解交联剂。本发明的另一实施例是聚合物颗粒，包括交联共聚物，其结构由式（I）、（II）和（III）表示，其中式（I）、（II）和（III）在说明书中有定义。本发明的其他实施例包括制备甲基丙烯酸酯末端的大分子单体的方法，制备交联剂的方法以及通过分散聚合制备治疗剂载药纳米球的方法。
• Low molecular weight polymers
  申请人：Huang Yujin

  公开号：US20050238618A1

  公开（公告）日：2005-10-27

  The invention relates to a procedure for purifying low molecular weight polylactic acid polymers by use of reduced temperature liquid-liquid phase separation of the polymers in methanol, ethanol or isopropanol based solvents, compositions comprising the polymers and methods of using the same.

  本发明涉及一种用于通过在甲醇、乙醇或异丙醇基溶剂中使用降温液-液相分离来纯化低分子量聚乳酸聚合物的方法，以及包含该聚合物的组合物和使用方法。
• Combination treatment for alcoholism and alcohol dependence
  申请人：Pfizer Inc.

  公开号：US20030130322A1

  公开（公告）日：2003-07-10

  The present invention relates to a method of treating alcoholism or alcohol dependence in a mammal, including a human, by administering to the mammal a monoamine reuptake inhibitor in combination with an opioid antagonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a monoamine reuptake inhibitor and an opioid antagonist.

  本发明涉及一种治疗哺乳动物（包括人类）酗酒或酒精依赖的方法，该方法包括给哺乳动物以单胺再摄取抑制剂与阿片受体拮抗剂的组合。本发明还涉及含有药学上可接受的载体、单胺再摄取抑制剂和阿片受体拮抗剂的制药组合物。
• Dopamine analog amide
  申请人：——

  公开号：US20010056116A1

  公开（公告）日：2001-12-27

  The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

  该发明涉及使用脂肪酸载体和神经活性药物形成前药。该前药在胃和血液流动环境中稳定，并可通过口服递送。该前药容易穿过血脑屏障。一旦进入中枢神经系统，前药被水解成脂肪酸载体和药物以释放药物。在首选实施方式中，载体是4,7,10,13,16,19二十二碳六烯酸，药物是多巴胺。两者都是中枢神经系统的正常成分。药物和载体之间的共价键通常是酰胺键，这种键可以在胃的条件下存活。因此，前药可以被摄入，并且不会在胃中完全水解成载体分子和药物分子。