Isospirilene

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: Isospirilene
• 英文别名: 8-[(Z)-4-(4-fluorophenyl)pent-3-enyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
• 化学式: C₂₄H₂₈FN₃O
• 分子量: 393.5
• InChiKey: YBPJJOQQWQASHM-SWNXQHNESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  35.6
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Technology for the Preparation of Microparticles
  申请人：Malakhov Michael

  公开号：US20090098207A1

  公开（公告）日：2009-04-16

  Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

  微球是通过将溶液中的大分子或小分子与抗溶剂和对离子接触，并冷却溶液而制备的。这些微球可用于制备具有明确定义尺寸的药物、营养保健品、化妆品等产品。
• Compositions and methods to effect the release profile in the transdermal administration of active agents
  申请人：——

  公开号：US20020004065A1

  公开（公告）日：2002-01-10

  Compositions and methods for the transdermal delivery of active agents up to a period of seven days or more at substantially a zero-order release rate comprising a pharmaceutically acceptable adhesive matrix and a polymeric plastic material that provides a release rate regulating effect on the active agents.

  本发明涉及一种用于经皮递送活性药剂的组合物和方法，该组合物和方法能够在持续时间为七天或更长时间内以几乎零阶释放速率递送活性药剂，包括一种药学上可接受的粘合基质和一种聚合物塑料材料，该聚合物塑料材料对活性药剂具有释放速率调节作用。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Human 5-HT1D receptor (serotonin receptor), process for preparing the same, its uses, antibodies directed against this receptor and transgenics expressing it
  申请人：SYNAPTIC PHARMACEUTICAL CORPORATION

  公开号：EP0787797A1

  公开（公告）日：1997-08-06

  This invention provides isolated nucleic acid molecules encoding human 5-HT1D receptors, isolated proteins which are human 5-HT1D receptors, vectors comprising isolated nucleic acid molecules encoding human 5-HT1D receptors, mammalian cells comprising such vectors, antibodies directed to the human 5-HT1D receptors, nucleic acid probes useful for detecting nucleic acid encoding human 5-HT1D receptors, antisense oligonucleotides complementary to any sequences of a nucleic acid molecule which encodes a human 5-HT1D receptor, pharmaceutical compounds related to human 5-HT1D receptors, and nonhuman transgenic animals which express DNA a normal or a mutant human 5-HT1D receptor. This invention further provides methods for determining ligand binding, detecting expression, drug screening, and treatment involving the human 5-HT1D receptor.

  本发明提供了编码人5-HT1D受体的分离核酸分子、作为人5-HT1D受体的分离蛋白质、包含编码人5-HT1D受体的分离核酸分子的载体、包含此类载体的哺乳动物细胞、针对人5-HT1D受体的抗体、用于检测编码人 5-HT1D 受体的核酸的核酸探针、与编码人 5-HT1D 受体的核酸分子的任何序列互补的反义寡核苷酸、与人 5-HT1D 受体有关的药物化合物，以及表达正常或突变人 5-HT1D 受体 DNA 的非人类转基因动物。本发明进一步提供了涉及人 5-HT1D 受体的配体结合测定、表达检测、药物筛选和治疗方法。
• Transdermal device containing polyvinylpyrrolidone as solubility enhancer
  申请人：NOVEN PHARMACEUTICALS, INC.

  公开号：EP1329225A2

  公开（公告）日：2003-07-23

  A blend of at least three polymers, including a soluble polyvinylpyrrolidone, in combination with a drug provides a pressure-sensitive adhesive composition for a transdermal drug delivery system in which the drug is delivered from the pressure-sensitive adhesive composition and through dermis when the pressure-sensitive adhesive composition is in contact with human skin. Soluble polyvinylpyrrolidone increases the solubility of drug without negatively affecting the adhesivity of the composition or the rate of drug delivery from the pressure-sensitive adhesive composition

  包括可溶性聚乙烯吡咯烷酮在内的至少三种聚合物与药物的混合物为透皮给药系统提供了一种压敏粘合剂组合物，当压敏粘合剂组合物与人体皮肤接触时，药物可从压敏粘合剂组合物中通过真皮输送。可溶性聚乙烯吡咯烷酮增加了药物的溶解度，而不会对组合物的粘附性或压敏胶组合物的给药速率产生负面影响。