Estrapronicate | 4140-20-9

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: Estrapronicate
• 英文别名: [(8R,9S,13S,14S,17S)-13-methyl-3-propanoyloxy-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] pyridine-3-carboxylate
• CAS: 4140-20-9
• 化学式: C₂₇H₃₁NO₄
• 分子量: 433.5
• InChiKey: FXMSQUVSUXBBAB-TXDQRGGKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  65.5
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• 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。
• Pharmaceutical preparations based on active ingredients susceptible to illict administration
  申请人：ALTERGON S.A.

  公开号：EP1273301A2

  公开（公告）日：2003-01-08

  The present invention provides oral pharmaceutical preparations unsuitable for illicit administration to victims.

  本发明提供了不适合非法给受害者服用的口服药物制剂。
• Fulvestrant formulation
  申请人：AstraZeneca AB

  公开号：EP1669073A2

  公开（公告）日：2006-06-14

  The invention relates to a novel sustained release pharmaceutical formulation adapted for administration by injection containing the compound 7α-[9-(4,4,5,5,5-pentafluoropentylsulphmyl)nonyl]oestra-1,3,5(10)-thene-3,17β-diol, more particularly to a formulation adapted for administration by injection containing the compound 7α-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17β-diol in solution in a ricinoleate vehicle which additionally comprises at least one alcohol and a non-aqueous ester solvent which is miscible in the ricinoleate vehicle.

  本发明涉及一种适用于注射给药的新型缓释药物制剂，该制剂含有化合物 7α-[9-(4,4,5,5,5-五氟戊基亚磺酰基)壬基]雌甾-1,3,5(10)-三烯-3,17β-二醇，特别是涉及一种适用于注射给药的制剂，该制剂含有化合物 7α-[9-(4、7α-[9-(4,5,5,5-五氟戊基亚磺酰基)壬基]雌甾-1,3,5(10)-三烯-3,17β-二醇在蓖麻油酸盐载体中的溶液。
• METHOD FOR MANUFACTURING VAGINAL DRUG DELIVERY SYSTEMS USING A THREE DIMENSIONAL PRINTER
  申请人：Delim Cosmetics & Pharma S.r.l.

  公开号：EP3501543A1

  公开（公告）日：2019-06-26

  The present invention relates to a method for manufacturing a controlled release vaginal ring using a three-dimensional (3D) printer, said vaginal ring comprising: a) a core, said core consisting of a composition comprising one or more thermoplastic polyurethanes and one or more active pharmaceutical ingredients dissolved or dispersed in said core, b) a membrane, substantially or completely surrounding said core, said membrane consisting of a composition comprising one or more thermoplastic polyurethanes.

  本发明涉及一种使用三维（3D）打印机制造控释阴道环的方法，所述阴道环包括 a) 核心，所述核心由一种或多种热塑性聚氨酯组成，以及一种或多种溶解或分散在所述核心中的活性药物成分、 b) 基本或完全围绕所述核心的膜，所述膜由一种或多种热塑性聚氨酯组成。
• Methods of dissociating nongenotropic from genotropic activity of steroid receptors
  申请人：——

  公开号：US20020137209A1

  公开（公告）日：2002-09-26

  This invention concerns the fundamental discovery of the understanding of the mechanism of action of steroidal nongenotropic effects and their relation to steroidal genotropic effects. It has been discovered that (i) steroidal nongenotropic effects and genotropic effects can be mediated by the same steroid receptor; (ii) both effects are ligand-induced; (iii) the nongenotropic effect occurs due to a ligand-induced activation of the ligand binding domain, which can be fast and loose fitting; (iv) the genotropic effect occurs due to a ligand-induced activation of the DNA-binding domain of the steroid receptor, which is typically a result of a slower, stronger interaction; and (v) the nongenotropic effect of a ligand interaction can be dissociated from the genotropic effect of a ligand interaction, in such a manner to effect a selective response. This invention also describes, for the first time, that certain steroids are capable of inducing a nongenotropic effect via binding to an unrelated steroid receptor

  本发明涉及对类固醇非肾上腺素作用的作用机理及其与类固醇趋基因作用的关系的认识的基本发现。研究发现：(i) 类固醇的非趋肾作用和趋基因作用可以由同一个类固醇受体介导；(ii) 这两种作用都是配体诱导的；(iii) 非趋肾作用是由于配体诱导激活配体结合域而产生的，这种激活可以是快速的，也可以是松散的；(iv) 促基因作用是由于配体诱导激活了类固醇受体的 DNA 结合结构域，这通常是较慢、较强相互作用的结果；以及 (v) 配体相互作用的非促基因作用可以从配体相互作用的促基因作用中分离出来，从而产生选择性反应。本发明还首次描述了某些类固醇能够通过与不相关的类固醇受体结合而诱导非肾上腺素效应。