苯乙利定 | 469-80-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 苯乙利定
• 中文别名: 苄其度冷丁
• 英文名称: 1-phenethyl-4-phenyl-piperidine-4-carboxylic acid ethyl ester
• 英文别名: 1-Phenaethyl-4-phenyl-piperidin-4-carbonsaeure-aethylester；Ethyl-4-phenyl-1-phenethylpiperidin-4-carboxylat；1-Phenethyl-4-phenyl-4-ethoxycarbonyl-piperidin；Pheneridine；ethyl 4-phenyl-1-(2-phenylethyl)piperidine-4-carboxylate
• CAS: 469-80-7
• 化学式: C₂₂H₂₇NO₂
• 分子量: 337.462
• InChiKey: IUNKCJPURQMGKG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  25
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  1-(β-hydroxy-phenethyl)-4-phenyl-piperidine-4-carboxylic acid ethyl ester; hydrochloride 在 palladium on activated charcoal 、 乙醇 作用下， 生成 苯乙利定
  参考文献：
  名称：

  The Preparation and Analgesic Activity of 4-Carbethoxy-4-phenyl-1-(2-phenylethyl)piperidine and Related Compounds

  摘要：

  DOI：

  10.1021/jo01107a028

文献信息

• Lipid-rich plaque inhibitors
  申请人：——

  公开号：US20030232809A1

  公开（公告）日：2003-12-18

  The present invention provides a lipid-rich plaque regressing agent comprising a compound represented by Formula: 1 in which ring A is a cyclic hydrocarbon or the like; ring B is a heterocyclic ring or the like; each of X and Y is —NR 1 — (in which R 1 is a hydrocarbon or the like); D is a C 1-3 alkylene group or the like; E is —NH— or the like; G is a bond or the like; and Ar is an aryl or the like; D may be taken together with a constituent atom of the ring B to form a ring, and R 4 may be taken together with a constituent atom of the ring B to form a ring.

  本发明提供了一种富含脂质的斑块退行剂，包括一种由式:1所代表的化合物，其中环A是环烃或类似物；环B是杂环或类似物；X和Y中的每一个是—NR1—（其中R1是烃或类似物）；D是C1-3烷基或类似物；E是—NH—或类似物；G是键或类似物；Ar是芳基或类似物；D可以与环B的一个构成原子结合形成环，R4可以与环B的一个构成原子结合形成环。
• Opioids and efflux transporters. Part 1: P-Glycoprotein substrate activity of N-substituted analogs of meperidine
  作者：Susan L. Mercer、Hazem E. Hassan、Christopher W. Cunningham、Natalie D. Eddington、Andrew Coop

  DOI：10.1016/j.bmcl.2006.12.042

  日期：2007.3

  to the development of central tolerance to opioids. The studies herein focus on the development of SAR for P-gp substrate activity in the meperidine series of compounds, and show that a meperidine analog of greater potency, N-phenylbutyl-N-normeperidine, has low activity as a P-gp substrate and has the potential to be utilized as a tool to study the contribution of P-gp to the development of central

  P-糖蛋白 (P-gp) 是一种外排转运蛋白，在吗啡和羟考酮耐受大鼠的血脑屏障中上调。大量研究表明，许多临床使用的阿片类镇痛药是 P-gp 的底物，表明 P-gp 的上调可能有助于阿片类药物中枢耐受的发展。本文的研究重点是哌替啶系列化合物中 P-gp 底物活性的 SAR 开发，并表明效力更强的哌替啶类似物 N-苯基丁基-N-去甲哌替啶作为 P-gp 底物的活性较低，并且有潜力用作研究 P-gp 对阿片类药物中枢耐受性发展的贡献的工具。
• [EN] COUMARIN DERIVATIVE AND USE THEREOF<br/>[FR] DÉRIVÉ DE COUMARINE ET UTILISATION DE CELLE-CI
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2005082879A1

  公开（公告）日：2005-09-09

  The present invention relates to an alkaline earth metal salt or an organic amine salt of a compound represented by the formula [I]: wherein R1 and R2 are each a hydrogen atom, a halogen atom, or an optionally substituted linear hydrocarbon group; ring A is an optionally further substituted benzene ring; B is an optionally substituted benzene ring; R is a carboxyl group or a linear hydrocarbon group substituted with a carboxyl group and the like.

  本发明涉及一种由式[I]所表示的化合物的碱土金属盐或有机胺盐，其中R1和R2分别是氢原子、卤原子或可选择取代的线性碳氢基团；环A是可选择进一步取代的苯环；B是可选取代的苯环；R是羧基或用羧基取代的线性碳氢基团等。
• Abuse-deterrent pharmaceutical compositions of opiods and other drugs
  申请人：Collegium Pharmaceuticals, Inc.

  公开号：US20040052731A1

  公开（公告）日：2004-03-18

  An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

  已经开发了一种滥用抑制药物组合物，旨在降低药物的不当使用的可能性，特别是像阿片类药物这样的药物。在优选实施例中，药物被改性以增加其亲脂性。在优选实施例中，改性药物均匀分散在由缓慢溶解或不溶于水的材料组成的微粒中。在某些实施例中，含药微粒或药物颗粒被涂覆上一层或多层涂层，其中至少一层涂层是不溶于水且最好是有机溶剂不溶性的，但可被人类胃肠道中存在的酶降解。即使该组合物的物理完整性被破坏（例如通过切割或压碎）， resulting material仍然被放入水中、吸入或吞咽，该滥用抑制组合物也会延缓药物的释放。然而，当按照指示使用时，药物会缓慢地从组合物中释放出来，因为组合物会逐渐被酶降解、胆汁酸的表面活性作用和机械侵蚀逐渐破坏或溶解在胃肠道内。
• 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。