4-苯基-1-(4-苯基丁基)哌啶 | 136534-70-8

• 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: 4-苯基-1-(4-苯基丁基)哌啶
• 英文名称: 4-PPBP
• 英文别名: 4-phenyl-1-(4-phenylbutyl)piperidine
• CAS: 136534-70-8
• 化学式: C₂₁H₂₇N
• 分子量: 293.452
• InChiKey: HQGDPZPNAXRCSA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  22
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  4-苯基丁酰氯 在 lithium aluminium tetrahydride 、 三乙胺 作用下， 以 四氢呋喃 、 乙醚 为溶剂， 反应 2.0h， 生成 4-苯基-1-(4-苯基丁基)哌啶
  参考文献：
  名称：

  Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity .sigma. ligands

  摘要：

  Sigma-receptors may represent an exciting new approach for the development of novel psychotherapeutic agents. Unfortunately, many of the commonly used sigma-ligands lack selectivity (e.g., many bind at phencyclidine or dopamine receptors) or suffer from other serious drawbacks. Recently, we described a series of 2-phenylaminoethanes that bind at sigma-receptors with high affinity and selectivity. Because there is evidence that 1-phenylpiperazines can structurally mimic the 2-phenylaminoethane moiety, we prepared a series of 1-phenylpiperazines and related analogues and incorporated structural features already shown to enhance the sigma-binding of the 2-phenylaminoethanes. Several of these derivatives bind at sigma-receptors with high affinity (K(i) = 1-10 nM) and lack appreciable affinity for phencyclidine and dopamine receptors. In as much as certain of these agents structurally resemble the high-affinity, but nonselective, sigma-ligand haloperidol, and because they bind with 10 times the affinity of haloperidol, we have apparently identified what appears to be the primary sigma-pharmacophore of that agent.

  DOI：

  10.1021/jm00116a003

文献信息

• Haircare use of cyclic amine derivatives
  申请人：Cavezza Alexandre

  公开号：US20060193804A1

  公开（公告）日：2006-08-31

  The present invention relates to a process for treating human keratin fibers and/or the skin from which the said fibers emerge, in order to induce and/or stimulate the growth of the human keratin fibers and/or to stop their loss and/or to increase their density, comprising at least the application, to the human keratin fibers and/or the skin, of a cosmetic composition comprising an effective amount of at least one piperidine derivative of general formula (I), in which: R 1 denotes a halogen or a radical chosen from a linear or branched C 1 -C 6 alkyl radical, a group OR, a group NRR′, a CF 3 group, a group NHCOR or a group CONRR′; R 2 denotes a linear or branched C 1 -C 20 alkyl or alkenyl radical, the hydrocarbon-based chain of which may be optionally interrupted with a —CO— function optionally substituted with at least one group OR, COOR, NRR′, NHCOR or CONRR′ and/or with a phenyl group optionally substituted with one or more radicals R 1 ; with R and R′ denoting, independently of each other, a hydrogen atom or a linear or branched C 1 -C 6 alkyl radical, m represents an integer ranging from 0 to 5; and n represents an integer ranging from 0 to 5. or a salt or isomer thereof, leaving the said composition in contact with the keratin fibers and/or the skin from which the fibers emerge, and optionally rinsing the keratin fibers and/or the skin.

  本发明涉及一种处理人类角蛋白纤维和/或这些纤维生长的皮肤的方法，以诱导和/或刺激人类角蛋白纤维的生长和/或阻止它们的脱落和/或增加它们的密度，包括至少将含有至少一种一般式(I)的哌啶衍生物的有效量的化妆品组合物施用于人类角蛋白纤维和/或皮肤，其中： R1表示卤素或从线性或支链的C1-C6烷基基团、OR基团、NRR′基团、CF3基团、NHCOR基团或CONRR′基团中选择的基团； R2表示线性或支链的C1-C20烷基或烯基基团，其碳氢基链可以选配地被具有至少一个OR、COOR、NRR′、NHCOR或CONRR′基团和/或一个苯基（该苯基可以选择地被一个或多个基团R1取代）的—CO—功能中断，其中R和R′独立地表示氢原子或线性或支链的C1-C6烷基基团，m表示一个范围从0到5的整数；n表示一个范围从0到5的整数，或者其盐或异构体，将该组合物留在与角蛋白纤维和/或这些纤维生长的皮肤接触，然后选择性地冲洗角蛋白纤维和/或皮肤。
• [EN] USE OF PIPERIDINE DERIVATIVES AS DERMO-DECONTRACTING AGENTS<br/>[FR] UTILISATION DE DERIVES PIPERIDINES EN TANT QU'AGENTS DE DERMO-DECONTRACTION
  申请人：OREAL

  公开号：WO2006003030A1

  公开（公告）日：2006-01-12

  The present invention relates to a cosmetic process for treating wrinkled skin, in particular the skin of the face and/or of the forehead, through a dermo-decontracting effect, comprising the topical application to said skin of a composition comprising, in a physiologically acceptable medium, at least one piperidine derivative chosen from the compounds of formula (I). These compounds make it possible to combat expression wrinkles according to a mechanism of dermo-decontraction.

  本发明涉及一种用于治疗皱纹皮肤的化妆过程，特别是面部和/或前额皮肤，通过皮肤-去收缩效应，包括将含有至少一种哌啶衍生物的组成物局部应用于该皮肤中，所述哌啶衍生物选择自式（I）化合物。这些化合物能够通过皮肤-去收缩机制对抗表情皱纹。
• Butyrophenones and sigma-1 receptor antagonists protect against oxidative-stress
  申请人：Schetz A. John

  公开号：US20060106064A1

  公开（公告）日：2006-05-18

  The present invention includes compositions and methods for the protection of one or more central nervous system cells from trauma, when administered before, during or after the trauma, wherein the composition includes an effective amount of a butyrophenone, e.g., a 1-linked phenyl butyrophenone that is electronegative along the butyl chain and/or a Sigma-1 receptor antagonist.

  本发明涉及一种组合物和方法，用于在创伤前、期间或后保护一个或多个中枢神经系统细胞，其中该组合物包括有效量的丁酰苯类化合物，例如，沿着丁基链电负性的1-连接苯基丁酰苯类化合物和/或Sigma-1受体拮抗剂。
• Use of Piperidine Derivatives as Dermo-Decontracting Agents
  申请人：Cavezza Alexandre

  公开号：US20070259915A1

  公开（公告）日：2007-11-08

  The present invention relates to a cosmetic process for treating wrinkled skin, in particular the skin of the face and/or of the forehead, through a dermo-decontracting effect, comprising the topical application to said skin of a composition comprising, in a physiologically acceptable medium, at least one piperidine derivative chosen from the compounds of formula (I). These compounds make it possible to combat expression wrinkles according to a mechanism of dermo-decontraction.

  本发明涉及一种美容处理方法，用于治疗皱纹皮肤，特别是面部和/或额头皮肤，通过皮肤松弛效应，包括将一种含有至少一种哌啶衍生物的组合物局部应用于所述皮肤中，所述哌啶衍生物选择自式（I）化合物。这些化合物可以通过皮肤松弛机制来对抗表情皱纹。
• USE OF PIPERIDINE DERIVATIVES AS DERMO-DECONTRACTING AGENTS
  申请人：Cavezza Alexandre

  公开号：US20100048624A1

  公开（公告）日：2010-02-25

  The present invention relates to a cosmetic process for treating wrinkled skin, in particular the skin of the face and/or of the forehead, through a dermo-decontracting effect, comprising the topical application to said skin of a composition comprising, in a physiologically acceptable medium, at least one piperidine derivative chosen from the compounds of formula (I): These compounds make it possible to combat expression wrinkles according to a mechanism of dermo-decontraction.

  本发明涉及一种用于治疗皱纹皮肤的化妆过程，特别是面部和/或额头皮肤，通过皮肤松弛效应，包括将含有至少一种从式(I)化合物中选择的哌啶衍生物的组合物局部应用于该皮肤中，所述组合物在生理上可接受的介质中。这些化合物能够通过皮肤松弛机制来对抗表情皱纹。