N-cyclohexanoylphenylalanine Aldehyde | 209127-92-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-cyclohexanoylphenylalanine Aldehyde
• 英文别名: cyclohexanoyl-phenylalanine aldehyde；N-[(2S)-1-oxo-3-phenylpropan-2-yl]cyclohexanecarboxamide
• CAS: 209127-92-4
• 化学式: C₁₆H₂₁NO₂
• 分子量: 259.348
• InChiKey: ITFVSOSPSXRHDM-HNNXBMFYSA-N

物化性质

• 沸点：
  453.7±34.0 °C(Predicted)
• 密度：
  1.089±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  46.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  甲基 3-苯基-DL-丙氨酸酯 、 环己甲酰氯 以 吡啶 为溶剂， 生成 N-cyclohexanoylphenylalanine Aldehyde 、 N-cyclohexanoylphenylalanine methyl ester
  参考文献：
  名称：

  Compositions and methods for enhanced mucosal delivery of Y2 receptor-binding peptides and methods for treating and preventing obesity

  摘要：

  描述了包含至少一种Y2受体结合肽（如肽YY（PYY）、神经肽Y（NPY）或胰岛素肽（PP））和一种或多种黏膜传递增强剂的药物组合物和方法，以增强肽YY在鼻黏膜中的传递，用于治疗哺乳动物主体中的多种疾病和病况，包括肥胖。

  公开号：

  US20040157777A1

文献信息

• Oral drug delivery compositions and methods
  申请人：Emisphere Technologies, Inc.

  公开号：US05766633A1

  公开（公告）日：1998-06-16

  The present invention relates to an oral drug delivery system, and in particular to modified amino acids and modified amino acid derivatives for use as a delivery system of sensitive agents such as bioactive peptides. The modified amino acids and derivatives can form non-covalent mixtures with active biological agents and in an alternate embodiment can releasably carry active agents. Modified amino acids can also form drug containing microspheres. These mixtures are suitable for oral administration of biologically active agents to animals. Methods for the preparation of such amino acids are also disclosed.

  本发明涉及口服药物输送系统，特别是用作敏感剂（如生物活性肽）输送系统的改性氨基酸和改性氨基酸衍生物。这些改性氨基酸和衍生物可以与活性生物制剂形成非共价混合物，并在另一实施例中可以可释放地携带活性剂。改性氨基酸还可以形成含药微球。这些混合物适用于将生物活性剂口服给动物。还公开了制备这种氨基酸的方法。
• Active agent transport systems
  申请人：Emisphere Technologies, Inc.

  公开号：US20010039258A1

  公开（公告）日：2001-11-08

  Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of: (a) providing a biologically active agent which can exist in a native conformational state, a denatured conformational state, and an intermediate conformational state which is reversible to the native state and which is conformationally between the native and denatured states; (b) exposing the biologically active agent to a complexing perturbant to reversibly transform the biologically active agent to the intermediate state and to form a transportable supramolecular complex; and (c) exposing the membrane or bilayer to the supramolecular complex, to transport the biologically active agent across the membrane or bilayer. The perturbant has a molecular weight between about 150 and about 600 daltons, and contains at least one hydrophilic moiety and at least one hydrophobic moiety. The supramolecular complex comprises the perturbant non-covalently bound or complexed with the biologically active agent. In the present invention, the biologically active agent does not form a microsphere after interacting with the perturbant. A method for preparing an orally administrable biologically active agent comprising steps (a) and (b) above is also provided as are oral delivery compositions. Additionally, mimetics and methods for preparing mimetics are contemplated.

  跨越细胞膜或脂质双层传输生物活性物质的方法。第一种方法包括以下步骤：（a）提供一种生物活性物质，该生物活性物质可以存在于原生构象状态、变性构象状态和中间构象状态，该中间构象状态可逆转至原生状态，且在构象上介于原生态和变性态之间；（b）将生物活性物质暴露于复合扰动剂中，以可逆地将生物活性物质转变为中间状态，并形成可传输的超分子复合物；（c）将膜或双层暴露于超分子复合物中，以跨越膜或双层传输生物活性物质。扰动剂的分子量介于约150至约600道尔顿之间，并含有至少一个亲水性基团和至少一个疏水性基团。超分子复合物包括非共价地结合或复合的扰动剂和生物活性物质。在本发明中，生物活性物质与扰动剂相互作用后不会形成微球。还提供了一种制备口服生物活性物质的方法，包括上述步骤（a）和（b），以及口服给药组合物。此外，还考虑了类似物和制备类似物的方法。
• COMPOSITIONS AND METHODS FOR ENHANCED MUCOSAL DELIVERY OF PYY PEPTIDE
  申请人：Quay C. Steven

  公开号：US20070129299A1

  公开（公告）日：2007-06-07

  Pharmaceutical compositions are described comprising PYY(3-36) (SEQ ID NO: 2), a solubilizing agent, a lipid, a polyol.

  本文描述了一种药物组合物，其中包含PYY(3-36) (序列ID号：2)，一种溶解剂，一种脂质和一种多元醇。
• A DEVICE FOR ENHANCED EPITHELIAL PERMEATION OF Y2 RECEPTOR-BINDING PEPTIDES
  申请人：Quay C. Steven

  公开号：US20070161563A1

  公开（公告）日：2007-07-12

  A pharmaceutical device comprising a composition comprising an aqueous solution of PYY(3-36), a cyclodextrin, and a compound selected from phosphatidylcholine or diglyceride, wherein the cyclodextrin and the compound selected from phosphatidylcholine or diglyceride are present in an amount sufficient to enhance epithelial permeation, and wherein the composition is present in a container; and an actuator fluidly connected to the container, wherein the actuator has a tip which defines a passage through which the solution is ejected to produce a spray of the solution.

  一种药物器具，包括一种组合物，该组合物包括PYY（3-36）的水溶液、环糊精和从磷脂酰胆碱或二甘酸选择的化合物，其中环糊精和从磷脂酰胆碱或二甘酸选择的化合物的含量足以增强上皮渗透，且该组合物存在于容器中；以及与容器流体连接的作动器，其中作动器具有一个尖端，其定义了一个通道，通过该通道喷射出解液以产生解液喷雾。
• COMPOSITIONS FOR ENHANCED EPITHELIAL PERMEATION OF Y2 RECEPTOR-BINDING PEPTIDES
  申请人：Quay C. Steven

  公开号：US20070197437A1

  公开（公告）日：2007-08-23

  Pharmaceutical compositions comprising a PYY peptide, a cyclodextrin, and a compound selected from phosphatidylcholine or diglyceride, wherein the cyclodextrin and the compound selected from phosphatidylcholine or diglyceride are present in an amount sufficient to enhance epithelial permeation.

  药物组合物包括PYY肽、环糊精和从磷脂酰胆碱或二甘酸酯中选择的化合物，其中环糊精和从磷脂酰胆碱或二甘酸酯中选择的化合物的含量足以增强上皮渗透。