N,alpha,alpha-三甲基苯乙胺硫酸盐(2:1) | 1212-72-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N,alpha,alpha-三甲基苯乙胺硫酸盐(2:1)
• 中文别名: 美芬丁胺半硫酸盐 标准品
• 英文名称: Mephentermin-hemisulfat
• 英文别名: (1,1-dimethyl-2-phenyl-ethyl)-methyl-amine; sulfate；(1,1-Dimethyl-2-phenyl-aethyl)-methyl-amin; Sulfat；mephentermine sulphate；mephentermine sulfate；N,2-dimethyl-1-phenylpropan-2-amine;sulfuric acid
• CAS: 1212-72-2
• 化学式: C₁₁H₁₇N*H₂O₄S
• 分子量: 261.342
• InChiKey: NZKLHVGUPFNBFD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.57
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  95
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N,alpha,alpha-三甲基苯乙胺硫酸盐(2:1) 、 N-BOC-亚氨基二乙酸 在 二乙胺 、 bromo-tris(1-pyrrolidinyl)phosphonium hexafluorophosphate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 48.0h， 以20%的产率得到N,N'-Bis-(α,α-dimethylphenyethyl)-N,N'-dimethyl-tert-butyloxycarbonyl-iminodiacetamid
  参考文献：
  名称：

  Unterhalt; Wenning, Pharmazie, 2001, vol. 56, # 1, p. 58 - 60

  摘要：

  DOI：

文献信息

• Skin penetration system for salts of amine-functional drugs
  申请人：THE PROCTER & GAMBLE COMPANY

  公开号：EP0351897A2

  公开（公告）日：1990-01-24

  The invention involves pharmaceutical compositions for topical application comprising: (a) a pharmaceutically-acceptable salt of addition of an amine-functional drug (other than opioid analgesic drugs); (b) a C₇ to C₂₂ straight-chain or branched-chain, saturated or unsaturated, fatty acid having a melting point of less than about 50°C; and (c) a C₃-C₄ alkane diol.

  本发明涉及用于局部应用的药物组合物，包括 (a) 一种胺功能药物（阿片类镇痛药除外）的药学上可接受的加成盐； (b) C₇ 至 C₂₂ 直链或支链、饱和或不饱和脂肪酸，熔点低于约 50°C；以及 (c) C₃-C₄ 烷二醇。
• An otorhinological drug delivery device
  申请人：Schering Oy

  公开号：EP1438942A1

  公开（公告）日：2004-07-21

  The invention relates to an otorhinological delivery device comprising at least one pharmaceutically active agent. According to the invention the device comprises a core comprising said at least one pharmaceutically active agent wherein said core is made of an elastomer composition selected from the group consisting of poly(dimethylsiloxane), a siloxane-based elastomer comprising 3,3,3-trifluoropropyl groups attached to the Si-atoms of the siloxane units, a siloxane-based elastomer comprising poly(alkylene oxide) groups and mixtures thereof.

  本发明涉及一种包含至少一种药用活性剂的耳鼻喉给药装置。根据本发明，该装置包括一个包含所述至少一种药物活性剂的芯体，其中所述芯体由弹性体组合物制成，该弹性体组合物选自聚（二甲基硅氧烷）、硅氧烷基弹性体（包含连接到硅氧烷单元S原子上的3,3,3-三氟丙基）、硅氧烷基弹性体（包含聚（环氧烷）基团）及其混合物组成的组。
• Preparation of submicron sized particles with polymorph control
  申请人：——

  公开号：US20030096013A1

  公开（公告）日：2003-05-22

  The present invention provides a method of preparing particles with polymorph and size control of a pharmaceutical compound, the method including the steps of: (1) providing a pharmaceutical compound in a first phase; (2) seeding the compound; (3) causing a phase change in the pharmaceutical compound to a second phase of a desired polymorphic form; and (4) wherein the mean particle size of the particles is less than 7 &mgr;m.

  本发明提供了一种制备具有多晶型和尺寸控制的药物化合物颗粒的方法，该方法包括以下步骤：(1)提供第一相中的药物化合物；(2)播种该化合物；(3)使药物化合物发生相变，变成所需多晶型的第二相；(4)其中颗粒的平均粒度小于7&mgr;m。
• Synthesis and Structure−Activity Relationships of Trisubstituted Phenyl Urea Derivatives as Neuropeptide Y5 Receptor Antagonists
  作者：Christopher Fotsch、Jennifer D. Sonnenberg、Ning Chen、Clarence Hale、William Karbon、Mark H. Norman

  DOI：10.1021/jm0004547

  日期：2001.7.1

  1-((1R,2R)-2-Hydroxy-1-methyl-2-phenylethyl)-1-methyl-3-(4-phenoxyphenyl)urea (1) was identified as a hit from the screening of the neuropeptide Y5 (NPY5) receptor. This lead was optimized for in vitro potency by changing the stereochemistry, the phenylethyl segment, the urea portion, and the 4-phenoxyphenyl group on the molecule. Over 40 analogues of 1 were prepared to study the structure-activity relationship for this series. The most potent compounds in this class have IC(50)s less than 0.1 nM at the NPY5 receptor (e.g., 40f, 44a, and 47). To determine the functional activity for this series of compounds, selected analogues were tested in acellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor. All urea analogues tested in the functional assay acted as antagonists (e.g., 1, 32, 40a, and 44e).
• PREPARATION OF SUBMICRON SIZED PARTICLES WITH POLYMORPH CONTROL AND NEW POLYMORPH OF ITRACONAZOLE
  申请人：BAXTER INTERNATIONAL INC.

  公开号：EP1534239A2

  公开（公告）日：2005-06-01