美克法胺 | 66960-34-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 美克法胺
• 英文名称: metkephamid
• 英文别名: (2S)-2-[[(2S)-2-[[2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]-methylamino]-4-methylsulfanylbutanamide
• CAS: 66960-34-7
• 化学式: C₂₉H₄₀N₆O₆S
• 分子量: 600.739
• InChiKey: FWDIKROEWJOQIQ-JMBSJVKXSA-N

物化性质

• 沸点：
  1009.0±65.0 °C(Predicted)
• 密度：
  1.275±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  42
• 可旋转键数：
  16
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  222
• 氢给体数：
  6
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  [(S)-1-{(R)-1-[({(S)-1-[((S)-1-Carbamoyl-3-methylsulfanyl-propyl)-methyl-carbamoyl]-2-phenyl-ethylcarbamoyl}-methyl)-carbamoyl]-ethylcarbamoyl}-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid tert-butyl ester 生成 美克法胺
  参考文献：
  名称：

  SMITHWICK, E. L. ,, JR;FREDERICKSON, R. C. A.;SHUMAN, R. T.

  摘要：

  DOI：

文献信息

• [EN] CARBONATE PRODRUGS AND METHODS OF USING THE SAME<br/>[FR] PROMÉDICAMENTS CARBONATÉS ET LEURS MÉTHODES D'UTILISATION
  申请人：NEUROGESX INC

  公开号：WO2009143297A1

  公开（公告）日：2009-11-26

  The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

  本发明提供了碳酸盐前药，其包括连接到母药基团的羟基或羧基上的碳酸磷酸酐前药基团。这些前药可能比母药具有改进的物理化学性质。还提供了使用碳酸盐前药治疗对母药具有响应的疾病或症状的方法，以及配套工具和单剂量。
• Novel lipidomimetic compounds and uses thereof
  申请人：Koninklijke Philips Electronics N.V.

  公开号：EP2535326A1

  公开（公告）日：2012-12-19

  Disclosed are lipidomimetic compounds of formula I wherein: G represents a group satisfying formula II:          HO-CH2-CH(OH)-CH2-O}p-CH2-C(=O)-O-CH2}q-     formula II each n independently is an integer from 1-30; p is an integer from 1-10; q is 0 or 1. These compounds can be added to the lipid bilayer of thermosensitive liposomes, for the purpose of aiding in the prevention of leakage of the liposomes' contents at 37°C, and retarding clearance from circulation.

  揭示了具有以下结构的脂类拟拟物化合物：其中：G代表满足以下结构的基团II：         HO-CH2-CH(OH)- -O}p- -C(=O)-O- }q-        结构II每个n独立地是1-30之间的整数；p是1-10之间的整数；q为0或1。这些化合物可以添加到热敏感脂质体的脂质双层中，以帮助防止在37°C时脂质体内容物的泄漏，并延缓从循环中清除。
• (S)-N-Stereoisomers of 7,8-Saturated-4,5-Epoxy-Morphinanium Analogs
  申请人：Perez Julio

  公开号：US20080207669A1

  公开（公告）日：2008-08-28

  Novel (S)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the (S)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs and methods for their pharmaceutical uses are also disclosed. Such analogs are disclosed as being useful in treating, among varying conditions, hypermotility of the gastrointestinal tract.

  本专利揭示了7,8-饱和-4,5-环氧-吗啡盐类的（S）-N-立体异构体。还揭示了含有7,8-饱和-4,5-环氧-吗啡盐类（S）-N-立体异构体的药物组合物，以及其药用方法。这些类似物被发现可用于治疗多种情况，包括胃肠道过度运动。
• DELAYED TOTAL RELEASE TWO PULSE GASTROINTESTINAL DRUG DELIVERY SYSTEM
  申请人：——

  公开号：US20020110593A1

  公开（公告）日：2002-08-15

  A two pulse gastrointestinal delivery system is provided. The system comprises a desired agent in combination with a swellable core material, the core being surrounded by an inner coat of a water-insoluble or relatively water-insoluble coating material in which particulate water-insoluble material is embedded. The inner coat is additionally surrounded by an outer coat that contains additional amounts of the desired agent. When the delivery device enters the gastrointestinal tract, the outer coat releases the desired agent contained therein and disintegrates, exposing the inner coat. The particulate matter in the inner coat takes up liquid, thus forming channels interconnecting the drug-containing core with the outside of the delivery device. Through these channels liquid enters the core which then swells to the point at which the inner coat is broken. When the integrity of the inner coat is destroyed, the core then disintegrates, immediately releasing all or most of the drug at a specific site. By controlling parameters in the device, such as the core material, carrier material in the coating, and particulate matter, the location of release of both pulses of the drug can be carefully controlled. The invention is also directed to a method of using the device for the treatment of disease by the release of drugs in the gastrointestinal tract in a location- and time-dependent manner.

  提供了一种双脉冲胃肠传递系统。该系统包括所需药剂与可膨胀的核心材料相结合，该核心被内层包裹着一层水不溶性或相对水不溶性的涂层材料，其中嵌入了颗粒状水不溶性材料。内层涂层另外被一个包含额外所需药剂的外层包裹。当传递装置进入胃肠道时，外层释放其中所含的所需药剂并分解，暴露内层涂层。内层涂层中的颗粒物质吸收液体，从而形成连接含药核心与传递装置外部的通道。通过这些通道，液体进入核心，然后核心膨胀到内层涂层破裂的程度。当内层涂层的完整性破坏时，核心随后分解，立即在特定部位释放全部或大部分药物。通过控制装置中的参数，如核心材料、涂层中的载体材料和颗粒物质，可以精确控制药物双脉冲释放的位置。该发明还涉及一种利用该装置以位置和时间依赖方式在胃肠道释放药物进行疾病治疗的方法。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。