司考维林 | 57558-44-8

• 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: 司考维林
• 英文名称: secoverine
• 英文别名: 3[N-ethyl-[1-methyl-2-(4-methoxyphenyl)]-ethylamino]-propylcyclohexylketone；1-cyclohexyl-4-[ethyl-[1-(4-methoxyphenyl)propan-2-yl]amino]butan-1-one
• CAS: 57558-44-8；90237-04-0
• 化学式: C₂₂H₃₅NO₂
• 分子量: 345.525
• InChiKey: WAVYHSURRZBQKO-UHFFFAOYSA-N

物化性质

• 沸点：
  471.8±35.0 °C(Predicted)
• 密度：
  0.999±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  25
• 可旋转键数：
  10
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.68
• 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：

  sodium 、 3-环己基-3-氧代丙酸乙酯 、 2-[N-ethyl-[1-methyl-2-(4-methoxy-phenyl)]-ethylamino]-ethylchloride 在 硫酸 、 potassium carbonate 作用下， 以 二氯甲烷 、 水 、 丙酮 、 甲苯 、 苯 为溶剂， 生成 司考维林
  参考文献：
  名称：

  Spasmolytics

  摘要：

  化学式为3的三级胺具有强烈且持久的解痉作用，即使经口服也能作用于胃肠道、泌尿道和支气管系统的平滑肌，且毒性低。这些化合物可以按照已知的方法合成，并制成药物组合物。

  公开号：

  US03996245A1

文献信息

• TRANSMUCOSAL DELIVERY OF PHARMACEUTICAL ACTIVE SUBSTANCES
  申请人：JON Sangyong

  公开号：US20070292387A1

  公开（公告）日：2007-12-20

  Provided is a conjugate including a pharmacologically active substance covalently bound to chitosan or its derivative and a method for transmucosal delivery of a pharmacologically active substance using the same. Specifically, a conjugate includes a pharmacologically active substance covalently bound via a linker to chitosan; and a pharmaceutical composition for transmucosal administration of a drug includes the aforementioned conjugate and a pharmaceutically acceptable carrier. Further provided is a method for in vivo delivery of a pharmacologically active substance via a transmucosal route, by covalent binding of the active substance with chitosan or its derivative via a linker. The conjugate in accordance with the present invention exhibits excellent absorption rate and biocompatibility in biological mucous membranes, particularly mucous membranes of the alimentary canal (especially the gastrointestinal tract), in vivo degradability, and superior bioavailability even with oral administration, thus enabling treatment of diseases via oral administration of a drug.

  提供的是一个包括药理活性物质与壳聚糖或其衍生物共价结合的共轭物，以及使用该共轭物进行药理活性物质经粘膜途径传递的方法。具体来说，该共轭物包括通过连接剂与壳聚糖共价结合的药理活性物质；以及用于经粘膜途径给药的药物组合物包括上述共轭物和药学上可接受的载体。此外，提供了一种通过药理活性物质与壳聚糖或其衍生物通过连接剂共价结合的方式，经粘膜途径在体内传递药理活性物质的方法。根据本发明的共轭物在生物粘膜，特别是消化道（尤其是胃肠道）的粘膜中表现出优异的吸收速率和生物相容性，在体内可降解性，以及即使口服也具有优越的生物利用度，从而使得通过口服给药治疗疾病成为可能。
• [EN] THIOSEMICARBAZONES WITH MDR1 - INVERSE ACTIVITY<br/>[FR] THIOSEMICARBAZONES À ACTIVITÉ ANTI-MDR1
  申请人：US HEALTH

  公开号：WO2012033601A1

  公开（公告）日：2012-03-15

  Disclosed herein are drug compounds that have MDR-inverse activity and thus are effective against multidrug-resistant cells. Exemplary compounds disclosed herein have the structure;Formula (I). Examples of the disclosed compounds have been found to have, inter alia, efficacy in directly treating multidrug resistant cells, rendering multidrug resistant cells susceptible to other chemotherapeutics and in some instances reversing multidrug resistance.

  本文披露了具有MDR逆转活性的药物化合物，因此对多药耐药细胞有效。本文披露的示例化合物具有下列结构；公式（I）。已发现披露的化合物的示例具有直接治疗多药耐药细胞的功效，使多药耐药细胞对其他化疗药物敏感，并在某些情况下逆转多药耐药。
• 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。
• 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。
• Spasmolytically active (+)S-enantiomer of secoverine
  申请人：DUPHAR INTERNATIONAL RESEARCH B.V

  公开号：EP0100569A1

  公开（公告）日：1984-02-15

  The invention concerns spasmolytically active pharmaceutical compositions, and the preparation thereof, containing (+) S-1-cyclohexyl-4-[ethyl-(p-methoxy-a-methylphenethyl)amino]-1-butanone or a salt thereof as the active component. It has been found that this (+) S-enantiomer is about twice as active as the racemate (which is known as secoverine). This better activity is not related with a proportional increase of undesired side-effects.

  本发明涉及具有解痉活性的药物组合物及其制备方法，其活性成分为(+) S-1-环己基-4-[乙基-(对甲氧基-a-甲基苯乙基)氨基]-1-丁酮或其盐。 研究发现，这种 (+) S-对映体的活性约为外消旋体（即 secoverine）的两倍。这种较好的活性与不良副作用的增加并不成正比。