2-(p-hydroxyphenyl) thio-5-thiophenesulfonamide | 63032-04-2

• 分子结构分类: 有机化合物 - 有机硫化合物 - 硫醚类
• 英文名称: 2-(p-hydroxyphenyl) thio-5-thiophenesulfonamide
• 英文别名: 2-Thiophenesulfonamide,5-[(4-hydroxyphenyl)thio]-；5-(4-hydroxyphenyl)sulfanylthiophene-2-sulfonamide
• CAS: 63032-04-2
• 化学式: C₁₀H₉NO₃S₃
• 分子量: 287.384
• InChiKey: JCMWXSNEOWKVAZ-UHFFFAOYSA-N

物化性质

• 熔点：
  124-126 °C(Solv: N,N-dimethylformamide (68-12-2))
• 沸点：
  578.8±60.0 °C(Predicted)
• 密度：
  1?+-.0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  142
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-(p-hydroxyphenyl) thio-5-thiophenesulfonamide 在 双氧水 作用下， 以 溶剂黄146 为溶剂， 反应 1.0h， 以70%的产率得到5-[(4-羟基苯基)磺酰基]-噻吩-2-磺酰胺
  参考文献：
  名称：

  Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 3. 5-(Arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides

  摘要：

  A series of 5-(arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides is described and anticonvulsant activities are listed for the compounds. In most cases, the sulfones had the highest activity and the sulfides the least. Sulfones with 3- or 4-halo substituents generally had the highest activity, and one analogue, 5-[(4-fluorophenyl)sulfonyl]thiophene-2-sulfonamide (51, UK-17022), had an anticonvulsant ED50 fo 2 mg/kg when administered orally to mice. Compound 51 selectively increased cerebral blood flow in animals without an unacceptable level of diuresis.

  DOI：

  10.1021/jm00140a009
• 作为产物：
  描述：

  5-溴噻吩-2-磺酰胺 、 4-羟基苯硫酚 在 sodium hydroxide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 4.0h， 以51%的产率得到2-(p-hydroxyphenyl) thio-5-thiophenesulfonamide
  参考文献：
  名称：

  Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 3. 5-(Arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides

  摘要：

  A series of 5-(arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides is described and anticonvulsant activities are listed for the compounds. In most cases, the sulfones had the highest activity and the sulfides the least. Sulfones with 3- or 4-halo substituents generally had the highest activity, and one analogue, 5-[(4-fluorophenyl)sulfonyl]thiophene-2-sulfonamide (51, UK-17022), had an anticonvulsant ED50 fo 2 mg/kg when administered orally to mice. Compound 51 selectively increased cerebral blood flow in animals without an unacceptable level of diuresis.

  DOI：

  10.1021/jm00140a009

文献信息

• Pharmaceutical composition of the type which undergoes liquid-gel phase transition
  申请人：LABORATOIRES MERCK, SHARP & DOHME-CHIBRET

  公开号：EP0227494A1

  公开（公告）日：1987-07-01

  The present invention relates to a pharmaceutical composition intended for contacting with a physiological liquid characterized in that said composition is intended to be administered as a non-gelled liquid form and is intended to gel in situ, this composition containing at least one polysaccharide in aqueous solution, of the type which undergoes liquid-gel phase transition gelling in situ under the effect of an increase in the ionic strength of said physiological liquid.

  本发明涉及一种用于与生理液体接触的药物组合物，其特征在于所述组合物以非凝胶液体形式给药，并可在原位凝胶，该组合物含有至少一种水溶液中的多糖，这种多糖在所述生理液体离子强度增加的作用下发生液-凝胶相变，在原位凝胶。
• Apparatus for removing components from solutions
  申请人：CIBA-GEIGY AG

  公开号：EP0567431A1

  公开（公告）日：1993-10-27

  An apparatus for removing components from solutions, in particular a dispensing device having a container body defining a solution retaining chamber therein, the container having an outlet for dispensing the solution from the chamber and means for removing a component from the solution as the solution is dispensed from the chamber through the container outlet. A method is provided for administering to a patient a pharmacologically active substance which substance is stable only at a pH value which is extreme in the acidic or alkaline region and at which pH value the substance cannot be administered without causing discomfort and/or injury to the patient. The substance is maintained in a solution or dispersion at the pH at which it is stable until the time of administration. At this time the substance is administered through a chamber containing an ion exchange resin which changes the pH of the solution or dispersion to a value which will not cause discomfort and/or injury to the patient.

  一种从溶液中去除成分的装置，特别是一种分配装置，它有一个容器体，其中限定了一个溶液保持腔，容器有一个出口，用于从腔中分配溶液，当溶液通过容器出口从腔中分配时，用于从溶液中去除成分的装置。本发明提供了一种向患者施用药理活性物质的方法，该物质只有在 pH 值处于酸性或碱性极端区域时才稳定，而在该 pH 值下施用该物质不会对患者造成不适和/或伤害。在给药之前，该物质一直保持在其稳定的 pH 值溶液或分散液中。此时，通过一个含有离子交换树脂的腔室给药，该树脂可将溶液或分散液的 pH 值改变到不会对患者造成不适和/或伤害的值。
• REVERSELY THERMO-REVERSIBLE HYDROGEL COMPOSITIONS
  申请人：Broda Technologies Co., Ltd

  公开号：EP2689774A1

  公开（公告）日：2014-01-29

  A reversely thermo-reversible hydrogel composition comprising a water soluble block copolymer comprising at least two blocks of polyethylene oxide and at least one block of polypropylene oxide, and at least one associative gelling adjuvant having water solubility less than 0.5 g/100ml, preferably less than 0.3 g/100 ml at 20 °C, and being capable of forming water soluble inter-molecular complexes with the water soluble block copolymer in water. The hydrogel composition exhibits improved gelling efficiency, enhanced solubility and/or stability for water sparely soluble and insoluble pharmaceutical agents. The hydrogel compositions are useful in a variety of pharmaceutical and cosmetic products and applications, such as esophageal, otic, vaginal, rectal, ophthalmic, and treatments of disorders and imperfections of the skin.

  一种反向热可逆水凝胶组合物，它包含一种水溶性嵌段共聚物，该嵌段共聚物由至少两个聚环氧乙烷嵌段和至少一个聚环氧丙烷嵌段组成；以及至少一种缔合胶凝佐剂，该佐剂在 20 °C 时的水溶性小于 0.5 克/100 毫升，最好小于 0.3 克/100 毫升，并能与水溶性嵌段共聚物在水中形成水溶性分子间络合物。这种水凝胶组合物的胶凝效率提高，对水溶性和不溶性药剂的溶解度和/或稳定性增强。这种水凝胶组合物适用于各种医药和化妆品及应用，如食道、耳道、阴道、直肠、眼科以及皮肤疾病和瑕疵的治疗。
• Ophthalmic compositions including oil-in-water emulsions, and methods for making and using same
  申请人：Allergan, Inc.

  公开号：US20030165545A1

  公开（公告）日：2003-09-04

  Ophthalmic compositions comprising an oil-in-water emulsion, preferably a self-emulsifying oil-in-water emulsion, including an oily component, an aqueous component and a surfactant component. The surfactant component may include three or more surfactants, for example, a polyoxyalkalene alkylene ether, a polyalkylene oxide ether of alkyl alcohol and a polyalkylene oxide ether of alkylphenol. The present compositions may include therapeutic components. Methods of making such compositions and using such compositions, for example, to treat eyes, to treat contact lenses and to provide desired therapeutic effects are provided.

  由水包油乳液（最好是自乳化型水包油乳液）组成的眼科组合物，包括油性组分、水性组分和表面活性剂组分。表面活性剂组分可包括三种或三种以上的表面活性剂，例如聚氧亚烷基烷基醚、烷基醇聚氧亚烷基醚和烷基酚聚氧亚烷基醚。本组合物可包括治疗成分。提供了制造这种组合物和使用这种组合物的方法，例如，治疗眼睛、治疗隐形眼镜和提供所需的治疗效果。
• Self-emulsifying compositions, methods of use and preparation
  申请人：——

  公开号：US20040185068A1

  公开（公告）日：2004-09-23

  Preparation of self-emulsifying compositions which are prepared without mechanical homogenization is described. These self-emulsifying compositions are prepared using one or two surfactants. This provides the advantage of a low weight ratio of emulsifying component to oil component and fewer chemical toxicity concerns, resulting in comfort and safety advantages over emulsions employing more than two emulsifiers. Consequently, the self-emulsifying compositions described are ideally suited for ophthalmic applications including administration of therapeutics to the eye. Self-emulsifying compositions prepared by the disclosed method are described.

  描述了无需机械均质即可制备的自乳化组合物的制备方法。这些自乳化组合物使用一种或两种表面活性剂制备。与使用两种以上乳化剂的乳液相比，这种自乳化组合物具有乳化剂成分与油成分重量比低、化学毒性问题少的优点，因而具有舒适性和安全性方面的优势。因此，所述自乳化组合物非常适合用于眼科应用，包括眼部给药。本文介绍了用所公开的方法制备的自乳化组合物。