N-2-(4-(3-thienyl)phenyl)propyl-2-propanesulfonamide | 211311-66-9

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: N-2-(4-(3-thienyl)phenyl)propyl-2-propanesulfonamide
• 英文别名: LY 392098；N-2-(4-(3-thienyl)phenyl)propyl 2-propanesulfonamide；N-[2-(4-thiophen-3-ylphenyl)propyl]propane-2-sulfonamide
• CAS: 211311-66-9
• 化学式: C₁₆H₂₁NO₂S₂
• 分子量: 323.48
• InChiKey: QFAUPDBCVKBKSH-UHFFFAOYSA-N

物化性质

• 沸点：
  444.6±55.0 °C(Predicted)
• 密度：
  1.180±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  21
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  82.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-(4-溴苯基)丙腈 在 四(三苯基膦)钯 aminomethylpolystyrene 、 dimethyl sulfide borane 、 碳酸氢钠 、 potassium carbonate 、 三乙胺 、 三氟乙酸 作用下， 以 四氢呋喃 、 二氯甲烷 、 氯仿 、 甲苯 为溶剂， 反应 21.0h， 生成 N-2-(4-(3-thienyl)phenyl)propyl-2-propanesulfonamide
  参考文献：
  名称：

  Biarylpropylsulfonamides as Novel, Potent Potentiators of 2-Amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic Acid (AMPA) Receptors

  摘要：

  DOI：

  10.1021/jm0002836

文献信息

• Compositions for enhancing memory and methods therefor
  申请人：Baudry Michel

  公开号：US20060063707A1

  公开（公告）日：2006-03-23

  Compositions for enhancing memory of a subject comprising a combination of a positive modulator of an AMPA receptor and a positive modulator of an NMDA receptor are provided, wherein each modulator of the combination is present at a subtherapeutic dose for effecting memory enhancement. Methods for using such compositions in the treatment of cognitive impairment associated with aging, age-related diseases, and CNS disorders, for example, are provided. New fusion molecules are also provided that combine the positive modulator functionalities into one molecule.

  提供了用于增强主体记忆的组合物，包括AMPA受体的正调节剂和NMDA受体的正调节剂，其中组合物中的每种调节剂均以次治疗剂量存在，以实现记忆增强效果。提供了在治疗与衰老、与年龄相关的疾病和中枢神经系统疾病相关的认知障碍中使用这种组合物的方法。还提供了将正调节剂功能结合到一个分子中的新融合分子。
• (BIS)sulfonamide derivatives
  申请人：——

  公开号：US20040054009A1

  公开（公告）日：2004-03-18

  The present invention provides (bis) sulfonamide derivatives of formula (I) useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

  本发明提供了公式(I)的(双)磺胺衍生物，可用于增强哺乳动物的谷氨酸受体功能，因此可用于治疗多种疾病，如精神疾病和神经系统疾病。
• [EN] N-SUBSTITUTED SULFONAMIDE DERIVATIVES<br/>[FR] SULFAMIDES N-SUBSTITUES
  申请人：LILLY CO ELI

  公开号：WO2000006537A1

  公开（公告）日：2000-02-10

  The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

  本发明提供了一些N-取代磺酰胺衍生物，用于增强哺乳动物的谷氨酸受体功能，因此，用于治疗广泛的疾病，如精神和神经系统疾病。
• Sulphonamide derivatives
  申请人：——

  公开号：US20020002158A1

  公开（公告）日：2002-01-03

  Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formula R 1 —L—NHSO 2 R 2 I in which R 1 represents an unsubstituted or substituted aromatic or heteroaromatic group; R 2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R 3 R 4 N in which R 3 and R 4 each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; and L represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are attached form a (3-8C)carbocyclic ring; and pharmaceutically acceptable salts thereof. Also disclosed are novel compounds of formula I, processes for preparing them and pharmaceutical compositions containing them.

  一种具有公式R1-L-NHSO2R2的化合物的有效量可以增强哺乳动物中的谷氨酸受体功能，其中R1表示未取代或取代的芳香或杂环芳香基团；R2表示（1-6C）烷基，（3-6C）环烷基，（1-6C）氟烷基，（1-6C）氯烷基，（2-6C）烯基，（1-4C）烷氧基（1-4C）烷基，苯基，该苯基未取代或通过卤素，（1-4C）烷基或（1-4C）烷氧基取代，或公式R3R4N的基团，其中R3和R4各自独立地表示（1-4C）烷基，或者与它们所连接的氮原子一起形成一个氮杂环基团，包括氮杂丙环基团，吡咯环基团，哌啶环基团，吗啉环基团，哌嗪环基团，六氢氮杂环基团或八氢氮杂环基团；L表示未取代或通过（1-6C）烷基，芳基（1-6C）烷基，（2-6C）烯基，芳基（2-6C）烯基和芳基中选择的一种或两种独立选择的取代基取代的（2-4C）烷基链，或者通过两种取代基与它们所连接的碳原子或碳原子一起形成一个（3-8C）碳环；以及其药学上可接受的盐。还公开了公式I的新化合物，制备它们的过程以及包含它们的制药组合物。
• SULPHONAMIDE DERIVATIVES
  申请人：Arnold B. Macklin

  公开号：US20060030599A1

  公开（公告）日：2006-02-09

  Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formula R 1 -L-NHSO 2 R 2 I in which R 1 represents an unsubstituted or substituted aromatic or heteroaromatic group; R 2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C) chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R 3 R 4 N in which R 3 and R 4 each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; and L represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are attached form a (3-8C)carbocyclic ring; and pharmaceutically acceptable salts thereof. Also disclosed are novel compounds of formula I, processes for preparing them and pharmaceutical compositions containing them.

  一种化合物可以增强哺乳动物中谷氨酸受体的功能，该化合物的化学式为R1-L-NHSO2R2，其中R1表示未取代或取代的芳香或杂芳基团；R2表示(1-6C)烷基，(3-6C)环烷基，(1-6C)氟代烷基，(1-6C)氯代烷基，(2-6C)烯基，(1-4C)烷氧基(1-4C)烷基，苯基，未取代或取代的卤素、(1-4C)烷基或(1-4C)烷氧基，或者公式R3R4N的基团，其中R3和R4各自独立地表示(1-4C)烷基，或者与它们连接的氮原子一起形成氮杂环丙烷基、吡咯烷基、哌啶基、吗啉基、哌嗪基、六氢氮杂环庚烷基或八氢氮杂环二十烷基；L表示未取代或取代的(2-4C)烷基链，该链通过一个或两个独立选择的取代基未取代或取代，这些取代基是(1-6C)烷基，芳基(1-6C)烷基，(2-6C)烯基芳基(2-6C)烯基芳基，或者通过两个取代基与它们连接的碳原子或碳原子形成(3-8C)环状碳基环；以及其药学上可接受的盐。还公开了公式I的新化合物，制备它们的方法以及含有它们的制药组合物。