N-(5-benzoyl-2-(4-(2-methoxyphenyl)piperazin-1-yl)thiazol-4-yl)pivalamide | 1137536-21-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-(5-benzoyl-2-(4-(2-methoxyphenyl)piperazin-1-yl)thiazol-4-yl)pivalamide
• 英文别名: KRO-105714；N-{5-benzoyl-2-[4-(2-methoxyphenyl)piperazin-1-yl]thiazoyl-4-yl}pivalamide；66G2Urf5HG；N-[5-benzoyl-2-[4-(2-methoxyphenyl)piperazin-1-yl]-1,3-thiazol-4-yl]-2,2-dimethylpropanamide
• CAS: 1137536-21-0
• 化学式: C₂₆H₃₀N₄O₃S
• 分子量: 478.615
• InChiKey: AMMLHWSENDUVHR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.1
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  103
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] NOVEL 2,4,5-TRISUBTITUTED-1,3-THIAZOLE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PREPARATION, THERAPEUTIC AGENT FOR INFLAMMATORY DISEASE INDUCED BY SPC ACTIVITY CONTAINING 2,4,5- TRISUBSTITUTED-1,3-THIAZOLE DERIVATIVES AS A<br/>[FR] NOUVEAU DÉRIVÉ 2,4,5-TRISUBTITUÉ-1,3-THIAZOLE ET SEL PHARMACEUTIQUEMENT ACCEPTABLE, PROCÉDÉ DE PRÉPARATION ET AGENT THÉRAPEUTIQUE UTILISÉ CONTRE UNE MALADIE INFLAMMATOIRE INDUITE PAR UNE ACTIVITÉ SPC CONTENANT LE DÉRIVÉ 2,4,5-TRISUBSTITUÉ-1,3-THIAZOL
  申请人：KOREA RES INST CHEM TECH

  公开号：WO2009041790A1

  公开（公告）日：2009-04-02

  Provided are a 2,4,5-trisubstiuted-l,3-thiazole derivative represented by the following Chemical Formula 1, a pharmaceutically acceptable salt thereof, a method for preparation thereof, and a use thereof as an effective ingredient in a therapeutic agent for inflammatory disease induced by sphingosylphosphorylcholine (SPC). The 2,4,5-trisubstiuted-l,3-thiazole derivative of the present invention has been confirmed to have superior inhibition activity against SPC receptor in an animal experiment using human-derived endothelial cells and mice. Thus, a pharmaceutical composition for treating inflammatory disease containing the 2,4,5-trisubstiuted-l,3-thiazole derivative or a pharmaceutically acceptable salt thereof as an effective ingredient may be useful for treating inflammation, itching or skin infection associated with atopic dermatitis or other disease induced by SPC receptor.

  本发明提供了一种由以下化学式1表示的2,4,5-三取代-1,3-噻唑衍生物，其药学上可接受的盐，其制备方法以及其作为治疗由鞘磷酰胆碱（SPC）引起的炎症性疾病的有效成分的用途。本发明的2,4,5-三取代-1,3-噻唑衍生物已在使用人源内皮细胞和小鼠进行的动物实验中被证实具有优异的SPC受体抑制活性。因此，含有2,4,5-三取代-1,3-噻唑衍生物或其药学上可接受的盐作为有效成分的用于治疗炎症性疾病的制药组合物，可能对治疗与特应性皮炎或其他由SPC受体引起的炎症、瘙痒或皮肤感染有用。
• 2,4-Disubstituted-5-Aminocarbonyl-1,3-Thiazole Derivatives For Therapeutic Agent Of Antiinflammatory Disease, Method Thereof For Preparation, Therapeutic Agent For Antiinflammatory Disease Induced By SPC Activity Containing The Same
  申请人：Gong Young-Dae

  公开号：US20100145043A1

  公开（公告）日：2010-06-10

  Disclosed herein are 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives, a preparation method thereof, and a therapeutic agent for treating inflammatory diseases induced by SPC, which contains the derivative as an active ingredient. The anti-inflammatory effect of the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives was analyzed through a test employing human dermal cells and an animal test using mice and, as a result, it was found that the derivatives showed excellent inhibitory activity on SPC receptor compared to thiazole derivatives known in the prior art. Thus, the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives or pharmaceutically acceptable salts thereof are useful as active ingredients in therapeutic agents for treating inflammatory diseases, such as inflammation, pruritus and skin infection, which appear in atopic dermatitis and other diseases induced by SPC activity. wherein R 1 , R 2 , R 3 and R 4 are as defined in the specification.

  本文公开了2,4-二取代-5-氨基甲酰基-1,3-噻唑衍生物及其制备方法，以及作为活性成分的治疗SPC引起的炎症性疾病的治疗剂。通过使用人皮肤细胞测试和小鼠动物测试分析了2,4-二取代-5-氨基甲酰基-1,3-噻唑衍生物的抗炎作用，结果发现与先前已知的噻唑衍生物相比，该衍生物对SPC受体表现出优异的抑制活性。因此，2,4-二取代-5-氨基甲酰基-1,3-噻唑衍生物或其药学上可接受的盐可用作治疗炎症性疾病的活性成分，例如在特应性皮炎和其他由SPC活性引起的疾病中出现的炎症，瘙痒和皮肤感染。其中，R1，R2，R3和R4如规范中所定义。
• US7915405B2
  申请人：——

  公开号：US7915405B2

  公开（公告）日：2011-03-29