5-Methanesulfonyl-thiophene-2-carbonyl chloride | 83933-23-7

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 5-Methanesulfonyl-thiophene-2-carbonyl chloride
• 英文别名: 5-Methylsulfonyl-2-thiophenecarbonyl chloride；5-methylsulfonylthiophene-2-carbonyl chloride
• CAS: 83933-23-7
• 化学式: C₆H₅ClO₃S₂
• 分子量: 224.689
• InChiKey: RSPDJOUYDNHVLG-UHFFFAOYSA-N

物化性质

• 沸点：
  416.9±45.0 °C(Predicted)
• 密度：
  1.527±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  87.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-Methanesulfonyl-thiophene-2-carbonyl chloride 在 氨 作用下， 以 乙醚 为溶剂， 生成 5-methylsulphonylthiophen-2-carboxamide
  参考文献：
  名称：

  Alberghina, Gaetano; Fisichella, Salvatore; Occhipinti, Salvatore, Journal of the Chemical Society. Perkin transactions II, 1982, p. 1223 - 1226

  摘要：

  DOI：

文献信息

• [EN] MODULATORS OF REV-ERB<br/>[FR] MODULATEURS DE REV-ERB
  申请人：SCRIPPS RESEARCH INST

  公开号：WO2015103527A1

  公开（公告）日：2015-07-09

  The subject matter herein concerns the identification and development of potent synthetic REV-ERB ligands, such as in vivo agonists and antagonists. These compounds allow for characterization of the effects of modulation of this receptor in vivo specifically on circadian behavior and metabolism, and have suitable characteristics for development of medicinal compounds useful for treatment of malconditions such as diabetes, obesity, atherosclerosis, dyslipidemia, a circadian rhythm disorder, coronary artery disease, bipolar disorder, depression, cancer, a sleep disorder, an anxiety disorder, an addiction disorder, a bone-related disorder such osteoporosis, a skeletal muscle disease, e.g., with compromised exercise capacity, or an autoimmune disorder such as psoriasis, multiple sclerosis, inflammatory bowel disease, and others.

  本文涉及识别和开发强效合成REV-ERB配体，例如体内激动剂和拮抗剂。这些化合物可用于特定在体内对昼夜节律行为和新陈代谢的调节效果进行表征，并具有适合开发用于治疗糖尿病、肥胖症、动脉粥样硬化、血脂异常、昼夜节律紊乱、冠状动脉疾病、躁郁症、抑郁症、癌症、睡眠障碍、焦虑障碍、成瘾障碍、骨相关疾病如骨质疏松症、骨骼肌肉疾病（例如，运动能力受损）、自身免疫性疾病如牛皮癣、多发性硬化、炎症性肠病等疾病的药用化合物的特性。
• 3-substituted-2-oxindole derivatives
  申请人：Pfizer Inc.

  公开号：US05047554A1

  公开（公告）日：1991-09-10

  This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

  本发明涉及新型的3-取代-2-氧吲哚衍生物，它们是前列腺素H.sub.2合酶、5-脂氧合酶和白细胞介素-1生物合成的抑制剂。本发明的化合物本身是前列腺素H.sub.2合酶和白细胞介素-1生物合成的抑制剂，并可用于治疗慢性炎症性疾病的镇痛、抗炎和抗关节炎剂。本发明还涉及包括所述3-取代-2-氧吲哚衍生物的药物组合物；抑制前列腺素H.sub.2合酶和白细胞介素-1生物合成的方法；以及使用该化合物治疗哺乳动物的慢性炎症性疾病。此外，本发明还涉及某些新型羧酸，它们是制备本发明的3-取代-2-氧吲哚衍生物的中间体，以及制备该3-取代-2-氧吲哚衍生物的方法。
• 2-carboxy-thiophene derivatives
  申请人：Pfizer Inc.

  公开号：US05300655A1

  公开（公告）日：1994-04-05

  This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

  本发明涉及新型的3-取代-2-氧化吲哚衍生物，其是前列腺素H.sub.2合酶、5-脂氧合酶和白细胞介素-1生物合成的抑制剂。本发明中的化合物本身作为前列腺素H.sub.2合酶和白细胞介素-1生物合成的抑制剂以及作为治疗慢性炎症性疾病的镇痛、抗炎和抗关节炎药物是有用的。本发明还涉及包含所述3-取代-2-氧化吲哚衍生物的制药组合物；抑制前列腺素H.sub.2合酶和白细胞介素-1生物合成的方法；以及使用该化合物治疗哺乳动物的慢性炎症性疾病。此外，本发明还涉及某些新型羧酸，其作为制备本发明的3-取代-2-氧化吲哚衍生物的中间体，以及制备3-取代-2-氧化吲哚衍生物的过程。
• 3-substituted-2-oxindoles derivatives
  申请人：Pfizer Inc.

  公开号：US06174883B1

  公开（公告）日：2001-01-16

  This invention relates to novel 3-substituted-2-oxindole derivatives of the formula and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

  本发明涉及一种新的3-取代-2-氧化吲哚衍生物及其药物接受的盐，它们是前列腺素H2合酶、5-脂氧合酶和白细胞介素-1生物合成的抑制剂。本发明的化合物本身就是前列腺素H2合酶和白细胞介素-1生物合成的抑制剂，可用于治疗慢性炎症性疾病的镇痛、抗炎和抗关节炎药物。本发明还涉及包括所述3-取代-2-氧化吲哚衍生物的制药组合物；抑制前列腺素H2合酶和白细胞介素-1的生物合成的方法；以及使用该化合物治疗哺乳动物的慢性炎症性疾病。此外，本发明还涉及一些新的羧酸，可用作制备本发明的3-取代-2-氧化吲哚衍生物的中间体，以及制备3-取代-2-氧化吲哚衍生物的方法。
• 3-substituted-2-oxindole derivatives as antiinflammatory agents
  申请人：PFIZER INC.

  公开号：EP0393936A1

  公开（公告）日：1990-10-24

  This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

  本发明涉及新型 3-取代-2-氧化吲哚衍生物，它们是前列腺素 H2 合酶、5-脂氧合酶和白细胞介素-1 生物合成的抑制剂。本发明的化合物本身可用作前列腺素 H2 合酶和白细胞介素-1 生物合成的抑制剂，也可用作治疗慢性炎症性疾病的镇痛、抗炎和抗关节炎药物。本发明还涉及包含所述 3-取代-2-氧化吲哚衍生物的药物组合物；涉及抑制前列腺素 H2 合酶和白细胞介素-1 生物合成的方法；涉及用所述化合物治疗哺乳动物的慢性炎症疾病。此外，本发明还涉及某些可用作制备本发明 3-取代-2-吲哚衍生物中间体的新型羧酸，以及制备 3-取代-2-吲哚衍生物的工艺。