2-(4-Ethylsulfonylphenyl)-3-(4-pyridyl)-6,7-dihydro-[5H]-pyrrolo-[1,2-a]-imidazole | 122454-64-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-(4-Ethylsulfonylphenyl)-3-(4-pyridyl)-6,7-dihydro-[5H]-pyrrolo-[1,2-a]-imidazole
• 英文别名: 5h-Pyrrolo[1,2-a]imidazole,2-[4-(ethylsulfonyl)phenyl]-6,7-dihydro-3-(4-pyridinyl)-；2-(4-ethylsulfonylphenyl)-3-pyridin-4-yl-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole
• CAS: 122454-64-2
• 化学式: C₁₉H₁₉N₃O₂S
• 分子量: 353.445
• InChiKey: GZYVBZFDOYTHTL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  73.2
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Monokine activity interference
  申请人：SMITHKLINE BEECHAM CORPORATION

  公开号：EP0403251A2

  公开（公告）日：1990-12-19

  A method of treating a human afflicted with a T Cell Viral (TIV) infection, such as a human immunodeflciency virus (HIV) infection ,which comprises administering to such human an effective, monokine activity interfering amount of a monokine activity interfering agent.

  一种治疗 T 细胞病毒（TIV）感染（如人类免疫缺陷病毒（HIV）感染）患者的方法，包括向患者施用有效的、可干扰单核因子活性的单核因子活性干扰剂。
• Medicament for the inhibition of interleukin-1 or tumor necrosis factor production by monocytes and/or macrophages
  申请人：SMITHKLINE BEECHAM CORPORATION

  公开号：EP0411754A2

  公开（公告）日：1991-02-06

  A method of inhibiting the production of interleukin-1 by monocytes and/or macrophages in a human in need thereof which comprises administering to such a human an effective, interleukin-1 production inhibiting amount of a diaryl-substituted imidazole fused to a second heterocyclic ring containing a nitrogen bridgehead atom wherein said second ring may also contain sulfur, oxygen or an additional nitrogen atom, and may contain additional unsaturation. This invention relates to a method of inhibiting the production of Tumor Necrosis Factor (TNF) by monocytes or macrophages in a human in need thereof which comprises administering to such mammal an effective, TNF production inhibiting amount of a compound of Formula (I) as described herein. The compounds of Formula (II) are generally described as diaryl-substituted imidazole fused to a second heterocyclic ring containing a nitrogen bridgehead wherein said ring may also contain sulfur, oxygen, or an additional nitrogen atom, and may contain additional unsaturation.

  一种抑制有需要的人的单核细胞和/或巨噬细胞产生白细胞介素-1的方法，它包括向这种人施用有效的、抑制白细胞介素-1产生量的二芳基取代的咪唑与含有氮桥头原子的第二杂环融合，其中所述第二环也可含有硫、氧或另外的氮原子，并可含有另外的不饱和度。 本发明涉及一种抑制有需要的人体内的单核细胞或巨噬细胞产生肿瘤坏死因子（TNF）的方法，该方法包括向该哺乳动物施用有效的、可抑制 TNF 产生量的本文所述的式 (I) 化合物。式(II)化合物一般描述为二芳基取代的咪唑与含有氮桥头的第二个杂环融合，其中所述环还可含有硫、氧或额外的氮原子，并可含有额外的不饱和。
• Pyrrolo(1,2-a)imidazole and imidazo(1,2-a)pyridine derivatives and their use as 5-lipoxygenase pathway inhibitors
  申请人：SMITHKLINE BEECHAM CORPORATION

  公开号：EP0306300B1

  公开（公告）日：1995-05-03
• US5317019A
  申请人：——

  公开号：US5317019A

  公开（公告）日：1994-05-31
• [EN] INHIBITION OF INTERLEUKIN-1 AND TUMOR NECROSIS FACTOR PRODUCTION BY MONOCYTES AND/OR MACROPHAGES
  申请人：SMITHKLINE BEECHAM CORPORATION

  公开号：WO1991000092A1

  公开（公告）日：1991-01-10

  (EN) A method of inhibiting the production of interleukin-1 by monocytes and/or macrophages in a human in need thereof which comprises administering to such a human an effective, interleukin-1 production inhibiting amount of a diaryl-substituted imidazole fused to a second heterocyclic ring containing a nitrogen bridgehead atom wherein said second ring may also contain sulfur, oxygen or an additional nitrogen atom, and may contain additional unsaturation. This invention relates to a method of inhibiting the production of Tumor Necrosis Factor (TNF) by monocytes or macrophages in a human in need thereof which comprises administering to such mammal an effective, TNF production inhibiting amount of a compound of formula (I) as described herein. The compounds of formula (II) are generally described as diaryl-substituted imidazole fused to a seond heterocyclic ring containing a nitrogen bridgehead wherein said ring may also contain sulfur, oxygen, or an additional nitrogen atom, and may contain additional unsaturation.(FR) Un procédé d'inhibition de la production d'interleukine-1 par des monocytes et/ou des macrophages chez un être humain consiste à administrer à ce dernier une quantité d'inhibition efficace de la production d'interleukine-1 d'un imidazole à substitution diaryl fusionné sur un second anneau hétérocyclique contenant un atome de tête de pont d'azote, ce second anneau pouvant contenir également un atome de soufre, d'oxygène ou d'azote supplémentaire, et pouvant contenir une insaturation additionnelle. Cette invention concerne un procécé d'inhibition de la production du facteur de nécrose de tumeur (TNF) par des monocytes ou des macrophages chez un être humain en ayant besoin, et consiste à administrer à ce mammifère une quantité d'inhibition efficace de production de TNF d'un composé de formule (I) ci-décrite. Les composés de formule (II) sont généralement un imidazole à subsitution diaryl fusionné sur un second anneau hétérocyclique contenant un atome de tête de pont d'azote, cet anneau pouvant contenir également un atome de soufre, d'oxygène ou d'azote supplémentaire, et pouvant contenir une insaturation additionnelle.