XT-611

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: XT-611
• 英文别名: 3,4-Dipropyl-7,8-dihydroimidazo[2,1-f]purin-5-one
• 化学式: C₁₃H₁₉N₅O
• 分子量: 261.327
• InChiKey: ZWAPPZIVBZAGKZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  53.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  6-(2-hydroxyethylamino)-3-propyl-7H-purin-2(3H)-one 在 potassium carbonate 、 甲基磺酰氯 、 三乙胺 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 8.0h， 生成 XT-611
  参考文献：
  名称：

  Selective Inhibitors of Cyclic AMP-Specific Phosphodiesterase:  Heterocycle-Condensed Purines

  摘要：

  To reverse the adverse reactions of alkylxanthines and to develop novel inhibitors of cyclic AMP-specific phosphodiesterase (PDE IV), a series of heterocycle-condensed purines were designed and synthesized. Some of these new compounds had similar or more potent and selective inhibitory activity against PDE IV than known PDE IV inhibitors. The tracheal-relaxant activity of these compounds was closely correlated with their PDE IV-inhibitory activity. Moreover, these purine analogues did not have any positive-chronotropic action or adenosine-antagonistic action on isolated heart preparations, which are the particular adverse reactions of alkylxanthines. Among them, 3,4-dipropyl-4,5,7,8-tetrahydro-3H-imidazo[1,2-i]purin-5-one (1c), which was the most selective and potent PDE TV inhibitor, did not cause emesis in Suncus murinus at a dosage range of 10-100 mg/kg (po), while an imidazole analogue of 1c (4c) and known PDE IV inhibitors such as rolipram and denbufylline caused emesis even at 10 or 30 mg/kg.

  DOI：

  10.1021/jm970089s

文献信息

• Combination of a pde iv inhibitor and a tnf-alpha antagonist
  申请人：Warner M James

  公开号：US20060083714A1

  公开（公告）日：2006-04-20

  The subject invention relates to therapeutic combinations and methods for the treatment of inflammatory conditions and diseases. Particularly the present invention relates to treatments and methods for PDE IV-related conditions and for TNF-alpha-related conditions using a combination of a PDE IV inhibitor and a TNF-alpha antagonist.

  本发明涉及治疗炎症和疾病的治疗组合和方法。特别是本发明涉及使用 PDE IV 抑制剂和 TNF-α 拮抗剂组合治疗 PDE IV 相关疾病和 TNF-α 相关疾病的治疗方法。
• TREATMENT OF INFLAMMATORY DISEASE USING INGESTIBLE DEVICE TO RELEASE IMMUNE MODULATOR
  申请人：Progenity, Inc.

  公开号：US20200323772A1

  公开（公告）日：2020-10-15

  This disclosure features methods and compositions for treating inflammatory disorders or conditions that arise in a tissue originating from the endoderm using an immune modulator.
• TREATMENT OF A DISEASE OF THE GASTROINTESTINAL TRACT WITH A PDE4 INHIBITOR
  申请人：Progenity, Inc.

  公开号：US20210031012A1

  公开（公告）日：2021-02-04

  This disclosure features methods and compositions for treating diseases of the gastrointestinal tract with a PDE4 inhibitor.
• [EN] COMBINATION OF A PDE IV INHIBITOR AND A TNF-ALPHA ANTAGONIST<br/>[FR] COMBINAISON D'UN INHIBITEUR DE LA PDE IV ET D'UN ANTAGONISTE DU TNF-ALPHA
  申请人：PHARMACIA CORP

  公开号：WO2004067006A1

  公开（公告）日：2004-08-12

  The subject invention relates to therapeutic combinations and methods for the treatment of inflammatory conditions and diseases. Particularly the present invention relates to treatments and methods for PDE IV-related conditions and for TNF-alpha-related conditions using a combination of a PDE IV inhibitor and a TNF-alpha antagonist.
• [EN] TREATMENT OF INFLAMMATORY DISEASE USING INGESTIBLE DEVICE TO RELEASE IMMUNE MODULATOR<br/>[FR] TRAITEMENT DE MALADIE INFLAMMATOIRE FAISANT APPEL À UN DISPOSITIF INGÉRABLE POUR LIBÉRER UN IMMUNOMODULATEUR
  申请人：PROGENITY INC

  公开号：WO2019036382A1

  公开（公告）日：2019-02-21

  This disclosure features methods and compositions for treating inflammatory disorders or conditions that arise in a tissue originating from the endoderm using an immune modulator.