(3E)-3-[hydroxy-[(5-methyl-1,3-thiazol-2-yl)amino]methylidene]-2-methyl-1,1-dioxo-1λ6,2-benzothiazin-4-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 英文名称: (3E)-3-[hydroxy-[(5-methyl-1,3-thiazol-2-yl)amino]methylidene]-2-methyl-1,1-dioxo-1λ6,2-benzothiazin-4-one
• 化学式: C₁₄H₁₃N₃O₄S₂
• 分子量: 351.4
• InChiKey: DWMREKMVXIFPFM-ACCUITESSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  136
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• [EN] 3-HETEROCYCLYL-4-PHENYL-TRIAZOLE DERIVATIVES AS INHIBITORS OF THE VASOPRESSIN V1A RECEPTOR<br/>[FR] DERIVES 3-HETEROCYCLYL-4-PHENYL-TRIAZOLE COMME INHIBITEURS DE LA VASOPRESSINE PAR RECEPTEUR
  申请人：PFIZER LTD

  公开号：WO2005105779A1

  公开（公告）日：2005-11-10

  Compounds of formula (I): or a pharmaceutically acceptable derivative thereof, wherein R represents C1-6alkyl (optionally substituted by C1-6alkyloxy or Het) or C1-6alkyloxy; R1 and R2 independently represent hydrogen, halo or C1-6alkyl, ring A represents Het1; X represents O or NR3; R3 represents hydrogen or C1-6alkyl; ring B represents a phenyl group or Het2, either of which may be optionally substituted with one or more groups selected from halo, CN, C1-6alkyloxy, CF3, C1-6alkyl, NH2 and NO2; Het and Het1 independently represent a 5- or 6-membered saturated, partially unsaturated or aromatic heterocyclic group comprising either (a) 1 to 4 nitrogen atoms, (b) one oxygen or one sulphur atom or (c) 1 oxygen atom or 1 sulphur atoms and 1 or 2 nitrogen atoms are useful for treating anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (including motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis) mittlesmerchz, preclampsia, premature ejaculation, premature (preterm) labour and Raynaud’s disease.

  式(I)的化合物：或其药学上可接受的衍生物，其中R代表C1-6烷基（可选地被C1-6烷氧基或Het取代）或C1-6烷氧基；R1和R2独立地代表氢、卤素或C1-6烷基，环A代表Het1；X代表O或NR3；R3代表氢或C1-6烷基；环B代表苯基或Het2，其中任一者可选地被一个或多个从卤素、CN、C1-6烷氧基、CF3、C1-6烷基、NH2和NO2中选择的基团取代；Het和Het1独立地代表含有（a）1至4个氮原子、（b）一个氧原子或一个硫原子或（c）1个氧原子或1个硫原子和1或2个氮原子的5-或6元饱和、部分不饱和或芳香杂环基团，对于治疗焦虑、心血管疾病（包括心绞痛、动脉粥样硬化、高血压、心力衰竭、水肿、高钠血症）、月经痛（原发性和继发性）、子宫内膜异位症、呕吐（包括晕动病）、子宫内生长迟缓、炎症（包括类风湿关节炎）、中间痛、子痫前症、早泄、早产、雷诺氏病等疾病有用。
• Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia
  申请人：Palani Anandan

  公开号：US20060264489A1

  公开（公告）日：2006-11-23

  A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.

  具有通式（I）的一种化合物： 或其药学上可接受的盐、溶剂化合物、酯或互变异构体，其中： Q选自以下群组： 和 L选自以下群组： 或其药学上可接受的盐、溶剂化合物、酯或互变异构体，可用于治疗代谢综合征和血脂异常等疾病、疾患或症状。
• [EN] METHODS AND COMPOSITIONS FOR WOUND HEALING<br/>[FR] PROCÉDÉS ET COMPOSITIONS POUR LA CICATRISATION DE PLAIES
  申请人：QBIOTICS LTD

  公开号：WO2014169356A1

  公开（公告）日：2014-10-23

  The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds and compositions for use in wound healing are also described.

  本发明涉及环氧-蒽烯化合物及其在促进伤口愈合中的应用。具体实施例中，环氧-蒽烯化合物是环氧-蒽烯-3-酮化合物。描述了诱导或促进伤口愈合的方法，以及减少疤痕并改善伤口愈合后的美容效果的方法。还描述了用于伤口愈合的化合物和组合物。
• [EN] COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS<br/>[FR] COMPOSÉS DESTINÉS AU TRAITEMENT DE TROUBLES MÉDICAUX
  申请人：ACHILLION PHARMACEUTICALS INC

  公开号：WO2017035360A1

  公开（公告）日：2017-03-02

  Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

  化合物、使用方法和制备抑制补体因子D的方法，包括式（I）的药用盐或其组合物。本文描述的抑制剂针对因子D并抑制或调节补体级联反应。本文描述的因子D的抑制剂减少了过度激活的补体。
• [EN] ALKYNE COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS<br/>[FR] COMPOSÉS ALCYNE POUR LE TRAITEMENT DE TROUBLES IMMUNITAIRES ET INFLAMMATOIRES
  申请人：ACHILLION PHARMACEUTICALS INC

  公开号：WO2017035415A1

  公开（公告）日：2017-03-02

  Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I'" or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

  提供含有公式I、I"和I'"的补体因子D抑制剂、使用方法和制备过程，或其药物可接受的盐或组合物。本文所述的抑制剂针对因子D并抑制或调节补体级联反应。本文所述的因子D抑制剂减少了补体的过度激活。