Janagliflozin | 1800115-22-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: Janagliflozin
• 英文别名: (2S,3R,4R,5S,6R)-2-[3-[[4-[[(1R,5S)-3-bicyclo[3.1.0]hexanyl]oxy]phenyl]methyl]-4-chlorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
• CAS: 1800115-22-3
• 化学式: C₂₅H₂₉ClO₆
• 分子量: 460.9
• InChiKey: WDBIPGHUEJEKTC-VWQPKTIXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  99.4
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• OPTICALLY PURE BENZYL-4-CHLOROPHENYL-C-GLUCOSIDE DERIVATIVE
  申请人：XUANZHU PHARMA CO., LTD.

  公开号：US20150191502A1

  公开（公告）日：2015-07-09

  The present invention belongs to the field of pharmaceutical technology, more specifically relates to optically pure benzyl-4-chlorophenyl-C-glucoside derivatives represented by formulae (II) and (III), a process for preparing these compounds and intermediates thereof, a pharmaceutical formulation and a pharmaceutical composition containing these compounds, and the use of the optically pure benzyl-4-chlorophenyl-C-glucoside derivative as a sodium glucose co-transporter (SGLT) inhibitor in manufacture of a medicament for treating and/or preventing diabetes mellitus (including insulin-dependent diabetes mellitus and non-insulin-dependent diabetes mellitus) or diabetes-associated diseases (including insulin resistance disease and obesity)

  该发明属于制药技术领域，更具体地涉及由化学式（II）和（III）代表的光学纯苄基-4-氯苯基-C-葡萄糖苷衍生物，以及制备这些化合物及其中间体的方法，包含这些化合物的制药配方和制药组合物，以及将光学纯苄基-4-氯苯基-C-葡萄糖苷衍生物用作钠葡萄糖共转运蛋白（SGLT）抑制剂，用于制造治疗和/或预防糖尿病（包括胰岛素依赖型糖尿病和非胰岛素依赖型糖尿病）或与糖尿病相关疾病（包括胰岛素抵抗症和肥胖症）的药物。
• CRYSTAL FORM OF SODIUM-GLUCOSE COTRANSPORTER 2 INHIBITOR
  申请人：HAINAN XUANZHU PHARMA CO., LTD.

  公开号：US20200131216A1

  公开（公告）日：2020-04-30

  The present invention relates to a crystalline form of a co-crystal of an inhibitor against sodium-glucose cotransporter 2 with L-proline, a method for preparing the same, a pharmaceutical composition comprising the same, and use thereof. Specifically, the present invention relates to a crystalline form of a co-crystal of an inhibitor against sodium-glucose cotransporter 2 represented by formula (1), i.e., (2S,3R,4R,5S,6R)-2-(3-(4-(((1R,3s,5S)-bicyclo[3.1.0]hexan-3-yl)oxy)benzyl)-4-chlorophenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, with L-proline, a method for preparing the same, a pharmaceutical composition comprising the same, and use thereof.

  本发明涉及一种抗钠-葡萄糖共转运体2的抑制剂与L-脯氨酸的共晶形态，其制备方法，包含其的药物组合物以及其用途。具体来说，本发明涉及一种抗钠-葡萄糖共转运体2的抑制剂的共晶形态，其化学式表示为(1)，即(2S,3R,4R,5S,6R)-2-(3-(4-(((1R,3s,5S)-双环[3.1.0]己烷-3-基)氧基)苯基)-4-氯苯基)-6-(羟甲基)四氢-2H-吡喃-3,4,5-三醇，与L-脯氨酸的共晶形态，其制备方法，包含其的药物组合物以及其用途。
• Crystal form of sodium-glucose cotransporter 2 inhibitor
  申请人：HAINAN XUANZHU PHARMA CO., LTD.

  公开号：US10793588B2

  公开（公告）日：2020-10-06

  The present invention relates to a crystalline form of a co-crystal of an inhibitor against sodium-glucose cotransporter 2 with L-proline, a method for preparing the same, a pharmaceutical composition comprising the same, and use thereof. Specifically, the present invention relates to a crystalline form of a co-crystal of an inhibitor against sodium-glucose cotransporter 2 represented by formula (1), i.e., (2S,3R,4R,5S,6R)-2-(3-(4-(((1R,3s,5S)-bicyclo[3.1.0]hexan-3-yl)oxy)benzyl)-4-chlorophenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, with L-proline, a method for preparing the same, a pharmaceutical composition comprising the same, and use thereof.

  本发明涉及一种葡萄糖钠同转运体 2 抑制剂与 L-脯氨酸共晶体的结晶形式、其制备方法、包含其的药物组合物及其用途。具体而言，本发明涉及一种由式（1）表示的葡萄糖钠-共转运体 2 抑制剂共晶体的结晶形式，即、(2S,3R,4R,5S,6R)-2-(3-(4-(((1R,3s,5S)-双环[3.1.0]己烷-3-基)氧基)苄基)-4-氯苯基)-6-(羟甲基)四氢-2H-吡喃-3,4,5-三醇与 L-脯氨酸的共晶体、制备方法、包含其的药物组合物及其用途。
• [EN] CRYSTAL FORM OF SODIUM-GLUCOSE COTRANSPORTER 2 INHIBITOR<br/>[FR] FORME CRISTALLINE DE L'INHIBITEUR DU COTRANSPORTEUR DE SODIUM-GLUCOSE DE TYPE 2<br/>[ZH] 钠-葡萄糖协同转运蛋白2抑制剂的晶型
  申请人：XUANZHU PHARMA CO LTD

  公开号：WO2017206827A1

  公开（公告）日：2017-12-07

  本发明公开了钠-葡萄糖协同转运蛋白2抑制剂的L-脯氨酸共结晶体的晶型、其制备方法、药物组合物及应用。具体地涉及钠-葡萄糖协同转运蛋白2抑制剂的式(1)所示化合物(2S,3R,4R,5S,6R)-2-(3-(4-(((1R,3s,5S)-二环[3.1.0]己烷-3-基)氧基)苄基)-4-氯苯基)-6-(羟甲基)四氢-2H-吡喃-3,4,5-三醇的L-脯氨酸共结晶体的晶型、其制备方法、药物组合物和应用。
• Optically pure benzyl-4-chlorophenyl-C-glucoside derivatives as SGLT inhibitors (diabetes mellitus)
  申请人：Xuanzhu Pharma Co., Ltd.

  公开号：EP2891654B1

  公开（公告）日：2016-06-22