N-[(1R,2R)-1-(3,4-dimethoxyphenyl)-1-hydroxy-3-pyrrolidin-1-ylpropan-2-yl]octanamide | 1092468-71-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-[(1R,2R)-1-(3,4-dimethoxyphenyl)-1-hydroxy-3-pyrrolidin-1-ylpropan-2-yl]octanamide
• CAS: 1092468-71-7
• 化学式: C₂₃H₃₈N₂O₄
• 分子量: 406.566
• InChiKey: WMTGNHQKBLVRRQ-AUSIDOKSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  29
• 可旋转键数：
  13
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  71
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• Glucosylceramide Synthase Inhibition For The Treatment Of Collapsing Glomerulopathy And Other Glomerular Disease
  申请人：Ibraghimov-Beskrovnaya Oxana

  公开号：US20110166134A1

  公开（公告）日：2011-07-07

  A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.

  一种治疗肾小球疾病的方法，所述肾小球疾病选择自系列包括系膜增生性肾小球肾炎、崩解性肾小球病、增生性狼疮性肾炎、新月体性肾小球肾炎和膜性肾病，该方法包括向患者投予有效量的葡糖鞘氨酸合成酶抑制剂。
• 2-Acylaminopropoanol-Type Glucosylceramide Synthase Inhibitors
  申请人：Siegel Craig

  公开号：US20110184021A1

  公开（公告）日：2011-07-28

  A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

  用于治疗多囊肾病的化合物由结构式（I）表示，或其药学上可接受的盐。一种制药组合物包括由结构式（I）表示的化合物或其药学上可接受的盐。一种治疗需要的多囊肾病的方法包括向患者施用由结构式（I）表示的化合物或其药学上可接受的盐的治疗有效量。分别治疗需要的多囊肾病的方法包括向患者施用由结构式（I）表示的化合物或其药学上可接受的盐的治疗有效量。
• 2-ACYLAMINOPROPOANOL-TYPE GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
  申请人：Siegel Craig

  公开号：US20100256216A1

  公开（公告）日：2010-10-07

  A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-α, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

  一种化合物由结构式（I）表示，或其药学上可接受的盐。一种药物组合物包括由结构式（I）表示的化合物或其药学上可接受的盐。一种治疗需要的受试者的方法包括向受试者施用结构式（I）表示的化合物或其药学上可接受的盐的治疗有效量。该受试者患有2型糖尿病；与糖尿病性肾病相关的肾肥大或增生；Tay-Sachs病；高氏病；或Fabry病。分别降低受试者血浆TNF-α、降低血糖水平、降低糖化血红蛋白水平、抑制葡糖鞘氨醇合成酶和降低糖脂浓度的方法包括向受试者施用结构式（I）表示的化合物或其药学上可接受的盐的治疗有效量。
• GLUCOSYLCERAMIDE SYNTHASE INHIBITION FOR THE TREATMENT OF COLLAPSING GLOMERULOPATHY AND OTHER GLOMERULAR DISEASE
  申请人：Genzyme Corporation

  公开号：US20130225573A1

  公开（公告）日：2013-08-29

  A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.

  一种治疗肾小球疾病的方法，所述肾小球疾病选自系列包括系膜增生性肾小球肾炎、崩解性肾小球病、增生性狼疮性肾炎、新月体性肾小球肾炎和膜性肾病，该方法包括向受试者施用有效量的葡糖鞘氨醇合成酶抑制剂。
• PHARMACEUTICAL COMPOSITION OF THE GLUCOSYLCERAMIDE SYNTHASE INHIBITOR ELIGLUSTAT FOR THE TREATMENT GAUCHER'S DISEASE COMPRISING ADJUSTING THE INDIVIDUAL THERAPEUTICAL DOSE TO THE P450 METABOLISM OF THE PATIENT
  申请人：Genzyme Corporation

  公开号：EP3599237A1

  公开（公告）日：2020-01-29

  The present invention relates to a pharmaceutical composition comprising the hemitartrate salt of Eliglustat (Genz 112638; N-[(1R,2R)-2-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]-octanamide) represented by the following structural formula: (Formula I Hemitartrate) as an inhibitor of the glucosylceramide synthase (GCS) for use in a method of treating Fabry's or Gaucher's disease, the method comprising adjusting the individual therapeutical dose to the P450 metabolism of the patient. Particular single crystalline forms of Eliglustat Hemitartrate are characterized by a variety of properties and physical measurements as well as methods of producing crystalline Eliglustat Hemitartrate and using it to inhibit glucosylceramide synthase or lowering glycosphingolipid concentrations 10 in subjects to treat Fabry's or Gaucher's disease, are also discussed.

  本发明涉及一种药物组合物，该药物组合物包含艾力司他（Genz 112638；N-[(1R,2R)-2-(2,3-二氢-1,4-苯并二恶烷-6-基)-2-羟基-1-(1-吡咯烷基甲基)乙基]-辛酰胺的酒石酸盐，其结构式如下： (式 I 半酒石酸盐） 作为葡萄糖甘油酰胺合成酶（GCS）的抑制剂，用于治疗法布里氏病或戈谢氏病的方法，该方法包括根据患者的 P450 代谢情况调整个体治疗剂量。 此外，还讨论了酒石酸艾利司他的特定单晶形式的各种特性和物理测量方法，以及生产酒石酸艾利司他结晶并用其抑制受试者体内的葡萄糖甘油酰胺合成酶或降低糖磷脂浓度10以治疗法布里氏病或戈谢氏病的方法。