(4S)-5-(4-chlorophenyl)-N'-(4-chlorophenyl)sulfonyl-4-(3-fluorophenyl)-N-methoxy-3,4-dihydropyrazole-2-carboximidamide

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: (4S)-5-(4-chlorophenyl)-N'-(4-chlorophenyl)sulfonyl-4-(3-fluorophenyl)-N-methoxy-3,4-dihydropyrazole-2-carboximidamide
• 化学式: C₂₃H₁₉Cl₂FN₄O₃S
• 分子量: 521.4
• InChiKey: IQWVGXPEIYCTSM-OAQYLSRUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  91.7
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Pharmaceutical compositions comprising CB1 cannabinoid receptor antagonists and potassium channel openers for the treatment of obesity and related conditions
  申请人：Firnges Michael

  公开号：US20060128673A1

  公开（公告）日：2006-06-15

  Described is a novel combination therapy for diabetes mellitus type I and/or for obesity and its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, by administering a combination of at least one K ATP channel opener as a first active agent and at least one CB 1 cannabinoid receptor antagonist as a second active agent. The invention is further directed to such novel combination therapy wherein a dually acting compound with combined K ATP channel opening and CB 1 antagonistic properties is used. The invention also relates to novel pharmaceutical compositions comprising K ATP channel openers and CB 1 antagonists and the use of said pharmaceutical compositions in the treatment, delayed progression, delayed onset of and/or inhibition of diabetes mellitus type 1, and the prophylaxis and treatment, of obesity as well as the prophylaxis, treatment, delayed onset and/or inhbition of its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, in mammals and humans. The invention is further directed to such novel pharmaceutical compositions comprising a dually acting compound with combined K ATP channel opening and CB 1 antagonistic properties.

  所述的是一种新型组合疗法，用于治疗 I 型糖尿病和/或肥胖症及其伴随和/或继发疾病或病症，特别是代谢综合征和/或 X 综合征和/或 II 型糖尿病，其方法是给药至少一种 K ATP 通道开启剂作为第一活性剂与至少一种 CB 1 大麻素受体拮抗剂作为第二活性制剂。本发明进一步涉及这种新型组合疗法，其中一种双重作用的化合物联合 K ATP 通道开放和 CB 1 拮抗特性的双重作用化合物。本发明还涉及包含 K ATP 通道开启剂和 CB 1 拮抗剂的新型药物组合物，以及将所述药物组合物用于治疗、延缓进展、延缓发病和/或抑制 1 型糖尿病，预防和治疗肥胖症，以及预防、治疗、延缓发病和/或抑制其伴随和/或继发疾病或病症，特别是哺乳动物和人类的代谢综合征和/或 X 综合征和/或 II 型糖尿病。本发明进一步涉及这种新型药物组合物，其中包含一种具有联合 K ATP 通道开放和 CB 1 拮抗特性的双重作用化合物。
• PHARMACEUTICAL COMPOSITIONS COMPRISING CB1 CANNABINOID RECEPTOR ANTAGONISTS AND POTASSIUM CHANNEL OPENERS FOR THE TREATMENT OF DIABETES MELLITUS TYPE I, OBESITY AND RELATED CONDITIONS
  申请人：Solvay Pharmaceuticals GmbH

  公开号：EP1807063A2

  公开（公告）日：2007-07-18
• METHODS OF USING POTASSIUM CHANNEL INHIBITING COMPOUNDS
  申请人：Antel Jochen

  公开号：US20070191357A1

  公开（公告）日：2007-08-16

  Described herein are methods of treating, preventing or inhibiting a variety of medical conditions by administering to subjects in need thereof an effective amount of at least one potassium K v1.3 channel inhibiting compound which can optionally also have either or both CB x modulating properties and/or potassium K (atp) channel opening properties. Also described is the use of potassium K v1.3 channel inhibiting compounds in a pharmaceutical composition for the prophylaxis, treatment, delayed progression, delayed onset and/or inhibition of a variety of medical conditions.
• Use of CBx cannabinoid receptor modulators as potassium channel modulators
  申请人：Antel Jochen

  公开号：US20070254863A1

  公开（公告）日：2007-11-01

  Methods of treating one or more medical conditions by administering to a subject in need thereof an effective amount of a CB x modulator having K ATP channel modulating properties are described herein. Also described are methods of using a CB x modulator having K ATP channel modulating properties to treat one or more medical conditions.
• Pharmaceutical compositions comprising CBx cannabinoid receptor modulators and potassium channel modulators
  申请人：Antel Jochen

  公开号：US20070254862A1

  公开（公告）日：2007-11-01

  Described herein are pharmaceutical compositions comprising therapeutically effective quantities of (i) a K ATP channel modulator; and (ii) a CB x modulator. Also described herein are methods of making and using these compositions.