O-Methyltramadol | 541506-09-6

• 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: O-Methyltramadol
• 英文别名: (S,S)-O-Methyltramadol；O-methyl tramadol；1-[(1R,2R)-2-methoxy-2-(3-methoxyphenyl)cyclohexyl]-N,N-dimethylmethanamine
• CAS: 541506-09-6
• 化学式: C₁₇H₂₇NO₂
• 分子量: 277.407
• InChiKey: VWXSFQRIRPPNDO-WBVHZDCISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.65
• 拓扑面积：
  21.7
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Tramadol analogs and uses thereof
  申请人：SEPRACOR INC.

  公开号：US20030171440A1

  公开（公告）日：2003-09-11

  Compounds of formula I are effective in treating disorders modulated by opiate receptor activity and/or monoamine activity. 1 In formula I, R 1 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl; R 2 is selected from hydrogen, hydroxy, cyano, haloalkyl, glycosyl, SO 2 R 5 , and OR 5 ; R 3 and R 4 are independently selected from hydrogen and lower alkyl, or R 3 and R 4 taken together with nitrogen form a five- or six-membered heterocyclic or substituted heterocyclic ring; and R 5 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl.

  式I化合物可有效用于治疗受阿片受体活性和/或单胺活性调节的疾病。在式I中，R1选择自烷基、芳基、烷基芳基、取代烷基、取代芳基和取代烷基芳基；R2选择自氢、羟基、氰基烷基、糖基、SO2R5和OR5；R3和R4独立地选择自氢和低烷基，或R3和R4与氮一起形成五元或六元杂环或取代杂环环；R5选择自烷基、芳基、烷基芳基、取代烷基、取代芳基和取代烷基芳基。
• Liquid parenteral formulation comprising a tramadol material and paracetamol
  申请人：Uni-Pharma Kleon Tsetis Pharmaceutical Laboratories S.A.

  公开号：EP2377514A2

  公开（公告）日：2011-10-19

  The present invention provides a liquid parenterally deliverable formulation comprising a tramadol material, particularly tramadol HCl, and paracetamol and its use in treating conditions or disorder wherein an urgent treatment with analgesics is indicated. This formulation is particularly useful whenever fast relief is required in lesser time, especially in acute or chronic painful conditions. The formulation of the present invention is stable upon storage at room temperature and in refrigerated temperature.

  本发明提供了一种由曲马多材料（尤其是盐酸曲马多）和扑热息痛组成的液态肠外给药制剂，并将其用于治疗需要紧急使用镇痛剂治疗的病症或紊乱。 这种制剂特别适用于需要在较短时间内快速缓解疼痛的情况，尤其是急性或慢性疼痛。 本发明的制剂在室温和冷藏条件下储存稳定。
• US6780891B2
  申请人：——

  公开号：US6780891B2

  公开（公告）日：2004-08-24
• [EN] TRAMADOL ANALOGS AND USES THEREOF<br/>[FR] ANALOGUES DE TRAMADOLE ET LEURS UTILISATIONS
  申请人：SEPRACOR INC

  公开号：WO2003048113A1

  公开（公告）日：2003-06-12

  Compounds of formula I are effective in treating disorders modulated by opiate receptor activity and/or monoamine activity. In formula I, R1 is selected from alkyl, aryl, alkylaryl, substitured alkyl, substituted aryl, and substituted alkylaryl; R2 is selected from hydrogen, hydroxy, cyano, haloalkyl, glycosyl, SO2R5, and OR5; R3 and R4 are independently selected from hydrogen and lower alkyl, or R3 and R4 taken together with nitrogen form a five-or six-membered heterocyclic or substituted heterocyclic ring; R5 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl.
• [EN] EXTENDED RELEASE COMPOSITION CONTAINING TRAMADOL<br/>[FR] COMPOSITION A LIBERATION MODIFIEE CONTENANT DU TRAMADOL
  申请人：GALEPHAR PHARMACEUTICAL RES IN

  公开号：WO2004110410A1

  公开（公告）日：2004-12-23

  The present invention relates to a once daily extended release pharmaceutical preparation of Tramadol or its acceptable pharmaceutical salts. The preparation provides, effective blood concentration for a period of about 24 hours with reduced peak concentrations. It is characterized that effective Tramadol levels appear within the first hours after administration, the time to maximal Tramadol content Tmax is at least 10 hours and the peak Tramadol concentration is less than three times the concentration obtained after 24 hours of said administration.