酚丙氢吡咯 | 428-37-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: 酚丙氢吡咯
• 中文别名: 普罗法多；普罗法朵
• 英文名称: profadol
• 英文别名: m-(1-Methyl-3-propyl-3-pyrrolidinyl)-phenol；3-(1-methyl-3-propylpyrrolidin-3-yl)phenol
• CAS: 428-37-5
• 化学式: C₁₄H₂₁NO
• 分子量: 219.327
• InChiKey: VFUGCQKESINERB-UHFFFAOYSA-N

物化性质

• 保留指数：
  1748

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  23.5
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Combination of benzyl-4, 5-dihydro-1H-imidazole derivative and an opioid receptor ligand
  申请人：Laboratorios del Dr. Esteve S.A.

  公开号：EP2014288A1

  公开（公告）日：2009-01-14

  The present invention refers to a combination of a Compound A, a benzyl-4,5-dihydro-1 H-imidazole derivative according to formula (I) and a Compound B, an opioid receptor ligand; especially of xylometazoline or oxymetazoline and a µ-opioid receptor agonist, most preferably of xylometazoline or oxymetazoline and morphine; a medicament comprising this combination; a pharmaceutical formulation for nasal application comprising this combination; or the use of this combination for the treatment of the symptoms of pain, or the prevention or the prophylaxis of the symptoms of pain, whereas pain particularily encompasses visceral pain, chronic pain, cancer pain, acute pain or neuropathic pain, specifically involving also breakthrough pain.

  本发明涉及一种化合物A，即按照式(I)的苄基-4,5-二氢-1H-咪唑衍生物和一种化合物B，一种阿片受体配体的组合；特别是甲苯鼻塞或鼻塞通或一种μ-阿片受体激动剂，最好是甲苯鼻塞或鼻塞通和吗啡；包括这种组合的药物；包括这种组合的鼻用制剂；或者使用这种组合治疗疼痛症状，或者预防或预防疼痛症状，其中疼痛特别包括内脏疼痛、慢性疼痛、癌症疼痛、急性疼痛或神经病理性疼痛，特别还涉及突破性疼痛。
• [EN] CARBONATE PRODRUGS AND METHODS OF USING THE SAME<br/>[FR] PROMÉDICAMENTS CARBONATÉS ET LEURS MÉTHODES D'UTILISATION
  申请人：NEUROGESX INC

  公开号：WO2009143297A1

  公开（公告）日：2009-11-26

  The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

  本发明提供了碳酸盐前药，其包括连接到母药基团的羟基或羧基上的碳酸磷酸酐前药基团。这些前药可能比母药具有改进的物理化学性质。还提供了使用碳酸盐前药治疗对母药具有响应的疾病或症状的方法，以及配套工具和单剂量。
• Combination of a 5-HT7 receptor ligand and an opioid receptor ligand
  申请人：Laboratorios del Dr. Esteve S.A.

  公开号：EP1997493A1

  公开（公告）日：2008-12-03

  The present invention refers to a combination of a 5HT7 receptor ligand and an opioid recptor ligand, especially of a 5HT7 receptor agonist and an opioid recptor agonist, a medicament comprising this combination, or the use of this combination for the treatment of the symptoms of pain, the prevention or the prophylaxis of the symptoms of pain.

  本发明涉及一种5HT7受体配体和阿片受体配体的组合，特别是一种5HT7受体激动剂和阿片受体激动剂，包含该组合的药物，或者利用该组合治疗疼痛症状，预防或预防疼痛症状的用途。
• [EN] COMPOUNDS AND COMPOSITIONS USEFUL AS CATHEPSIN S INHIBITORS<br/>[FR] COMPOSES ET COMPOSITIONS UTILISES COMME INHIBITEURS DE LA CATHEPSINE S
  申请人：NOVARTIS AG

  公开号：WO2006018284A1

  公开（公告）日：2006-02-23

  The present invention relates to the use of a 2-cyanopyrimidine compound of the formula (I), wherein R1, R2, R3 and X are as defined in the specification and in the claims, in free form or in salt form, and , where possible, in tautomeric form, as an inhibitor of the activity of cathepsin S.

  本发明涉及使用式(I)的2-氰基嘧啶化合物，其中R1、R2、R3和X如规范和权利要求中定义的那样，以自由形式或盐形式，并在可能的情况下以互变异构形式，作为猫hepsin S活性的抑制剂。
• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。

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