Ethanol, 2-((2,3-dihydro-1-(4-methoxy-2-methylphenyl)-6-(2,2,2-trifluoroethoxy)-1H-pyrrolo(3,2-C)quinolin-4-yl)amino)- | 220854-06-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: Ethanol, 2-((2,3-dihydro-1-(4-methoxy-2-methylphenyl)-6-(2,2,2-trifluoroethoxy)-1H-pyrrolo(3,2-C)quinolin-4-yl)amino)-
• 英文别名: 2-[[1-(4-methoxy-2-methylphenyl)-6-(2,2,2-trifluoroethoxy)-2,3-dihydropyrrolo[3,2-c]quinolin-4-yl]amino]ethanol
• CAS: 220854-06-8
• 化学式: C₂₃H₂₄F₃N₃O₃
• 分子量: 447.4
• InChiKey: ZCVASKPNMMKIKS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  66.8
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• 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。
• Follicle stimulating hormones
  申请人：——

  公开号：US20020127652A1

  公开（公告）日：2002-09-12

  Heterodimeric polypeptide conjugates exhibiting FSH activity, comprising a dimeric polypeptide comprising an FSH-&agr; subunit and an FSH-&bgr; subunit, wherein at least one of the FSH-&agr; and FSH-&bgr; subunits differs from the corresponding wildtype subunit in that at least one amino acid residue acid residue comprising an attachment group for a non-polypeptide moiety has been introduced or removed, and having at least one non-polypeptide moiety bound to an attachment group of at least one of said subunits are provided. Preferably, at least one attachment group, e.g., an N- or O-glycosylation site or an attachment site for a polymer molecule such as polyethylene glycol, has been introduced, e.g., at an N-terminal. The polypeptide conjugates exhibit improved properties, in particular an increased half-life, compared to human FSH.

  显示 FSH 活性的异源二聚体多肽共轭物，包括由 FSH-&agr; 亚基和 FSH-&bgr; 亚基组成的二聚体多肽，其中 FSH-&agr; 亚基和 FSH-&bgr; 亚基中至少有一个与相应的野生型亚基不同，即至少有一个包含非多肽分子连接基团的氨基酸残基被引入或移除，并具有至少一个非多肽分子连接基团；亚基与相应野生型亚基的不同之处在于，引入或移除了至少一个包含非多肽分子连接基团的氨基酸残基，并且至少有一个非多肽分子与至少一个所述亚基的连接基团结合。最好引入至少一个连接基团，如 N 或 O-糖基化位点或聚合物分子如聚乙二醇的连接位点，如在 N 端。与人 FSH 相比，多肽共轭物的性能有所改善，特别是半衰期延长。
• Compositions useful for treating gastrointestinal motility disorders
  申请人：Landau B. Steven

  公开号：US20050059704A1

  公开（公告）日：2005-03-17

  The present invention relates to method of treating a gastrointestinal motility disorder in a subject in need of treatment comprising coadministering to said subject a first amount of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof; and a second amount of at least one gastric acid suppressing agent (e.g., a proton pump inhibitor, an H 2 receptor antagonist or a pharmaceutically acceptable salt, hydrate or solvate thereof; or an acid pump antagonist or pharmaceutically acceptable salt, hydrate or solvate thereof) wherein the first and second amounts together comprise a therapeutically effective amount. In particular, the method is for treating GERD, including nocturnal GERD. The invention further relates to a method of treating nocturnal GERD comprising administering to a subject in need thereof a therapeutically effective amount of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The invention further relates to a method of increasing esophageal motility in a subject in need thereof. The method of increasing esophageal motility can be achieved by administration of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The coadministration can also be used to increase esophageal motility.

  本发明涉及治疗需要治疗的受试者胃肠道运动紊乱的方法，包括向所述受试者联合施用第一种量的具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液；以及第二种量的至少一种胃酸抑制剂（如质子泵抑制剂、H 2 受体拮抗剂或其药学上可接受的盐、水合物或溶液；或酸泵拮抗剂或其药学上可接受的盐、水合物或溶液），其中第一和第二量共同构成治疗有效量。特别是，该方法用于治疗胃食管反流病，包括夜间胃食管反流病。本发明进一步涉及一种治疗夜间胃食管反流病的方法，该方法包括向有需要的受试者施用治疗有效量的具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液。本发明进一步涉及一种增加需要者食管蠕动的方法。增加食管蠕动的方法可通过给予具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液。联合给药也可用于增加食管运动。
• Compositions useful for increasing lower esophageal sphincter pressure
  申请人：Landau B. Steven

  公开号：US20060189648A1

  公开（公告）日：2006-08-24

  The present invention relates to a method of increasing the pressure of the lower esophageal sphincter in a subject in need thereof comprising administering to said subject a specified amount of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The subject in need of treatment is suffering from GERD, including nocturnal GERD.

  本发明涉及一种增加有需要的受试者食管下括约肌压力的方法，包括向所述受试者施用指定量的具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液。需要治疗的受试者患有胃食管反流病，包括夜间胃食管反流病。
• COMPOSITIONS USEFUL FOR TREATING GASTROINTESTINAL MOTILITY DISORDERS
  申请人：Dynogen Pharmaceuticals Inc.

  公开号：EP1663313A2

  公开（公告）日：2006-06-07