1-(9H-fluoren-9-ylmethoxycarbonyl)-5-phenylpyrrolidine-2-carboxylic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: 1-(9H-fluoren-9-ylmethoxycarbonyl)-5-phenylpyrrolidine-2-carboxylic acid
• 化学式: C₂₆H₂₃NO₄
• 分子量: 413.5
• InChiKey: JEEBFSSXASHKSF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Pharmaceutically active sulfanilide derivatives
  申请人：——

  公开号：US20040072816A1

  公开（公告）日：2004-04-15

  The present invention relates to sulfanilide derivatives of formula (I), in which R 1 and R 2 are optionally substituted aryl and heteroaryl groups and the other variables are as defined in the claims, for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such sulfanilide derivatives. Said derivatives are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to sulfanilide derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin, including preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. The present invention is furthermore related to novel sulfanilide derivatives as well as to methods of their preparation.

  本发明涉及式(I)的磺胺基苯酰胺衍生物，其中R1和R2是可选择取代的芳基和杂环芳基基团，其他变量如权利要求中所定义，用作药用活性化合物，以及含有这种磺胺基苯酰胺衍生物的药物配方。所述衍生物在治疗和/或预防早产、早产、痛经、抗利尿素分泌不当、充血性心力衰竭、动脉高血压、肝硬化、肾病综合征和眼压增高方面具有用途。具体而言，本发明涉及显示对催产素和/或抗利尿素受体具有显著调节作用，特别是拮抗活性的磺胺基苯酰胺衍生物。更具体地说，所述化合物在治疗和/或预防由催产素和/或抗利尿素介导的疾病状态方面具有用途，包括早产、早产、痛经、抗利尿素分泌不当、充血性心力衰竭、动脉高血压、肝硬化、肾病综合征和眼压增高。本发明还涉及新型磺胺基苯酰胺衍生物以及其制备方法。
• Novel amino acid and peptide inhibitors of Staphylococcus virulence
  申请人：——

  公开号：US20030050248A1

  公开（公告）日：2003-03-13

  Isolated synthetic modified amino acids and peptides, which inhibit of the production of virulence factors in bacteria, particularly Staphylococcus, are described. The amino acids and peptides can be used in a method for treatment or prevention of Staphylococcal infections or can be integrated into a medical device to inhibit the development of infection associated with the use of such devices.

  本文描述了可抑制细菌（尤其是葡萄球菌）产生毒力因子的分离合成修饰氨基酸和肽。这些氨基酸和肽可用于治疗或预防葡萄球菌感染的方法中，也可集成到医疗设备中，以抑制与使用此类设备相关的感染的发生。
• NOVEL AMINO ACID AND PEPTIDE INHIBITORS OF STAPHYLOCOCCUS VIRULENCE
  申请人：Intermune, Inc.

  公开号：EP1261362A2

  公开（公告）日：2002-12-04
• PHARMACEUTICALLY ACTIVE SULFANILIDE DERIVATIVES
  申请人：Merck Serono SA

  公开号：EP1335901B1

  公开（公告）日：2010-04-14
• US7312358B2
  申请人：——

  公开号：US7312358B2

  公开（公告）日：2007-12-25