4-(3,4-difluorophenyl)-2-oxo-N-(3-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylpropyl)-1,3-oxazolidine-3-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异香豆素
• 英文名称: 4-(3,4-difluorophenyl)-2-oxo-N-(3-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylpropyl)-1,3-oxazolidine-3-carboxamide
• 化学式: C₂₅H₂₇F₂N₃O₄
• 分子量: 471.5
• InChiKey: HFQLTFPKRSLOMH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  71.1
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] SPIRO[BICYCLIC -AZACYCLOALKYL AND -CYCLOALKYL] DERIVATIVES AND USES THEREOF<br/>[FR] DERIVES DE SPIRO[AZACYCLOALKYLE ET CYCLOALKYLE BICYCLIQUES] ET UTILISATIONS DE CEUX-CI
  申请人：MERCK & CO INC

  公开号：WO2001022919A2

  公开（公告）日：2001-04-05

  Spiro[bicyclic -azacycloalkyl and -cycloalkyl] derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.