4-(3-pyrrolidinyloxy)1-(thien-2-ylsulfonyl)-1H-indole | 474003-00-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 4-(3-pyrrolidinyloxy)1-(thien-2-ylsulfonyl)-1H-indole
• 英文别名: 4-Pyrrolidin-3-yloxy-1-thiophen-2-ylsulfonylindole
• CAS: 474003-00-4
• 化学式: C₁₆H₁₆N₂O₃S₂
• 分子量: 348.447
• InChiKey: PBWZPMOOKRLPMG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  97
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Heterocyclyloxy-, -thioxy- and -aminobenzazole derivatives as 5-hydroxytryptamine-6 ligands
  申请人：Wyeth

  公开号：US20030069278A1

  公开（公告）日：2003-04-10

  The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor. 1

  本发明提供了一种I式化合物及其用途，用于治疗与或受到5-HT6受体影响的疾病。
• 1-phenyl imidazol-2-one biphenylmethyl compounds for treatment of circulatory disorders
  申请人：G.D. Searle & Co.

  公开号：US20020038035A1

  公开（公告）日：2002-03-28

  A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula 1 wherein each of R 1 , R 2 and R 3 is independently selected from hydrido, alkyl, alkoxy, cyano, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; alkylcarbonyl and haloalkylcarbonyl; with the proviso that at least one of R 1 , R 2 and R 3 must be a substituent other than hydrido, and with the further proviso that when each of R 1 and R 3 is hydrido, then R 2 cannot be chloro; wherein R 4 is hydrido; wherein R 5 is alkyl; and wherein R 6 is tetrazolyl; or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

  描述了一类1-苯基咪唑-2-酮联苯甲基化合物，用于治疗循环系统疾病。特别感兴趣的化合物是式1的血管紧张素II拮抗剂，其中R1、R2和R3中的每个都是独立选择的，包括氢基、烷基、烷氧基、氰基、卤基、羟基、羧基、烷氧羰基、甲酰基和乙酰基；烷基羰基和卤代烷基羰基；但必须满足R1、R2和R3中至少有一个是除氢基以外的取代基，并且进一步必须满足当R1和R3都是氢基时，R2不能是氯；其中R4是氢基；其中R5是烷基；其中R6是四唑基；或其立体异构体或互变异构体或其药学上可接受的盐。这些化合物在治疗或控制高血压和充血性心力衰竭方面特别有用。
• Heterocyclyloxy-, -thioxy-and-aminobenzazole derivatives as 5-hydroxytryptamine-6 ligands
  申请人：Zhou Ping

  公开号：US20050065186A1

  公开（公告）日：2005-03-24

  The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

  本发明提供了一种I式化合物及其用途，用于治疗与5-HT6受体相关或受其影响的疾病。
• 1-(substituted phenyl)-4-biphenylmethyl-imidazol-2-one derivatives, their preparation and their use as angiotensin II antagonists
  申请人：G.D. SEARLE & CO.

  公开号：EP0978515A2

  公开（公告）日：2000-02-09

  A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula wherein each of R1, R2 and R3 is independently selected from hydrogen, alkyl, alkoxy, cyano, halo, hydroxy, nitro, amino, alkylamino,carboxyl, alkoxycarbonyl, formyl, alkylcarbonyl and haloalkylcarbonyl; with the proviso that at least one of R1, R2 and R3 must be a substituent other than hydrogen, and with the further proviso that when each of R1 and R3 is hydrogen, then R2 cannot be chloro; wherein R4 is selected from hydrogen, alkyl, halo, haloalkyl, formyl, carboxyl and alkoxyalkyl; wherein R5 is selected from alkyl, phenyl, phenylalkyl, cycloalkyl and cycloalkylalkyl; and wherein R6 is an acidic group selected from COOH and or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

  描述了一类用于治疗循环系统疾病的 1-苯基咪唑-2-酮联苯甲基化合物。特别感兴趣的化合物是式中的血管紧张素 II 拮抗剂 其中 R1、R2 和 R3 各自独立地选自氢、烷基、烷氧基、氰基、卤代、羟基、硝基、氨基、烷基氨基、羧基、烷氧羰基、甲酰基、烷基羰基和卤代烷基羰基；但 R1、R2 和 R3 中至少有一个必须是除氢以外的取代基，而且当 R1 和 R3 都是氢时，R2 不能是氯；其中 R4 选自氢、烷基、卤代、卤代烷基、甲酰基、羧基和烷氧基烷基； 其中 R5 选自烷基、苯基、苯基烷基、环烷基和环烷基烷基；以及其中 R6 是选自 COOH 和 或其立体异构体或同系物或其药学上可接受的盐。 这些化合物尤其适用于治疗或控制高血压和充血性心力衰竭。
• 1-PHENYL-IMIDAZOL-2-ONE BIPHENYLMETHYL COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS
  申请人：G.D. SEARLE & CO.

  公开号：EP0690854B1

  公开（公告）日：2000-07-12