2-[4-[(5-Methyl-4-oxo-2-propyliminoimidazolidin-1-yl)methyl]phenyl]benzoic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-[4-[(5-Methyl-4-oxo-2-propyliminoimidazolidin-1-yl)methyl]phenyl]benzoic acid
• 英文别名: 2-[4-[(5-methyl-4-oxo-2-propyliminoimidazolidin-1-yl)methyl]phenyl]benzoic acid
• 化学式: C₂₁H₂₃N₃O₃
• 分子量: 365.4
• InChiKey: UBPUWIWGTTXDSS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  27
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  82
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• 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。
• 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。
• [EN] 1-PHENYL-IMIDAZOL-2-ONE BIPHENYLMETHYL COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS<br/>[FR] COMPOSES 1-PHENYLE-IMIDAZOLE-2-ONE BIPHENYLMETHYLE DESTINES AU TRAITEMENT DES DESORDRES CIRCULATOIRES
  申请人：G.D. SEARLE & CO.

  公开号：WO1994021629A1

  公开（公告）日：1994-09-29

  (EN) 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 formula (I) wherein each of R1, R2 and R3 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 R1, R2 and R3 must be a substituent other than hydrido, and with the further proviso that when each of R1 and R3 is hydrido, then R2 cannot be chloro; wherein R4 is hydrido; wherein R5 is alkyl; and wherein R6 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.(FR) Classe de composés 1-phényle-imidazole-2-one biphénylméthyle destinés au traitement des désordres circulatoires. Les composés présentant un intérêt particulier sont des antagonistes de l'angiotensine II de la formule (I) dans laquelle R1, R2 et R3 sont choisis indépendamment parmi hydrido, alkyle, alcoxy, cyano, halo, hydroxy, carboxyle, alcoxycarbonyle, formyle et acétyle, alkylcarbonyle et haloalkylcarbonyle, sous réserve que l'un au moins de R1, R2 et R3 soit un substituant autre que hydrido et sous réserve en outre que R1 et R3 soient chacun hydrido, R2 ne pouvant pas alors être chloro; dans la formule R4 est hydrido, R5 est alkyle, et R6 est un tétrazolyle. On décrit également un stéréoisomère ou un tautomère de cette substance, ou un sel pharmaceutiquement acceptable de celle-ci. Ces composés se révèlent particulièrement utiles pour le traitement ou la prévention de l'hypertension et de l'insuffisance cardiaque congestive.

  这类1-苯基imidazol-2-酮双苯甲基化合物被描述为用于治疗循环系统障碍的药物。特别 interest is focused on angiotensin II antagonists of formula (I)，其中R1、R2和R3各自独立地从选 hydrido、alkyl、alkoxy、cyano、halo、hydroxy、carboxyl、alcosy carbonyl、formyl和acetyl中选择；其中至少一个选自R1、R2、R3，必须是非调研的取代基；在 R1和R3均为调研的情况下，R2不能为氯；在式中，R4是调研；R5是烷基；R6是四环噻Vue。这些化合物在治疗或控制高血压和心力衰竭方面特别有用。此外还可以形成它们的立体异构体或同分异构体，或在药学上可接受的盐形式。
• 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
• US5177097A
  申请人：——

  公开号：US5177097A

  公开（公告）日：1993-01-05