1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-(2,5-dioxopyrrolidin-1-yl)propane | 255861-53-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-(2,5-dioxopyrrolidin-1-yl)propane
• 英文别名: 2,5-Pyrrolidinedione, 1-[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]-；1-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl]pyrrolidine-2,5-dione
• CAS: 255861-53-1
• 化学式: C₁₈H₂₅N₃O₃
• 分子量: 331.415
• InChiKey: XLPKXRVQNPNZRJ-UHFFFAOYSA-N

物化性质

• 沸点：
  535.3±50.0 °C(Predicted)
• 密度：
  1.185±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  53.1
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  丁二酰亚胺 、 1-(2-methoxyphenyl)-4-(3-chloropropyl)piperazine 、 potassium carbonate 在 四丁基溴化铵 氯仿 、 水 、 Sodium sulfate-III 作用下， 以 丙酮 为溶剂， 反应 12.0h， 生成 1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-(2,5-dioxopyrrolidin-1-yl)propane
  参考文献：
  名称：

  1-(4-arylpiperazin-1-yl)-.omega.-[n-(.alpha...

  摘要：

  新型哌嗪衍生物，其中一氮原子被芳香族系统取代，另一氮原子被(2,5-二氧代吡咯烷-1-基)烷或(2,6-二氧代哌嗪-1-基)烷取代，已被发现具有选择性的α1A肾上腺素能活性。这些化合物可用于治疗疾病，如周围血管疾病、充血性心力衰竭、高血压，尤其是良性前列腺肥大的治疗。

  公开号：

  US06090809A1

文献信息

• 1-(4-arylpiperazin-1-yl)-.omega.-[n-(.alpha.,.omega.-dicarboximido)]-alka
  申请人：Ranbaxy Laboratories Limited

  公开号：US06083950A1

  公开（公告）日：2000-07-04

  Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective .alpha..sub.1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.

  新型哌嗪衍生物，其中一个氮原子被芳香系统取代，另一个氮原子被(2,5-二氧吡咯烷-1-基)烷基或(2,6-二氧哌啶-1-基)烷基取代，被发现具有选择性的α1A肾上腺素能活性。这些化合物可用于治疗疾病状况，如外周血管疾病、充血性心力衰竭、高血压，特别是良性前列腺增生。
• 1-(4-arylpiperazin-1-y1)-&ohgr;-[N-(&agr;,&ohgr;-dicarboximido)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers
  申请人：Ranbaxy Laboratories Limited

  公开号：US06410735B1

  公开（公告）日：2002-06-25

  Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.

  新型吡哆啉衍生物，其中一氮原子被芳香基取代，另一氮原子被(2,5-二氧代吡咯烷-1-基)烷基或(2,6-二氧代哌啶-1-基)烷基取代，已被发现具有选择性α1A肾上腺素能活性。这些化合物可用于治疗疾病，如外周血管疾病、充血性心力衰竭、高血压和尤其是良性前列腺增生症。
• 1-(4-arylpiperazin-1-yl)-&ohgr;-[N-(&agr;&ohgr;-dicarboximido)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers
  申请人：Ranbaxy Laboratories Limited

  公开号：US06420366B1

  公开（公告）日：2002-07-16

  Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.

  一种新型的哌嗪衍生物，其中一个氮原子被芳香族系统置换，另一个氮原子被(2,5-二氧代吡咯烷-1-基)烷基或(2,6-二氧代哌嗪-1-基)烷基置换，已被发现具有选择性的α1A肾上腺素能活性。这些化合物可用于治疗疾病，如周围血管疾病、充血性心力衰竭、高血压以及尤其是良性前列腺肥大症。
• 1-(4-arylpiperazin-1-yl)-&ohgr;-[N-(&agr;,&ohgr;-dicarboximido)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers
  申请人：Ranbaxy Laboratories Limited

  公开号：US06420559B1

  公开（公告）日：2002-07-16

  Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.

  一些新型的吡哆啉衍生物，在一氮原子上被芳香族系统取代，在另一氮原子上被(2,5-二氧代吡咯烷-1-基)烷基或(2,6-二氧代哌啶-1-基)烷基取代，已经被发现具有选择性的α1A肾上腺素能活性。这些化合物可用于治疗疾病，如周围血管疾病、充血性心力衰竭、高血压，尤其是良性前列腺增生症。
• 1-(4-Arylpiperazin-1-yl)-&ohgr;-[N-(&agr;,&ohgr;-dicarboximidoL)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers
  申请人：Ranbaxy Laboratories Limited

  公开号：US06812344B1

  公开（公告）日：2004-11-02

  The present invention relates to certain novel piperazine derivatives having protracted uro-selective &agr;1-adrenoceptor antagonistic activity exceeding those of previously described compounds. The compounds of the present invention hold promise for treating benign prostratic hyperplasia (BPH). This invention also relates to methods for making the novel compounds, pharmaceutical compositions containing the compounds, and methods of treating benign prostatic hyperplasia using the compounds.

  本发明涉及某些新型哌嗪衍生物，具有持久的选择性尿道α1-肾上腺素受体拮抗活性，超过先前描述的化合物。本发明的化合物有望治疗良性前列腺增生症（BPH）。本发明还涉及制备新化合物的方法，含有该化合物的药物组合物以及使用该化合物治疗良性前列腺增生症的方法。