5-chloro-2-methoxy-N-[2-(1-sulfamoyl-piperidin-4-yl)-ethyl]-benzamide | 58603-84-2

• 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: 5-chloro-2-methoxy-N-[2-(1-sulfamoyl-piperidin-4-yl)-ethyl]-benzamide
• 英文别名: 4-(2-(5-chloro-2-methoxybenzamido)ethyl)piperidine-1-sulfonamide；5-chloro-2-methoxy-N-[2-(1-sulfamoylpiperidin-4-yl)ethyl]benzamide
• CAS: 58603-84-2
• 化学式: C₁₅H₂₂ClN₃O₄S
• 分子量: 375.876
• InChiKey: JVKFIUJHIIXEKZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  5-chloro-2-methoxy-N-[2-(1-sulfamoyl-piperidin-4-yl)-ethyl]-benzamide 以76%的产率得到
  参考文献：
  名称：

  SARGES R.; KUHLA D. E.; WIEDERMANN H. E.; MAYHEW D. A., J. MED. CHEM. , 1976, 19, NO 5, 695-709

  摘要：

  DOI：
• 作为产物：
  描述：

  5-chloro-2-methoxy-N-(2-piperidin-4-ylethyl)benzamide;hydrochloride 、 磺酰胺 以43%的产率得到
  参考文献：
  名称：

  SARGES R.; KUHLA D. E.; WIEDERMANN H. E.; MAYHEW D. A., J. MED. CHEM. , 1976, 19, NO 5, 695-709

  摘要：

  DOI：

文献信息

• Piperidinesulfonylureas and -thioureas, their preparation, their use and pharmaceutical compositions comprising them
  申请人：HACHTEL Stephanie

  公开号：US20080033016A1

  公开（公告）日：2008-02-07

  The present invention relates to piperidinesulfonylureas and piperidinesulfonylthioureas of formula I, in which A, X, R(1), R(2) and R(3) have the meanings indicated in the claims. The compounds of formula I are valuable active pharmaceutical ingredients which show in particular an inhibiting effect on ATP-sensitive potassium channels of the cardiac muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies or reduced contractility of the heart or for the prevention of sudden cardiac death. The invention further relates to processes for preparing the compounds of formula I, their use and pharmaceutical compositions comprising them.

  本发明涉及式I的哌啶磺酰脲和哌啶磺酰硫脲，其中A、X、R（1）、R（2）和R（3）具有声明中所示的含义。式I的化合物是有价值的活性药物成分，特别表现出对心脏肌肉的ATP敏感性钾通道的抑制作用，适用于治疗心血管系统疾病，如冠心病、心律失常、心力衰竭、心肌病或心脏收缩力降低，或用于预防突发性心脏死亡。本发明还涉及制备式I化合物的方法、其用途以及含有它们的药物组合物。
• WO2006/63722
  申请人：——

  公开号：——

  公开（公告）日：——
• PIPERIDINESULFONYLUREAS AND -THIOUREAS, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：EP1828131B1

  公开（公告）日：2008-06-04
• US8586612B2
  申请人：——

  公开号：US8586612B2

  公开（公告）日：2013-11-19
• [EN] PIPERIDINESULFONYLUREAS AND -THIOUREAS, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM<br/>[FR] PIPERIDINESULFONYLUREES ET -THIOURLEES, LEUR PREPARATION, LEUR UTILISATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：SANOFI AVENTIS DEUTSCHLAND

  公开号：WO2006063722A1

  公开（公告）日：2006-06-22

  [EN] The present invention relates to piperidinesulfonylureas and piperidinesulfonylthioureas of the formula (I), in which A, X, R(1), R(2) and R(3) have the meanings indicated in the claims. The compounds of the formula (I) are valuable active pharmaceutical ingredients which show in particular an inhibiting effect on ATP-sensitive potassium channels of the cardiac muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies or reduced contractility of the heart or for the prevention of sudden cardiac death. The invention further relates to processes for preparing the compounds of the formula (I), their use and pharmaceutical compositions comprising them.
  [FR] L'invention concerne des pipéridinesulfonylurées et des pipéridinesulfonylthiourées de la formule (I) dans laquelle A, X, R(1), R(2) et R(3) ont les significations indiquées dans les revendications. Les composés de la formule (I) sont des ingrédients pharmaceutiques actifs de valeur qui présentent notamment un effet inhibiteur sur les canaux potassiques sensibles à ATP du muscle cardiaque et sont aptes, par exemple, au traitement de troubles du système cardio-vasculaire tel que les coronaropathies, les arythmies, les insuffisances cardiaques, les cardiomyopathies ou la faible contractilité du coeur ou bien dans la prévention d'une mort cardiaque subite. L'invention concerne également des procédés de préparation des composés de la formule (I), leur utilisation ainsi que des compositions pharmaceutiques les contenant.