Ethyl 2-acetamido-4-(4-methoxyphenyl)-5-methylthiophene-3-carboxylate

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: Ethyl 2-acetamido-4-(4-methoxyphenyl)-5-methylthiophene-3-carboxylate
• 化学式: C₁₇H₁₉NO₄S
• mdl: MFCD06003870
• 分子量: 333.4
• InChiKey: TZDQOKNMHQUQAJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  92.9
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Composition for Prevention or Treatment of Heart Failure
  申请人：Park Woo Jin

  公开号：US20110245179A1

  公开（公告）日：2011-10-06

  Provided are a composition for preventing or treating heart failure and a method for screening an agent for treating heart failure. The present disclosure demonstrates for the first time that administration of PKCζ inhibitor provides inotropic effect by increasing myocardial contractility. Thus, the present disclosure will contribute greatly to the prevention or treatment of heart failure. Also, since the present disclosure is based on the change in calcium sensitivity in cardiac myocytes unlike the existing inotropic agents, it can enhance the myocardial contractility without increasing oxygen demand or the risk of arrhythmia.

  提供了一种预防或治疗心力衰竭的组合物以及一种筛选治疗心力衰竭药物的方法。本公开首次证明了PKCζ抑制剂的给药通过增加心肌收缩力提供正性肌力作用。因此，本公开将极大地有助于预防或治疗心力衰竭。此外，由于本公开基于心肌细胞中钙敏感性的变化，不同于现有的正性肌力药物，它可以增强心肌收缩力而不增加氧需求或心律失常的风险。
• PROTEIN KINASE C ZETA INHIBITION TO TREAT VASCULAR PERMEABILITY
  申请人：Antonetti David A.

  公开号：US20080021036A1

  公开（公告）日：2008-01-24

  Methods of treating or preventing a disease or disorder in a subject are provided by the present invention which include administering a composition including a therapeutically effective amount of a protein kinase C (PKC) zeta inhibitor. A disease or disorder treated or prevented by administration of a PKC zeta inhibitor is characterized by abnormal vascular permeability. Diseases or disorders treated or prevented by administration of a composition including a therapeutically effective amount of a PKC zeta inhibitor include cancer, an ischemic condition and microvascular complications of a systemic or local condition in the subject, such as diabetes and/or diabetic macular edema. Additionally, methods of inhibiting PKC zeta are provided which include incubating PKC zeta in vivo, in vitro and/or in silico with a PKC zeta inhibitor.
• US7585865B2
  申请人：——

  公开号：US7585865B2

  公开（公告）日：2009-09-08
• US8211893B2
  申请人：——

  公开号：US8211893B2

  公开（公告）日：2012-07-03
• [EN] PROTEIN KINASE C ZETA INHIBITION TO TREAT VASCULAR PERMEABILITY<br/>[FR] INHIBITION DE LA PROTÉINE KINASE C ZÊTA POUR TRAITER LA PERMÉABILITÉ VASCULAIRE
  申请人：PENN STATE RES FOUND

  公开号：WO2008011621A2

  公开（公告）日：2008-01-24

  [EN] Methods of treating or preventing a disease or disorder in a subject are provided by the present invention which include administering a composition including a therapeutically effective amount of a protein kinase C (PKC) zeta inhibitor. A disease or disorder treated or prevented by administration of a PKC zeta inhibitor is characterized by abnormal vascular permeability. Diseases or disorders treated or prevented by administration of a composition including a therapeutically effective amount of a PKC zeta inhibitor include cancer, an ischemic condition and microvascular complications of a systemic or local condition in the subject, such as diabetes and/or diabetic macular edema. Additionally, methods of inhibiting PKC zeta are provided which include incubating PKC zeta in vivo, in vitro and/or in silico with a PKC zeta inhibitor.
  [FR] L'invention porte sur des méthodes de traitement et de prévention de troubles ou maladies consistant à administrer à un patient une dose à efficacité thérapeutique d'un inhibiteur de la proteine kinase C zêta (PKC zêta), de tels troubles ou maladies se caractérisant par une perméabilité vasculaire anormale, et l'administration de compositions contenant une quantité à efficacité thérapeutique la PKC zêta peut également traiter le cancer, l'ischémie, et des complications microvasculaires d'états systémiques ou locaux tels que le diabète et/ou l'oedème maculaire diabétique. L'invention porte également sur des méthodes d'inhibition de la PKC zêta consistant à l'incuber in vivo, in vitro et/ou in silico avec un inhibiteur de la PKC zêta.