15-amino-N-[3-(1-hydroxyethyl)phenyl]-4,7-dioxa-13-thia-11-azatetracyclo[8.7.0.03,8.012,16]heptadeca-1(17),2,8,10,12(16)-pentaene-14-carboxamide

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 15-amino-N-[3-(1-hydroxyethyl)phenyl]-4,7-dioxa-13-thia-11-azatetracyclo[8.7.0.03,8.012,16]heptadeca-1(17),2,8,10,12(16)-pentaene-14-carboxamide
• 化学式: C₂₂H₂₁N₃O₄S
• 分子量: 423.5
• InChiKey: AJZOMXHDIQKOQD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  132
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• [EN] NOVEL INHIBITORS OF PROTEIN KINASE C EPSILON SIGNALING<br/>[FR] NOUVEAUX INHIBITEURS DE LA SIGNALISATION DE LA PROTÉINE KINASE C EPSILON
  申请人：MEDIZINISCHE UNIVERSITÄT INNSBRUCK

  公开号：WO2014207213A1

  公开（公告）日：2014-12-31

  The present invention relates to novel inhibitors of protein kinase C epsilon (PKCε) signaling, including in particular the compounds of formula (I) as described and defined herein, pharmaceutical compositions comprising these inhibitors, and their use in the treatment or prevention of disorders such as, e.g., a cardiovascular disorder, cardiac hypertrophy, heart failure, anxiety, pain, chronic pain, migraine, an allergy, an inflammatory disorder, an autoimmune disorder, diabetes, diabetic complications, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic neuropathy, cancer, metastatic cancer, drug-resistant cancer, stomach cancer, lung cancer, thyroid cancer, colon cancer, breast cancer, a neurological disorder, Alzheimer's disease, Parkinson's disease, bipolar disorder, stroke, alopecia, or alcoholism.

  本发明涉及新型蛋白激酶Cε（PKCε）信号的抑制剂，特别是本说明中描述和定义的化合物（I）的药物组合物，以及它们在治疗或预防心血管疾病、心肌肥大、心力衰竭、焦虑、疼痛、慢性疼痛、偏头痛、过敏、炎症性疾病、自身免疫性疾病、糖尿病、糖尿病并发症、糖尿病视网膜病变、糖尿病肾病、糖尿病心肌病、糖尿病神经病变、癌症、转移性癌症、耐药癌症、胃癌、肺癌、甲状腺癌、结肠癌、乳腺癌、神经系统疾病、阿尔茨海默病、帕金森病、躁郁症、中风、脱发或酗酒等疾病的治疗或预防中的使用。