(3r)-3-Benzyl-4-[(4-Methoxyphenyl)sulfonyl]-1-[(1-Methyl-1h-Imidazol-5-Yl)methyl]-2,3,4,5-Tetrahydro-1h-1,4-Benzodiazepine-7-Carbonitrile

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 英文名称: (3r)-3-Benzyl-4-[(4-Methoxyphenyl)sulfonyl]-1-[(1-Methyl-1h-Imidazol-5-Yl)methyl]-2,3,4,5-Tetrahydro-1h-1,4-Benzodiazepine-7-Carbonitrile
• 英文别名: (3R)-3-benzyl-4-(4-methoxyphenyl)sulfonyl-1-[(3-methylimidazol-4-yl)methyl]-3,5-dihydro-2H-1,4-benzodiazepine-7-carbonitrile
• 化学式: C₂₉H₂₉N₅O₃S
• 分子量: 527.6
• InChiKey: BJWZXDNEKWSGQH-RUZDIDTESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  38
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  99.8
• 氢给体数：
  0
• 氢受体数：
  7

文献信息

• [EN] RAB GERANYLGERANYL TRANSFERASE INHIBITORS<br/>[FR] INHIBITEURS DE LA GÉRANYLEGÉRANYLE TRANSFÉRASE VERS RAB
  申请人：LEAD DISCOVERY CENTER GMBH

  公开号：WO2015181272A1

  公开（公告）日：2015-12-03

  The present invention relates to novel Rab geranylgeranyl transferase inhibitors of general formula (I) and stereoisomeric forms, hydrates, solvates and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing at least one of said Rab geranylgeranyl transferase inhibitors together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said Rab geranylgeranyl transferase inhibitors are particularly useful for the treatment and/or prophylaxis of proliferative diseases, tumors, cancers, metastases, diseases caused by pathological vesicle transport abnormalities, neuronal disorders (e.g. Charcotte-Marie-Tooth disease), infective diseases, thrombocytosis and clotting diseases and diseases where Rab mutations have been identified.

  本发明涉及一般式(I)及其立体异构体、水合物、溶剂化物和药学上可接受的盐的新型Rab靶向酰基转移酶抑制剂，以及至少包含其中一种Rab靶向酰基转移酶抑制剂和至少一种药学上可接受的载体、赋形剂和/或稀释剂的制药组合物。所述Rab靶向酰基转移酶抑制剂特别适用于治疗和/或预防增生性疾病、肿瘤、癌症、转移瘤、由病理性囊泡转运异常引起的疾病、神经系统疾病（如Charcotte-Marie-Tooth病）、感染性疾病、血小板增多症和凝血疾病以及已经确定存在Rab突变的疾病。