4-(dimethylamino)-3,10,12,12a-tetrahydroxy-7-{[methoxy(methyl)amino]methyl}-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 四环素类
• 英文名称: 4-(dimethylamino)-3,10,12,12a-tetrahydroxy-7-{[methoxy(methyl)amino]methyl}-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
• 化学式: C24H29N3O8
• InChiKey: PQJQFLNBMSCUSH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.11
• 重原子数：
  35.0
• 可旋转键数：
  5.0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  173.86
• 氢给体数：
  5.0
• 氢受体数：
  10.0

文献信息

• [EN] METHODS OF USING (4S,4AS,5AR,12AS)-4- DIMETHYLAMINO-3,10,12,12A-TETRAHYDROXY-7-[(METHOXY(METHYL)AMINO)-METHYL]-1,11-DIOXO-1,4,4A,5,5A,6,11,12A-OCTAHYDRO-NAPHTHACENE-2-CARBOXYLIC ACID AMIDE<br/>[FR] PROCÉDÉS D'UTILISATION DU (4S,4AS,5AR,12AS)-4- DIMÉTHYLAMINO-3,10,12,12A-TÉTRAHYDROXY-7-[(MÉTHOXY(MÉTHYL)AMINO)-MÉTHYL]-1,11-DIOXO-1,4,4A,5,5A,6,11,12A-OCTAHYDRO-NAPHTACÈNE-2-CARBOXAMIDE
  申请人：PARATEK PHARM INNC

  公开号：WO2013173326A1

  公开（公告）日：2013-11-21

  A method of treating a bacterial infection, e.g., a bacterial infection with methicillin resistant Staphylococcus aureus, Helicobacter pylori, Chlamydia trachomatis, or Chlamydia pneumonia, comprising administering to a subject (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7- [(methoxy(methyl)amino)-methyl] -1,11-dioxo-1,4,4a,5,5a,6, 11, 12a-octahydronaphthacene-2-carboxylic acid amide or a pharmaceutically acceptable salt thereof is disclosed. More specifically, a method of treating a bacterial infection comprising administering to a subject crystalline mono hydrochloride salt, crystalline mono mesylate salt or crystalline mono sulfate salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7- [(methoxy(methyl)amino)-methyl]-l,l l-dioxo-l,4,4a,5,5a,6,l l,12a-octahydro- naphthacene-2-carboxylic acid amide is disclosed.

  本发明涉及一种治疗细菌感染的方法，例如甲氧苄青霉素耐药金黄色葡萄球菌、幽门螺杆菌、沙眼衣原体或肺炎衣原体感染，包括向受试者给予(4S,4aS,5aR,12aS)-4-二甲氨基-3,10,12,12a-四羟基-7-[(甲氧基(甲基)氨基)-甲基]-1,11-二氧-1,4,4a,5,5a,6,11,12a-八氢萘并噻吩-2-羧酸酰胺或其药学上可接受的盐。更具体地，本发明揭示了一种治疗细菌感染的方法，包括向受试者给予(4S,4aS,5aR,12aS)-4-二甲氨基-3,10,12,12a-四羟基-7-[(甲氧基(甲基)氨基)-甲基]-1,11-二氧-1,4,4a,5,5a,6,11,12a-八氢萘并噻吩-2-羧酸酰胺的结晶单盐酸盐、结晶单甲磺酸盐或结晶单硫酸盐。
• TETRACYCLINE DERIVATIVES FOR THE TREATMENT OF BACTERIAL, VIRAL AND PARASITIC INFECTIONS
  申请人：Paratek Pharmaceuticals, Inc.

  公开号：EP2109602B1

  公开（公告）日：2014-02-12
• METHODS OF USING (4S,4AS,5AR,12AS)-4- DIMETHYLAMINO-3,10,12,12A-TETRAHYDROXY-7-[(METHOXY(METHYL)AMINO)-METHYL]-1,11-DIOXO-1,4,4A,5,5A,6,11,12A-OCTAHYDRO-NAPHTHACENE-2-CARBOXYLIC ACID AMIDE
  申请人：Paratek Pharmaceuticals, Inc.

  公开号：EP2849757A1

  公开（公告）日：2015-03-25