4-(2-{[(6R,7R)-7-{[(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(ethoxyimino)acetyl]amino}-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]sulfanyl}-1,3-thiazol-4-yl)-1-methylpyridinium

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: 4-(2-{[(6R,7R)-7-{[(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(ethoxyimino)acetyl]amino}-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]sulfanyl}-1,3-thiazol-4-yl)-1-methylpyridinium
• 英文别名: (6R,7R)-7-[[(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-ethoxyiminoacetyl]amino]-3-[[4-(1-methylpyridin-1-ium-4-yl)-1,3-thiazol-2-yl]sulfanyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
• 化学式: C22H21N8O5S4+
• 分子量: 605.7
• InChiKey: RGFBRLNVZCCMSV-BIRGHMBHSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  39
• 可旋转键数：
  9
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  284
• 氢给体数：
  3
• 氢受体数：
  14

文献信息

• [EN] PROCESS FOR PREPARING CEFTAROLINE SALTS OR HYDRATES THEREOF<br/>[FR] PROCÉDÉ DE PRÉPARATION DE SELS DE CEFTAROLINE OU D'HYDRATES DE CEUX-CI
  申请人：RANBAXY LAB LTD

  公开号：WO2013084171A1

  公开（公告）日：2013-06-13

  The present invention relates to a process for the preparation of ceftaroline salts or hydrates thereof.

  本发明涉及一种制备头孢替安盐酸盐或其水合物的方法。
• PROCESS FOR PREPARING CEFTAROLINE SALTS OR HYDRATES THEREOF
  申请人：RANBAXY LABORATORIES LIMITED

  公开号：US20140350240A1

  公开（公告）日：2014-11-27

  The present invention relates to a process for the preparation of ceftaroline salts or hydrates thereof.

  本发明涉及一种用于制备头孢他啶盐或其水合物的方法。
• USE OF PRODRUGS TO AVOID GI MEDIATED ADVERSE EVENTS
  申请人：Franklin Richard

  公开号：US20120202756A1

  公开（公告）日：2012-08-09

  The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.

  本发明涉及各种药物的前药和含有这些前药的制药组合物。还提供了一种方法，用于最小化与未衍生药物相关的局部介导（来自肠腔内）不良胃肠事件，并使用上述前药增加血浆药物水平的持续性。因此，本发明涉及使用各种药物（除阿片类药物外）的前药，以短暂地使它们失活，从而减少通常在给予原始化合物后出现的直接、局部介导的不良胃肠（GI）副作用。此外，这些前药可能提供改善的药代动力学。
• COMPOSITIONS AND METHODS FOR TREATING BACTERIAL INFECTIONS USING CEFTAROLINE
  申请人：Thye Dirk

  公开号：US20110071114A1

  公开（公告）日：2011-03-24

  The present invention relates to compositions comprising ceftaroline or a prodrug thereof (e.g., ceftaroline fosamil) and methods for treating bacterial infections, such as complicated skin and structure infections (cSSSI) and community-acquired bacterial pneumonia (CABP) by administering ceftaroline or a prodrug thereof, (e.g., ceftaroline fosamil).
• NOVEL CRYSTALLINE FORMS OF TRANS-7-OXO-6-(SULPHOOXY)-1,6-DIAZABICYCLO[3,2,1]OCTANE-2-CARBOXAMIDE SODIUM SALT
  申请人：Forest Laboratories Holdings Limited

  公开号：US20130267480A1

  公开（公告）日：2013-10-10

  The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.