Ceftaroline anhydrous base | 402741-13-3

• 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: Ceftaroline anhydrous base
• 英文别名: (6R,7R)-7-[[(2Z)-2-ethoxyimino-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetyl]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
• CAS: 402741-13-3
• 化学式: C22H22N8O8PS4+
• 分子量: 685.7
• InChiKey: ZCCUWMICIWSJIX-NQJJCJBVSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  43
• 可旋转键数：
  11
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  328
• 氢给体数：
  5
• 氢受体数：
  17

ADMET

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用总结：尽管没有关于在哺乳期间使用头孢洛林的资料，但一般来说，头孢菌素类药物不太可能在哺乳婴儿中引起不良反应。偶尔有报道头孢菌素类药物会破坏婴儿的胃肠道菌群，导致腹泻或鹅口疮，但这些影响尚未得到充分评估。头孢洛林在哺乳期母亲中是可以接受的。 ◉ 对哺乳婴儿的影响：截至修订日期，没有找到相关的已发布信息。 ◉ 对泌乳和母乳的影响：截至修订日期，没有找到相关的已发布信息。

◉ Summary of Use during Lactation:Although no information is available on the use of ceftaroline during breastfeeding, cephalosporins are generally not expected to cause adverse effects in breastfed infants. Occasionally disruption of the infant's gastrointestinal flora, resulting in diarrhea or thrush have been reported with cephalosporins, but these effects have not been adequately evaluated. Ceftaroline is acceptable in nursing mothers. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.

来源:Drugs and Lactation Database (LactMed)

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。
• NOVEL PROCESS FOR PREPARING CEFTAROLINE FOSAMIL
  申请人：Sandoz AG

  公开号：EP2909219B1

  公开（公告）日：2019-02-13
• COMPOSITIONS AND METHODS OF TREATMENT COMPRISING CEFTAROLINE
  申请人：Biek Donald

  公开号：US20100197650A1

  公开（公告）日：2010-08-05

  The present invention provides compositions comprising ceftaroline or a pharmaceutically acceptable salt, solvate or a prodrug thereof alone or in combination with an antibacterial agent. The present invention provides methods of treating bacterial infection, which include administering an effective amount of ceftaroline or a pharmaceutically acceptable salt, solvate or a prodrug thereof alone or in combination with an antibacterial agent.
• 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.