Cefepime conjugate acid

• 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: Cefepime conjugate acid
• 英文别名: (6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-[(1-methylpyrrolidin-1-ium-1-yl)methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
• 化学式: C19H25N6O5S2+
• 分子量: 481.6
• InChiKey: HVFLCNVBZFFHBT-ZKDACBOMSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  201
• 氢给体数：
  3
• 氢受体数：
  10

ADMET

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用概述：尽管没有关于母乳喂养期间使用头孢匹姆的信息，但母乳中的水平似乎较低，而且通常不期望头孢菌素对哺乳婴儿产生不良影响。偶尔会有报道头孢菌素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。头孢匹姆在哺乳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 cefepime during breastfeeding, the levels in breastmilk appear to be low and cephalosporins are generally not be 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. Cefepime 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

• BATE-LACTAMASE INHIBITORS
  申请人：Dmitrienko Gary I.

  公开号：US20110046101A1

  公开（公告）日：2011-02-24

  The present invention relates to broad spectrum β-lactamase inhibitors. More particularly, the invention relates to inhibitors of Class B metallo (MBL) and Class D (OXA) β-lactamases. A method of treating a bacterial infection is provided, wherein the method comprises administering to a mammalian patient in need of such treatment a compound of formula (I) wherein R 1 is selected from R 2 is selected from with certain provisos as herein defined; in combination with a pharmaceutically acceptable β-lactam antibiotic in an amount which is effective for treating the bacterial infection.

  本发明涉及广谱β-内酰胺酶抑制剂。更具体地，本发明涉及类B金属酶(MBL)和类D（OXA）β-内酰胺酶的抑制剂。提供了一种治疗细菌感染的方法，其中该方法包括向需要此类治疗的哺乳动物患者施用具有以下结构的化合物（I）其中R1从中选择R2从中选择与此处定义的某些条件一起；与一种对治疗细菌感染有效的药用β-内酰胺抗生素结合在一起。
• [EN] PROCESS FOR THE DIRECT PREPARATION OF CEFEPIME FOR INJECTABLE USE<br/>[FR] PROCÉDÉ DE PRÉPARATION DIRECTE DE CÉFÉPIME POUR UTILISATION PAR VOIE INJECTABLE
  申请人：CORDEN PHARMA LATINA S P A CON UNICO SOCIO

  公开号：WO2013114319A1

  公开（公告）日：2013-08-08

  The present invention concerns a direct process, without the need to isolate any intermediate, for the preparation of Cefepime dihydrochloride monohydrate of sterile quality (for injective use) comprising a preliminary decolorization step in water of the compound of formula (II) in the presence of base or acid, an acylation step with MAEM in the presence of at least one solvent miscible in water, an extraction step in the presence of a solvent immiscible with water, a decolorization step of the rich water solution containing the dissolved product and, lastly, a crystallisation step of the product with acetone in the presence of hydrochloric acid.

  本发明涉及一种直接工艺，无需分离任何中间体，用于制备注射用的Cefepime双氯化物一水合物的无菌质量，包括以下步骤：在水中存在碱或酸的情况下，对式（II）化合物进行预处理脱色步骤；在至少一种可溶于水的溶剂存在下，使用MAEM进行酰化步骤；在与水不相溶的溶剂存在下进行萃取步骤；对含有溶解产品的富水溶液进行脱色步骤；最后，在盐酸存在下，使用丙酮结晶步骤对产品进行结晶。
• Processes for the preparations of cefepime
  申请人：Ludescher Johannes

  公开号：US20070105830A1

  公开（公告）日：2007-05-10

  This invention provides processes for preparing cefepime, including crystalline intermediates of Formula V.

  这项发明提供了制备头孢匹酮的方法，包括公式V的结晶中间体。
• CEPHALOSPORIN COMPOUND
  申请人：Cubist Pharmaceuticals, Inc.

  公开号：US20150025053A1

  公开（公告）日：2015-01-22

  The cephalosporin compound of formula (I) is disclosed, which exhibits antibiotic activity against Gram-negative (e.g., Pseudomonas aeruginosa ) and Gram-positive (e.g., methicillin-resistant Staphylococcus aureus ) bacteria. Methods of manufacturing the compound of formula (I), and uses of the compound in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

  公开了化合物式（I）的头孢菌素化合物，该化合物对革兰氏阴性菌（例如铜绿假单胞菌）和革兰氏阳性菌（例如甲氧西林耐药金黄色葡萄球菌）表现出抗生素活性。还公开了制造化合物式（I）的方法以及在制备制药组合物和抗菌应用中使用该化合物的用途。
• CEPHEM COMPOUND HAVING CATECHOL GROUP
  申请人：Shionogi & Co., Ltd.

  公开号：EP2557082A1

  公开（公告）日：2013-02-13

  A compound of the formula: wherein X is -N=, -CH=, or the like; W is -CH2- or the like; U is -S- or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; R3 is hydrogen or the like; each R4 is independently hydrogen, halogen, or the like; m is an integer from 0 to 2; Q is a single bond, or the like; G is -C(=O)-, or the like; D is a single bond, -NH-, or the like; and E is a cyclic quaternary ammonium group, or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.

  式中的化合物： 其中 X是-N=、-CH=或类似的物质； W 是-CH2-或类似物 U 是 -S- 或类似物； R1 和 R2 各自独立地为氢、卤素、任选取代的低级烷基或类似物； R3 是氢或类似物 每个 R4 独立地为氢、卤素或类似物； m 是 0 至 2 的整数； Q 是单键或类似物； G 是 -C(=O)- 或类似物； D 是单键、-NH- 或类似物；以及 E 是环状季铵基团、 或酯、7-侧链中环上氨基处的受保护化合物、药学上可接受的盐或其溶液。