7-[[2-amino-2-(4-hydroxyphenyl)acetyl]amino]-8-oxo-3-[(E)-prop-1-enyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic 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: 7-[[2-amino-2-(4-hydroxyphenyl)acetyl]amino]-8-oxo-3-[(E)-prop-1-enyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
• 化学式: C₁₈H₁₉N₃O₅S
• 分子量: 389.4
• InChiKey: WDLWHQDACQUCJR-NSCUHMNNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.4
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  158
• 氢给体数：
  4
• 氢受体数：
  7

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：有限的信息表明，头孢丙烯在乳汁中产生的水平较低，预计不会对哺乳婴儿造成不良影响。偶尔有报道称，使用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。头孢丙烯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:Limited information indicates that cefprozil produces low levels in milk that are 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. Cefprozil 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

• New derivatives of cephalosporin for treating cancer
  申请人：Institut Curie

  公开号：EP2926815A1

  公开（公告）日：2015-10-07

  The present invention relates to a new class of cephalosporin derivatives of formula (I), notably having CXCR4 receptor antagonist effect, useful as a therapeutic agent for treating cancer, in particular for treating breast cancer, lung cancer and uveal melanoma. The invention further relates to a pharmaceutical composition comprising a compound of formula (I) and an additional antitumor drug for treating cancer.

  本发明涉及一类新的式(I)头孢菌素衍生物，特别是具有 CXCR4 受体拮抗剂作用的衍生物，可作为治疗癌症，特别是治疗乳腺癌、肺癌和葡萄膜黑色素瘤的治疗剂。本发明还涉及一种药物组合物，该药物组合物包含式（I）化合物和另一种治疗癌症的抗肿瘤药物。
• Derivatives of cephalosporin for treating cancer
  申请人：INSTITUT CURIE

  公开号：US10821114B2

  公开（公告）日：2020-11-03

  The present invention relates to a new class of cephalosporin derivatives of formula (I), notably having CXCR4 receptor antagonist effect, useful as a therapeutic agent for treating cancer, in particular for treating breast cancer, lung cancer and uveal melanoma. The invention further relates to a pharmaceutical composition comprising a compound of formula (I) and an additional antitumor drug for treating cancer.

  本发明涉及一类新的式(I)头孢菌素衍生物，特别是具有 CXCR4 受体拮抗剂作用的衍生物，可作为治疗癌症，特别是治疗乳腺癌、肺癌和葡萄膜黑色素瘤的治疗剂。本发明还涉及一种药物组合物，该药物组合物包含式（I）化合物和另一种治疗癌症的抗肿瘤药物。
• COMPOSITIONS AND MEANS FOR DIAGNOSING MICROBIAL INFECTIONS
  申请人：Statens Serum Institut

  公开号：EP2181330B1

  公开（公告）日：2013-11-20
• EFFERVESCENT FORMULATIONS COMPRISING CEFPROZIL AS ACTIVE AGENT
  申请人：Bilgic, Mahmut

  公开号：EP2528593A2

  公开（公告）日：2012-12-05
• NEW DERIVATIVES OF CEPHALOSPORIN FOR TREATING CANCER
  申请人：Institut Curie

  公开号：EP3125901A1

  公开（公告）日：2017-02-08