公开(公告)号：WO2011103686A1

公开(公告)日：2011-09-01

申请号：PCT/CA2011/050115

申请日：2011-02-25

Applicant: DMITRIENKO , Gary Igor ,  GHAVAMI , Ahmad ,  GOODFELLOW , Valerie Joy ,  JOHNSON , Jarrod W. ,  KRISMANICH , Anthony Paul ,  MARRONE , Laura ,  VISWANATHA , Sundaramma

Inventor： DMITRIENKO , Gary Igor ,  GHAVAMI , Ahmad ,  GOODFELLOW , Valerie Joy ,  JOHNSON , Jarrod W. ,  KRISMANICH , Anthony Paul ,  MARRONE , Laura

IPC: C07D501/36 ,  A61K31/545 ,  A61P31/04

CPC classification number: C07D501/36 ,  A61K31/545 ,  C07D501/26 ,  C07D501/28 ,  Y02A50/47 ,  Y02A50/471 ,  Y02A50/475 ,  Y02A50/481 ,  Y02A50/483

Abstract: The present invention relates to cephalosporin derivatives having β- lactamase inhibitory activity. The compounds are useful in preventing or treating bacterial resistance to an antibiotic, e.g. a β-lactam antibiotic. Disclosed herein are compounds that are inhibitors of class B metallo-β-lactamases, as well as class A, C, and D serine β-lactamases. In some preferred embodiments, the compounds are 3'- thiobenzoate derivatives of a cephalosporin. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the compounds are also disclosed.

Abstract translation: 本发明涉及具有β-内酰胺酶抑制活性的头孢菌素衍生物。 该化合物可用于预防或治疗对抗生素的细菌耐药性，例如， 一种β-内酰胺抗生素。 本文公开了作为B类金属β-内酰胺酶以及A，C和D类丝氨酸β-内酰胺酶的抑制剂的化合物。 在一些优选的实施方案中，化合物是头孢菌素的3'-硫代苯甲酸酯衍生物。 还公开了包含化合物的药物组合物，方法，用途，试剂盒和商业包装。