公开(公告)号：WO2009114921A1

公开(公告)日：2009-09-24

申请号：PCT/CA2008/000515

申请日：2008-03-17

Applicant: DMITRIENKO, Gary I. ,  VISWANATHA, Thammaiah ,  JOHNSON, Jarrod W. ,  RAMADHAR, Timothy R.

Inventor： DMITRIENKO, Gary I. ,  VISWANATHA, Thammaiah ,  JOHNSON, Jarrod W. ,  RAMADHAR, Timothy R.

IPC: A61K31/165 ,  A61K31/496 ,  A61P31/04 ,  C12N9/99

CPC classification number: A61K31/165 ,  A61K31/496 ,  C12N9/99

Abstract: The present invention relates to broad spectrum β-lactamase inhibitors; more particularly, 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 (II), and (III); R 2 is selected from (IV), and (V); with the proviso that: if R 1 is (VI), then R 2 is selected from (VII), or (VIII); if R 1 is (IX), then R 2 is (X) or (XI); if R 1 is (XII), or (XIII) then R 2 is (XIV); and if R1 is (XV), then R 2 is (XVI); in combination with a pharmaceutically acceptable β-lactam antibiotic in an amount which is effective for treating the bacterial infection.

Abstract translation: 本发明涉及广谱β-内酰胺酶抑制剂; 更具体地，涉及B类金属（MBL）和D类（OXA）β-内酰胺酶的抑制剂。 提供了治疗细菌感染的方法，其中所述方法包括向需要这种治疗的哺乳动物患者施用其中R 1选自（II）和（III）的式（I）化合物; R2选自（IV）和（V）; 条件是：如果R1是（VI），则R2选自（VII）或（VIII）; 如果R1是（IX），则R2是（X）或（XI）; 如果R1是（XII）或（XIII），则R2是（XIV）; 并且如果R1是（ⅩⅤ），则R2是（ⅩⅥ）; 与药学上可接受的β-内酰胺抗生素组合，其量对于治疗细菌感染是有效的。

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。