公开(公告)号：US10227331B2

公开(公告)日：2019-03-12

申请号：US15737334

申请日：2016-06-24

Applicant: Merck Sharp & Dohme Corp.

Inventor： Frank Bennett ,  Jinlong Jiang ,  Alexander Pasternak ,  Shuzhi Dong ,  Xin Gu ,  Jack D. Scott ,  Haiqun Tang ,  Zhiqiang Zhao ,  Yuhua Huang ,  David Hunter ,  Dexi Yang ,  Katherine Young ,  Li Xiao ,  Zhibo Zhang ,  Jianmin Fu ,  Yunfeng Bai ,  Zhixiang Zheng ,  Xu Zhang

IPC: C07D403/10 ,  C07D403/12 ,  C07D413/14 ,  C07D401/10 ,  C07D403/14 ,  C07D407/14 ,  C07D413/10 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  A61P31/04 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D487/04 ,  A61K31/198 ,  A61K31/407 ,  A61K31/41 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/431 ,  A61K31/439 ,  A61K31/496 ,  A61K31/541 ,  A61K31/546 ,  C07D405/14 ,  C07D453/02 ,  C07D487/10 ,  C07D493/04 ,  C07D493/08 ,  C07D495/08

Abstract: The present invention relates to metallo-β-lactamase inhibitor compounds of Formula I: (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and RB are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.

公开(公告)号：US20180179190A1

公开(公告)日：2018-06-28

申请号：US15737334

申请日：2016-06-24

Applicant: Merck Sharp &Dohme Corp.

Inventor： Frank Bennett ,  Jinlong Jiang ,  Alexander Pasternak ,  Shuzhi Dong ,  Xin Gu ,  Jack D. Scott ,  Haiqun Tang ,  Zhiqiang Zhao ,  Yuhua Huang ,  David Hunter ,  Dexi Yang ,  Katherine Young ,  Li Xiao ,  Zhibo Zhang ,  Jianmin Fu ,  Yunfeng Bai ,  Zhixiang Zheng ,  Xu Zhang

IPC: C07D403/14 ,  A61K45/06 ,  A61K31/4184 ,  C07D401/14 ,  A61K31/454 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4545 ,  C07D487/04 ,  A61K31/5025 ,  C07D403/10 ,  A61K31/416 ,  A61K31/4439 ,  C07D417/14 ,  A61K31/428 ,  A61K31/4375 ,  C07D413/14 ,  A61K31/423 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/506 ,  A61K31/498 ,  A61K31/5377 ,  A61P31/04

CPC classification number: C07D403/10 ,  A61K31/198 ,  A61K31/407 ,  A61K31/41 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/431 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/546 ,  A61K45/06 ,  A61P31/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D493/04 ,  C07D493/08 ,  C07D495/08

Abstract: The present invention relates to metallo-β-lactamase inhibitor compounds of Formula I: (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and RB are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.