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1.发明公开3-TETRAZOLYL-BENZENE-1,2-DISULFONAMIDE DERIVATIVES AS METALLO-BETA-LACTAMASE INHIBITORS 审中-公开作为金属β内酰胺酶抑制剂的3-四唑基 - 苯-1,2-二磺酰胺衍生物
公开(公告)号：EP3313832A1
公开(公告)日：2018-05-02
申请号：EP16734151.0
申请日：2016-06-24
Applicant: Merck Sharp & Dohme Corp.
Inventor： BENNETT, Frank , JIANG, Jinlong , PASTERNAK, Alexander , DONG, Shuzhi , GU, Xin , SCOTT, Jack, D. , TANG, Haiqun , ZHAO, Zhiqiang , HUANG, Yuhua , YANG, Dexi , YOUNG, Katherine , XIAO, Li , ZHANG, Zhibo , FU, Jianmin
IPC: C07D403/12 , C07D413/14 , C07D401/10 , C07D403/10 , C07D403/14 , C07D407/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , A61K31/41 , A61K31/4184 , A61K31/428 , A61K31/4439 , 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-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X 2 and R1are as defined herein. The present invention also relates to compositions which comprise a metallo-beta-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.
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公开(公告)号：EP3867232A1
公开(公告)日：2021-08-25
申请号：EP19872407.2
申请日：2019-10-11
Applicant: Merck Sharp & Dohme Corp.
Inventor： CLAUSEN, Dane , CHEN, Ping , FRADERA, Xavier , GUO, Liangqin , HAN, Yongxin , HE, Shuwen , LIM, Jongwon , MARTINOT, Theodore, A. , PASTERNAK, Alexander , XIAO, Li , YU, Wensheng
IPC: C07D231/38 , C07D401/06 , C07D401/10
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公开(公告)号：EP3654968A1
公开(公告)日：2020-05-27
申请号：EP18835337.9
申请日：2018-07-12
Applicant: Merck Sharp & Dohme Corp.
Inventor： PASTERNAK, Alexander , DONG, Shuzhi , SCOTT, Jack, D. , TANG, Haiqun , ZHAO, Zhiqiang , YANG, Dexi , GU, Xin , JIANG, Jinlong , XIAO, Li
IPC: A61K31/395 , A61K31/41 , C07D257/02
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公开(公告)号：EP3313828A1
公开(公告)日：2018-05-02
申请号：EP16815358.3
申请日：2016-06-24
Applicant: Merck Sharp & Dohme Corp.
Inventor： BENNETT, Frank , JIANG, Jinlong , PASTERNAK, Alexander , DONG, Shuzhi , GU, Xin , SCOTT, Jack, D. , TANG, Haiqun , ZHAO, Zhiqiang , HUANG, Yuhua , HUNTER, David , YANG, Dexi , YOUNG, Katherine , XIAO, Li , ZHANG, Zhibo , FU, Jianmin , BAI, Yunfeng , ZHENG, Zhixiang , ZHANG, Xu
IPC: C07D257/02 , C07D257/04 , A61K31/41 , A61K31/395
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-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X 2 and R1are as defined herein. The present invention also relates to compositions which comprise a metallo-beta-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.
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5.发明公开
公开(公告)号：EP3886845A1
公开(公告)日：2021-10-06
申请号：EP19888409.0
申请日：2019-11-25
Applicant: Merck Sharp & Dohme Corp.
Inventor： CLAUSEN, Dane , CHEN, Ping , FRADERA, Xavier , GUO, Liangqin , HAN, Yongxin , HE, Shuwen , HUANG, Xianhai , KOZLOWSKI, Joseph , LI, Guoqing , MARTINOT, Theodore, A. , PASTERNAK, Alexander , VERRAS, Andreas , XIAO, Li , YU, Wensheng , ZHANG, Rui
IPC: A61K31/416 , C07D231/56
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Patent Agency Ranking
公开(公告)号：EP3139918B1
公开(公告)日：2019-12-25
申请号：EP15789928.7
申请日：2015-05-04
Applicant: Merck Sharp & Dohme Corp.
Inventor： TANG, Haifeng , YANG, Shu-Wei , MANDAL, Mihir , SU, Jing , LI, Guoqing , PAN, Weidong , TANG, Haiqun , DEJESUS, Reynalda , PAN, Jianping , HAGMANN, William , DING, Fa-Xiang , XIAO, Li , PASTERNAK, Alexander , HUANG, Yuhua , DONG, Shuzhi , YANG, Dexi
IPC: A61K31/41 , A61K31/192 , C07D403/12 , C07D401/14 , C07D413/14 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/10 , C07D409/06 , C07D413/06 , C07D417/06 , C07D471/04 , C07D471/10 , C07D257/04 , C07D487/04
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7.发明公开
公开(公告)号：EP3836928A1
公开(公告)日：2021-06-23
申请号：EP19850118.1
申请日：2019-08-12
Applicant: Merck Sharp & Dohme Corp.
Inventor： CLAUSEN, Dane , FRADERA, Xavier , HAN, Yongxin , PASTERNAK, Alexander , XIAO, Li , ZHANG, Hongjun
IPC: A61K31/47 , C07D215/08 , C07D215/14
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公开(公告)号：EP3810116A1
公开(公告)日：2021-04-28
申请号：EP19811446.4
申请日：2019-05-28
Applicant: Merck Sharp & Dohme Corp.
Inventor： HE, Shuwen , CLAUSEN, Dane , GUO, Liangqin , HAN, Yongxin , HUANG, Xianhai , PASTERNAK, Alexander , PU, Qinglin , XIAO, Dong , XIAO, Li , ZHANG, Hongjun
IPC: A61K31/166 , C07C13/08 , C07C233/65
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公开(公告)号：EP3096754B1
公开(公告)日：2018-08-29
申请号：EP15740828.7
申请日：2015-01-16
Applicant: Merck Sharp & Dohme Corp.
Inventor： MANDAL, Mihir , TANG, Haifeng , XIAO, Li , SU, Jing , LI, Guoqing , YANG, Shu-Wei , PAN, Weidong , TANG, Haiqun , DEJESUS, Reynalda , HICKS, Jacqueline , LOMBARDO, Matthew , CHU, Hong , HAGMANN, William , PASTERNAK, Alex , GU, Xin , JIANG, Jinlong , DONG, Shuzhi , DING, Fa-Xiang , LONDON, Clare , BISWAS, Dipshikha , YOUNG, Katherine , HUNTER, David N. , ZHAO, Zhiqiang , YANG, Dexi
IPC: C07D257/04 , A61P31/04 , A61K31/41 , A61K31/4184 , C07D401/04 , C07D401/10 , C07D403/10 , C07D405/10 , C07D405/12
CPC classification number: C07D491/048 , A61K31/197 , A61K31/407 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D257/04 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D451/04 , C07D471/04 , C07D471/10 , C07D487/04 , Y02A50/473 , A61K2300/00
Abstract: The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
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公开(公告)号：EP3096754A1
公开(公告)日：2016-11-30
申请号：EP15740828.7
申请日：2015-01-16
Applicant: Merck Sharp & Dohme Corp.
Inventor： MANDAL, Mihir , TANG, Haifeng , XIAO, Li , SU, Jing , LI, Guoqing , YANG, Shu-Wei , PAN, Weidong , TANG, Haiqun , DEJESUS, Reynalda , HICKS, Jacqueline , LOMBARDO, Matthew , CHU, Hong , HAGMANN, William , PASTERNAK, Alex , GU, Xin , JIANG, Jinlong , DONG, Shuzhi , DING, Fa-Xiang , LONDON, Clare , BISWAS, Dipshikha , YOUNG, Katherine , HUNTER, David N. , ZHAO, Zhiqiang , YANG, Dexi
IPC: A61K31/41 , A61K31/4184 , C07D257/04
CPC classification number: C07D491/048 , A61K31/197 , A61K31/407 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D257/04 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D451/04 , C07D471/04 , C07D471/10 , C07D487/04 , Y02A50/473 , A61K2300/00
Abstract: The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
Abstract translation: 本发明涉及金属-β-内酰胺酶抑制剂的式（I）化合物，这种化合物的合成，以及这些化合物与β-内酰胺抗生素一起用于克服抗性的用途。
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