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US 12,703,709 B2Granted
Cephalosporin antibacterial compound and preparation method therefor
AssigneesShanghai Senhui Medicine Co., Ltd., Shanghai Shengdi Pharmaceutical Co., Ltd., Jiangsu Hengrui Pharmaceuticals Co., Ltd.
InventorsJian Huang, Lingjian Zhu, Yang Zou, Cili Zhang
Life of this patent
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Abstract
The present disclosure relates to a cephalosporin antibacterial compound and a preparation method therefor. The cephalosporin antibacterial compound can exhibit antibacterial activity against Gram-negative bacteria and other bacteria.
Claims18
A compound of formula I or a pharmaceutically acceptable salt thereof,
- wherein,
- X is N, CH or C—Cl;
- T is S, S═O, CH2 or O;
- E is
- wherein R1 and R2 are each independently selected from the group consisting of hydrogen, halogen, phenyl, alkylthio, and alkyl optionally substituted with carbamoyl;
- R11 and R12 are each independently selected from the group consisting of hydrogen, carboxyl, and alkyl optionally substituted with carbamoyl;
- m is an integer of 1-5;
- F is a single bond;
- A is C1-C6 alkylene, C2-C6 alkenylene or C2-C6 alkynylene;
- each R5 is independently selected from the group consisting of halogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl and C1-C6 haloalkoxy;
- G1 is
- R1′ and R2′ are each independently selected from the group consisting of hydrogen, halogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl and C1-C6 haloalkoxy;
- R3 is C1-C6 alkyl substituted with
- R3′ is selected from the group consisting of hydrogen, hydroxy, C1-C6 alkyl and C1-C6 alkoxy, wherein the alkyl and alkoxy are optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halogen, hydroxy, sulfhydryl, —NRiRj,
- oxo, thio, —C(O)Rk, —C(O)ORk, —C(S)Rk, nitro, cyano, C1-C6 alkoxy and C1-C6 alkylthioether group;
- each Rm is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxy, 6- to 10-membered aryl and 5- to 8-membered heteroaryl, wherein the alkyl, alkoxy, aryl and heteroaryl are optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halogen, hydroxy, sulfhydryl, amino, carboxyl, nitro, cyano and C1-C6 alkoxy;
- each R4 is independently selected from the group consisting of halogen, hydroxy, sulfhydryl and —NRiRj;
- Ri and Rj are each independently selected from the group consisting of hydrogen, hydroxy, C1-C6 alkyl and C1-C6 alkoxy;
- each Rk is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 haloalkyl, hydroxy, C1-C6 alkoxy and —NRiRj, wherein the alkyl, haloalkyl and alkoxy are optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halogen, hydroxy, sulfhydryl, —NRiRj, oxo, thio, carboxyl, nitro, cyano, C1-C6 alkoxy, C1-C6 alkylthioether group, 3- to 6-membered cycloalkyl, 3- to 6-membered heterocyclyl, 6- to 10-membered aryl and 5- to 8-membered heteroaryl;
- p is an integer of 0-5;
- q is an integer of 0-5;
- x is 3;
- n is an integer of 0-3.
20 more elements
Dependencies are inferred from the claim text.