| 摘要 |
The present invention is directed to compounds which are beta-lacatamase inhibitors. The compounds and their pharmaceutically acceptable salts, are useful in combination with beta-lactam antibiotics, or alone, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to formula (Ia):;
or a pharmaceutically acceptable salt thereof, wherein the values of R1, R2, R3 and R4 are described herein. |
| 主权项 |
1. A compound according to formula (Ia):or a pharmaceutically acceptable salt thereof, wherein:
R1 is —CONR′R″, —CN, or an C1-C3 alkyl substituted with C1-C3 alkoxy, —OH, —CN, —NR′R″, or —CONR′R″; R2 and R3 are independently selected from H, halo, —CN, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C1-C6 alkoxy, —CONR′R″, or C(O)2R′; wherein the alkyl, alkenyl, cycloalkyl, and alkoxy represented by R2 or R3 are independently and optionally substituted by one or more halo, —CN, —OH, C1-C3 alkyl, C1-C3 haloalkyl, C3-C6 cycloalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy, —NR′R″, 5-7 membered heterocycle, —C(O)NR′R″ or —NR′C(O)R″; and each R′ and R″ are independently selected from hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, phenyl, 5 to 6 membered heterocyclyl or a 5 to 6 membered heteroaryl; wherein each alkyl, cycloalkyl, phenyl, heterocyclyl and heteroaryl is optionally and independently substituted with one or more halo, —CN, —OH, C1-C3 alkyl, C1-C3 haloalkyl, C3-C6 cycloalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy, —C(O)(C1-C6 alkyl), —C(O)(C1-C6 alkoxy), —NH2, —NH(C1-C3 alkyl), —N(C1-C3 alkyl)2, a 5-7 membered heterocyclyl or a 5-7 membered heteroaryl; provided that R2 and R3 are not both hydrogen; and when R1 is —C(O)NR′R″, then neither of R2 or R3 is —C(O)NR′R″. |
