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US 10,208,041 B2Granted
Diazabicyclooctane compounds
AssigneeHoffman-La Roche Inc.
InventorsPaul Spurr, Christelle Carl, Martin Binder, Kewei Yang, Valérie Verhoeven
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Abstract
The present invention relates to compounds according to Formula (II): or a stereoisomer, tautomer or pharmaceutically acceptable salt or ester thereof, wherein A, R1 and R2 are defined herein. Also described are pharmaceutically acceptable compositions of Formula (II) compounds as well as methods for utilizing the compounds of Formula (II) and the pharmaceutically acceptable compositions of Formula (II) compounds as antibacterial agents and β-lactamase inhibitors, useful in the treatment of infectious diseases.
Claims10
A compound of Formula (II)
- wherein
- R1 is benzyl, H or SO3M;
- M is H, or an inorganic or organic cation;
- R2 is H, (C1-C8)alkyl, —NHC(O)CH2-aryl, —NHC(O)CH2-heteroaryl, —NHC(O)CH(NH2)-aryl or —NHC(O)(CH2)3CH(NH2)—CO2R3;
- A is a 5- to 6-membered heterocyclic ring containing at least one nitrogen atom and substituted with one or more groups selected from halogen, CN, (C1C8)alkyl, (C1-C8)haloalkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, OR3, NR3R3, C(O)R3, [(C1-C8)alkylene]OR3, [(C1-C8)alkylene]OC(O)R3, [(C1-C8)alkylene]OC(O)NR3R3, [(C1-C8)alkylene]NR3R3, C(O)NR3R3, C(O)[(C1-C8)alkylene]NR3R3, CO2R3, C(S)NR3R3, SR3, S(O)R3, SO2R3 and SO2NR3R3;
- R3 is independently H, (C1-C8)alkyl, (C1-C8)haloalkyl, cycloalkyl, heterocyclyl, [(C1-C8)alkylene] heterocyclyl, aryl, [(C1-C8)alkylene] aryl or heteroaryl;
- and
- wherein any alkyl, cycloalkyl, heterocyclyl, heteroaryl or aryl is optionally substituted with 1, 2, or 3 groups selected from OH, CN, SH, SO2NH2, halogen, NH2, NHCNH, C(O)NH2, C(O)N(CH3)2, C(O)NH(aryl-COOH), C(NH)CH3, CH2(NH)SO2NH2, COOH, COOCH3, acetyl, (C1-C8)alkyl, S(C1-C8)alkyl, S(C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C1-C8)haloalkyl, (C1-C8)thioalkyl and heterocyclyl,
- or a pharmaceutically acceptable salt or ester thereof.
6 more elements
Dependencies are inferred from the claim text.