WATER-SOLUBLE O-CARBONYL PHOSPHORAMIDATE PRODRUGS FOR THERAPEUTIC ADMINISTRATION

摘要

The present invention provides certain water-soluble O-carbonyl phosphoramidate prodrugs of the following formula I:;;or pharmaceutically acceptable salts thereof that are therapeutic or antibacterial agents, pharmaceutical compositions containing them, methods for their use, and reagents and methods for preparing these compounds.

主权项

1. A compound of the following formula I or a pharmaceutically acceptable salt or solvate thereof, wherein: R1 is H, C1-20alkyl, C3-6cycloalkyl, C2-4alkenyl, C2-4alkynyl, C1-4heteroalkyl, aryl, heteroaryl, Het1, Het2, C(═O)C1-4alkyl, C(═O)OH, C(═O)OC1-4alkyl, (CH2)mC(═O)OH, (CH2)mC(═O)C1-4alkyl, (CH2)mC(═O)OC1-4alkyl, NH2, NHC1-4alkyl, N(C1-4alkyl) C1-4alkyl, N(C1-4alkyl)aryl, OC1-4alkyl, SC1-4alkyl, (CH2)mC3-6cycloalkyl, (CH2)mC(═O)-aryl, or (CH2)mC(═O)-Het1, wherein m is 0, 1, or 2; and R2 and R3 are independently selected from H, C1-20alkyl, C3-6cycloalkyl, C2-4alkenyl, C2-4alkynyl, C1-20heteroalkyl, aryl, heteroaryl, [3-(2,3,5-trifluoro-4-(4-oxo-3,4-dihydropyridin-1(2H)-yl)phenyl)oxazolidin-2-one-5-yl]methyl, [3-(3-fluoro-4-morpholinophenyl)oxazolidin-2-one-5-yl]methyl, [3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-oxazolidin-2-one-5-yl]methyl, [3-(3-fluoro-4-(6-(1-methyl-1H-tetrazol-5-yl)pyridin-3-yl)phenyl)-oxazolidin-2-one-5-yl]methyl, Het1, Het2, C(═O)C1-4alkyl, (CH2)mC(═O)C1-4alkyl, (CH2)mC3-6cycloalkyl, (CH2)mC(═O)-aryl, and (CH2)mC(═O)-Het1.