Back to results
US 6,713,455 B2Granted
6-O-carbamate-11,12-lacto-ketolide antimicrobials
AssigneeOrtho-McNeil Pharmaceutical, Inc.
InventorsEugene B. Grant, III, Todd C. Henninger, Mark J. Macielag, Deodialsingh Guiadeen
Life of this patent
Estimating the term…
Abstract
6-O-Carbamate-11,12-lacto-ketolide antimicrobials of the formula: wherein R1, R2, R3 R7, and R8 are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
Claims24
A compound of Formula 1:
- wherein
- R1 and R2 are independently selected from hydrogen, optionally substituted C1-C8-alkyl, optionally substituted —CH2—C2-8 alkenyl, and optionally substituted —CH2—C2-8 alkynyl, wherein the substituents are selected from the group consisting of C1-C8 alkyl, —CH2—C2-8 alkenyl, —CH2—C2-8 alkynyl, C3-C8 cycloalkyl, aryl, heteroaryl, substituted aryl, substituted heteroaryl, hydroxy, and C1-8alkoxy;
- R3 is selected from hydrogen, OR4, SR4 and NR5R6, wherein R4, R5, and R6 are independently selected from the group consisting of C1-8alkyl, C3-8alkenyl, and C3-8 alkynyl, said C1-8alkyl, C3-8alkenyl, and C3-8alkynyl being optionally substituted with one or more substituents selected from the group consisting of aryl, substituted aryl, heteroaryl, substituted heteroaryl, hydroxy, and C1-6alkoxy;
- R7 is hydrogen or a hydroxy protecting group;
- and
- R8 is selected from hydrogen, alkyl, C2-C10-alkenyl, C2-C10-alkynyl, aryl, heteroaryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl, C3-C6-cycloalkyl, C5-C8-cycloalkenyl, alkoxyalkyl containing 1-6 carbon atoms in each alkyl or alkoxy group, and alkylthioalkyl containing 1-6 carbon atoms in each alkyl or thioalkyl group;
- or an optical isomer, enantiomer, diastereomer, racemate or racemic mixture thereof, or a pharmaceutically acceptable salt, esters or pro-drugs thereof.
4 more elements
Dependencies are inferred from the claim text.