PYRIDONE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF TUBERCULOSIS

摘要

A compound of Formula (I) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the inhibition of mycolic acid biosynthesis through inhibition of M. tuberculosis Enoyl Acyl Carrier Protein Reductase enzyme (InhA):;;wherein R1, R2, R3, R4 and R5 are as defined herein.

主权项

1. A compound of Formula (I)wherein
R1 is H, methyl or ethyl; R2 is phenyl, pyrrole or pyrazole, wherein said phenyl is optionally substituted with one or more substituents independently selected from fluoro or chloro; provided that when said substituent is chloro, said chloro is on the meta or ortho position of said phenyl and the number of chloro substituent is not more than one; R3 is a structural formula selected from the group consisting ofwhere R100 and R200 are each independently selected from the group consisting of H, (C1-C6)alkyl, cycloalkyl, an organic cation and an inorganic cation;
R4 is H or —C(═O)NH2; R5 is selected from the group consisting of (C1-C6)alkyl, cycloalkyl, phenyl, heterocycle and heteroaryl, optionally substituted with one or more independent R300 substituents; and R300 is selected from the group consisting of H, (C1-C6)alkyl, cycloalkyl, hydroxy, amino and F;or a pharmaceutically acceptable salt thereof.