SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY

摘要

This invention relates to substituted 4-pyridones of formula 1;;and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.

主权项

1. A compound of formula 1 wherein A is phenyl or pyridinyl; R1a is R1a.1 is C1-4-alkyl-;R1a.2 is NC—; R1b is H; R2 is C1-6-alkyl or a residue selected from the group consisting of C3-6-cycloalkyl-, phenyl-C1-4-alkyl- and a five- or six-membered, aromatic heteroring containing one or two nitrogen atoms, each of the above rings optionally substituted with C1-4-alkyl-, halogen or NC—; R3 is methyl; R4 is phenyl, a five- or six-membered, aromatic ring containing one or two nitrogen atom, each ring optionally substituted with one or two residues selected independently from each other from the group consisting of C1-4-alkyl-, halogen or C1-4-haloalkyl-; R5 is H; R6 is H; R7 is H;or a pharmaceutically acceptable salt thereof.