SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY

摘要

Substituted bicyclic dihydropyrimidinones of formula 1;;and their use as inhibitors of neutrophil elastase activity. An exemplary compound is;

主权项

1. A compound of formula 1 wherein R1 is phenyl,
substituted with CN andsubstituted with a second substituent R1.1,R1.1 is selected from the group consisting of
—SO2—CH3, —SO—CH3, —CH2—OH, —SO2—CH2CH2—OH, —SO2—CH2CH2—OCH3 and —SO2—CH2CH2CH2—OH, R2 is phenyl substituted with CF3, R3 is selected from the group consisting of H, CH3, —CO—NH—CH3, —CH2CH2—OH and —CH2-oxetane, or a pharmaceutically acceptable salt thereof, provided that a compound of formula 1 is not a compound selected from the group consisting of