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

摘要

Substituted bicyclic dihydropyrimidinones of formula 1;;which are inhibitors of neutrophil elastase and useful as medicaments for the treatment of, inter alia, COPD. 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
—CH2OH, —CH(CH3)OH, —C(CH3)2OH,—SO2—CH2CH3, —SO2—CH3, —SO2—CH2CH2—OCH3, —SO2—CH2CH2—OH, —SO2—CH2CH2CH2—OH and —SO—CH2CH3, —SO—CH3, R2 is phenyl or pyridyl, each ring substituted with R2.1,
R2.1 is selected from the group consisting of
CF3, CHF2, Br and Cl, R3 is selected from the group consisting of
H, CH3, —CO—NH—CH3, —CO—NH—CH2CH3,—CH2CH2—OH, —CH2CH2CH2—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