Leukocyte Function-Associated Antigen One (LFA-1) is a cell adhesion molecule selectively expressed on leukocytes, and plays a major role in the activation and trafficking of T lymphocytes in the tissue at sites of inflammation. In the last decade a large body of preclinical data has accumulated to establish the importance of LFA-1 as a biological target, 10 particularly in chronic, T-cell driven inflammatory conditions. The present invention provides pharmaceutically active 1,4-diazepan-2-ones of formula I useful for the treatment of conditions related to LFA-1 activity.