Acylpiperazines as Inhibitors of Transglutaminase and Their Use in Medicine

摘要

The present invention relates to novel compounds of Formula I capable of inhibiting tissue transglutaminase, and uses of the same in medicine. In particular, the invention provides compounds for use in the treatment of prevention of disease and conditions such as fibrosis (e.g. cystic fibrosis), scarring, neurodegenerative diseases (e.g. Alzheimer's disease, Huntington's disease and Parkinson's disease), autoimmune diseases (e.g. multiple sclerosis and coeliac disease), thrombosis, proliferative disorders (e.g. cancers), AIDS, psoriasis and inflammation (e.g. chronic inflammatory diseases).

主权项

1. A compound of Formula I wherein R1 is selected from the group consisting of R4C(O)—, R5OC(O)— and R6S(O)2—
whereinR4 is a lower alkyl groupR5 and R6 are selected from the group consisting of heterocyclic groups, aralkyl groups and lower alkyl groups R2 is a side chain of an amino acid; and R3 is selected from the group consisting of —C(O)R7 and —S(O)2CHCH2 whereinR7 is selected from the group consisting of alkyl halide, alkylene dialkyl sulfonium, alkylenethioimidazolium, lower alkyl, lower alkenyl, epoxide and alkylene dihydroisoxazole groups or a pharmaceutically and/or veterinarily acceptable derivative thereof.