abstract |
The present invention relates to particular forms of a novel 1-substituted-N- [2-methyl-1- (trifluoroacetyl) propyl] pyrrolidine-2-carboxamide, which are inhibitors of human leukocyte elastase (HLE), as well known as human neutrophil elastase (ENH). In particular the invention relates to a 1- [2- (methoxycarbonylamino) -3-methylbutyryl] -N- [2-methyl -1- (trifluoroacetyl) propyl] pyrrolidine-2-carboxamide compound of the formula (I) or a solvated thereof, or a ketal or hemiketal thereof, as a diastereomeric mixture comprising 50% or more of the diastereoisomer formula (Ia) or a solvated form thereof, or a ketal or hemiketal thereof, in which they are useful when desired the inhibition of ENH, such as research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which ENH is implicated. The invention also includes pharmaceutical compositions containing such forms, processes for preparing the forms, and intermediates useful in the synthesis of the starting forms and compounds. |