The present invention relates in part to a process for the preparation of a proline derivative of formula I ##STR00001## wherein, R.sup.1 is C.sub.1-7-alkyl or ##STR00002## wherein R.sup.4 is selected from the group consisting of C.sub.1-7-alkyl, halogen-C.sub.1-7-alkyl and phenyl optionally substituted by halogen; R.sup.2 is halogen or halogen-C.sub.1-7-alkyl; and R.sup.3 is selected from the group consisting of hydrogen, halogen, halogen-C.sub.1-7-alkyl, C.sub.1-7-alkoxy, halogen-C.sub.1-7-alkoxy and a 5- or 6-membered heterocyclic ring containing one or two nitrogen atoms, said ring being optionally substituted by C.sub.1-7-alkyl or halogen. The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.

peripheral arterial disease/protease

Process for the preparation of proline derivatives

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