Hoffmann-La Roche Inc.

Michael Pech

Hans Peter Wessel

Gerard Schmid

Thomas B Tschopp

Hans P Marki

Marianne Rouge

Niggi Iberg

Rita Muller

Jurgen Fingerle

Alexander Chucholowski

Tobias Gabriel

Rosa Maria Rodriguez Sarmiento

Sabine Wallbaum

Nitrile derivatives that inhibit cathepsin K

The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.

Beta-amino acid nitrile derivatives as cathepsin K inhibitors

Compounds of the formula ##STR1## wherein n.sup.1 -n.sup.9 are each independently 0 or 1;

Sulfuric acid esters of sugar alcohols

Compounds of formulas ##STR1## wherein, B is lower alkylene or an optionally substituted aromatic ring system;

Sulfuric acid esters of amino sugars

The present invention is concerned with novel sulfuric acid esters of sugar alcohols and sugar alcohol-like compounds of the formula ##STR1## Also described are methods for the treatment and/or prophylaxis of arteriosclerotic changes in the vascular wall as well as a process for the manufacture of the compounds of formula I and their salts.

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Hartheim, Germany

Michael Pech