Compounds according to the following formula (I): ##STR1##wherein the variables Q and R.sub.1 to R.sub.6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.

Boehringer Ingelheim Pharmaceuticals Inc.

Cyanamides useful as reversible inhibitors of cysteine proteases

Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds. ##STR00001##

Boehringer Ingelheim Pharmaceuticals, Inc.

Nitriles useful as reversible inhibitors of cysteine proteases

Methods and kits for treating inflammatory conditions are described that include modulating kallikrein 6 protease activity.

Mayo Foundation for Medical Education and Research

Florida State University Research Foundation, Inc.

Method of treating multiple sclerosis with anti-K6 antibody

Alpha-aminoketone derivatives of the present invention strongly inhibit thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L and calpain or the like and have excellent properties in absorbance on oral administration, tissue distribution and cell membrane permeability. The alpha-aminoketone derivatives can thus be used as therapeutic agents for treating muscular dystrophy, amyotrophy, cardiac infarction, stroke, Alzheimer's disease, disturbance of consciousness or dyskinesia caused upon brain trauma, multiple sclerosis, peripheral nervous neuropathy, cataract, inflammation, allergosis, fulminant hepatitis, osteoporosis, hypercalcemia, breast carcinoma, prostatic carcinoma or prostatomegaly. They may also be used as therapeutic agents for suppressing growth of cancer cells, preventing metastasis of cancer or suppressing aggregation of plaques.

multiple sclerosis/protease

Cyanamides useful as reversible inhibitors of cysteine proteases

Nitriles useful as reversible inhibitors of cysteine proteases

Method of treating multiple sclerosis with anti-K6 antibody

.alpha.-aminoketone derivatives

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