.alpha.-aminoketone derivatives

Details .alpha.-aminoketone derivatives .alpha.-aminoketone derivatives

1993-12-22

1995-06-06

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514374, 514438, 514471, 514427, 514629, 548204, 548236, 548561, 549 77, 549487, 564192, A61K 3134, A61K 31425, C07D21330, C07D21332

Patent

active

054223598

ABSTRACT:
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.

REFERENCES:
Robinson et al., Chemical Abstracts, vol. 117, No. 3, 20 Jul. 1992 Abstract No. 22302m.
Ochi et al., Tetrahedron Letters, vol. 33, No. 49, pp. 7531-7534 (1992).

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