Substituted phosphinic acid-containing peptidyl derivatives as a

Details Substituted phosphinic acid-containing peptidyl derivatives as a Substituted phosphinic acid-containing peptidyl derivatives as a

1995-11-09

1997-10-21

McKane, Joseph

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514417, 514422, 514429, 514399, 514418, 514419, 548413, 548414, 548415, 548481, 548472, 548491, 548112, 549 58, 549 5, 549220, 549 48, 549221, 546145, 546117, 544243, 544337, 568 15, 558170, A61K 3140, C07F 930

Patent

active

056797001

ABSTRACT:
Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. These inhibitors may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation. ##STR1##

REFERENCES:
patent: 4511504 (1985-04-01), McCullugh et al.
patent: 4568666 (1986-02-01), McCullugh et al.
patent: 4771037 (1988-09-01), Roberts et al.
patent: 4885283 (1989-12-01), Broadhurst et al.
patent: 4935404 (1990-06-01), Hunter et al.
patent: 4937243 (1990-06-01), Markwell et al.
patent: 5006651 (1991-04-01), Broadhurst et al.
Grobelny, et al., Biochemistry vol. 28, pp. 4948-4951 (1989).
D.T. Parker, et al., Ciba-Geigy Corporation, Pharmaceuticals Division, "CGS27023A: A Novel, Potent, and Orally Active Matrix Metalloprotease Inhibitor", presented at Inflammation Research Assoc., 7th Intl. Conf., Sep. 25-29, 1994 at Whitehaven PA.
Eversole, et al., Presentation at 207th ACS Natl Mtg, San Diego, CA Mar. 13-17, 1994, "Development of Stromelysin INhibitors".
Caldwell, et al.,Submitted Nov. 26, 1995 to Bioorg. Med. Chem. Lett., "Phosphinic Acid Inhibitors of Matrix Metalloproteinases".
Grobelny, et al., Biochemical & Biophysical Research Comm., vol. 169, No. 3, pp. 1111-1116 (1990).
Birketal-Hansen, et al., Critical Rev. In Oral Biology and Medicine, vol. 4, No. 2, pp. 197-250 (1993).
Vincenti, et al., Arthritis & Rheumatism, vol. 37, pp. 1115-1126 (1994).
Goulet et al., Bioorg. Med. Lett., 4(10), 1221-4 1994.

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