Peptidomimetic inhibitors of cathepsin D and plasmepsins I and I

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 11, 530317, A61K 3800, C07K 512

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active

058496912

ABSTRACT:
The present invention relates to the design and synthesis of linear and cyclic inhibitors of cathepsin D and plasmepsins I and II. The present invention also relates to the uses of these inhibitors for inhibiting invasion and metastasis of cancerous cells. The present invention further relates to the use of cathepsin D and plasmepsin I and II inhibitors for the prevention and treatment of Alzheimer's disease and malaria.

REFERENCES:
patent: 4477441 (1984-10-01), Boger et al.
patent: 4485099 (1984-11-01), Boger et al.
International Search Report, PCT/US97/02930.
Agarwal, Nirankar and Rich, Daniel, 1986, "Inhibition of Cathepsin D by Substrate Analogues Containing Statine and by Analogues of Pepstatin", J. Med. Chem., vol. 29 pp. 2519-2524.
Reily, Michael, et al., 1992, "Design, synthesis and solution structure of a renin inhibtor", Federation of European Biochemical Societies, vol. 302 (1), pp. 97-103.
Wu, H. et al., 1994, "The Structure of Qingjingmycin A Novel Peptide-Type Metabolite of a Hybrid Strain FM3-32 Derived from Streptomyces Qingfengmyceticus and S. hydroscopius var. jinggangensis", National Product Letters, vol. 5, pp. 89-93.
Maibaum, Juergen and Rich, Daniel, 1988, "Inhibition of Porcine Pepsin by Two Substrate Analogues Containing Statine. The Effect of Histidine at the P2 Subsite on the Inhibition of Aspartic Proteinases", J. Med. Chem. vol. 31, pp. 625-629.

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