Di- and tripeptide renin inhibitors containing non-peptidal...

C - Chemistry – Metallurgy – 07 – K

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530/5.02, 530/5.

C07K 5/083 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07D 487/04 (2006.01) C07D 498/04 (2006.01) C07K 5/02 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2034524

10/JET5 32/JETll 17701 TITLE OF THE INVENTION DI- AND TRIPEPTIDE RENIN INHIBITORS CONTAINING NON-PEPTIDAL CONFORMATIONALLY-CONSTRAINED TRIPEPTIDE MIMIC FOR LEU10-VAL11-ILE12 ABSTRACT OF THE DISCLOSURE Di- and tripeptide enzyme inhibitors of the formula. Image : : 10/JET5 32/JET11 -i- 17701 and analogs thereof, which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestlve heart failure; compositions containing these renin- inhibitory peptides, optionally with other antihyper- tensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor ;n these problems which employ these novel peptides. In addition, these renin inhibitors are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceu- tically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. .

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