PEPTIDES HAVING NOVEL POLAR N-TERMINAL GROUPS

摘要

The present invention provides novel peptides having a non-cleavable transition state insert corresponding to the 10,11-position of the renin substrate (angiotensinogen) and having a novel polar group of formula (L1) (wherein X1 is H2N-, H2NC(CH3)2-, HO2C-, (H2N)(HO2C)CH-, or (HO)2P(O)O-) at the N-terminus of the peptide. These peptides are useful as renin inhibitors and as inhibitors of retroviral proteases. Renin inhibitors are useful for the diagnosis and control of renin-dependent hypertension, congestive heart failure, renin-dependent hyperaldosterism, other renin-dependent cardiovascular disorders and ocular disorders. Inhibitors of retroviral proteases, such as the HIV-I protease, are useful for treating diseases caused by retroviruses, such as human acquired immunodeficiency disease syndrome (AIDS).