The present invention provides compounds of formula (I) ##STR00001## wherein X.sup.1 to X.sup.8 and R.sup.1 to R.sup.8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof:

##STR00001##

which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

An antimicrobial compound, as well as the salts, derivatives and analogs thereof, said compound being represented by the general formula (I): ##STR00001##
wherein R.sub.1 represents a peptide part P1 or a peptide part P2.

Granzyme B inhibitor compounds, compositions that include the compounds, and methods for using the compounds. The compounds of the invention have advantageous water solubility and effectively inhibit Granzyme B.

Compounds of Formula I are disclosed

##STR00001##

As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.

The present invention relates to prodrugs of protease inhibitors, such as inhibitors of the proteosome, DPP IV, FAP and the like. Thesepro-inhibitors are activated, i.e., cleaved, by an activated protease to release an active inhibitor moiety in proximity to a target protease. The identity of activating protease and target protease can be the same (such as pro-inhibitors being referred to as Target-Activated Smart Protease Inhibitors or TASPI) or different (e.g., Target-Directed Smart Protease Inhibitors or TDSPI). After activation of the pro-inhibitor, the active inhibitor moiety can self-inactivate by, e.g., intramolecular-cyclization or cis-trans isomerization.

The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

An antimicrobial compound, as well as the salts, derivatives and analogues thereof, said compound being represented by the general formula (I):

##STR00001## wherein R.sub.1 represents a peptide part P1 or a peptide part P2.

The invention suggests amphoteric lipids wherein one or more amphoteric groups having an isoelectric point between 4 and 9 are substituted on a membranous or membrane-forming amphiphilic substance, as well as liposomes containing such compounds.