Disclosed is a new process and intermediates for preparing dipyrrolidine peptide compounds such as, for example, rapastinel. Advantageously, the process may be industrially scalable and cost-effective and use less toxic reagents and/or solvents. Further, the process may be used to prepare peptide compounds having improved purity.

The present disclosure relates to methods of preparing and crystallizing -turn cyclic peptidomimetic salts of formula I: ##STR00001##
where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.10, X, Y and n are as defined in the specification. The present disclosure provides a more efficient route for preparing a crystalline form of -turn cyclic peptidomimetic compounds and salts thereof.

The invention relates to a ligand compound having a structure A-B-C, wherein (a) A represents a mono- or polyphosphorylated amino acid linked to part B by its amino group to form an amide bond; B represents (i) a carboxylic acid, and (ii) an amino acid or peptidyl group of 2-10 amino acids, an alkyl or alkenyl group comprising 1-26 carbon atoms, a polyethylene glycol group comprising 1-26 carbon atoms or a combination thereof covalently linked to the carboxylic acid; and C represents a hydrophilic group covalently linked to the group of B (ii) or (b) A represents a mono-or polyphosphorylated amino acid linked to B by its carboxylic acid to form an amide bond; B represents an amino acid or peptidyl group of 2-10 amino acids, an amino substituted alkyl or alkenyl group comprising 1-26 carbon atoms, an amino substituted polyethylene glycol group comprising 1-26 carbon atoms or a combination thereof covalently linked to A by their amino group; C represents a hydrophilic group covalently linked to the group of B. The invention further relates to a coated metal nanoparticle such as super paramagnetic iron oxide nanoparticle (SPIONs) coated with a plurality of the aforementioned ligands and a method of producing thereof.

The present invention relates to compounds of formula (I), which are modulators of sortilin activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions where modulation of sortilin activity is beneficial.

The present invention concerns compositions comprising and methods of identification and use of imaging agents. The imaging agents comprise a growth hormone secretagogues having a conjugated fluoride. The imaging agents of the present invention may be used for detection, diagnosis and/or staging of prostate or other forms of cancer, and may also be used for cardiac disease.

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.

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.

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 present invention relates to a new class of compounds based on alkylated oligopeptides featuring distinct head and tail modifications at their termini. The compounds are useful as inhibitors of viral proteases, particularly of flaviviral proteases, and can therefore be used for treatment of viral infections.

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.