The present invention provides bivalent and multivalent ligands with a view to improving the affinity and pharmacokinetic properties of a urea class of PSMA inhibitors. The compounds and their synthesis can be generalized to multivalent compounds of other target antigens. Because they present multiple copies of the pharmacophore, multivalent ligands can bind to receptors with high avidity and affinity, thereby serving as powerful inhibitors. The modular multivalent scaffolds of the present invention, in one or more embodiments, contains a lysine-based (, -) dialkyne residue for incorporating two or more antigen binding moieties, such as PSMA binding Lys-Glu urea moieties, exploiting click chemistry and one or more additional lysine residues for subsequent modification with an imaging and/or therapeutic nuclides or a cytotoxic ligands for tumor cell killing.

Covalent Granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. A method for treating cutaneous scleroderma, epidermolysis bullosa, radiation dermatitis, alopecia areata, and discoid lupus erythematosus are provided.

A compound having the formula: ##STR00001## wherein X is S, SO or SO.sub.2; one of R.sup.1, R.sup.2, and R.sup.3 is O and the others of R.sup.1, R.sup.2 and R.sup.3 are independently, the same or different, CH.sub.2, or CR.sup.13 wherein, R.sup.13 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or (CH.sub.2).sub.mOR.sup.15, wherein R.sup.15 is an alkyl group or an aryl group and m is an integer in the range of 1 to 10, and one of R.sup.5, R.sup.6, and R.sup.7 is O and the others of R.sup.5, R.sup.6 and R.sup.7 are independently, the same or different, CH.sub.2, or CR.sup.14 wherein, R.sup.14 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or (CH.sub.2).sub.nOR.sup.16, wherein R.sup.16 is an alkyl group or an aryl group and n is an integer in the range of 1 to 10; R.sup.4 and R.sup.8 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group, a C.sub.1-C.sub.3 alkoxy group, an aryloxy group, or (CH.sub.2).sub.qOR.sup.17, wherein R.sup.17 is an alkyl group or an aryl group and q is an integer in the range of 1 to 10, provided that R.sup.4 is not a C.sub.1-C.sub.3 alkoxy group or an aryloxy group when R.sup.1 or R.sup.3 is O and R.sup.8 is not a C.sub.1-C.sub.3 alkoxy group or an aryloxy group when R.sup.5 or R.sup.7 is O; R.sup.9, R.sup.10, R.sup.11 and R.sup.12 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, or an aryl group.

The present invention provides a particular branched chain-containing aromatic compound. The branched chain-containing aromatic compound of the present invention is easily-soluble in isopropyl acetate superior in liquid-separation operability, and can be used for a production method of peptide and the like, which provides a final product simply by extraction separation, without crystallization and isolation of each intermediate in each step.

Pyrrolidine carboxamido derivatives, optical isomers thereof, and salts thereof that are able to prevent, improve, and/or treat inflammatory conditions, including inflammatory bowel disease, and methods for preparing and using the same are provided.

The invention is directed to the use of at least one peptide of formula: X-(Xaa.sub.1).sub.n-Pro*-(Xaa.sub.2).sub.m-Y (I) With: n=0, or 2; m=0 or 1 and if m=0 then n0Xaa is: An hydrophobic aminoacid; A polar aminoacid; or Glycine (Gly, G); When n=2 the two aminoacids Xaa.sub.1 can be the same or different; Xaa.sub.2 is: An hydrophobic amino acid; A basic aminoacid; Glycine (Gly, G) or Serine (Ser, S); At the N terminal end of the peptide, X is selected from H, COR.sub.1 and SO.sub.2R.sub.1; At the C terminal end of the peptide, Y is selected from OH, OR.sub.1, NH.sub.2, NHR.sub.1 or NR.sub.1R.sub.2, R.sub.1 and R.sub.2 being independently from each other, selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group; Pro* Excluding the peptides where X=H and Y=OH, for a non therapeutical cosmetic pro-pigmenting treatment of skin.

The present invention relates to a compound for stabilizing enzymes, the use of said compound for stabilizing an enzyme, a composition comprising said compound, a method of preparing the composition comprising said compound, a detergent composition comprising said compound and a method of preparing said compound.

Azole tripeptides may function as vasodilators. These compounds may contain three azole groups connected in a peptide-like structure. The azole groups may be monocyclic or fused bicyclic heteroaryl groups. Each azole group may be substituted or unsubstituted. The compounds may include various end cap moieties. A pharmaceutical composition may include an azole tripeptide compound and a pharmaceutically acceptable carrier. Methods of vasodilation may include administering an azole tripeptide compound to a subject in a therapeutically effective amount. The administration may cause vasodilation in the subject. The vasodilation may provide treatment for various conditions. The azole tripeptide compounds may be synthesized through multi-step chemical processes.

Peptide compounds and their use in treating diseases and disorders that cause, are caused by, or are characterized by cellular oxidative stress.

Disclosed are proteasome inhibitors, FAP-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.