The present invention provides processes for preparation of eptifibatide that involve coupling of amino acids in a (2+5), (4+3) and (3+4) sequence method. The invention further provides products produced by the described processes, novel compounds that can be used as synthetic intermediates for the preparation of eptifibatide.

A method of treating a disorder in a subject. The method comprises administering to said subject an effective amount of an agonist of the melanocortin-4 receptor (MC4R). The subject is a heterozygous carrier of an MC4R mutation, and the disorder results from an attenuated response of MC4R to a-melanocortin stimulating hormone (a-MSH).

Peptides having activity as protein binding agents are disclosed. The peptides have the following structure (I):

##STR00001##

including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R.sup.1, L.sup.1, L.sup.2, G, M, Y.sup.1 Y.sup.2 and SEQ are as defined herein. Methods associated with preparation and use of such peptides, as well as pharmaceutical compositions comprising such peptides, are also disclosed.

Peptides having activity as protein binding agents are disclosed. The peptides have the following structure (I):

##STR00001##

including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R.sup.1, L.sup.1, L.sup.2, G, M, Y.sup.1 Y.sup.2 and SEQ are as defined herein. Methods associated with preparation and use of such peptides, as well as pharmaceutical compositions comprising such peptides, are also disclosed.

The present disclosure provides targeting peptides and vectors containing a sequence that encodes targeting peptides that deliver agents to the brain.

The present disclosure provides targeting peptides and vectors containing a sequence that encodes targeting peptides that deliver agents to the brain.

Short tri- and tetrapeptides according to the following Formula I Ar(CH2).sub.mX.sup.1—X.sup.2—CO—X.sup.3—X.sup.4—X.sup.5-(Trp).sub.n-NX.sup.6R are potent, selective agonists of melanocortin 1 receptor (MC1R). Provided herein are pharmaceutical compositions including Formula I peptide agonists of MC1R and methods of treating skin diseases and disorders that include administering to an individual in need thereof a therapeutic amount of a Formula I peptide. The peptides, pharmaceutical compositions, and methods described herein are useful in the treatment of diseases and disorders that benefit from agonism of MCIR, including melanoma, basal cell carcinoma, squamous cell carcinoma, porphyria, polymorphous light eruption, vitiligo, and solar urticaria.

Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

A method for preparing a pyrazole of formula (I) in which R,R′ and R″ have different meanings, characterised in that it involves reacting a sydnone of formula (II) in which R and R′ have the meanings already indicated, with an alkyne of formula (III) in which R″ has the meaning already indicated, in the presence of copper, to obtain a pyrazole compound of formula (I) that is then isolated and salified if desired. ##STR00001##