Abstract: Novel compounds and compositions including those compounds, as well as methods of using and making the compounds are herein described. The compounds are useful in therapeutic applications, including modulation of disease or disease symptoms in a subject (e.g., mammal, human, dog, cat, horse). The compounds are useful as modulators of the mu opioid receptor (MOR) through their binding affinity with that receptor.

Abstract: A method of generating a compound having at least one biological activity of a peptide. The method includes identifying a biologically active peptide, providing a first monomer which contains terminal reactive moieties and at least one functionalizable group, providing a second monomer which contains terminal reactive moieties and at least one functionalizable group, and reacting first and second monomer under stereo-and/or regiochemically controlled conditions to yield a compound in which the monomers are attached by way of terminal reactive moieties.

Abstract: The present invention provides a system for the production of chemical compounds and libraries of compounds that are complex, stereochemically and regioselectively pure, and may mimic the structural or functional properties of a peptide. The invention provides methods for producing collections of peptidomimetic compounds which, in one preferred embodiment, comprises (1) providing two diversifiable monomers containing terminal reactive moieties; (2) reacting the monomers under conditions that allow for the control of stereochemistry as well as chemoselectivity; and (3) generating diversifiable isolable compounds or libraries of compounds.