Oligomer-diarylpiperazine conjugates
View Patent ↗The invention relates to (among other things) oligomer-diarylpiperazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated diarylpiperazine compounds.
1. A method of treatment comprising administering a therapeutically effective amount of a compound to a subject in need of opioid receptor agonism, wherein the compound has a structure selected from the group consisting of
wherein, in each structure, R 3 is either H or CH 3 , R 5 is either H or CH 3 , X is a spacer moiety, and POLY is a water-soluble, non-peptidic oligomer.
2. The method of claim 1 , wherein the water-soluble, non-peptidic oligomer is a poly(alkylene oxide).
3. The method of claim 2 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).
4. The method of claim 1 , wherein the water-soluble, non-peptidic oligomer has between 1 and 30 monomers.
5. The method of claim 4 , wherein the water-soluble, non-peptidic oligomer has between 1 and 10 monomers.
6. The method of claim 2 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxy end-capping moiety.
7. The method of claim 1 , wherein the water-soluble, non-peptidic oligomer is covalently attached via a stable linkage.
8. The method of claim 1 , wherein the water-soluble, non-peptidic oligomer is covalently attached via a degradable linkage.
9. The method of claim 1 , wherein X is an oxygen.
10. The method of claim 1 , wherein X is an ester.
11. The method of claim 1 , wherein the opioid receptor is a delta opioid receptor.