Oligomer-opioid agonist conjugates
View Patent ↗The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
1. An opioid agonist compound selected from the formula
wherein n is an integer from 1 to 15; and pharmaceutically acceptable salts thereof.
2. The opioid agonist compound of claim 1 , wherein n is an integer from 1 to 10.
3. The compound of claim 1 , wherein n is 1.
4. The compound of claim 1 , wherein n is 2.
5. The compound of claim 1 , wherein n is 3.
6. The compound of claim 1 , wherein n is 4.
7. The compound of claim 1 , wherein n is 5.
8. The compound of claim 1 , wherein n is 6.
9. The compound of claim 1 , wherein n is 7.
10. The compound of claim 1 , wherein n is 8.
11. The compound of claim 1 , wherein n is 9.
12. The compound of claim 1 , wherein the pharmaceutically acceptable salt is the HCl (hydrochloric acid) salt.
13. The compound of claim 1 , wherein the pharmaceutically acceptable salt is the TFA (triflouroacetic acid) salt.
14. A composition comprising a compound of claim 1 , and optionally, a pharmaceutically acceptable excipient.
15. The composition of claim 14 , wherein the composition is suitable for oral administration.
16. A composition of matter comprising a compound of claim 1 , wherein the compound is present in a dosage form.
17. A method of treating pain in a patient, comprising administering a therapeutically effective amount of a compound of claim 1 to the patient in need thereof.
18. A method of treating pain in a patient, comprising administering the composition of claim 14 to the patient in need thereof.
19. The compound of claim 1 , wherein the pharmaceutically acceptable salts are selected from a hydrochloric acid salt, a hydrobromic acid salt, a hydroiodic acid salt, a sulfuric acid salt, a phosphoric acid salt, a p-toluenesulfonic acid salt, a methanesulfonic acid salt, an oxalic acid salt, a p-bromophenyl-sulfonic acid salt, a carbonic acid salt, a succinic acid salt, a citric acid salt, a benzoic acid salt, and an acetic acid salt.