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 of the formula
wherein
R 1 is methyl;
R 2 is OH;
R 3 is methyl;
R 4 is hydrogen;
Y 1 is oxygen; and
n is an integer from 1 to 30.
2. The compound of claim 1 , wherein n is an integer from 1 to 10.
3. The compound of claim 2 , wherein n is 1.
4. The compound of claim 2 , wherein n is 2.
5. The compound of claim 2 , wherein n is 3.
6. The compound of claim 2 , wherein n is 4.
7. The compound of claim 2 , wherein n is 5.
8. The compound of claim 2 , wherein n is 6.
9. The compound of claim 2 , wherein n is 7.
10. The compound of claim 2 , wherein n is 8.
11. The compound of claim 2 , wherein n is 9.
12. An opioid agonist compound of the formula
wherein n is an integer from 1 to 30.
13. A composition comprising a compound of claim 1 , and optionally, a pharmaceutically acceptable excipient.
14. The composition of claim 13 , wherein the composition is suitable for oral administration.
15. A composition of matter comprising a compound of claim 1 , wherein the compound is present in a dosage form.
16. 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.