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Claims for Patent: 8,617,530

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Claims for Patent: 8,617,530

Title:Polymer conjugates of opioid antagonists
Abstract: The invention provides polymer conjugates of opioid antagonists comprising a polymer, such as poly(ethylene glycol), covalently attached to an opioid antagonist. The linkage between the polymer and the opioid antagonist is preferably hydrolytically stable. The invention also includes a method of treating one or more side effects associated with the use of opioid analgesics, such as constipation, nausea, or pruritus, by administering a polymer conjugate of the invention.
Inventor(s): Roberts; Michael James (Williamsburg, VA), Shen; Xiaoming (Madison, AL), Cheng; Lin (Huntsville, AL), Bentley; Michael David (Hunstville, AL)
Assignee: Nektar Therapeutics (San Francisco, CA)
Application Number:13/689,640
Patent Claims: 1. A method of treating constipation resulting from the administration of an opioid agonist to a patient in need thereof, said method comprising administering to the patient in need thereof a therapeutically effective amount of a polymer conjugate of the formula: ##STR00010## or pharmaceutically acceptable salt thereof, wherein: Y is allyl; Z is OH; X is --NHC(O)--, --NH--, --OC(O)NH--, --O--, --S-- or --NHC(O)NH--; and POLY is methoxy poly(ethylene glycol), wherein POLY has a molecular weight of from about 100 Da to about 2,000 Da.

2. A method of treating nausea resulting from the administration of an opioid agonist to a patient in need thereof, said method comprising administer to the patient in need thereof a therapeutically effective amount of a polymer conjugate of the formula: ##STR00011## or pharmaceutically acceptable salt thereof, wherein: Y is allyl; Z is OH: X is --NHC(O)--, --NH--, --OC(O)NH--, --O--, --S-- or --NHC(O)NH--; and POLY is methoxy poly(ethylene glycol), wherein POLY has a molecular weight of from about 100 Da to about 2.000 Da.

3. A method of treating pruritus resulting from the administration of an opioid agonist to a patient in need thereof, said method comprising administering to the patient in need thereof a therapeutically effective amount of a polymer conjugate of the formula: ##STR00012## or pharmaceutically acceptable salt thereof, wherein: Y is allyl; Z is OH; X is --NHC(O)--, --NH--, --OC(O)NH--, --O--, --S-- or --NHC(O)NH--; and POLY is methoxy poly(ethylene glycol), wherein POLY has a molecular weight of from about 100 Da to about 2,000 Da.

4. The method of claim 1, wherein POLY has the formula: CH.sub.3O--(CH.sub.2CH.sub.2O).sub.n--CH.sub.2CH.sub.2--, wherein n is from 2 to 45.

5. The method of claim 4, wherein n is from 2 to 20.

6. The method of claim 1, wherein POLY has a molecular weight of from about 100 Da to about 500 Da.

7. The method of claim 1, wherein X is --NHC(O)--.

8. The method of claim 1, wherein X is --NH--.

9. The method of claim 1, wherein X is --OC(O)NH--.

10. The method of claim 1, wherein X is --O--.

11. The method of claim 1, wherein X is --S--.

12. The method of claim 1, wherein X is --NHC(O)NH--.
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