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Last Updated: April 3, 2025

Claims for Patent: 8,617,530

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Summary 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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