Oligomer-opioid agonist conjugates

• US 8,946,285 B2
• Filed: 09/20/2013
• Issued: 02/03/2015
• Est. Priority Date: 03/12/2007
• Status: Active Grant

• Current Assignee: Nektar Therapeutics Incorporated
• Original Assignee: Nektar Therapeutics Incorporated
• Inventors: Riggs-Sauthier, Jennifer, Deng, Bo-Liang, Riley, Timothy A.
• Primary Examiner(s): Aulakh, Charanjit
• Application Number:
  US14/032,780
• Publication Number:
  US 20140187790A1
• Time in Patent Office: 501 Days
• Field of Search: 514/429, 548/568
• US Class Current: 514/429
• CPC Class Codes: A61K 31/402 1-aryl substituted, e.g. piretanide
• CPC Class Codes: A61K 31/4025 not condensed and containing further heterocyclic rings, e.g. cromakalim
• CPC Class Codes: A61K 31/439 the ring forming part of a bridged ring system, e.g. quinuclidine 8-azabicyclo [3.2.1] octanes A61K31/46
• CPC Class Codes: A61K 31/4468 having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/60 the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: C07D 489/02 with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

Abstract

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.

Claims

1. A compound having the structure

2. The compound of claim 1, wherein n is 1 to 10.

3. A composition comprising a compound of claim 1, and optionally, a pharmaceutically acceptable excipient.

4. A composition of matter comprising a compound of claim 1, wherein the compound is present in a dosage form.

5. A method for treating pain in a human, the method comprising administering to the human a compound of claim 1.

6. The compound of claim 2, wherein n is 1.

7. The compound of claim 2, wherein n is 2.

8. The compound of claim 2, wherein n is 3.

9. The compound of claim 2, wherein n is 4.

10. The compound of claim 2, wherein n is 5.

11. The compound of claim 2, wherein n is 6.

12. The compound of claim 2, wherein n is 7.

13. The compound of claim 2, wherein n is 8.

14. The compound of claim 2, wherein n is 9.

15. The compound of claim 2, wherein n is 10.