Oligomer-opioid agonist conjugates

• US 8,952,032 B2
• Filed: 09/20/2013
• Issued: 02/10/2015
• 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:
  US14/032,648
• Publication Number:
  US 20140200235A1
• Time in Patent Office: 508 Days
• Field of Search: 514/282, 546/44
• US Class Current: 514/282
• 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 formula:

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

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

4. The compound of claim 1, wherein n is 3.

5. The compound of claim 1, wherein n is 4.

6. The compound of claim 1, wherein n is 5.

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

8. The compound of claim 1, wherein n is 7.

9. The compound of claim 1, wherein n is 8.

10. The compound of claim 1, wherein n is 9.

11. The compound of claim 1, wherein n is an integer from 1 to 10.

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

13. The composition of claim 12, wherein the composition is suitable for oral administration.

14. The composition of claim 12, wherein the composition comprises about 0.001 mg to about 1000 mg of the compound.

15. The composition of claim 13, in tablet, caplet, or capsule form.

16. A method of treating pain, comprising administering a therapeutically effective amount of a compound of claim 1 to a patient in need thereof.

17. A method of treating pain, comprising administering a composition of claim 12 to a patient in need thereof.