Oligomer-opioid agonist conjugates

• US 10,307,416 B2
• Filed: 08/25/2016
• Issued: 06/04/2019
• 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:
  US15/247,472
• Publication Number:
  US 20160375009A1
• Time in Patent Office: 1,013 Days
• Field of Search: 546 39, 546 44, 514279, 514282
• 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 of the following structure:

2. A composition comprising a compound of claim 1 and a pharmaceutically acceptable excipient.

3. A composition of claim 2 present in a dosage form suitable for administration.

4. A method of treating pain comprising administering a compound of claim 1 to a patient in need thereof.

5. The compound of claim 1 wherein n is 3, 4, 5, 6, 7, 8, or 9.

6. The compound of claim 1 wherein n is 3.

7. The compound of claim 1 wherein n is 4.

8. The compound of claim 1 wherein n is 5.

9. The compound of claim 1 wherein n is 6.

10. The compound of claim 1 wherein n is 7.

11. The compound of claim 1 wherein n is 8.

12. The compound of claim 1 wherein n is 9.