IP Library Granted Patent US 10,081,602
Granted Patent B2
US 10,081,602 · App. 15/603,942 · Granted Sep 25, 2018

Opioid agonists and uses thereof

Inventors: Franco J. Duarte (Walnut Creek, CA); Neel K. Anand (San Mateo, CA); Pankaj Sharma (New Delhi, IN); Devendrapratap Singh (Mumbai, IN)
Assignee: Nektar Therapeutics
C07D221/26C07D401/12C07D513/08
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,081,602
App. No.
15/603,942
Granted
Sep 25, 2018
Kind
B2
Abstract

Provided are compounds, including those of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.

Claims (25)

1. A compound according to Formula VII:

wherein

X is —O—, —NHC(O)—, —CH 2 CHOHCH 2 NH—, or —NH—; and

POLY is a poly(alkylene oxide) oligomer.

2. The compound of claim 1 , wherein X is —O—.

3. The compound of claim 1 , wherein X is —NH—.

4. The compound of claim 1 , wherein X is —NHC(O)—.

5. The compound of claim 1 , according to Formula VIII:

wherein

n is an integer from 1 to 30.

6. The compound of claim 5 , wherein n is an integer from 1 to 10.

7. A compound of claim 1 , selected from:

(2S,6R,11R)-3-(Cyclopropylmethyl)-8-({2-[2-(2-methoxy)ethoxy]ethyl}amino-6, 11-dimethyl-3, 4, 5, 6-tetrahydro-2, 6-methano-3-benzazocin-1(2H)-one;

(2S,6R11R)-3-(Cyclopropylmethyl)-6,11-dimethyl-8-(2,5,8,11,14-pentaoxahexadecan-16-ylamino)-3,4,5,6-tetrahydro-2,6-methano-3-benzazocin-1(2H)-one;

(2S,6R,11R)-3-(Cyclopropylmethyl)-8-(2,5,8,11,14,17,20-heptaoxadocosan-22-ylamino)-6,11-dimethyl-3,4,5,6-tetrahydro-2,6-methano-3-benzazocin-1(2H)-one;

(2S,6R,11R)-3-(Cyclopropylmethyl)-8-{2-[2-(2-methoxyethoxy)ethoxy]ethoxy}-6,11-dimethyl-3,4,5,6-tetrahydro-2,6-methano-3-benzazocin-1(2H)-one;

(2S,6R,11R)-3-(Cyclopropylmethyl)-6,11-dimethyl-8-(2,5,8,11,14-pentaoxahexadecan-16-ylamino)-3,4,5,6-tetrahydro-2,6-methano-3-benzazocin-1(2H)-one;

(2S,6R,11R)-3-(Cyclopropylmethyl)-8-(2,5,8,11,14,17,20-heptaoxadocosan-22-yloxy)-6,11-dimethyl-3,4,5,6-tetrahydro-2,6-methano-3-benzazocin-1(2H)-one;

N-((2S,6R,11R)-3-(cyclopropylmethyl)-6,11-dimethyl-1-oxo-1,2,3,4,5,6-hexahydro-2,6-methanobenzo[d]azocin-8-yl)-2-(2-methoxyethoxy)acetamide;

(2S,6R, 11R)-3-(cyclopropylmethyl)-N-(2-methoxyethyl)-6, 11-dimethyl-1-oxo-1,2, 3,4, 5,6-hexahydro-2,6-methanobenzo[d]azocine-8-carboxamide;

N,N-(((2S,6R, 11R)-3-(cyclopropylmethyl)-6, 11-dimethyl-1-oxo-1,2,3,4,5,6-hexahydro-2,6-methanobenzo[d]azocin-8-yl)methyl)-2-(2-methoxyethoxy)acetamide; and

(2S,6R, 11R)-3-(cyclopropylmethyl)-8-((16-(hydroxymethyl)-2,5,8,11,14-pentaoxaheptadecan-17-yl)amino)-6,11-dimethyl-3,4,5,6-tetrahydro-2,6-methanobenzo[d]azocin-1(2H)-one; and pharmaceutically acceptable salts thereof.

8. A pharmaceutical composition comprising a compound of claim 1 and at least one pharmaceutically acceptable excipient.

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

10. A method comprising administering a compound of claim 1 to a patient in need thereof.

Assignments (2)
RELEASE OF SECURITY INTEREST Recorded Apr 17, 2020
From: TC LENDING, LLC, AS COLLATERAL AGENT
To: NEKTAR THERAPEUTICS
Reel/Frame 053180/0009 →
SECURITY INTEREST Recorded Jun 29, 2017
From: NEKTAR THERAPEUTICS
To: TC LENDING, LLC, AS COLLATERAL AGENT
Reel/Frame 042869/0463 →
Priority Claims (2)
IN 3456/DEL/2013 · Nov 27, 2013 · national
IN 401/DEL/2014 · Feb 13, 2014 · national
Continuity (2)
Continuation 15039686
Related Publication 20170253565A1 · Sep 7, 2017