Opioid agonists and uses thereof

Patent metadata

Field	Value
Publication number	US-10081602-B2
Application number	US-201715603942-A
Country	US
Kind code	B2
Filing date	May 24, 2017
Priority date	Nov 27, 2013
Publication date	Sep 25, 2018
Grant date	Sep 25, 2018

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.

First claim

What is claimed is:

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.

Assignees

• Nektar Therapeutics

Inventors

• Duarte Franco J
• Anand Neel K
• Sharma Pankaj
• Singh Devendrapratap

Classifications

• C07D221/26 Primary

  Benzomorphans · CPC title

• C07D401/12

  linked by a chain containing hetero atoms as chain links · CPC title

• A61P25/04

  Centrally acting analgesics, e.g. opioids · CPC title

• C07D513/08

  Bridged systems · CPC title