IP Library Granted Patent US 10,766,864
Granted Patent B2
US 10,766,864 · App. 15/569,726 · Granted Sep 8, 2020

Morphinan derivatives for the treatment of neuropathic pain

Inventors: Neel K. Anand (San Mateo, CA); Natalia Aurrecoechea (Oakland, CA); Lin Cheng (Sunnyvale, CA); Bo-Liang Deng (San Ramon, CA); Donogh John Roger O'Mahony (San Mateo, CA); YongQi Mu (Los Altos, CA); Erik Krogh-Jespersen (Greenbrae, CA)
Assignee: Nektar Therapeutics
C07D221/28A61P25/04C07D401/12C07D407/04C07D407/12C07D417/12C07D471/08C07D513/08
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Quick Facts
Patent No.
US 10,766,864
App. No.
15/569,726
Granted
Sep 8, 2020
Kind
B2
Abstract

The present invention relates to compounds and their use as ligands for mu opioid receptors. Also included are methods for preparing the compounds and pharmaceutical compositions containing the compounds. In one or more embodiments of the invention, a compound according to Formula I is provided: and pharmaceutically acceptable salts thereof, wherein R 1 -R 11 are as described herein.

Claims (28)

1. A compound of Formula I:

wherein:

R 1 is —N(R 17 )(R 18 );

R 2 , R 3 , R 4 , R 5 , R 6 , R 7 R 9 , R 19 , and R 11 are hydrogen;

R 8 is —CH 3 ;

R 17 is a heteroaryl substituted with —X-POLY;

R 18 is hydrogen;

X is a linker;

POLY is a poly(alkylene oxide); and

pharmaceutically acceptable salts thereof.

2. The compound of claim 1 , having a structure of Formula II,

wherein:

—X-POLY is —X—(CH 2 CH 2 O) n —R, where n is 1 to 30 and R is selected from hydrogen, lower alkyl, haloalkyl and carboxyl.

3. A method for treating an individual in need of treatment for neuropathic pain, the method comprising the step of administering to the individual a compound having the following formula:

wherein:

R 1 is —N(R 17 )(R 18 );

R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , R 10 , and R 11 are hydrogen

R 8 is —CH 3 ;

R 17 is a heteroaryl substituted with X-POLY;

R 18 is hydrogen;

X is a linker;

POLY is a poly(alkylene oxide); and

pharmaceutically acceptable salts thereof.

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

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

6. The compound of claim 1 , wherein a heteroatom of the heterocycle is selected from O, N, and S.

7. The compound of claim 1 , wherein the heterocycle is selected from an imidazole, a pyrimidine, a thiazole, and a pyridine.

8. The compound of claim 1 , wherein R 17 is selected from

Assignments (6)
RELEASE OF SECURITY INTEREST Recorded Apr 17, 2020
From: TC LENDING, LLC, AS COLLATERAL AGENT
To: NEKTAR THERAPEUTICS
Reel/Frame 053180/0009 →
CORRECTIVE ASSIGNMENT TO CORRECT THE APPLICATION NUMBER 15/835,115 PREVIOUSLY RECORDED AT REEL: 044515 FRAME: 0727. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Aug 10, 2018
From: NEKTAR THERAPEUTICS
To: TC LENDING, LLC, AS COLLATERAL AGENT
Reel/Frame 046762/0412 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 23, 2018
From: ANAND, NEEL K.; AURRECOECHEA, NATALIA; CHENG, LIN; DENG, BO-LIANG; O'MAHONY, DONOGH JOHN ROGER; MU, YONGQI
To: NEKTAR THERAPEUTICS
Reel/Frame 045327/0203 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 23, 2018
From: KROGH-JESPERSEN, ERIK
To: NANOSYN INC.
Reel/Frame 045327/0245 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 23, 2018
From: NANOSYN INC.
To: NEKTAR THERAPEUTICS
Reel/Frame 045720/0635 →
SECURITY INTEREST Recorded Jan 2, 2018
From: NEKTAR THERAPEUTICS
To: TC LENDING, LLC, AS COLLATERAL AGENT
Reel/Frame 044515/0727 →