IP Library Granted Patent US 9,133,125
Granted Patent B2
US 9,133,125 · App. 14/286,456 · Granted Sep 15, 2015

Morphan and morphinan analogues, and methods of use

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Quick Facts
Patent No.
US 9,133,125
App. No.
14/286,456
Granted
Sep 15, 2015
Kind
B2
Abstract

The present application relates to analogs of morphan and morphinan, compositions thereof, and methods for treating a disease or condition comprising administering an effective amount of the compounds or compositions to a subject in need thereof.

Claims (15)

1. A compound selected from

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein the compound is a μ opioid receptor agonist having an Emax of 5% to 45% in a GTPγS binding assay.

3. The compound of claim 2 , wherein the Emax is 15% to 35% in a GTPγS binding assay.

4. The compound of claim 1 , having a maximal dopamine efflux in the nucleus accumbens of 125% to 300% over baseline in a rat.

5. The compound of claim 4 , having a maximal dopamine efflux in the nucleus accumbens of 200% to 300% over baseline in a rat.

6. The compound of claim 1 , wherein the compound does not attenuate thermal pain in a rodent hot plate model when administered at a dose of at least 1 mg/kg.

7. The compound of claim 6 , wherein the compound does not attenuate thermal pain in a rodent hot plate model when administered at a dose of at least 3 mg/kg.

8. The compound of claim 6 , wherein the compound does not attenuate thermal pain in a rodent hot plate model when administered at a dose of 10 mg/kg.

9. A method of treating a depressive symptom in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of claim 2 .

10. A method of treating a depressive symptom in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of claim 4 .

11. A method of treating a depressive symptom in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of claim 6 .

12. A method of treating a depressive symptom in a subject in need thereof, comprising administering to the subject the compound of claim 1 , or a pharmaceutically acceptable salt thereof.

13. A compound having the following structural formula:

or a pharmaceutically acceptable salt thereof.

Assignments (4)
SECURITY INTEREST Recorded Feb 13, 2026
From: ALKERMES PHARMA IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 074858/0405 →
RELEASE OF SECURITY INTEREST IN PATENTS PREVIOUSLY RECORDED AT REEL/FRAME (073213/0302) Recorded Feb 13, 2026
From: JPMORGAN CHASE BANK, N.A., AS ADMINISTRATIVE AGENT
To: ALKERMES PHARMA IRELAND LIMITED
Reel/Frame 074858/0429 →
SECURITY INTEREST Recorded Oct 23, 2025
From: ALKERMES PHARMA IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 073213/0302 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 26, 2014
From: BLUMBERG, LAURA COOK; DEAVER, DAN; EYERMAN, DAVID
To: ALKERMES PHARMA IRELAND LIMITED
Reel/Frame 033186/0905 →