IP Library Granted Patent US 10,052,308
Granted Patent B2
US 10,052,308 · App. 15/337,605 · Granted Aug 21, 2018

Spiro-lactam NMDA receptor modulators and uses thereof

Inventors: John A. Lowe, III (Stonington, CT); M. Amin Khan (Evanston, IL)
Assignee: Aptinyx Inc.
A61K31/407A61K31/397
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Quick Facts
Patent No.
US 10,052,308
App. No.
15/337,605
Granted
Aug 21, 2018
Kind
B2
Abstract

Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Claims (18)

1. A method of treating neuropathic pain associated with fibromyalgia, in a patient in need thereof, the method comprising administering to the patient a pharmaceutically effective amount of a compound having the formula:

or a stereoisomer and/or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound has the formula:

or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the compound has the formula:

or a pharmaceutically acceptable salt thereof.

4. A method of treating fibromyalgia, in a patient in need thereof, the method comprising administering to the patient a pharmaceutically effective amount of a compound having the formula:

or a stereoisomer and/or a pharmaceutically acceptable salt thereof.

5. The method of claim 4 , wherein the compound has the formula:

or a pharmaceutically acceptable salt thereof.

6. The method of claim 4 , wherein the compound has the formula:

or a pharmaceutically acceptable salt thereof.

7. A method of treating neuropathic pain associated with diabetic neuropathy, in a patient in need thereof, the method comprising administering to the patient a pharmaceutically effective amount of a compound having the formula:

or a stereoisomer and/or a pharmaceutically acceptable salt thereof.

8. The method of claim 7 , wherein the compound has the formula:

or a pharmaceutically acceptable salt thereof.

9. The method of claim 7 , wherein the compound has the formula:

or a pharmaceutically acceptable salt thereof.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 1, 2023
From: APTINYX INC.
To: TENACIA BIOTECHNOLOGY (HONG KONG) CO., LIMITED
Reel/Frame 065426/0673 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2017
From: LOWE, III, JOHN A.; KHAN, M. AMIN
To: NAUREX, INC.
Reel/Frame 043639/0815 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2017
From: NAUREX, INC.
To: APTINYX INC.
Reel/Frame 043639/0867 →
Continuity (3)
Continuation 14764395
Provisional Application 61757903 · Jan 29, 2013
Related Publication 20170231956A1 · Aug 17, 2017