IP Library Granted Patent US 10,196,401
Granted Patent B2
US 10,196,401 · App. 15/830,378 · Granted Feb 5, 2019

Spiro-lactam NMDA receptor modulators and uses thereof

Inventor: M. Amin Khan (Evanston, IL)
Assignee: Aptinyx Inc.
C07D487/10A61K31/4025C07D471/20A61K38/00C07K16/00
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Quick Facts
Patent No.
US 10,196,401
App. No.
15/830,378
Granted
Feb 5, 2019
Kind
B2
Abstract

Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds can be used 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 (14)

1. A compound having formula I:

or a stereoisomer, an N-oxide, and/or a pharmaceutically acceptable salt thereof, wherein:

R b is selected from the group consisting of hydrogen, halogen, hydroxyl, cyano, and C 1 -C 6 alkyl;

R 1 is selected from the group consisting of hydrogen, halogen, and C 1 -C 6 alkyl; and

R 2 is selected from the group consisting of hydrogen, halogen, and C 1 -C 6 alkyl.

2. The compound of claim 1 , wherein R b is hydrogen.

3. The compound of claim 1 , wherein R 1 is hydrogen.

4. The compound of claim 2 , wherein R 1 is hydrogen.

5. The compound of claim 1 , wherein R 2 is hydrogen.

6. The compound of claim 2 , wherein R 2 is hydrogen.

7. The compound of claim 3 , wherein R 2 is hydrogen.

8. A pharmaceutical composition comprising the compound of claim 1 ; and a pharmaceutically acceptable excipient.

9. The pharmaceutical composition of claim 8 , suitable for oral administration.

10. The pharmaceutical composition of claim 8 , suitable for intravenous, intranasal, subcutaneous, and/or sublingual administration.

Assignments (2)
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 Jan 16, 2018
From: KHAN, M. AMIN
To: APTINYX INC.
Reel/Frame 044627/0735 →
Continuity (4)
Continuation 15638669 · Jun 30, 2017
Continuation PCTUS2017033323 · May 18, 2017
Provisional Application 62338767 · May 19, 2016
Related Publication 20180093994A1 · Apr 5, 2018