IP Library Granted Patent US 11,944,616
Granted Patent B2
US 11,944,616 · App. 17/825,082 · Granted Apr 2, 2024

Dizocilpine derivatives as peripheral NMDA receptor antagonists

Inventors: Sylvia Cohen-Kaminsky (Le Plessis-Robinson, FR); Marc Humbert (Le Plessis-Robinson, FR); Sebastien Dumas (Le Plessis-Robinson, FR); Gilles Bru-Mercier (Le Plessis-Robinson, FR); Samir Messaoudi (Chatenay-Malabry, FR); Jean-Daniel Brion (Chatenay-Malabry, FR); Mouad Alami (Chatenay-Malabry, FR); Gilles Galvani (Chatenay-Malabry, FR)
Assignees: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS); UNIVERSITÉ PARIS-SACLAY; ASSISTANCE PUBLIQUE—HOPITAUX DE PARIS (APHP); HOPITAL MARIE LANNELONGUE
A61K31/46A61K45/06A61P9/12C07D451/00C07D451/02
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Quick Facts
Patent No.
US 11,944,616
App. No.
17/825,082
Granted
Apr 2, 2024
Kind
B2
Abstract

The present invention relates to compounds of formula (I): for use as peripheral NMDA receptor antagonists.

Claims (19)

1. Compound of formula (I):

wherein:

R 1 represents a cyclobutyl group;

R 2 represents a (C 1 -C 10 )alkyl group;

n is 1;

R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 represent a hydrogen atom; and X − is an anionic counterion selected from the group consisting of I − , Cl − , Br − , and OH − .

2. Compound according to claim 1 , wherein R 2 represents a methyl group or an ethyl group.

3. Compound according to claim 1 , wherein R 2 represents a methyl group.

4. Compound according to claim 1 , wherein R 2 represents an ethyl group.

5. Compound according to claim 1 , wherein the anionic counterion X − is selected from the group consisting of I − and Cl − .

6. Compound according to claim 1 , wherein the anionic counterion X − is I − .

7. Compound according to claim 1 , wherein the anionic counterion X − is Cl − .

8. Compound according to claim 1 , wherein the anionic counterion X − is Br − .

9. Compound according to claim 1 , wherein the anionic counterion X − is OH − .

10. Compound according to claim 1 , chosen from:

11. A pharmaceutical composition comprising at least one compound according to claim 1 , and at least one pharmaceutically acceptable excipient.

12. A method for treating a disease or condition in a subject comprising administering to the subject a compound according to claim 1 , wherein the disease or the condition is pulmonary hypertension.

13. A method for treating a disease or condition in a subject comprising administering to the subject a compound according to the claim 1 , wherein the disease or the condition is selected from the group consisting of pulmonary arterial hypertension and thromboembolic pulmonary hypertension.

14. A method for treating a disease in a subject comprising administering to the subject a compound according to claim 1 , wherein the disease is pulmonary arterial hypertension.

Assignments (2)
CORRECTIVE ASSIGNMENT TO CORRECT THE ASSIGNEE'S ADDRESS PREVIOUSLY RECORDED ON REEL 063094 FRAME 0158. ASSIGNOR(S) HEREBY CONFIRMS THE MERGER. Recorded Apr 4, 2023
From: UNIVERSITÉ PARIS SUD
To: UNIVERSITÉ PARIS-SACLAY
Reel/Frame 063264/0150 →
MERGER Recorded Mar 24, 2023
From: UNIVERSITÉ PARIS SUD
To: UNIVERSITÉ PARIS-SACLAY
Reel/Frame 063094/0158 →
Priority Claims (1)
EP 16305712 · Jun 13, 2016 · regional
Continuity (2)
Division 16308654
Related Publication 20220280498A1 · Sep 8, 2022