IP Library Granted Patent US 11,376,245
Granted Patent B2
US 11,376,245 · App. 16/308,654 · Granted Jul 5, 2022

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); UNIVERSITE PARIS SUD; ASSISTANCE PUBLIQUE—HOPITAUX DE PARIS (APHP); HOPITAL MARIE LANNELONGUE
A61K31/46A61K45/06A61P9/12C07D451/00C07D451/02
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Quick Facts
Patent No.
US 11,376,245
App. No.
16/308,654
Granted
Jul 5, 2022
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 cyclopropyl 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 the anionic counterion X − is selected from the group consisting of I − and Cl −.

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

5. A method for 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.

6. 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.

7. 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.

8. Compound according to claim 1 , chosen from:

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

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

11. Compound according to claim 1 , wherein X − is I −.

12. Compound according to claim 1 , wherein X − is Cl −.

13. Compound according to claim 1 , wherein X − is Br −.

14. Compound according to claim 1 , wherein X − is OH −.

Assignments (4)
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 →
CORRECTIVE ASSIGNMENT TO CORRECT THE THE FOURTH ASSIGNEE NAME PREVIOUSLY RECORDED AT REEL: 048819 FRAME: 0632. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded May 23, 2019
From: COHEN-KAMINSKY, SYLVIA; HUMBERT, MARC; DUMAS, SEBASTIEN; BRU-MERCIER, GILLES; MESSAOUDI, SAMIR; BRION, JEAN-DANIEL; ALAMI, MOUAD; GALVANI, GILLES
To: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS); UNIVERSITE PARIS SUD; ASSISTANCE PUBLIQUE - HOPITAUX DE PARIS (APHP); HOPITAL MARIE LANNELONGUE
Reel/Frame 050254/0386 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 8, 2019
From: COHEN-KAMINSKY, SYLVIA; HUMBERT, MARC; DUMAS, SEBASTIEN; BRU-MERCIER, GILLES; MESSAOUDI, SAMIR; BRION, JEAN-DANIEL; ALAMI, MOUAD; GALVANI, GILLES
To: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS); UNIVERSITE PARIS SUD; ASSITANCE PUBLIQUE - HOPITAUX DE PARIS (APHP); HOPITAL MARIE LANNELONGUE
Reel/Frame 048819/0632 →
Priority Claims (1)
EP 16305712 · Jun 13, 2016 · regional
Continuity (1)
Related Publication 20190307738A1 · Oct 10, 2019
Cited By (1)
US 12,274,694