Dizocilpine derivatives as peripheral NMDA receptor antagonists

Patent metadata

Field	Value
Publication number	US-12274694-B2
Application number	US-202318296543-A
Country	US
Kind code	B2
Filing date	Apr 6, 2023
Priority date	Jun 13, 2016
Publication date	Apr 15, 2025
Grant date	Apr 15, 2025

Abstract

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

First claim

The invention claimed is:

1. A compound selected from the group consisting of the following compounds:

2. A pharmaceutical composition, comprising:
at least one compound of claim 1 , and
at least one pharmaceutically acceptable excipient.

3. The pharmaceutical composition of claim 2 , further comprising at least one other therapeutic agent.

4. The pharmaceutical composition of claim 2 , further comprising at least one other therapeutic agent selected from the group consisting of a vasodilator agent and a glutamate receptor antagonist, wherein the glutamate receptor antagonist is ionotropic and/or metabotropic.

5. The pharmaceutical composition of claim 2 , further comprising at least one other therapeutic agent selected from the group consisting of NMDAR antagonists.

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

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

8. A method for treating a disease in a subject, the method comprising:
administering the compound of claim 1 the subject,
wherein the disease is pulmonary arterial hypertension.

Assignees

• Inst Nat Sante Rech Med
• Centre Nat Rech Scient
• Univ Paris Saclay
• Assist Publique—Hopitaux De Paris Aphp
• Hopital Marie Lannelongue

Inventors

• Cohen-Kaminsky Sylvia
• Humbert Marc
• Dumas Sebastien
• Bru-Mercier Gilles
• Messaoudi Samir
• Brion Jean-Daniel
• Alami Mouad
• Galvani Gilles

Classifications

• C07D451/02 Primary

  containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof · CPC title

• C07D451/00

  Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title