Benzylideneaminoguanidine derivatives as NR2B-selective NMDA receptor antagonists and their therapeutic applications
AssigneeInflectis Bioscience
InventorsPierre MINIOU, Philippe GUEDAT
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Abstract
The present invention relates benzylidene aminoguanidine derivatives as NR2B-selective NMDA receptor antagonists and their therapeutic applications.
Claims18
A method of selectively inhibiting the subunit 2B (NR2B) of the N-methyl-D-aspartate (NMDA) receptor in a cell having NMDA receptor subunit 2B (NR2B)-containing NMDA receptors, the method comprising treating the cell with an effective amount of a compound of general formula (I):
- and the (Z) and/or (E) isomers thereof, or a tautomer thereof, or pharmaceutically acceptable salts thereof,
- wherein:
- R1, R2, R3, R4, R5 are independently hydrogen, deuterium, halogen, haloalkyl, alkyl, alkoxy, hydroxyl, aryl, or aryloxy,
- so as to effect a neuroprotective reduction in the effect of excitotoxic NMDA receptor activity.
A method of selectively inhibiting the subunit 2B (NR2B) of the N-methyl-D-aspartate (NMDA) receptor in a subject having NMDA receptor subunit 2B (NR2B)-containing NMDA receptors, the method comprising administering an effective amount of a compound of general formula (I):
- and the (Z) and/or (E) isomers thereof, or a tautomer thereof, or pharmaceutically acceptable salts thereof,
- wherein:
- R1, R2, R3, R4, R5 are independently hydrogen, deuterium, halogen, haloalkyl, alkyl, alkoxy, hydroxyl, aryl, or aryloxy,
- in said subject in need thereof.
A method for preventing or treating a disease, disorder, or medical condition caused by overactivation of the N-methyl-D-aspartate (NMDA) receptor containing a subunit 2B (NR2B) by selectively targeting the NR2B subunit of said NMDA receptor, wherein said method comprises administering to a subject in need thereof an effective amount of a compound of general formula (I):
- and the (Z) and/or (E) isomers thereof, or a tautomer thereof, or pharmaceutically acceptable salts thereof,
- wherein:
- R1, R2, R3, R4, R5 are independently hydrogen, deuterium, halogen, haloalkyl, alkyl, alkoxy, hydroxyl, aryl, or aryloxy.
A compound selected from the group consisting in:
- 2-(2,4,6-Trifluorobenzylidene)hydrazinecarboximidamide acetate salt
- 2-(2,6-Difluoro-4-chlorobenzylidene)hydrazinecarboximidamide
- 2-(2-Chloro-4,6-difluorobenzylidene)hydrazinecarboximidamide
- 2-(2-Chloro-4-hydroxybenzylidene)hydrazinecarboximidamide
- 2-(2,4-Dichloro-6-fluorobenzylidene)hydrazinecarboximidamide
- 2-(2,6-Dichloro-4-fluorobenzylidene)hydrazinecarboximidamide
- 2-(2-Dichloro-3, 5-difluorobenzylidene)hydrazinecarboximidamide
- and the (Z) and/or (E) isomers thereof, or a tautomer thereof, or pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.