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US 10,538,482 B2Granted
Adamantane and memantine derivatives as peripheral NMDA receptor antagonists
AssigneesInstitut National De La Sante Et De La Recherche Medicale (Inserm), Assistance Publique-Hopitaux de Paris, Centre National de la Recherche Scientifique (CNRS), Universite Paris-Sud
InventorsMarc Humbert, Sylvia Cohen-Kaminsky, Sébastien Dumas, Gilles Bru-Mercier, Mouad Alami, Jean-Daniel Brion, Samir Messaoudi, Gilles Galvani
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Abstract
The present invention relates to cationic compounds of formula (I) for use as peripheral NMDA receptor antagonists.
Claims16
Cationic compound of formula (I):
- wherein:
- R1 and R2 represent, independently of each other, a hydrogen atom or a (C1-C6)alkyl group;
- the group —(CH2)n-A is linked to the cycle in position (a) or (b);
- n is 0, 1, 2 or 3;
- A represents a —NR3R4 group or a —N+R3R4R5 group;
- R3, R4 and R5 represent, independently of each other, a hydrogen atom, a (C1-C10)alkyl group, a (C1-C10)alkoxy group, a (C1-C10)alkyl-C(═NH)(—OH) group, a (C3-C8)cycloalkane group, a 6- to 10-membered aryl group or a 5- to 12-membered heteroaryl group;
- said alkyl or alkoxy groups being optionally substituted with one or more —NR6R7 group, —N+R6R7R8 group, (C3-C8)cycloalkane group, 6- to 10-membered aryl group or 5- to 12-membered heteroaryl group;
- with R6, R7 and R8 represent, independently of each other, a hydrogen atom or a (C1-C6)alkyl;
- and
- the compound of formula (I) contains at least one positive charged nitrogen atom;
- provided that R1 and R2 are not both a hydrogen atom;
- and
- provided that when R1 and R2 are a methyl group, the group —(CH2)n-A is linked to the cycle in position (a), and n is 0, then A is not a group —N+H3.
10 more elements
Dependencies are inferred from the claim text.