Amide derivatives as NMDA receptor antagonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S322000, C546S198000, C546S199000

Reexamination Certificate

active

06919355

ABSTRACT:
New Formula (I) compounds are disclosed having NR2B selective NMDA receptor antagonist activity:whereinone of the neighboring R1, R2, R3and R4groups is OH or NH2 and the others are each hydrogen , ortwo of the neighboring R1, R2R3and R4groups in given case together with one or more identical or different additional hetero atom and —CH═ and/or —CH2— groups forms a 5-6 membered homo- or heterocyclic ring, preferably pyrrole, pyrazole, imidazole, oxazole, oxo-oxazolidine, or 3-oxo-1,4-oxazine ring, and the other two of R1, R2, R3and R4groups are hydrogen atoms,R5and R6together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by hydroxy group, and/or in given case phenyl or phenoxy, phenyl-(C1-C4alkyl), phenyl-(C1-C4alkoxy), phenoxy-(C1-C4alkyl), anilino, phenyl-(C1-C4alkylamino), [phenyl-(C1-C4alkyl)]-amino, benzoyl, hydroxy-diphenylmethyl, C1-C4alkoxycarbonyl-phenoxymethyl or benzhydrylidene group, optionally substituted on the aromatic ring by one or more halogen atom, cyano or hydroxy group, C1-C4alkyl or C1-C4alkoxy group,X is independently oxygen, —NH— or a CH2 group,Y is independently a nitrogen atom or a —CH— group, and the salts thereof formed with acids and bases.

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