Pyridine derivatives as nmda-receptor subtype blockers

Details Pyridine derivatives as nmda-receptor subtype blockers Pyridine derivatives as nmda-receptor subtype blockers

C - Chemistry, Metallurgy

07

D

C07D 409/04 (2006.01) A61K 31/381 (2006.01) A61K 31/44 (2006.01) A61K 31/4436 (2006.01) C07D 213/38 (2006.01) C07D 213/73 (2006.01) C07D 213/74 (2006.01)

Patent

CA 2464888

The present invention relates to compounds of formulas (IA) or (IB) wherein R1/R2 independently from each other hydrogen, lower alkyl, -(CH2)nNR5R5' or - (CH2)n+1OH; R5 and R5' are independently from each hydrogen, lower alkyl; R3/R4 are independently from each other hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl or hydroxy; Ar is phenyl or thiophenyl; the dotted line is -CH2-CH2-, -CH2-CHR'-, wherein R' is lower alkyl or are two hydrogen atoms, not forming a bridge and; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof, with the exception of 6-styryl-pyridin- 2-yl-amine. The compounds of the present invention are NMDA (N-methyl-D- aspartate)-receptor subtype blockers and may be used in the treatment of diseases related to this receptor.

Composés de correspondants aux formules (lA) ou (lB) dans lesquelles R?1¿ et R?2¿ représentant indépendamment l'un de l'autre hydrogène, alkyle inférieur, -(CH¿2?)¿n?NR?5¿R?5'¿ ou -(CH¿2?)¿n+1?OH, R?5¿ et R?5'¿ étant indépendamment l'un de l'autre hydrogène ou alkyle inférieur, R?3¿ et R?4¿ représentent indépendamment l'un de l'autre hydrogène, alkyle inférieur, halogène, trifluorométhyle ou hydroxy, Ar représente phényle ou thiophényle, la ligne en pointillés représente -CH¿2?-CH¿2?- ou -CH¿2?-CHR'- dans laquelle R' représente alkyle inférieur ou deux atomes d'hydrogène ne formant pas un pont et n vaut 0, 1 ou 2, ainsi que sels d'addition d'acide pharmaceutiquement acceptables, à l'exception de la 6-styryl-pyridin-2-yl-amine. Les composés selon la présente invention sont des bloquants d'un sous-type du récepteur NMDA (N-méthyl-D-aspartate) et peuvent être utilisés dans le traitement de maladies liées à ce récepteur.

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