3-heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1h)...

C - Chemistry – Metallurgy – 07 – D

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C07D 215/36 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/53 (2006.01) C07D 215/20 (2006.01) C07D 215/22 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2150645

3-Heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1H)quinolone derivatives of formula I Image (I) wherein the radicals R1, R2, R3 and R4 are each independently of the others hydrogen, an aliphatic hydrocarbon radical, free or etherified hydroxy, mercapto or etherified and/or oxidised mercapto, unsubstituted or aliphatically substituted amino, nitro, free or esterified or amidated carboxy, cyano, free or amidated sulfamoyl, halogen or trifluoromethyl, X is oxy or optionally oxidised thio, A is a divalent aliphatic radical and R5 is an optionally partially hydrogenated aryl or heteroaryl radical that is unsubstituted or substituted by aliphatic or araliphatic hydrocarbon radicals, by free or etherified hydroxy, by mercapto or etherified and/or oxidised mercapto, by unsubstituted or aliphatically substituted amino, by aliphatic acyl, by free or esterified or amidated carboxy, by cyano, by free or amidated sulfamoyl, by halogen and/or by trifluoromethyl; free or etherified hydroxymethyl; cyano; or free or esterified or amidated carboxy, and tautomers and/or salts thereof, have antagonistic properties with respect to excitatory amino acids and can be used for the treatment of pathological conditions that are responsive to glycine-antagonistic blocking of NMDA- sensitive receptors.

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