Unsaturated aminodicarboxylic acid derivatives

C - Chemistry – Metallurgy – 07 – F

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167/250, 167/261

C07F 9/38 (2006.01) A61K 31/66 (2006.01)

Patent

CA 2013919

4-17544/- Unsaturated aminodicarboxylic acid derivatives Abstract of the Disclosure Unsaturated aminodicarboxylic acid derivatives of formula I Image (I), wherein A is a divalent aliphatic hydrocarbon radical containing 2 carbon atoms and R1 and R2 are each independently of the other free or esterified carboxyl groups, and salt thereof, have a pronounced and selective antagonistic action against N-methyl-D-aspartic acid (NMDA)-sensitive excitatory amino acid receptors. These compounds are prepared, for example, by converting, in a formula of formula II Image (II), wherein Z1 and Z2 are hydroxy or protected hydroxy and Z3 is protected amino, Z3 into amino and, if present, converting protected hydroxyl groups Z1 and/or Z2 into hydroxy and, if desired, converting a resultant compound into another compound of formula I, resolving a resultant mixture of isomers into the individual components and separating the desired preferred isomer and/or converting a resultant free compound into a salt or a resultant salt into the corresponding free compound.

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