Piperazin- und Piperidinisoxazol-Derivate

摘要

Compounds of the formula (I> <IMAGE> wherein R is OH, COR2, PO(R2)2, C1-C4 alkoxy or halogen; R1 is hydrogen, halogen, trifluoromethyl, C1-C4 alkyl, C3-C7 cycloalkyl, C1-C4 alkoxy, benzyloxy, benzyloxy in which the phenyl moiety is substituted by halogen or C1-C4 alkyl, phenyl or phenyl substituted by halogen; R2 is OH, C1-C4 alkoxy, benzyloxy, substituted benzyloxy, amino or amino substituted by one or two C1-C4 alkyl groups; A is C1-C4 alkylene and Y is nitrogen or carbon, A is C2-C4 alkenylene or (CH2)tCH= wherein t is 0, 1, 2 or 3 and Y is carbon or A is (CH2)p-CC or CC-(CH2)q wherein p and q are independently 0, 1 or 2 and Y is nitrogen; and = represents a single or double bond; or a pharmaceutically acceptable salt thereof, are excitatory amino acid antagonists and are useful in the treatment of disease states such as epilepsy and other CNS disorders. Precursors of the above compounds are of the formulae: <IMAGE> wherein R' is chlorine, bromine or ethoxycarbonyl; R'1 is methyl, ethyl, t-butyl or phenyl; m is 1, 2, 3 or 4; and R" is a dialkylphosphoric group or a fluorine atom, and <IMAGE> wherein X is Cl, Br, I, a leaving group, an imidazole group, triphenylphosphonium or dialkyl phosphonate.