ARYL SUBSTITUTED AMINO ACIDS, CNS INFLUENCING AGENTS

摘要

Compounds of formula (I) are disclosed, wherein: Ar is an aromatic group having up to 10 carbon atoms substituted by at least one substituent selected from hydroxy, carboxy, phosphono, -PO2H(OR6), phosphinico, -PO¿2H(R?6), -OPO¿3?H2, -OPO2H(OR?6¿), arsono, -AsO¿2H(OR?6), arsinico, -AsO¿2H(R?6), tetrazolyl, sulpho, sulphino, sulpheno, thio, -OSO¿3?H and -(CR?7R8)¿qY, where Y is carboxy, phosphono, -PO2H(OR6), phosphinico, -PO¿2H(R?6), -OPO¿3?H2, -OPO2H(OR?6¿), arsono, -AsO¿2H(OR?6), arsinico, -AsO¿2H(R?6), tetrazolyl, sulpho, sulphino, sulpheno, -OSO¿3?H and R?7 and R8¿ are the same or different and are selected from hydrogen, C¿1? to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl or halo or R?7 and R8¿ together constitute an oxo group, q is an integer from 0 to 3; Ar being optionally further substituted by one or more substituents selected from fluoro, chloro, bromo, iodo, nitro, cyano, C¿1? to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, haloalkyl (such as trifluoromethyl), aryl or azido; R?3¿ is hydrogen, C¿1? to C6 alkyl, C2 to C6 alkenyl or C2 to C6 alkynyl, aryl, aralkyl, biaryl or C3 to C8 cycloalkyl, haloalkyl or hydroxyalkyl; R?1, R2, R4 and R5¿ are the same or different and are selected from hydrogen, C¿1? to C6 alkyl, C2 to C6 alkenyl and C2 to C6 alkynyl; R?6 is C¿1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, aryl, aralkyl, biaryl or C3 to C8 cycloalkylene; Q is carboxy, C1 to C6 alkoxycarbonyl, aminocarbonyl, C1 to C6 alkylaminocarbonyl or hydroxamic acid; and p is an integer form 0 to 3; R?1 and R2, R3¿ and Ar, R1 and Ar, R2 and Ar and R?3 and NR4R5¿ optionally being linked to form a carbocyclic ring and pharmaceutically acceptable acid or base addition salts thereof. The compounds may be used as agents to influence the central nervous system.