ANTICONVULSIVE AMINOSÄURE-DERIVATE

• Main Authors: KOHN, HAROLD L, WATSON, DARRELL
• Format: Patent
• Language: German
• Published: 15.03.2002
• Edition: 7
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to compounds exhibiting central nervous system (CNS) activity which are useful in the treatment of epilepsy and other CNS disorders. The compounds of this invention have the following general formula: and pharmaceutically acceptable salts thereof wherein R is aryl, aryl lower alkyl, heterocyclic or heterocyclic lower alkyl, wherein R is unsubstituted or is substituted with at least one electron withdrawing group or an electron donating group; R1 is hydrogen or lower alkyl and R1 is unsubstituted or is substituted with at least one electron withdrawing substituent or at least one electron donating substituent; R2 and R3 are independently each hydrogen, lower alkenyl, lower alkynyl, aryl lower alkyl, aryl, heterocycli, heterocycli lower alkyl or Z-Y, wherein R2 and R3 may be unsubstituted or substituted with at least one electron withdrawing group or electron donating group; Z is O, S, NR4, PR4 or a chemical bond; Y is hydrogen, lower alkyl, aryl, aryl lower alkyl, lower alkenyl, lower alkynyl, or halo, and Y may be unsubstituted or substituted with at least one electron donating group or electron donating group; provided that when Y is halo, Z is a chemical bond or ZY taken together is NR4NR5R6, NR4OR5, ONR4R5, OPR4R5, PR4OR5, SNR4R5, NR4SR5, SPR4R5, PR4SR5, NR4PR5R6 or PR4NR5R6, R4, R5 and R6 are independently hydrogen, lower alkyl, aryl, aryl lower alkyl, lower alkenyl, lower alkynyl, and R4, R5 and R6 may be unsubstituted or substituted with an electron withdrawing group or an electron donating group and n is 1-4. u