Amino acid derivative anticonvulsant

Details Amino acid derivative anticonvulsant Amino acid derivative anticonvulsant

C - Chemistry, Metallurgy

07

K

167/179, 260/316

C07K 5/04 (2006.01) A61K 31/00 (2006.01) A61K 38/04 (2006.01) C07C 237/02 (2006.01) C07C 237/22 (2006.01) C07D 207/337 (2006.01) C07D 207/34 (2006.01) C07D 209/42 (2006.01) C07D 295/15 (2006.01) C07D 307/00 (2006.01) C07D 307/54 (2006.01) C07D 307/85 (2006.01) C07D 333/38 (2006.01) C07D 333/70 (2006.01)

Patent

CA 2017217

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: Image 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 of 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, heterocyclic, heterocyclic 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, 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.

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