5,10-dihydrodipyrido2,3-b:2,3-epyrazin and 5,10-dihydro-dipyrido 2,3-b:3,2-epyrazin compounds, a process for their preparation and pharmaceutical compositions containing them.

摘要

5,10-Dihydrodipyrido (2,3-b:2,3-e) pyrazine and 5,10-dihydrodipyrido (2,3-b:3,2-e) pyrazine derivatives (I) are new. 5,10-Dihydrodipyrido (2,3-b:2,3-e) pyrazine and 5,10-dihydrodipyrido (2,3-b:3,2-e) pyrazine derivatives of formula (I) and their salts are new. X = N, CR2 or CH; Y1 = N, CR2 or CH; R1 = 1-6C alkyl (optionally substituted by halo, 1-6C alkylthio, 1-6C alkoxy, 1-6C mono- or dialkylamino, aryl, OH, formyl, 1-6C alkyloxycarbonyl or carboxy); R2, R3 = Z or W1; Z = H, halo, 1-6C alkyl (optionally substituted by OH, 1-6C alkyloxy, aryl, amino (optionally substituted by one or two 1-6C alkyl, aryl, 1-6C arylalkyl, 1-6C aminoalkyl, 1-6C monoalkylaminoalkyl, 1-6C dialkylaminoalkyl, 1-6C hydroxyalkyl or 1-6C alkoxyalkyl) or formyl), amino (optionally substituted by one or two 1-6C alkyl, aryl, 1-6C arylalkyl, 1-6C alkylsulfonyl, arylsulfonyl, 1-6C aminoalkyl, 1-6C mono- or dialkylaminoalkyl, 1-6C hydroxyalkyl, 1-6C alkoxyalkyl), nitro, 1-6C alkylthio, formyl, hydroxycarbonyl, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C mono- or dialkylaminocarbonyl; W1 = 5-24C alkene (optionally substituted on terminal position by groups of formulae (i) or (ii); and carbons of alkene optionally replaced by O, imine, -N(R4)-CO-, -CO-N(R4)- or -N(R4)-); R2a, R3a = Z; R4 = H, 1-6C alkyl, aryl, 1-6C arylalkyl; and provided that Y1 is N when X is CR2 or CH, or Y1 is CR2 or CH when X is N; that R2 and R3 are both Z or R2 is Z when R3 is W1 and R2 is W1 when R3 is Z. Independent claim are also included for: (1) the preparation of (I) (2) the intermediates of (I) of formulae (A)-(C); (3) the preparation of (A)-(C). R1'' = 1-6C alkyl; R = H, 1-5C alkyl; and G1 = Sn, B, Si (substituted by at last one 1-6 C alkyl).