| abstract |
Naphthyridine derivs. of formula (I), as racemates or optical isomers, and their suitable salts with acids are new. In (I) R1=H, 1-4C alkyl, 2-oxopropyl, 2-hydroxypropyl, 3-oxobutyl, 3-hydroxybutyl, cyclopropyl methyl, benzyl (opt. halogenated esp. by F or Cl), acetyl, cyclopropylcarbonyl, benzoyl or (CH2)nR1. R2=H, halo, CH3 or CH3O. R6=H or COR7. R3=CH3 or C2H5, and R4=OH or H and R5=H, or R3+R4=oxo and R5=H, or R3=CH3 or C2H5 and R4+R5=an additional C-C bond. n=1 or 2. R1=(m)ethoxycarbonyl or CN. R7=OH, 1-4C alkoxy, NH2(opt. substd. by 1 or 2 CH3 or by one cyclopropyl). The following cpds. are excluded: R3+R4=oxo; (a) R1=H=R6 and R2=10-CH3O and (b) R1=R2=R6=H; but when R6=alkoxycarbonyl stereoisomers are included. Dose is 10-100 mg/day. In an example methyl 1,2,3,3a,4,5,-hexahydro-3-methyl-6-oxo-6H-indolo 3,2,1-de 1,5 naphthyridine-4-carboxylate was prepd. fron Nb-methyltryptamine and diethyl alpha-formyl succinate. |