ANTIDEPRESSIVA INDOLDERIVAT

摘要

1502038 Pyrido[3,4 - b]indole derivatives ENDO LABORATORIES Inc 20 Aug 1976 [22 Aug 1975 22 June 1976] 34864/76 Heading C2C The invention comprises compounds of formula and their pharmaceutically suitable salts, wherein one of R 1 and R 3 is Me or Et and the other is H, Me or Et; and R 2 is H, C 1-3 alkyl, allyl or propargyl, provided that the total no. of C atoms in R 1 +R 2 +R 3 is #4. In examples, these compounds are prepared by reducing with BH 3 or NaBH 4 , followed by acid treatment, of the 4a,9a-dehydro analogues in which the 2- substituent is R 2 , MeCO or EtCO, or by hydrolysis of the corresponding 2-cyano compounds (for R 2 =H). Starting materials otherwise prepared are the corresponding 3,4 - dihydropyrido[3,4-b)indoles and their quaternary salts, 2-acyl analogues of the compounds of the invention, and compounds of formulae QCH:CRNO 2 , QCH 2 CHRNH 2 and QCH 2 CHRNHCOR1, where R is H, Me or Et, and R1 is Me or Et. Therapeutic compositions having antidepressant activity comprise compounds of the above formula and may be administered orally, parenterally or rectally.