| 摘要 |
(A)3-Substd.-beta-carboline derivs. of formula (I) are new. (R' is H, F, Cl, Br, I, NO2, CN, Me, CF3, MeS, NR16R17, NHCOR16, PO(OR23)(OR24), CHR33-OR39, OR18, R35-ethynyl, COOOR2, SR2, SO2R2 or SO2NR21R22; R16 and R17 are H or alkyl, alkenyl or alkynyl each having up to 6C, or aralkyl or cycloalkyl each having up to 10C, all 5 gps. being opt. substd. by halogen, OH, SH, SR23, COOR23, CN, CONR23R24, CH(OR23)OR24 or CH(SR23)SR24 or NR16R17 is a satd. or unsatd. 3- to 7-membered heterocyclic ring opt. substd. by 1-3C alkyl, :S, :O, OR23, SR23 or NR23R24 and a C atom in the ring is opt. replaced by S, O or NR23; R23 and R24 are H or 1-3C alkyl; R33 and R39 are H or 1-3C alkyl and R39 may also be R33CO; R18 is alkyl, aryl or aralkyl each having up to 13C; R35 is H, 1-3C alkyl, 6-12C aryl, CHR33R30 or P(O)(OR23)(OR24); R30 is halogen, OR40 or NR41R42; R40 is H, 1-3C alkyl or 4-5C alkylene to form a 5- or 6-membered heterocyclic ring contg. O; R41 and R42 are H or 1-6C alkyl; R2 is 1-6C alkl; R21 and R2 are H or 1-6C alkyl; m is 1-4; R'' is e.g. H, 1-6C alkyl or 2-6C alkoxyalkyl; R20 is e.g. 1-6C alkyl; n is 1-3; Y s H2, NOR1, CH-COOR3 or CONR4R5; R1 is H, 1-6C alkyl, aryl, aralkyl or COR2; R3 is H or 1-6C alkyl; R4 and R5 are H, 1-6C alkyl, 6-10C aryl or 7-10C aralkyl; Z is e.g. H, or alkoxy or aralkoxy, or CYZ is a 5- or 6-membered heterocyclic ring contg. an O atom, adjoining O and N atoms or up to 4N and opt. substd. b 1-6C alkl, OH or oxo). (B) Cpds. (I) are new when Y is also O with certain limitations on other substituents. Cpds. (I) are CNS active agents esp. tranquillisers, non-sedating anticonvulsants, anti-aggressive agents and anxiolytics and stress protection agents. Dose is 0.1-300 mg daily. |
