PURPOSE: To obtain new β-carboline-derived compounds exhibiting compatibility with benzodiazepine receptors and on the other hand having an inverse agonist and antagonist effect.
CONSTITUTION: Compounds of formula I or II [X is O, S, NR5 or -C(-R1)-X which represents N(R6)-C(=O)-CH2-X-; R1 is OH, alkoxy or alkyl substd. with OH or alkoxy; R2 is H, alkyl, OH, alkoxy, acyloxy or benzyloxy (these may be optionally substd.); R3-R6 are each H or alkyl optionally substd. (with OH, alkoxy or alkoxycarbonylmethyl)], as well as corresponding tetrahydro derivatives of β-carboline, such as 1,12-dihydro-2-methylindro[3',2';4,5- d]pyrido-[2,3-f]-1H,3H,6H-1,4-diazepine-3,12-dione are provided. The compounds are used in combination with benzodiazepine in order to compensate undesirable side effect owing to the use of the latter.
PIEERU POCHI
JIYAN ROTSUSHI
GIRUBAATO DOREI
ROORAN DEYUBOA
RIA PURADO DOU KARUBARO
