TRICYCLIC DIAZEPINE VASOPRESSIN AND OXYTOCIN ANTAGONISTS, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT

摘要

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to tricyclic diazepine antagonists of vasopressin and oxytocin of the general formula (I) where Y means -(CH2)n where n = 0 or 1; A-B means -NR3-(CH2)m- where m = 1 or 2 and fragment means condensed phenyl, 5-membered aromatic (unsaturated) heterocyclic ring containing one sulfur heteroatom. Fragment means 5-membered heterocyclic, unsaturated, condensed ring containing nitrogen atom where D, E and F are taken from carbon or nitrogen atoms and where carbon atoms can be optionally substituted with substituents taken from halogen atom, , -C(O)O-lower-(C1-C3)-alkyl and others; substituent R means a fragment of the formula where Ar means a residue where R and R are hydrogen, lower-(C1-C3)-alkyl, lower-(C1-C3)-alkoxy-group and halogen atom. Compound is taken from fragments of formulas and others where Ra is hydrogen, CH2 or ; q = 1; Rb is CH3 or C2H5; is taken from fragments of formulas where means S; R and R are taken independently from hydrogen atom, lower-(C1-C3)-alkyl, -S-lower-(C1-C3)-alkyl, halogen atom, OH, NO2, -O-lower-(C1-C3)-alkyl, CF3; R is taken from hydrogen, halogen atoms, lower-(C1-C3)-alkyl, and its pharmaceutically acceptable salts and prodrugs. Method of synthesis of compounds of the formula (I) involves an interaction of compound of the formula (II) with compound of the formula Ar-C(O)-Q where subst