3-SUBSTITUTED DERIVATIVES OF 3,4,5,6,7,8-HEXAHYDRO-PYRIDO-[4',3':4,5]-THIENO[2,3- D]-PYRIMIDINE Russian patent published in 2003 - IPC

FIELD: organic chemistry, heterocyclic compounds, pharmacy. SUBSTANCE: invention relates to novel 3-substituted derivatives of 3,4,5,6,7,8-hexa-hydropyrido-[4', 3': 4,5] -thieno- [2,3-d]-pyrimidine of the general formula (I) and their physiologically acceptable salts exhibiting selective effect of antagonists of 5HT_1B and 5HT_1A and eliciting inhibitory effect of serotonin reuptake. Compounds can be used for preparing medicinal agents, in part, agents used for treatment of patients with depressions and related diseases. In compounds of the formula (I) R¹ means hydrogen atom, alkyl with 1-4 carbon atoms, acetyl or benzoyl group, phenylalkyl residue with 1-4 carbon atoms in alkyl moiety being aromatic fragment can be substituted with halogen atom, alkyl with 1-4 carbon atoms, trifluoromethyl group, hydroxyl group, alkoxy-group with 1-4 carbon atoms, amino-group, cyano-group or nitro-group, naphthyl-alkyl residue with 1-3 carbon atoms in alkyl moiety, phenylalkanone residue with 2-3 carbon atoms in alkane moiety or phenylcarbamoyl-alkyl residue with 2 carbon atoms in alkyl moiety being phenyl group can be substituted with halogen atom; R² means unsubstituted phenyl, pyridyl, pyrimidinyl or pyrazinyl group or these groups can be mono-, di- or trisubstituted with halogen atom, alkyl with 1-4 carbon atoms, trifluoromethyl, trifluoromethoxyl, hydroxyl groups, alkoxy-groups with 1-4 carbon atoms, amino-groups, monomethylamino-groups, dimethyl-amino-, cyano- or nitro- groups being these groups can be anellated with six-membered aromatic ring that can comprise one or two substituted taken among halogen atom, alkyl with 1-4 carbon atoms, hydroxyl group, trifluoromethyl group, alkoxy-group with 1-4 carbon atoms, amino-group, cyano-group or nitro-group and if necessary it can comprise one nitrogen atom or with 5- or 6-membered ring that can comprise 1-2 oxygen atoms or can be substituted with phenylalkyl group or phenylalkoxy-group with 1-2 carbon atoms in alkyl moiety being phenyl residue can be substituted with halogen atom, methyl group, trifluoromethyl group or methoxy-group; A means imino-group or oxygen atom; B means hydrogen atom or methyl group; C means hydrogen atom, methyl group or hydroxyl group; X means nitrogen atom; Y means CH₂,CH₂-CH₂,CH₂-CH₂-CH₂ or CH₂-CH; Z means nitrogen atom, carbon atom or CH being a bond between Y and Z can be double also; n means a number 2, 3 or 4. Invention relates also to their physiologically acceptable salts. EFFECT: valuable medicinal properties of compounds. 6 cl, 1 tbl