FIELD: organic chemistry, medicine, endocrinology, pharmacy.
SUBSTANCE: invention describes polycyclic thiazolidine-2-ylidene amines of the formula (I):
and also their physiologically acceptable salts wherein A): Y means an ordinary bond; X means CH2; R1 means (C2-C6)-alkyl wherein one hydrogen atom can be replaced for OC(O)CH3; (C2-C6)-alkenyl; (C2-C6)-alkynyl; O-CF3, O-CH2-CF3, O-CH2-CF2-CF3, O-CH2-CFCF2-CF3, O-(C4-C6)-alkyl wherein in alkyl residues one, more or all hydrogen atom(s) can be replaced for fluorine atom; S-(C1-C6)-alkyl, S-(CH2)n-phenyl, SO2-(C1-C6)-alkyl, SO2-(CH2)n-phenyl wherein n = 0-1, and phenyl residue can be substituted up to two times with (C1-C6)-alkyl; phenyl, O-(CH2)n-phenyl wherein n = 0-1; 1- or 2-naphthyl, 2-, 3- or 4-pyridyl being phenyl cycles can be substituted from one to three times with F, Cl, CF3, OCF3, (C1-C6)-alkyl, SO2-CH3, O-(C1-C6)-alkyl; R1' means hydrogen atom (H); R2 means hydrogen atom (H); R3 means hydrogen atom (H); R4 means (C1-C6)-alkyl; R5 means (C1-C6)-alkyl; or B): Y means a direct bond; X means CH2; R1 and R1' mean independently of one another hydrogen (H), chlorine (Cl) atom. (C1-C6)-alkyl wherein one hydrogen atom is substituted for OH; R2 means hydrogen atom (H); R3 means fluorine atom (F), C(O)OCH3, C(O)OH; R4 means (C1-C6)-alkyl, (CH2)n-phenyl wherein n = 1; R5 means (C1-C6)-alkyl, (CH2)n-phenyl wherein n = 1; or C): Y means a direct bond; X means CH2; R1 and R1' mean independently of one another hydrogen (H) atom, chlorine (Cl) atom, phenyl substituted with CF3; R2 means (C1-C6)-alkyl, (C2-C8)-alkenyl; R3 means hydrogen (H) atom, fluorine (F) atom; R4 means (C1-C6)-alkyl, (CH2)n-phenyl wherein n = 0 and phenyl can be substituted with chlorine atom (Cl), O-(C1-C6)-alkyl; R5 means (C1-C6)-alkyl, (CH2)n-phenyl wherein n = 0 and phenyl can be substituted with chlorine atom (Cl), O-(C1-C6)-alkyl; or D): Y means a direct bond, -CH2- or -CH2-CH2-; X means CH(phenyl) wherein phenyl residue can be substituted with chlorine atom (Cl), oxygen (O), sulfur (S) atom, SO2; R1 and R1' mean independently of one another hydrogen atom (H), chlorine atom (Cl), NO2, CN, SO2-(C1-C6)-alkyl, SO2-(CH2)n-phenyl wherein n = 0; R2 means hydrogen atom (H); R3 means hydrogen atom (H); R4 means (C1-C6)-alkyl; R5 means (C1-C6)-alkyl, or R4 and R5 in together can mean -CH2-CH2 or -CH2-C(CH3)2-group; or E): Y means a direct bond; X means CH2; R1 means chlorine atom (Cl); R1' means hydrogen atom (H); R2 means hydrogen atom (H); R3 means hydrogen atom (H); R4 means phenyl being phenyl residue can be up to two times is substituted with fluorine atom (F), chlorine atom (Cl), O-(C1-C3)-alkyl, (C1-C6)-alkyl; R5 means phenyl being phenyl residue can be up to two times is substituted with fluorine atom (F), chlorine atom (Cl), (C1-C6)-alkyl, O-(C1-C3)-alkyl. Compounds are useful for treatment of obesity, for prophylaxis or treatment of non-insulin-dependent diabetes mellitus (type II). The invention describes a medicinal agent for suppression of appetite and/or lose weight also and a medicinal agent for prophylaxis and treatment of diabetes mellitus of type II, and a method for preparing a medicinal agent by mixing an active substance with pharmaceutically acceptable vehicle and this mixture is converted to the form useful for application.
EFFECT: improved preparing method, valuable medicinal properties of compounds.
11 cl, 2 tbl, 24 ex
