Patent RU-2236405-C2 (RU)
Title: Polycyclic thiazolidine-2-ylidene amines, medicinal agents containing thereof and method for preparing medicinal agent
Inventor: JENE GERKHARD
IPC: C07D277/60
Filed: 1999-07-03
Granted: 2004-09-20
Abstract: 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 CH 2 ; R1 means (C 2 -C 6 )-alkyl wherein one hydrogen atom can be replaced for OC(O)CH 3 ; (C 2 -C 6 )-alkenyl; (C 2 -C 6 )-alkynyl; O-CF 3 , O-CH 2 -CF 3 , O-CH 2 -CF 2 -CF 3 , O-CH 2 -CFCF 2 -CF 3 , O-(C 4 -C 6 )-alkyl wherein in alkyl residues one, more or all hydrogen atom(s) can be replaced for fluorine atom; S-(C 1 -C 6 )-alkyl, S-(CH 2 ) n -phenyl, SO 2 -(C 1 -C 6 )-alkyl, SO 2 -(CH 2 ) n -phenyl wherein n = 0-1, and phenyl residue can be substituted up to two times with (C 1 -C 6 )-alkyl; phenyl, O-(CH 2 ) 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, CF 3 , OCF 3 , (C 1 -C 6 )-alkyl, SO 2 -CH 3 , O-(C 1 -C 6 )-alkyl; R1' means hydrogen atom (H); R2 means hydrogen atom (H); R3 means hydrogen atom (H); R4 means (C 1 -C 6 )-alkyl; R5 means (C 1 -C 6 )-alkyl; or B): Y means a direct bond; X means CH 2 ; R1 and R1' mean independently of one another hydrogen (H), chlorine (Cl) atom. (C 1 -C 6 )-alkyl wherein one hydrogen atom is substituted for OH; R2 means hydrogen atom (H); R3 means fluorine atom (F), C(O)OCH 3 , C(O)OH; R4 means (C 1 -C 6 )-alkyl, (CH 2 ) n -phenyl wherein n = 1; R5 means (C 1 -C 6 )-alkyl, (CH 2 ) n -phenyl wherein n = 1; or C): Y means a direct bond; X means CH 2 ; R1 and R1' mean independently of one another hydrogen (H) atom, chlorine (Cl) atom, phenyl substituted with CF 3 ; R2 means (C 1 -C 6 )-alkyl, (C 2 -C 8 )-alkenyl; R3 means hydrogen (H) atom, fluorine (F) atom; R4 means (C 1 -C 6 )-alkyl, (CH 2 ) n -phenyl wherein n = 0 and phenyl can be substituted with chlorine atom (Cl), O-(C 1 -C 6 )-alkyl; R5 means (C 1 -C 6 )-alkyl, (CH 2 ) n -phenyl wherein n = 0 and phenyl can be substituted with chlorine atom (Cl), O-(C 1 -C 6 )-alkyl; or D): Y means a direct bond, -CH 2 - or -CH 2 -CH 2 -; X means CH(phenyl) wherein phenyl residue can be substituted with chlorine atom (Cl), oxygen (O), sulfur (S) atom, SO 2 ; R1 and R1' mean independently of one another hydrogen atom (H), chlorine atom (Cl), NO 2 , CN, SO 2 -(C 1 -C 6 )-alkyl, SO 2 -(CH 2 ) n -phenyl wherein n = 0; R2 means hydrogen atom (H); R3 means hydrogen atom (H); R4 means (C 1 -C 6 )-alkyl; R5 means (C 1 -C 6 )-alkyl, or R4 and R5 in together can mean -CH 2 -CH 2  or -CH 2 -C(CH 3 ) 2 -group; or E): Y means a direct bond; X means CH 2 ; 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-(C 1 -C 3 )-alkyl, (C 1 -C 6 )-alkyl; R5 means phenyl being phenyl residue can be up to two times is substituted with fluorine atom (F), chlorine atom (Cl), (C 1 -C 6 )-alkyl, O-(C 1 -C 3 )-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