Patent RU-2245331-C2 (RU)
Inventor: KHODSON GAROL D FREHNSIS
IPC: C07D498/04
Filed: 2000-01-06
Granted: 2005-01-27
Abstract: FIELD: organic chemistry, biochemistry, medicine. 
     SUBSTANCE: invention describes a method for prophylaxis or treatment of states that involves inhibition of activity of enzyme that catalyzes hydrolysis of ester functional groups and wherein indicated state represents obesity or accompanying disorder, and wherein compound of the formula (1): 
     
       
     
     is prescribed, or its pharmaceutically acceptable salt, ester, amide or a precursor. Also, invention relates to a method for manufacturing the medicinal preparation used for prophylaxis or treatment of states wherein inhibition of activity of enzyme is required wherein indicated enzyme catalyzes hydrolysis of ester functional groups. In the formula (1) A means a 6-membered aromatic or heteroaromatic ring; R 1  means a branched or unbranched alkyl (its carbon chain can be broken by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or their substituted derivative wherein a substitute is taken independently among the following group: halogen atom, alkyl, alkyl substituted with halogen atom, aryl, arylalkyl, heteroaryl, reduced heteroaryl, reduced heteroarylalkyl, arylalkoxy-, cyano-, nitro-group, -C(O)R 4 , -CO 2 R 4 , -SOR 4 , -SO 2 R 4 , -NR 6 R 7 , -OR 6 , -SR 6 , -C(O)CX 1 X 2 NR 6 R 7 , -C(O)NR 4 R 5 , -C(O)N(OR 5 )R 6 , -NR 6 C(O)R 4 , -CR 6 (NH 2 )CO 2 R 6 , -NCX 1 X 2 CO 2 R 6 , -N(OH)C(O)NR 6 R 7 , -N(OH)C(O)R 4 , -NHC(O)NR 6 R 7 , -C(O)NHNR 6 R 7 , -C(O)N(OR 5 )R 6  or lipid, or steroid (natural or synthetic) under condition that any substituting heteroatom in R 1  or R 2  must be separated from exocyclic nitrogen atom by at least two carbon atoms (preferably, saturated atoms), and wherein R 4  represents hydrogen atom, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, reduced heteroaryl or reduced heteroarylalkyl, OR 6 , NHCX 1 X 2 CO 2 R 6  or NR 6 R 7 ; R 5  represents hydrogen atom, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, reduced heteroaryl or reduced heteroarylalkyl; R 6  and R 7  are taken independently among hydrogen atom, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heteroaryl, reduced heteroaryl, heteroarylalkyl, reduced heteroarylalkyl or -(CH 2 ) n (OR 5 ) m  wherein n = from 1 to 12, preferably, from 2 to 10; m = from 1 to 3; R 5  means preferably (C 2 -C 10 )-alkyl; X 1  and X 2  represent independently hydrogen atom, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heteroaryl, reduced heteroaryl, heteroarylalkyl or reduced heteroarylalkyl. Also, invention describes compound of formulae (II), (IIa) and (IIb) given in the description and a method for preparing compound of formulae (II), (IIa) and (IIb), pharmaceutical composition used for prophylaxis or treatment of obesity and/or accompanying disorder, nutrition product, a method for prophylaxis or treatment of obesity or accompanying disorders, a method for inhibition of activity of enzymes, a method for reducing fat content in animals, a cosmetic method for maintaining this weight and a new intermediate compound of the formula (IV) indicated in the description. Invention discloses the possibility for prophylaxis or treatment of obesity or accompanying disorders. 
     EFFECT: valuable medicinal properties of compounds. 
     33 cl, 1 dwg, 2 tbl, 5 ex