Patent RU-2244711-C2 (RU)
Inventor: KHODSON GAROL D FREHNSIS
IPC: A61K31/536
Filed: 2000-01-06
Granted: 2005-01-20
Abstract: FIELD: organic chemistry, biochemistry, medicine. 
     SUBSTANCE: invention describes a method for prophylaxis or treatment of states wherein inhibition of enzyme activity is required wherein this enzyme catalyzes hydrolysis reaction of ester functional groups and wherein indicated disorder represents obesity or accompanying disease. Method involves prescribing compound of the formula (1):    
     or its pharmaceutically acceptable salt, ester, amide or precursor wherein in the formula (1) a means six-membered aromatic or heteroaromatic ring; R 1  means a branched or unbranched alkyl (its carbon chain can be broken possibly 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 represents one or more group taken independently among the following group: halogen atom, alkyl, halogen-substituted alkyl, aryl, arylalkyl, heteroaryl, reduced heteroaryl, reduced heteroarylalkyl, arylalkoxy-, cyano-, -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 one) under condition that any substituting heteroatom in R 1  or R 2  must be segregated from nitrogen exocyclic atom by at least two carbon atoms (preferably, saturated ones); R 2  means hydrogen atom or group, such as determined for R 1  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, heteroarylakyl, reduced heteroarylalkyl or -(CH 2 ) n (OR 5 ) m  wherein n = from 1 to 12 but preferably from 2 to 10; m = from 1 to 3; for R 5  (C 2 -C 10 )-alkyl is preferable; 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 compounds of formulas (II), (IIa), (IIb) given in the invention description, method for preparing compound of the formula (II), pharmaceutical composition used for prophylaxis or treatment of obesity or accompanying disorder, the nutrition foodstuff, method for prophylaxis or treatment of obesity or accompanying disorders, method for inhibition of enzymes activity, method for reducing the fat content in animals, cosmetic method for maintaining this weight of animals. Invention discloses the possibility for prophylaxis or treatment of obesity or accompanying disorders. 
     EFFECT: valuable medicinal properties of compounds. 
     30 cl, 1 dwg, 2 tbl, 5 ex