FIELD: organic chemistry, biochemistry, medicine, pharmacy.
SUBSTANCE: invention relates to compounds of the general formula (1): 
wherein R1 means (C1-C6)-alkyl that can be substituted with phenyl; R2, R3, R4 and R5 represent independently each of other hydrogen halogen atom, nitro-group, (C1-C4)-alkyl, (C6-C10)-aryl-(C1-C4)-alkyloxy-, (C6-C10)-aryloxy-group, (C6-C10)-aryl that can be mono-, di- or tri-substituted with halogen atom; 2-oxopyrrolidine-1-yl, 2,5-dimethylpyrrole-1-yl or -NR6-A-R7 under condition that R2, R3, R4 and R5 can't mean simultaneously hydrogen atom and at least one residue among R2, R3, R4 and R5 represents 2-oxopyrrolidine-1-yl, 2,5-dimethylpyrrole-1-yl or -NR6-A-R7 at value R6 - hydrogen atom, (C1-C4)-alkyl or (C6-C10)-aryl-(C1-C4)-alkyl wherein aryl can be substituted with halogen atom; A means a simple bond, -COn, -SOn or -CONH; n = 1 or 2; R7 means hydrogen atom; (C1-C18)-alkyl or (C2-C18)-alkenyl that can be substituted from one to three times with (C1-C4)-alkyl, (C1-C4)-alkyloxy-group, -N-((C1-C4)-alkyl)2-group, -COOH, (C1-C4)-alkyloxycarbonyl, (C6-C12)-aryl, (C6-C12)-aryloxy-group, (C6-C12)-arylcarbonyl, (C6-C10)-aryl-(C1-C4)-alkoxy-group, halogen atom, -CF3 or oxo-group wherein aryl, in turn, can be substituted with halogen atom, (C1-C)-alkyl, aminosulfonyl- or methylmercapto-group; (C6-C10)-aryl-(C1-C4)-alkyl, (C5-C8)-cycloalkyl-(C1-C4)-alkyl, (C5-C8)-cycloalkyl, (C6-C10)-aryl-(C2-C6)-alkenyl, (C6-C10)-aryl, diphenyl, diphenyl-(C1-C4)-alkyl, indanyl that can be mono- or di-substituted with (C1-C18)-alkyl, (C1-C18)-alkyloxy-group, (C3-C8)-cycloalkyl, hydroxy-group, (C1-C4)-alkylcarbonyl, (C6-C10)-aryl-(C1-C4)-alkyl, (C6-C10)-aryl-(C1-C4)-alkyloxy-group, (C6-C10)-aryloxy-group, nitro-, cyano-group, (C6-C10)-aryl, fluorosulfonyl, (C1-C6)-alkyloxycarbonyl, (C6-C10)-arylsulfonyloxy-group, pyridyl, -NHSO2-(C6-C10)-aryl, halogen atom, -CF3 or -OCF3 wherein alkyl can be substituted once again with halogen atom, -CF3 or (C1-C4)-alkyloxy-group; or group Het-(CH2)r wherein r = 0, 1, 2 or 3 wherein Het means saturated or unsaturated 5-7-membered heterocycle comprising atoms nitrogen (N), oxygen (O) or sulfur (S) and can be condensed with benzene and substituted with (C1-C4)-alkyl, (C6-C10)-aryl, halogen atom, (C1-C4)-alkyloxy-group, (C6-C10)-aryl-(C1-C4)-alkyl, (C6-C10)-aryl-(C1-C)-alkylmercapto- or nitro-group and wherein aryl condensed with benzene can be, in turn, substituted with halogen atom, (C1-C4)-alkyloxy-group; and to their pharmacologically acceptable salts and additive salts of acids, and to a method for their preparing. Proposed compounds show inhibitory effect on activity of hormone-sensitive lipase.
EFFECT: improved preparing method, valuable biochemical and medicinal properties of compounds.
14 cl, 199 ex
| Title | Year | Author | Number |
|---|---|---|---|
| SUBSTITUTED 3-PHENYL-5-ALKOXY-1,3,4-OXADIAZOL-2-ONES AND THEIR APPLYING AS LIPASE INHIBITORS | 2000 |
|
RU2265600C2 |
| DERIVATIVES OF OXADIAZOLE | 1997 |
|
RU2182905C2 |
| SUBSTITUTED DERIVATIVES OF OXAZOL-BENZOISOTHIAZOLDIOXIDE, METHOD FOR MAKING AND APPLYING THEREOF | 2005 |
|
RU2377242C2 |
| UREA AND SULPHAMIDE DERIVATIVES AS TAFIA INHIBITORS | 2007 |
|
RU2459619C2 |
| OBTAINING DIHYDROTHIENO[3,2-d]PYRIMIDINES AND INTERMEDIATE PRODUCTS, APPLIED FOR THEIR SYNTHESIS | 2008 |
|
RU2528340C2 |
| USING IkB KINASE INHIBITOR IN ANESTHETIZING TREATMENT | 2003 |
|
RU2320338C2 |
| SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES AS Rho-KINASE INHIBITORS | 2007 |
|
RU2455302C2 |
| NEW DIAMIDES PYRIMIDIN-4,6 OF DICARBOXYLIC ACID FOR SELECTIVE INHIBITION OF COLLAGENASES | 2003 |
|
RU2344129C2 |
| DERIVATIVES OF PHENYLUREA SUBSTITUTED WITH CARBOXYLIC ACID AMIDE AND THEIR USING AS MEDICINAL AGENTS | 2002 |
|
RU2291858C2 |
| METHOD OF RESIDUAL LIPOPROTEINS PRODUCING INHIBITION | 2004 |
|
RU2330682C2 |
