发明名称 DERIVATIVES OF 2-CYANOIMINOIMIDAZOLE INHIBITING ACTIVITY OF PHOSPHODIESTERASE IV (PDE IV), METHODS OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF, METHOD OF ITS PREPARING
摘要 organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to novel derivatives of 2-cyanoiminoimidazole of the general formula (I) where R1 and R2 mean hydrogen atom, C1-C6-alkyl, difluoromethyl, trifluoromethyl, C3-C6-cycloalkyl, saturated 5-membered heterocycle containing one oxygen atom, 6,7-dihydro-5H-cyclo-pentapyridinyl or C1-C6-alkyl substituted with phenyl, indanyl or C3-C6-cycloalkyl; R3 means hydrogen atom; R4 means hydrogen, halogen atom, C1-C6-alkyl, trifluoromethyl or R4 means a radical of the formula -O-R7 where R7 means hydrogen atom; R5 means hydrogen atom or R4 and R5 taken in common can form a bivalent radical of the formula -CH2-CH2-O-CH2-CH2-; R6 means hydrogen atom or C1-C6-alkyl; -A-B- means a bivalent radical of the formula or CHR10-CHR11 where each R10 and R11 means independently hydrogen atom or C1-C6-alkyl; L means hydrogen atom, C1-C6-alkyl, C1-C6-alkyloxycarbonyl, C1-C6-alkyl substituted with one or two phenyl groups. Also, invention relates to methods of synthesis of indicated compounds, pharmaceutical composition based on thereof eliciting inhibitory effect on activity of phosphodiesterase IV and method of the composition preparing. Invention can be used in medicine for treatment of patients with allergic, atopic and inflammatory diseases. EFFECT: new compounds indicated above, improved method of their synthesis and pharmaceutical composition preparing, valuable medicinal properties. 12 cl, 4 dwg, 3 tbl
申请公布号 RU2180902(C2) 申请公布日期 2002.03.27
申请号 RU19990109032 申请日期 1997.09.24
申请人 ZHANSEN FARMASETIKA N.V. 发明人 FREJN EHDDI ZHAN EHDGAR;FERNANDES-GADEA FRANSISKO KHAV'ER;ANDRES-KHIL' KHOSE IGNASIO
分类号 C07D233/44;A61K31/00;A61K31/415;A61K31/4164;A61K31/4168;A61P11/00;A61P11/06;A61P29/00;A61P37/00;A61P37/08;C07D233/48;C07D233/88;C07D405/12;(IPC1-7):C07D233/44 主分类号 C07D233/44
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