DERIVATIVES OF 2-CYANOIMINOIMIDAZOLE INHIBITING ACTIVITY OF PHOSPHODIESTERASE IV (PDE IV), METHODS OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF, METHOD OF ITS PREPARING Russian patent published in 2002 - IPC

Abstract RU 2180902 C2

FIELD: 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

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RU 2 180 902 C2

Authors

Frejn Ehddi Zhan Ehdgar

Fernandes-Gadea Fransisko Khav'Er

Andres-Khil' Khose Ignasio

Dates

2002-03-27Published

1997-09-24Filed