DERIVATIVES OF AMINOQUINOLINE AND THEIR USING AS ADENOSINE A3 LIGANDS Russian patent published in 2008 - IPC C07D215/54 C07D405/12 C07D409/12 A61K31/47 A61P9/00 A61P11/00 

Abstract RU 2317290 C2

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to novel compounds of the general formula (I): wherein R1 represents hydrogen atom or linear or branched (C1-C4)-alkyl group; R2 represents hydrogen atom or linear or branched (C1-C4)-alkyl group; R3 represents phenyl, thienyl or furyl group that are substituted optionally with one or more linear or branched (C1-C4)-alkyl group, linear or branched (C1-C4)-alkoxy-group or halogen atom; R4 and R5 represent independently of one another hydrogen atom, (C3-C6)-cycloalkyl group, linear or branched (C1-C4)-alkyl group comprising optionally amino-group or amino-group substituted with one or two linear or branched (C1-C4)-alkyl groups, hydroxy-group, carboxy-group or alkoxy-group substituted with linear or branched (C1-C4)-alkyl group; or R4 represents hydrogen atom or linear or branched (C1-C4)-alkyl group or benzyl group; R5 represents hydrogen atom, group -SO2OH or formyl group, or R4 and R5 in common with nitrogen atom form group of the general formula (a): wherein R7 and R8 represent independently one another hydrogen atom, linear or branched (C1-C4)-alkyl group; R6 represents phenyl, benzyl, thienyl or furyl group that are substituted optionally with methylenedioxy-group or one or more linear or branched (C1-C4)-alkyl group, linear or branched (C1-C4)-alkoxy-group or halogen atom; X represents group -NH or oxygen atom; Z represents oxygen atom, sulfur atom, group -CH2, group -NH or group -NR11 wherein R11 represents hydrogen atom, linear or branched (C1-C4)-alkyl group, group -SO2OH, linear or branched (C1-C4)-acyl group; n = 0, 1 or 2; m = 1, 2 or 3; o = 1, 2 or 3; p = 0 or 1; r = 0 or 1, and their salts and solvates. Also, invention relates to a method for synthesis of compounds of the general formula (I), to a pharmaceutical composition, its using and to compounds of the general formulas (I''), (II''), (III''), (IV''), (V''), (VI''), (VII''), (VIII'') and (XIII'') given in the invention description. Invention provides synthesis of novel biologically active compounds that are ligands of adenosine A3 receptors but as antagonists preferably.

EFFECT: valuable biological properties of compounds.

20 cl, 1 tbl, 40 ex

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RU 2 317 290 C2

Authors

Arani Peter

Batori Shandor

Timari Geza

Boehr Kinga

Kapui Zol'Tan

Mikush Ehndre

Urban-Sabo Katalin

Gerber Katalin

Vargane Seredi Judit

Finet Mishel'

Dates

2008-02-20Published

2004-07-23Filed