NEW DERIVATIVES OF 2-(1-AZA-BICYCLO[2,2,2]OCT-3-YL)-2,3-DIHYDROISOINDOL-1-ONE/5,6-DIHYDRO-FURO[2,3-c]PYRROL-4-ONE AS LIGANDS TO ALFA 7 NICOTINIC ACETYLCHOLINE RECEPTOR Russian patent published in 2009 - IPC C07D453/02 C07D491/04 C07D519/00 A61K31/439 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to new compounds with formula I: , where D is O; E is CH₂ or O; n equals 1 or 2, and R¹ is chosen from hydrogen, halogen or substituted or unsubstituted 5- or 6-member aromatic or heteroaromatic ring with 0, 1 or 2 nitrogen atoms, 0 or 1 oxygen atom, or is chosen from substituted or unsubstituted 8-, 9- or 10-member condensed heteroaromatic ring system with 0 or 1 nitrogen atom, 0 or 1 oxygen atom, where the said aromatic or heteroaromatic rings or ring systems, when they are substituted, have substitutes which are chosen from -C₁-C₆alkyl, -C₃-C₆cycloalkyl, -C₁-C₆alkoxy, halogen, -CF3, -S(O)_mR², where m equals 0, 1 or 2, -NR²R³, -NR²C(O)R³ or -C(O)NR²R³; R² and R³ are in each case independently chosen from hydrogen, -C₁-C₄alkyl, -C₃-C₆cycloalkyl, aryl; or its stereoisomers, enantiomers or pharmaceutically acceptable salts; under the condition that the given compound is not 2-(1-aza-bicyclo[2.2.2]oct-3-yl)-2,3-dihydroisoindol-1-one. The invention also relates to compounds with formulae II or III, to a pharmaceutical composition, as well as to use of compounds in paragraph 1.

EFFECT: obtaining new biologically active compounds with activity towards alpha 7 nicotinic acetylcholine receptors (α7 nAChRs).

8 cl, 72 ex, 1 tbl