FIELD: organic chemistry, medicine, pharmacology, pharmacy.
SUBSTANCE: invention relates to a new physiologically active composition effecting on nicotine receptors and prepared in the form of tablets, granules, capsules, suspensions, solutions and injections. As an active component the composition comprises pharmaceutically effective amount of substituted 1-oxo-1,2-dihydro[2,7]-naphthyridine of the general formula (1)
or its salt, N-oxide or hydrate wherein R1 represents hydrogen atom, inert substitute, optionally substituted (C1-C5)-alkyl, optionally substituted amino-group; R2 and R3 represent independently of one another hydrogen atom, nitrile group, formyl group, inert substitute, optionally substituted (C1-C5)-alkyl, carboxyl group, optionally substituted (C1-C6)-alkyloxycarbonyl group or optionally substituted carbamoyl group; R4 at carbon atoms of pyridine moiety represents: hydrogen atom, halogen atom, inert substitute, optionally substituted hydroxy-(C1-C5)-alkyl, optionally substituted amino-group, optionally substituted hydroxyl group, optionally substituted (C1-C6)-alkyloxycarbonyl group, optionally substituted carbamoyl group; R4 at nitrogen atom of pyridine moiety forms pyridinium salt with pharmacologically acceptable anion and represents inert substitute. Also, invention relates to new substituted 1-oxo-1,2-dihydro[2,7]naphthyridines of the general formula (1) or their salts, N-oxides or hydrates wherein R1 and R4 have value given in cl. 1, and R2 and R3 represent independently of one another carboxyl group, optionally substituted (C1-C6)-alkyloxycarbonyl group or optionally substituted carbamoyl group. Also, invention relates to a method for their preparing and to a method for modulating activity of nicotine receptor and using compounds of the general formula (1) by cl. 1 for preparing physiologically active composition, and as ligands of nicotine receptors for aims of experimental investigations of physiological processes as "pharmacological tools". Also, invention relates to a set for preparing the composition.
EFFECT: improved preparing method, valuable properties of compounds and compositions.
7 cl, 2 sch, 2 tbl, 5 ex
| Title | Year | Author | Number |
|---|---|---|---|
| SUBSTITUTED 1,2-DIHYDRO[2,7]NAPHTHIRIDINES, PHARMACEUTICAL COMPOSITION, METHOD FOR ITS PREPARING AND APPLYING | 2003 |
|
RU2243218C1 |
| SUBSTITUTED [1,3]OXAZOLO[4,5-d]PYRIDAZINES AND COMBINATORY LIBRARY | 2003 |
|
RU2229478C1 |
| 1-SULFONYL-1,3-DIHYDROINDOLE-2-ONES, PHARMACEUTICAL COMPOSITIONS (VARIANTS), METHOD FOR THEIR PREPARING AND APPLYING | 2003 |
|
RU2259999C2 |
| AZAHETEROCYCLES COMPRISING FRAGMENT OF PIPERIDIN-2-YL- FOCUSED LIBRARIES AND PHARMACEUTICAL COMPOSITIONS | 2004 |
|
RU2259364C1 |
| SUBSTITUTED 5-SULFO-2-OXO-1,2-DIHYDROQUINOLINE 4-CARBOXYLIC ACIDS AND THEIR DERIVATIVES (VARIANTS) AND FOCUSED LIBRARY | 2003 |
|
RU2260002C2 |
| SUBSTITUTED 3-PYRIDYLMETHYLAMINES AND FOCUSED LIBRARY | 2003 |
|
RU2228930C1 |
| HETEROCYCLIC COMPOUNDS COMPRISING 2-AMINOPYRIDINE-3-SULFOMIC FRAGMENT, METHODS FOR THEIR PREPARING (VARIANTS), FOCUSED LIBRARY AND PHARMACEUTICAL COMPOSITION | 2004 |
|
RU2263667C1 |
| SUBSTITUTED 7-SULFONYL-BENZO[B][1,4]DIAZEPINES (VARIANTS), METHODS FOR THEIR PREPARING (VARIANTS), FOCUSED LIBRARY AND PHARMACEUTICAL COMPOSITION | 2004 |
|
RU2261246C1 |
| 1,3-DIOXO-2,3-DIHYDRO-1H-PYRROLO[3,4-C]QUINOLINES (VARIANTS), PHARMACEUTICAL COMPOSITIONS (VARIANTS), METHOD FOR THEIR PREPARING (VARIANTS) AND METHOD FOR TREATMENT (VARIANTS) | 2003 |
|
RU2257385C2 |
| SUBSTITUTED 3,7-DIAZABICYCLO[3,3,1]NONANES, FOCUSED LIBRARY AND COMBINATORY LIBRARY | 2003 |
|
RU2228934C1 |
