SULFONAMIDE-SUBSTITUTED CHROMANS AND PHARMACEUTICAL COMPOSITION

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to compounds of the general formula (I): where R1 and R2 mean independently each of other hydrogen atom, alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms; R3 means R10-(CnH2n) where R10 is hydrogen atom; n = 0, 1-10; R4 means R13-CrH2r-Z-CqH...

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Hauptverfasser: BRENDEL JOAKHIM, LANG KHANS JOKHEN, VAJDMANN KLAUS, GERLAKH UVE
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creator BRENDEL JOAKHIM
LANG KHANS JOKHEN
VAJDMANN KLAUS
GERLAKH UVE
description FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to compounds of the general formula (I): where R1 and R2 mean independently each of other hydrogen atom, alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms; R3 means R10-(CnH2n) where R10 is hydrogen atom; n = 0, 1-10; R4 means R13-CrH2r-Z-CqH2q; q = 0, 1-8; r = 0, 1-8; Z means CO- NR14, -OCO-NR14, -OCxH2x-O-, -OCxH2x--CO-O, -CO-O-(CxH2x)-O- being addition is possible from both sides; x = 2, 3 or 4; R14 means hydrogen atom, alkyl with 1, 2 or 3 carbon atoms; R13 means hydrogen atom, -NR15R16, C(=NR17NR15-R16, -COOR17, phenyl or N-containing heterocycle with 1-9 carbon atoms being phenyl or N-containing heterocycle are unsubstituted or substituted with a single substitute taken among F, Cl, NO2, NH2, OH, aminosulfonyl; R15 and R16 mean independently each of other hydrogen atom or alkyl with 1-4 carbon atoms; or R15 and R16 mean in common chain consisting of 4 or 5 methylene groups one of that -CH2-group can be replaced for O-, -S-, -NH-, -N(CH3)- or N(benzyl); R17 means hydrogen atom; R5, R6, R7, R8 mean independently each of other hydrogen atom, F, Cl, alkyl with 1-5 carbon atoms, -y-CsH2sR18 where y means O-; R18 means hydrogen atom, phenyl; s = 0, 1-6; B means hydrogen atom, and their physiologically acceptable salts and pharmaceutical composition that is able to block K(camp)-channel or IKs-channel and containing effective amount of at least one compound of the formula (I) as an active component. Proposed compounds are not toxic practically, exhibit strong and specific blocking effect on K+ -channel that is opened by cyclic adenosine monophosphate (cAMP). EFFECT: valuable medicinal and pharmacological properties of compounds. 17 cl, 1 tbl, 62 ex
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SUBSTANCE: invention relates to compounds of the general formula (I): where R1 and R2 mean independently each of other hydrogen atom, alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms; R3 means R10-(CnH2n) where R10 is hydrogen atom; n = 0, 1-10; R4 means R13-CrH2r-Z-CqH2q; q = 0, 1-8; r = 0, 1-8; Z means CO- NR14, -OCO-NR14, -OCxH2x-O-, -OCxH2x--CO-O, -CO-O-(CxH2x)-O- being addition is possible from both sides; x = 2, 3 or 4; R14 means hydrogen atom, alkyl with 1, 2 or 3 carbon atoms; R13 means hydrogen atom, -NR15R16, C(=NR17NR15-R16, -COOR17, phenyl or N-containing heterocycle with 1-9 carbon atoms being phenyl or N-containing heterocycle are unsubstituted or substituted with a single substitute taken among F, Cl, NO2, NH2, OH, aminosulfonyl; R15 and R16 mean independently each of other hydrogen atom or alkyl with 1-4 carbon atoms; or R15 and R16 mean in common chain consisting of 4 or 5 methylene groups one of that -CH2-group can be replaced for O-, -S-, -NH-, -N(CH3)- or N(benzyl); R17 means hydrogen atom; R5, R6, R7, R8 mean independently each of other hydrogen atom, F, Cl, alkyl with 1-5 carbon atoms, -y-CsH2sR18 where y means O-; R18 means hydrogen atom, phenyl; s = 0, 1-6; B means hydrogen atom, and their physiologically acceptable salts and pharmaceutical composition that is able to block K(camp)-channel or IKs-channel and containing effective amount of at least one compound of the formula (I) as an active component. Proposed compounds are not toxic practically, exhibit strong and specific blocking effect on K+ -channel that is opened by cyclic adenosine monophosphate (cAMP). 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Proposed compounds are not toxic practically, exhibit strong and specific blocking effect on K+ -channel that is opened by cyclic adenosine monophosphate (cAMP). 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SUBSTANCE: invention relates to compounds of the general formula (I): where R1 and R2 mean independently each of other hydrogen atom, alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms; R3 means R10-(CnH2n) where R10 is hydrogen atom; n = 0, 1-10; R4 means R13-CrH2r-Z-CqH2q; q = 0, 1-8; r = 0, 1-8; Z means CO- NR14, -OCO-NR14, -OCxH2x-O-, -OCxH2x--CO-O, -CO-O-(CxH2x)-O- being addition is possible from both sides; x = 2, 3 or 4; R14 means hydrogen atom, alkyl with 1, 2 or 3 carbon atoms; R13 means hydrogen atom, -NR15R16, C(=NR17NR15-R16, -COOR17, phenyl or N-containing heterocycle with 1-9 carbon atoms being phenyl or N-containing heterocycle are unsubstituted or substituted with a single substitute taken among F, Cl, NO2, NH2, OH, aminosulfonyl; R15 and R16 mean independently each of other hydrogen atom or alkyl with 1-4 carbon atoms; or R15 and R16 mean in common chain consisting of 4 or 5 methylene groups one of that -CH2-group can be replaced for O-, -S-, -NH-, -N(CH3)- or N(benzyl); R17 means hydrogen atom; R5, R6, R7, R8 mean independently each of other hydrogen atom, F, Cl, alkyl with 1-5 carbon atoms, -y-CsH2sR18 where y means O-; R18 means hydrogen atom, phenyl; s = 0, 1-6; B means hydrogen atom, and their physiologically acceptable salts and pharmaceutical composition that is able to block K(camp)-channel or IKs-channel and containing effective amount of at least one compound of the formula (I) as an active component. Proposed compounds are not toxic practically, exhibit strong and specific blocking effect on K+ -channel that is opened by cyclic adenosine monophosphate (cAMP). EFFECT: valuable medicinal and pharmacological properties of compounds. 17 cl, 1 tbl, 62 ex</abstract><edition>7</edition><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title SULFONAMIDE-SUBSTITUTED CHROMANS AND PHARMACEUTICAL COMPOSITION
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