HUP0301932A2 - IL-1béta és TNF-a inhibitor benzofenon származékok, ezeket tartalmazó gyógyszerkészítmények és ezek alkalmazása gyógyszerkészítmények elżállítására - Google Patents

IL-1béta és TNF-a inhibitor benzofenon származékok, ezeket tartalmazó gyógyszerkészítmények és ezek alkalmazása gyógyszerkészítmények elżállítására

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Publication number
HUP0301932A2
HUP0301932A2 HU0301932A HUP0301932A HUP0301932A2 HU P0301932 A2 HUP0301932 A2 HU P0301932A2 HU 0301932 A HU0301932 A HU 0301932A HU P0301932 A HUP0301932 A HU P0301932A HU P0301932 A2 HUP0301932 A2 HU P0301932A2
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Hungary
Prior art keywords
general formula
group
alkyl
atom
alkenyl
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HU0301932A
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English (en)
Inventor
Anne Marie Horneman
Original Assignee
Leo Pharma A/S
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Publication date
Application filed by Leo Pharma A/S filed Critical Leo Pharma A/S
Publication of HUP0301932A2 publication Critical patent/HUP0301932A2/hu
Publication of HUP0301932A3 publication Critical patent/HUP0301932A3/hu

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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract

A találmány tárgya (I) általános képletű vegyületen, ahol a képletbenR1 jelentése elsősorban halogénatom, hidroxil-, merkapto -, ciano-,nitro-, amino -, alkil-, alkenil -, alkoxi-, alkiltio-,alkoxikarbonil-, alkilkarboniloxi-, -CONR9R10 általános képletűcsoport, ahol R9 és R10 jelentése egymástól függetlenül hidrogénatom,alkil- vagy arilcsoport; R2 jelentése elsősorban egy vagy több, azonosvagy különböző, a hidrogénatom, halogénatom, halogénalkil-, hidroxi-,merkapto-, ciano-, karboxi-, nitro-, amino-, alkil-, alkenil-,alkoxi-, alkiltio-, alkilamino-, alkoxikarbonil-, -CONR9R10- általánosképletű csoport közül kiválasztott szubsztituens; R3 jelentéseelsősorban egy orto-helyzetben levő szubsztituens a hidrogénatom,halogénatom, haloalkil-, hidroxi-, merkapto-, ciano -, nitro-, amino-,alkil-, alkenil-, alkoxi-, alkiltio-, alkoxikarbonil-, -CONR9R10általános képletű csoport közül kiválasztva; R4 jelentése elsősorbanhidrogénatom, alkil-, alkenil -, alkinil-, cikloalkil-, cikloalkenil-,karboxi- vagy arilcsoport; R5 jelentése heteroaromás mono- vagybiciklusos 1-4 heteroatomot tartalmazó gyűrű, amely triazintólkülönböző, és a gyűrűrendszer adott esetben szubsztituálva van Xjelentése oxigénatom, kénatom, N-OH vagy N R11 képletű csoport, aholR11 jelentése hidrogénatom vagy alkilcsoport; valamint ennekgyógyászatilag elfogadható savakkal képzett sói, hidrátjai ésszolvátjai és adott esetben N-oxidjai, ahol az R5 heterociklusosszubsztituens egy nitrogénatomja oxidálva van. A találmány tárgya ezenkívül az (I) általános képletű vegyületek alkalmazása gyulladásosbetegségek vagy állapotok kezelésére vagy megelőzésére használhatógyógyszer előállítására, valamint hatóanyagként az (I) általánosképletű vegyületeket tartalmazó gyógyszerkészítmény. A kezelhetőbetegség lehet például asztma, allergia, artritisz, atherosclerosis,gyulladt bélszindróma, Crohn-szindróma. Ó
HU0301932A 2000-05-22 2001-05-18 Benzophenones as inhibitors of il-1 beta and tnf-alpha, pharmaceutical compositions containing them and use of them for producing pharmaceutical compositions HUP0301932A3 (en)

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