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Tittel INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1
Status
Hovedstatus
Detaljstatus
I kraft info EP patent gjort gjeldende i Norge EP patent besluttet gjeldende i Norge
Patentnummer NO/EP3137169
Europeisk (EP) publiserings nummer EP3137169
EP levert
EP søknadsnummer 15785884.6
EP meddelt
Prioritet 2014.05.01, US 201461987354 P
Sakstype Europeisk
Løpedag
Utløpsdato
Allment tilgjengelig
Validert i Norge
Innehaver Celgene Quanticel Research, Inc. (US)
Oppfinner CHEN, Young, K. (US) .... se mer/flere nedenfor
Fullmektig ZACCO NORWAY AS (NO)
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Patentkrav1. Forbindelse som har strukturen av formel (I), eller et farmasøytisk akseptabelt salt derav,hvori,W er N, C-H eller C-F;X er hydrogen, halogen, -CN, eventuelt substituert alkyl, eventuelt substituert alkynyl, eventuelt substituert karbosyklylalkynyl, eventuelt substituert aryl eller eventuelt substituert heteroaryl;Y er hydrogen, eventuelt substituert alkyl, eventuelt substituert sykloalkyl eller eventuelt substituert sykloalkylalkyl;Z er en eventuelt substituert gruppe valgt fra alkyl, karbosyklyl, C-festet heterosyklyl, N-festet heterosyklyl, heterosyklylalkyl, heterosyklylalkenyl, -O-heterosyklyl, -N(R)-heterosyklyl, -O-heterosyklylalkyl,-N(R)-heterosyklylalkyl, -N(R)(C1-C4alkylen)-NR2, -O(C1-C4alkylen)-NR2; og R er hydrogen eller C1-C4alkyl.2. Forbindelsen ifølge krav 1, eller et farmasøytisk akseptabelt salt derav, hvori W er C-H eller hvori W er C-F.3. Forbindelsen ifølge et hvilket som helst av kravene 1–2, eller et farmasøytisk akseptabelt salt derav, hvori X er valgt fra gruppen som består av hydrogen, halogen, eventuelt substituert alkynalkynyl, eventuelt substituert karbosyklylalkynyl, eventuelt substituert aryl og eventuelt substituert heteroaryl.4. Forbindelsen ifølge krav 3, eller et farmasøytisk akseptabelt salt derav, hvori det eventuelt substituerte arylet er et eventuelt substituert fenyl. 5. Forbindelsen ifølge krav 3, eller et farmasøytisk akseptabelt salt derav, hvori det eventuelt substituerte heteroarylet er valgt fra et eventuelt substituert pyridinyl, eventuelt substituert pyrazolyl eller eventuelt substituert indazolyl.6. Forbindelsen ifølge et hvilket som helst av kravene 1–5, eller et farmasøytisk akseptabelt salt derav, hvori Z er valgt fra gruppen som består av eventuelt substituert -O-heterosyklylalkyl, eventuelt substituert -N(H)-heterosyklylalkyl, eventuelt substituert -N(Me)-heterosyklylalkyl og eventuelt substituert N-festet heterosyklyl.7. Forbindelsen ifølge krav 6, eller et farmasøytisk akseptabelt salt derav, hvori heterosyklylalkylgruppen har formelen ―Rc-heterosyklyl og Rc er en eventuelt substituert C1-C3alkylenkjede, ellerhvori heterosyklylalkylgruppen har formelen ―Rc-heterosyklyl og Rc er en eventuelt substituert C1alkylenkjede, ellerhvori heterosyklylalkylgruppen har formelen ―Rc-heterosyklyl og heterosyklylet er et eventuelt substituert nitrogenholdig 4-, 5-, 6- eller 7-leddet heterosyklyl.8. Forbindelsen ifølge krav 6, eller et farmasøytisk akseptabelt salt derav, hvori det eventuelt substituerte N-festede heterosyklylet er et 4-, 5-, 6- eller 7-leddet N-festet heterosyklyl, ellerhvori det eventuelt substituerte N-festede heterosyklylet er et 6-leddet N-festet heterosyklyl, ellerhvori det eventuelt substituerte N-festede heterosyklylet er et eventuelt substituert piperidin.9. Forbindelsen ifølge krav 8, eller et farmasøytisk akseptabelt salt derav, hvori det eventuelt substituerte piperidinet er 4-aminopiperidin.10. Forbindelsen ifølge et hvilket som helst av kravene 1–9, eller et farmasøytisk akseptabelt salt derav, hvori Y er valgt fra gruppen som består av hydrogen, eventuelt substituert sykloalkyl og eventuelt substituert alkyl. 11. Forbindelsen ifølge krav 10, eller et farmasøytisk akseptabelt salt derav, hvori det eventuelt substituerte alkylet er et eventuelt substituert C1-C3alkyl, ellerhvori det eventuelt substituerte alkylet er et eventuelt substituert C1alkyl, eller hvori det eventuelt substituerte alkylet er en metylgruppe.12. Forbindelsen ifølge krav 1, eller et farmasøytisk akseptabelt salt derav, som har en hvilken som helst av de følgende strukturene:13. Forbindelsen ifølge krav 1, eller et farmasøytisk akseptabelt salt derav, som har den følgende strukturen:14. Forbindelsen ifølge krav 1, eller et farmasøytisk akseptabelt salt derav, som har en hvilken som helst av de følgende strukturene:4-(2-(4-aminopiperidin-1-yl)-1-metyl-6-okso-5-p-tolyl-1,6-dihydropyrimidin-4-yl)benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydropyrimidin-4-yl]-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(6-metoksy-pyridin-3-yl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril 4-[2-(4-amino-piperidin-1-yl)-1-metyl-5-(6-metyl-pyridin-3-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydropyrimidin-4-yl]-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydropyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(6-metoksy-pyridin-3-yl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(6-metoksy-pyridin-3-yl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(6-etyl-pyridin-3-yl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril2-fluor-4-[5-(4-metoksy-fenyl)-1-metyl-2-(4-metylamino-piperidin-1-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril2-fluor-4-[5-(3-fluor-4-metoksy-fenyl)-1-metyl-2-(4-metylamino-piperidin-1-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril4-[2-(4-amino-piperidin-1-yl)-1-etyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-amino-piperidin-1-yl)-5-syklopentyletynyl-1-metyl-6-okso-1,6-dihydropyrimidin-4-yl]-2-fluor-benzonitril[2-(4-amino-piperidin-1-yl)-4-(4-cyano-3-fluor-fenyl)-5-(4-metoksy-fenyl)-6-okso-6H-pyrimidin-1-yl]-eddiksyre2-[2-(4-amino-piperidin-1-yl)-4-(4-cyano-3-fluor-fenyl)-5-(4-metoksy-fenyl)-6-okso-6H-pyrimidin-1-yl]-acetamid4-[2-(4-amino-piperidin-1-yl)-1-(3-hydroksy-propyl)-6-okso-1,6-dihydropyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-benzofuran-5-yl-1-metyl-6-okso-1,6-dihydropyrimidin-4-yl]-2-fluor-benzonitril2-(4-amino-piperidin-1-yl)-4-(4-cyano-3-fluor-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-5-karbonitril4-[2-(4-aminopiperidin-1-yl)-5-klor-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril 2-fluor-4-[1-metyl-2-(4-metylamino-piperidin-1-yl)-5-(6-metyl-pyridin-3-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril4-[2-(2,8-diaza-spiro[4.5]dec-8-yl)-5-(3-fluor-4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-{2-(4-aminopiperidyl)-1-metyl-6-okso-5-[6-(trifluormetyl)(3-pyridyl)]hydropyrimidin-4-yl}-2-fluorbenzenkarbonitril4-[2-(4-aminopiperidyl)-1-metyl-5-(2-metyl(2H-indazol-5-yl))-6-oksohydropyrimidin-4-yl]benzenkarbonitril4-[2-((3R)-3-aminopiperidyl)-5-(3-fluor-4-metoksyfenyl)-1-metyl-6-oksohydropyrimidin-4-yl]-2-fluorbenzenkarbonitril4-[2-(4-aminopiperidyl)-5-(5-fluor-6-metoksy(3-5,6-dihydropyridy1))-1-metyl-6-oksohydropyrimidin-4-yl]-2-fluorbenzenkarbonitril4-[2-((3R)-3-aminopyrrolidinyl)-5-(3-fluor-4-metoksyfenyl)-1-metyl-6-oksohydropyrimidin-4-yl]-2-fluorbenzenkarbonitril4-[2-((3S)-3-amino-piperidin-1-yl)-5-(3-fluor-4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-((3S)-3-amino-pyrrolidin-1-yl)-5-(3-fluor-4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-((3R)-3-aminopiperidyl)-5-(4-metoksyfenyl)-1-metyl-6-oksohydropyrimidin-4-yl]-2-fluorbenzenkarbonitril4-[2-((3S)-3-amino-piperidin-1-yl)-5-(4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-4-metyl-piperidin-1-yl)-5-(3-fluor-4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-aminopiperidyl)-1-metyl-5-(1-metyl(1H-indazol-5-yl))-6-oksohydropyrimidin-4-yl]benzenkarbonitril4-{2-(4-amino-piperidin-1-yl)-1-metyl-6-okso-5-[1-(2,2,2-trifluor-etyl)-1H-pyrazol-4-yl]-1,6-dihydro-pyrimidin-4-yl}-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-1-metyl-5-(1-metyl-1H-indazol-5-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-{2-(4-amino-piperidin-1-yl)-1-metyl-6-okso-5-[1-(2,2,2-trifluor-etyl)-1H-pyrazol-4-yl]-1,6-dihydro-pyrimidin-4-yl}-benzonitril 4-[2-(4-aminopiperidyl)-1-metyl-5-(2-metyl(2H-indazol-5-yl))-6-oksohydropyrimidin-4-yl]-2-fluorbenzenkarbonitril4-[2-(4-aminopiperidyl)-5-(3,5-difluor-4-metoksyfenyl)-1-metyl-6-oksohydropyrimidin-4-yl]benzenkarbonitril4-[2-(4-aminopiperidyl)-6-(4-cyano-3-fluorfenyl)-3-metyl-4-okso-3-hydropyrimidin-5-yl]benzosyre{4-[2-(4-aminopiperidyl)-6-(4-cyanofenyl)-3-metyl-4-okso(3-hydropyrimidin-5-yl)]-2-fluorfenyl}-N-metylkarboksamid4-[2-(4-aminopiperidyl)-6-(4-cyanofenyl)-3-metyl-4-okso(3-hydro pyrimidin-5-yl)]-2-fluorbenzamid4-[2-(4-amino-piperidin-1-yl)-1-metyl-6-okso-5-(1-okso-2,3-dihydro-1H-isoindol-5-yl)-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril3-[2-(4-amino-piperidin-1-yl)-4-(4-cyano-3-fluor-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-5-yl]-benzosyre4-{5-(3-fluor-4-metoksy-fenyl)-1-metyl-6-okso-2-[(3S)-(pyrrolidin-3-ylmetyl)-amino]-1,6-dihydro-pyrimidin-4-yl}-benzonitril4-{5-(3-fluor-4-metoksy-fenyl)-1-metyl-6-okso-2-[(3R)-(pyrrolidin-3-ylmetyl)-amino]-1,6-dihydro-pyrimidin-4-yl}-benzonitril4-[2-[1,4]diazepan-1-yl-5-(3-fluor-4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril2-fluor-4-[5-(3-fluor-4-metoksy-fenyl)-1-metyl-6-okso-2-piperazin-1-yl-1,6-dihydro-pyrimidin-4-yl]-benzonitril4-[5-(3-fluor-4-metoksy-fenyl)-1-metyl-6-okso-2-(piperidin-4-ylamino)-1,6-dihydro-pyrimidin-4-yl]-benzonitril4-[2-(4-amino-piperidin-1-yl)-2'-dimetylamino-1-metyl-6-okso-1,6-dihydro-[5,5']bipyrimidinyl-4-yl]-2-fluor-benzonitril5-[2-(4-amino-piperidin-1-yl)-4-(4-cyano-3-fluor-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-5-yl]-pyridin-2-karboksylsyremetylamid2-fluor-4-{5-(4-metoksy-fenyl)-1-metyl-6-okso-2-[(3S)-(pyrrolidin-3-ylmetyl)-amino]-1,6-dihydro-pyrimidin-4-yl}-benzonitril2-fluor-4-{5-(4-metoksy-fenyl)-1-metyl-6-okso-2-[(3R)-(pyrrolidin-3-ylmetyl)-amino]-1,6-dihydro-pyrimidin-4-yl}-benzonitril 2-fluor-4-[5-(4-metoksy-fenyl)-1-metyl-6-okso-2-(piperidin-4-ylamino)-1,6-dihydro-pyrimidin-4-yl]-benzonitril2-fluor-4-[5-(4-metoksy-fenyl)-1-metyl-2-(metyl-(3S)-pyrrolidin-3-ylmetylamino)-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril2-fluor-4-[5-(4-metoksy-fenyl)-1-metyl-2-(metyl-piperidin-4-yl-amino)-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril2-fluor-4-[5-(4-metoksy-fenyl)-1-metyl-2-(metyl-pyrrolidin-3-ylmetyl-amino)-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(6-dimetylamino-pyridin-3-yl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril2-fluor-4-[5-(6-metoksy-pyridin-3-yl)-1-metyl-2-(4-metylamino-piperidin-1-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(4-dimetylamino-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-1-metyl-6-okso-5-(6-pyrrolidin-1-yl-pyridin-3-yl)-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-[1,4]diazepan-1-yl-5-(6-metoksy-pyridin-3-yl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-[1,4]diazepan-1-yl-5-(6-metoksy-pyridin-3-yl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-[1,4]diazepan-1-yl-5-(6-dimetylamino-pyridin-3-yl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(3-amino-azetidin-1-yl)-5-(4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydropyrimidin-4-yl]-2-fluor-benzonitril2-fluor-4-[1-metyl-2-(4-metylamino-piperidin-1-yl)-5-(2-metyl-2H-indazol-5-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril4-[2-[1,4]diazepan-1-yl-1-metyl-5-(2-metyl-2H-indazol-5-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-[1,4]diazepan-1-yl-5-(6-dimetylamino-pyridin-3-yl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril4-[2-(4-amino-piperidin-1-yl)-1-metyl-5-(6-morfolin-4-yl-pyridin-3-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril 4-[2-(3-aminometyl-azetidin-1-yl)-5-(4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril2-fluor-4-[5-(4-metoksy-fenyl)-1-metyl-2-(3-metylaminometyl-azetidin-1-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-benzonitril4-[2-(4-dimetylamino-piperidin-1-yl)-1-metyl-5-(2-metyl-2H-indazol-5-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-dimetylamino-piperidin-1-yl)-1-metyl-5-(1-metyl-1H-indazol-5-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(1H-indol-5-yl)-1-metyl-6-okso-1,6-dihydropyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-1-metyl-5-(1-metyl-1H-indol-5-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(1H-indol-6-yl)-1-metyl-6-okso-1,6-dihydropyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-1-metyl-5-(1-metyl-1H-indol-6-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(1H-indazol-6-yl)-1-metyl-6-okso-1,6-dihydropyrimidin-4-yl]-2-fluor-benzonitril4-[2-((4R, 3S)-4-amino-3-fluor-piperidin-1-yl)-5-(4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-((4S, 3R)-4-amino-3-fluor-piperidin-1-yl)-5-(4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-dimetylamino-piperidin-1-yl)-1-metyl-5-(2-metyl-2H-indazol-6-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2'-dimetylamino-2-(4-dimetylamino-piperidin-1-yl)-1-metyl-6-okso-1,6-dihydro-[5,5']bipyrimidinyl-4-yl]-2-fluor-benzonitril4-[2-(4-dimetylamino-piperidin-1-yl)-1-metyl-5-(6-metyl-pyridin-3-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[5-(6-dimetylamino-pyridin-3-yl)-1-metyl-2-(4-metylamino-piperidin-1-yl)-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-dimetylamino-piperidin-1-yl)-5-(2H-indazol-6-yl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluor-4-metoksy-fenyl)-1-deuterert metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-5-(3-fluor-4-deuterert metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril2-fluor-4-[1-metyl-2-[4-(metylamino)piperidin-1-yl]-5-(1-metylindazol-5-yl)-6-oksopyrimidin-4-yl]benzonitril4-[2-(4-aminopiperidin-1-yl)-5-(1H-indazol-5-yl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[5-(4-aminofenyl)-2-(4-aminopiperidin-1-yl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-1-metyl-5-[4-(metylamino)fenyl]-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-[3-fluor-4-(metylamino)fenyl]-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-[4-(dimetylamino)piperidin-1-yl]-5-(6-metoksypyridin-3-yl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-(6-etoksy-5-fluorpyridin-3-yl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-(6-etoksypyridin-3-yl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-(4-etoksyfenyl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-[4-(2-hydroksyetoksy)fenyl]-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-[4-(2-hydroksyetoksy)fenyl]-1-metyl-6-oksopyrimidin-4-yl]benzonitril4-[2-(4-aminopiperidin-1-yl)-5-[4-(2-metoksyetoksy)fenyl]-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-[4-(2-hydroksyetyl)fenyl]-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-[4-(hydroksymetyl)fenyl]-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril 4-[2-(4-aminopiperidin-1-yl)-5-(4-fluorfenyl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-(3-fluorfenyl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-(3,5-difluorfenyl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-(3,4-difluorfenyl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-1-metyl-5-(4-metylsulfonylfenyl)-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-(4-klorfenyl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-5-[4-(metoksymetyl)fenyl]-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril4-[2-(4-aminopiperidin-1-yl)-1-metyl-6-oksopyrimidin-4-yl]-2-fluorbenzonitril 4-[2-(4-amino-piperidin-1-yl)-1-syklopropylmetyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril4-[2-(4-amino-piperidin-1-yl)-1-syklopropylmetyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril2-(4-amino-piperidin-1-yl)-4-(4-cyano-3-fluor-fenyl)-1 -metyl-6-okso-1,6-dihydro-pyrimidin-5-karbonitril4-[2-(4-aminopiperidin-1-yl)-5-(4-metoksyfenyl)-6-okso-1H-pyrimidin-4-yl]-2-fluorbenzonitrileller farmasøytisk akseptabelt salt derav.15. Forbindelsen ifølge krav 1, eller et farmasøytisk akseptabelt salt derav, som har den følgende strukturen:4-[2-(4-amino-piperidin-1-yl)-5-(3-fluor-4-metoksy-fenyl)-1-metyl-6-okso-1,6-dihydro-pyrimidin-4-yl]-2-fluor-benzonitril.16. Farmasøytisk sammensetning omfattende en forbindelse av formel (I), ifølge krav 1, eller et farmasøytisk akseptabelt salt derav, og en farmasøytisk akseptabel eksipiens.17. Forbindelsen av formel (I) eller et farmasøytisk akseptabelt salt derav, eller den farmasøytiske sammensetningen ifølge krav 16 for anvendelse som et medikament.18. Forbindelsen av formel (I) eller et farmasøytisk akseptabelt salt derav, eller den farmasøytiske sammensetningen ifølge krav 16 for anvendelse som et medikament for behandling av kreft.19. Forbindelsen eller et farmasøytisk akseptabelt salt derav, for anvendelse ifølge krav 18, hvori kreften er akutt myelogen leukemi (AML), prostatakreft og brystkreft.20. Forbindelse av formel (I), ifølge krav 1 eller et farmasøytisk akseptabelt salt derav, for anvendelse som et medikament for behandling av akutt myelogen leukemi AML , hvori forbindelsen har strukturen til:21. Forbindelse av formel (I), ifølge krav 1 eller et farmasøytisk akseptabelt salt derav, for anvendelse som et medikament for behandling av prostatakreft hvori forbindelsen har strukturen til:22. Forbindelse av formel (I), ifølge krav 1 eller et farmasøytisk akseptabelt salt derav, for anvendelse som et medikament for behandling av brystkreft hvori forbindelsen har strukturen til:
Hva betyr A1, B, B1, C osv? info
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Org.nummer: 982702887
Din referanse: V436698NO00
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2014.05.01, US 201461987354 P

HAN, H ET AL.: 'Synergistic Re-Activation of Epigenetically Silenced Genes by Combinatorial Inhibition of DNMTs and LSD1 in Cancer Cells.' PLOS ONE. vol. 8, no. 9, 2013, page E75136, XP055235759 (B1)

None (B1)

US-B2- 7 767 669 (B1)

US-A1- 2010 048 591 (B1)

US-B2- 7 037 918 (B1)

US-A1- 2004 242 608 (B1)

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Årsavgift 11. avg. år (EP) 4550,0 Forsinkelsesavgift patent 700,0 Totalbeløp 5250,0   Gå til betaling
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Årsavgift 10. avg. år (EP) 2024.04.09 4160 CPA GLOBAL LIMITED Betalt og godkjent
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32202241 expand_more 2022.02.11 5500 ZACCO NORWAY AS Betalt
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Hva betyr A1, B, B1, C osv? info
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