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Tittel BIARYL KINASE INHIBITORS
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I kraft info EP patent gjort gjeldende i Norge EP patent besluttet gjeldende i Norge
Patentnummer NO/EP3126351
Europeisk (EP) publiserings nummer EP3126351
EP levert
EP søknadsnummer 15717342.8
EP meddelt
Prioritet 2014.04.02, US 201461973942 P, .... se mer/flere nedenfor
Sakstype Europeisk
Løpedag
Utløpsdato
Allment tilgjengelig
Validert i Norge
Innehaver Bristol-Myers Squibb Company (US)
Oppfinner LUO, Guanglin (US) .... se mer/flere nedenfor
Fullmektig ZACCO NORWAY AS (NO)
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Patentkrav1. Forbindelse med formel (I)eller et farmasøytisk akseptabelt salt derav, hvori:A er valgt blantoghvori "" betegner festepunktet til B;B er valgt blanthvori "*" betegner festepunktet til R5 og "**" betegner festepunktet til ring A;R1 er valgt blant hydrogen, amino, -CO2H, difluormetyl, etyl, halogen, hydroksymetyl, metoksy, metyl, -NHC(O)CH3, -NHCO2CH3, trifluormetoksy, og trifluormetyl;R2 er valgt blant hydrogen, cyano, -CH2OH, halogen og metyl;R2 er valgt blant hydrogen, cyano, syklopropyl, difluormetyl, halogen, hydroksymetyl, metoksy, metyl, metylsulfonyl, trifluormetoksy, trifluormetyl, -CH2N(CH3)2 og en femleddet aromatisk ring som inneholder ett, to, eller tre heteroatomer valgt blant nitrogen, oksygen og svovel;R4 er valgt blant hydrogen, halogen og metyl; R5 er valgt blantR6 er valgt blant hydrogen, etyl, fluormetyl, difluormetyl, metyl og trifluormetyl; og R7 er metyl.2. Forbindelse ifølge krav 1, eller et farmasøytisk akseptabelt salt derav, hvori A er valgt blant3. Forbindelse ifølge krav 1, eller et farmasøytisk akseptabelt salt derav, hvori B er valgt blant4. Forbindelse ifølge krav 3, eller et farmasøytisk akseptabelt salt derav, hvori B er5. Forbindelse ifølge krav 1, hvori R5 er6. Forbindelse ifølge krav 1, valgt blant(S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3-fluorfenyl)pyridin-2-yl)acetamid;(S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3-metoksyfenyl)pyridin-2-yl)acetamid; (S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3-cyanofenyl)pyridin-2-yl)acetamid;(S)-2-((2-amino-4-metylpentyl)oksy)-5-(2-aminopyridin-4-yl)benzonitril;(S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3-(trifluormetyl)fenyl)pyridin-2-yl)acetamid; (S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3-(trifluormetoksy)fenyl)pyridin-2-yl)acetamid; (S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3-metylfenyl)pyridin-2-yl)acetamid;(S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3-klorfenyl)pyridin-2-yl)acetamid;(S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3,5-difluorfenyl)pyridin-2-yl)acetamid; (S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3-klor-5-fluorfenyl)pyridin-2-yl)acetamid; (S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3-fluor-5-(trifluormetyl)fenyl)pyridin-2-yl)acetamid;(S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-2,5-difluorfenyl)pyridin-2-yl)acetamid; (S)-metyl (4-(4-((2-amino-4-metylpentyl)oksy)-3-fluorfenyl)pyridin-2-yl)karbamat; (S)-metyl (4-(4-((2-amino-4-metylpentyl)oksy)-3-(isoksazol-5-yl)fenyl)pyridin-2-yl)karbamat;(S)-2-((2-amino-4-metylpentyl)oksy)-5-(2-metylpyridin-4-yl)benzonitril;(S)-2-((2-amino-4-metylpentyl)oksy)-5-(2-metoksypyridin-4-yl)benzonitril;(S)-2-((2-amino-4-metylpentyl)oksy)-5-(2-(trifluormetyl)pyridin-4-yl)benzonitril;(S)-1-(2-(isoksazol-5-yl)-4-(2-metylpyridin-4-yl)fenoksy)-4-metylpentan-2-amin;(S)-N-(4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(trifluormetyl)fenyl)pyridin-2-yl)acetamid;(S)-metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(trifluormetyl)fenyl)pyridin-2-yl)karbamat;(S)-N-(4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-cyanofenyl)pyridin-2-yl)acetamid; (S)-metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-cyanofenyl)pyridin-2-yl)karbamat; (S)-N-(4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(difluormetyl)fenyl)pyridin-2-yl)acetamid;(S)-metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(difluormetyl)fenyl)pyridin-2-yl)karbamat;(S)-N-(4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(trifluormetoksy)fenyl)pyridin-2-yl)acetamid;(S)-metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(trifluormetoksy)fenyl)pyridin-2-yl)karbamat;(S)-N-(4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-fluorfenyl)pyridin-2-yl)acetamid; (S)-metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-fluorfenyl)pyridin-2-yl)karbamat; metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-klorfenyl)pyridin-2-yl)karbamat; metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-metylfenyl)pyridin-2-yl)karbamat; metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-2,3-dimetylfenyl)pyridin-2-yl)karbamat; (S)-metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(hydroksymetyl)fenyl)pyridin-2-yl)karbamat;(S)-metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-syklopropylfenyl)pyridin-2-yl)karbamat; (S)-N-(4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(trifluormetyl)fenyl)-5-(hydroksymetyl)pyridin-2-yl)acetamid;(S)-1-(4-(2-(difluormetyl)pyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(2-(difluormetyl)pyridin-4-yl)benzonitril; (S)-1-(2-(difluormetyl)-4-(2-(difluormetyl)pyridin-4-yl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-1-(4-(2-(difluormetyl)pyridin-4-yl)-2-(trifluormetoksy)fenoksy)-2,4-dimetylpentan-2-amin;(S)-1-(4-(3-klor-2-fluorpyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-1-(4-(5-klor-2-fluorpyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-1-(4-(2-fluor-3-metylpyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-1-(4-(2,3-difluorpyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin; (S)-2,4-dimetyl-1-(4-(pyridin-4-yl)-2-(trifluormetyl)fenoksy)pentan-2-amin;(S)-1-(4-(2-fluorpyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-2,4-dimetyl-1-(4-(2-metylpyridin-4-yl)-2-(trifluormetyl)fenoksy)pentan-2-amin; (S)-1-(4-(3-metoksypyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin; (S)-1-(4-(3-fluorpyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(2-metylpyridin-4-yl)benzonitril;(S)-1-(2-syklopropyl-4-(2-metylpyridin-4-yl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-1-(2-(difluormetyl)-4-(2-metylpyridin-4-yl)fenoksy)-2,4-dimetylpentan-2-amin; Metyl-(6-((2-amino-2,4-dimetylpentyl)oksy)-[3,4'-bipyridin]-2'-yl)karbamat;(S)-metyl-(6-((2-amino-2,4-dimetylpentyl)oksy)-5-metyl-[3,4'-bipyridin]-2'-yl)karbamat;(S)-metyl-(6-((2-amino-2,4-dimetylpentyl)oksy)-5-cyano-[3,4'-bipyridin]-2'-yl)karbamat;(S)-metyl-(6-((2-amino-2,4-dimetylpentyl)oksy)-4-metyl-[3,4'-bipyridin]-2'-yl)karbamat;(S)-metyl-(6-((2-amino-2,4-dimetylpentyl)oksy)-5-klor-[3,4'-bipyridin]-2'-yl)karbamat; (S)-metyl-(6-((2-amino-2,4-dimetylpentyl)oksy)-5-metoksy-[3,4'-bipyridin]-2'-yl)karbamat;(S)-1-((2'-klor-5-metyl-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((2'-(difluormetyl)-5-metyl-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-6-((2-amino-2,4-dimetylpentyl)oksy)-2'-(difluormetyl)-[3,4'-bipyridin]-5-karbonitril; (S)-1-((5-klor-2'-metyl-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2',5-dimetyl-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((5-metoksy-2'-metyl-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin; Metyl-(5-((2-amino-2,4-dimetylpentyl)oksy)-[2,4'-bipyridin]-2'-yl)karbamat;(S)-metyl-(5-((2-amino-2,4-dimetylpentyl)oksy)-6-metyl-[2,4'-bipyridin]-2'-yl)karbamat;(S)-1-((2',6-dimetyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-metyl-(5-((2-amino-2,4-dimetylpentyl)oksy)-6-klor-[2,4'-bipyridin]-2'-yl)karbamat; (S)-1-((6-klor-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-metyl-(5-((2-amino-2,4-dimetylpentyl)oksy)-4-metyl-[2,4'-bipyridin]-2'-yl)karbamat;(S)-2,4-dimetyl-1-(4-(kinolin-4-yl)-2-(trifluormetyl)fenoksy)pentan-2-amin;(S)-2,4-dimetyl-1-(2-(trifluormetyl)-4-(7-(trifluormetyl)kinolin-4-yl)fenoksy)pentan-2-amin;(S)-1-(4-(7-fluorkinolin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin; (S)-1-(4-(5,7-difluorkinolin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin; (S)-1-(4-(6-fluorkinolin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin; (S)-1-(2-syklopropyl-4-(kinolin-4-yl)fenoksy)-2,4-dimetylpentan-2-amin;1-(2-klor-6-fluor-4-(kinolin-4-yl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-1-((5-(7-fluorkinolin-4-yl)-3-metylpyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(5,7-difluorkinolin-4-yl)nikotinonitril;(S)-1-((3-klor-5-(kinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((3-metoksy-5-(kinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(1,6-naftyridin-4-yl)nikotinonitril;(S)-2,4-dimetyl-1-((2-metyl-6-(kinolin-4-yl)pyridin-3-yl)oksy)pentan-2-amin;(S)-2,4-dimetyl-1-((4-metyl-6-(kinolin-4-yl)pyridin-3-yl)oksy)pentan-2-amin;(S)-1-((2-klor-6-(kinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-(4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-1-(4-(1,6-naftyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin; (S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(1,6-naftyridin-4-yl)benzonitril;(S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(1,5-naftyridin-4-yl)benzonitril;(S)-1-(4-(7-klorkinolin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(trifluormetyl)fenyl)kinolin-7-karbonitril; (S)-2,4-dimetyl-1-(2-metyl-4-(2-metylpyridin-4-yl)fenoksy)pentan-2-amin;(S)-1-(2-fluor-4-(2-metylpyridin-4-yl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-1-(4-(2-fluorpyridin-4-yl)-2-metylfenoksy)-2,4-dimetylpentan-2-amin;(S)-1-(2-fluor-4-(2-fluorpyridin-4-yl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(2-fluorpyridin-4-yl)benzonitril; (S)-1-((2'-fluor-5-metyl-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-4-(6-((2-amino-2,4-dimetylpentyl)oksy)-5-metylpyridin-3-yl)kinolin-7-karbonitril; (S)-1-((5-fluor-2'-metyl-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((3-fluor-5-(kinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-4-(6-((2-amino-2,4-dimetylpentyl)oksy)-5-fluorpyridin-3-yl)kinolin-7-karbonitril; (S)-metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-cyanofenyl)-3-fluorpyridin-2-yl)karbamat;(S)-6-((2-amino-2,4-dimetylpentyl)oksy)-2'-metyl-[3,4'-bipyridin]-5-karbonitril;(S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(7-metylkinolin-4-yl)benzonitril;(S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(3-fluor-2-metylpyridin-4-yl)benzonitril; (S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(kinolin-4-yl)benzonitril;(S)-2-((2-amino-2,4-dimetylpentyl)oksy)-5-(5-fluor-2-metylpyridin-4-yl)benzonitril; (S)-metyl (4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-cyanofenyl)-5-fluorpyridin-2-yl)karbamat;(S)-1-((6-fluor-2',4-dimetyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;Metyl-(5-((3-isobutylazetidin-3-yl)metoksy)-6-metyl-[2,4'-bipyridin]-2'-yl)karbamat; (S)-2-((2-amino-4-metylpentyl)oksy)-5-(6-metylpyridazin-4-yl)benzonitril;(S)-1-(2-(isoksazol-5-yl)-4-(kinolin-4-yl)fenoksy)-4-metylpentan-2-amin;(S)-4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(trifluormetyl)fenyl)-2-metylnikotinsyre; (S)-metyl(4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-((dimetylamino)metyl)fenyl)pyridin-2-yl)karbamat;(S)-metyl(4-(4-((2-amino-2,4-dimetylpentyl)oksy)-3-(metylsulfonyl)fenyl)pyridin-2-yl)karbamat;(S)-2,4-dimetyl-1-(4-(2-metylpyridin-4-yl)-2-(metylsulfonyl)fenoksy)pentan-2-amin; (S)-2,4-dimetyl-1-(2-(metylsulfonyl)-4-(kinolin-4-yl)fenoksy)pentan-2-amin;(S)-1-(2-(difluormetyl)-4-(6-fluorkinolin-4-yl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-metyl-(5-((2-amino-2,4-dimetylpentyl)oksy)-6-(difluormetyl)-[2,4'-bipyridin]-2'-yl)karbamat;(S)-1-((2-(difluormetyl)-6-(kinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((6-(difluormetyl)-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-metyl-(5-((2-amino-2,4-dimetylpentyl)oksy)-4-(difluormetyl)-[2,4'-bipyridin]-2'-yl)karbamat;(S)-1-((4-(difluormetyl)-6-(kinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((4-(difluormetyl)-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2',6-bis(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2',4-bis(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2'-(difluormetyl)-4-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-(2-syklopropyl-4-(2-(difluormetyl)pyridin-4-yl)fenoksy)-2,4-dimetylpentan-2-amin; (S)-1-((2-(difluormetyl)-6-(6-fluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((2-(difluormetyl)-6-(7-fluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((2-(difluormetyl)-6-(5,7-difluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-(difluormetyl)-6-(5,7-difluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-(difluormetyl)-6-(7-fluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-(difluormetyl)-6-(6-fluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;((S)-1-((4-(difluormetyl)-6-(6-(trifluormetyl)kinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-(difluormetyl)-6-(6-(trifluormetoksy)kinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((2-klor-6-(5,7-difluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2-klor-6-(7-fluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((6-(7-fluorkinolin-4-yl)-2-metylpyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((6-(6-fluorkinolin-4-yl)-2-metylpyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2-(difluormetyl)-6-(2-metylpyrimidin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((2-(difluormetyl)-6-(6-metylpyrimidin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-(difluormetyl)-2'-etyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2'-klor-4-(difluormetyl)-3'-fluor-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((2'-klor-4-(difluormetyl)-5'-fluor-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-2,4-dimetyl-1-((2'-metyl-4-(trifluormetyl)-[2,4'-bipyridin]-5-yl)oksy)pentan-2-amin; (S)-2,4-dimetyl-1-((6-(kinolin-4-yl)-4-(trifluormetyl)pyridin-3-yl)oksy)pentan-2-amin; (S)-metyl(5-((2-amino-2,4-dimetylpentyl)oksy)-4-(trifluormetyl)-[2,4'-bipyridin]-2'-yl)karbamat;(S)-1-((2'-klor-4-(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((4-(difluormetyl)-5'-fluor-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-(difluormetyl)-3'-fluor-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((4-(difluormetyl)-6-(2-metylpyrimidin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-(2-(difluormetyl)-4-(2-metylpyrimidin-4-yl)fenoksy)-2,4-dimetylpentan-2-amin; (S)-5-((2-amino-2,4-dimetylpentyl)oksy)-3'-fluor-6-metyl-[2,4'-bipyridin]-2'-amin ; (S)-1-((2'-klor-3'-fluor-6-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-metyl(5-((2-amino-2,4-dimetylpentyl)oksy)-5'-fluor-6-metyl-[2,4'-bipyridin]-2'-yl)karbamat;(S)-1-((2'-klor-5'-fluor-6-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-metyl (5-((2-amino-2,4-dimetylpentyl)oksy)-3'-fluor-6-metyl-[2,4'-bipyridin]-2'-yl)karbamat;(S)-1-((2'-klor-6-(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2'-klor-6-(difluormetyl)-3'-fluor-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((6-(difluormetyl)-3'-fluor-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;((S)-1-((6-klor-2'-(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((4-(difluormetyl)-6-(6-metylpyridazin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((2-(difluormetyl)-6-(6-metylpyridazin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(R)-2,4-dimetyl-1-((2'-metyl-4-(trifluormetyl)-[2,4'-bipyridin]-5-yl)oksy)pentan-2-amin; (R)-2,4-dimetyl-1-((6-(kinolin-4-yl)-4-(trifluormetyl)pyridin-3-yl)oksy)pentan-2-amin; (R)-metyl-(5-((2-amino-2,4-dimetylpentyl)oksy)-4-(trifluormetyl)-[2,4'-bipyridin]-2'-yl)karbamat;(R)-1-((2'-klor-4-(difluormetyl)-3'-fluor-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(R)-1-((2'-klor-4-(difluormetyl)-5'-fluor-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(R)-1-((2'-klor-4-(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (R)-1-((4-(difluormetyl)-2'-etyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (R)-1-((4-(difluormetyl)-5'-fluor-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(R)-1-((4-(difluormetyl)-3'-fluor-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(R)-metyl (5-((2-amino-2,4-dimetylpentyl)oksy)-6-metyl-[2,4'-bipyridin]-2'-yl)karbamat; (R)-1-((2',6-bis(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (R)-1-((2',4-bis(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-metyl-(4-(difluormetyl)-5-((2-hydroksy-2,4-dimetylpentyl)oksy)-[2,4'-bipyridin]-2'-yl)karbamat;(S)-1-((4-(difluormetyl)-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-ol; (S)-metyl-(5-((2-amino-2-(fluormetyl)-4-metylpentyl)oksy)-6-(difluormetyl)-[2,4'-bipyridin]-2'-yl)karbamat;(R)-metyl-(5-((2-amino-2-(fluormetyl)-4-metylpentyl)oksy)-6-(difluormetyl)-[2,4'-bipyridin]-2'-yl)karbamat;(S)-metyl-(5-((2-amino-2-(fluormetyl)-4-metylpentyl)oksy)-4-(difluormetyl)-[2,4'-bipyridin]-2'-yl)karbamat;(R)-metyl-(5-((2-amino-2-(fluormetyl)-4-metylpentyl)oksy)-4-(difluormetyl)-[2,4'-bipyridin]-2'-yl)karbamat;(S)-1-((2',6-bis(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2-(fluormetyl)-4-metylpentan-2-amin;(S)-1-((2',4-bis(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2-(fluormetyl)-4-metylpentan-2-amin;(R)-1-((2',6-bis(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2-(fluormetyl)-4-metylpentan-2-amin;(R)-1-((2',4-bis(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2-(fluormetyl)-4-metylpentan-2-amin;(S)-1-((4-(difluormetyl)-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2-(fluormetyl)-4-metylpentan-2-amin;(R)-1-((4-(difluormetyl)-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2-(fluormetyl)-4-metylpentan-2-amin;(S)-N-(4-(4-((2-amino-4-metylpentyl)oksy)-3-fluorfenyl)pyridin-2-yl)acetamid;(S)-1-((3-klor-5-(7-fluorkinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((3-klor-5-(6-fluorkinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((3-klor-5-(2-metylpyrimidin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2'-klor-5-(difluormetyl)-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((5-(difluormetyl)-2'-metyl-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((3-(difluormetyl)-5-(7-fluorkinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-metyl-(6-((2-amino-2,4-dimetylpentyl)oksy)-5-(difluormetyl)-[3,4'-bipyridin]-2'-yl)karbamat;(S)-1-((5-(7-klorkinolin-4-yl)-3-(difluormetyl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((3-(difluormetyl)-5-(2-metylpyrimidin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((2',5-bis(difluormetyl)-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((3-(difluormetyl)-5-(6-fluorkinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((3-(difluormetyl)-5-(5,7-difluorkinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((3-(difluormetyl)-5-(7-(trifluormetyl)kinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((5-(difluormetyl)-2',3'-dimetyl-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((3-(difluormetyl)-5-(kinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((3-(difluormetyl)-5-(7-metylkinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-metyl-(5-((2-amino-2,4-dimetylpentyl)oksy)-4-metoksy-[2,4'-bipyridin]-2'-yl)karbamat;(S)-1-((2'-(difluormetyl)-4-metoksy-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-metyl-(4-(4-((2-amino-2,4-dimetylpentyl)oksy)naftalen-1-yl)pyridin-2-yl)karbamat; (S)-2,4-dimetyl-1-((4-(kinolin-4-yl)naftalen-1-yl)oksy)pentan-2-amin;(S)-metyl-(4-(5-((2-amino-2,4-dimetylpentyl)oksy)pyrimidin-2-yl)pyridin-2-yl)karbamat; (S)-metyl-(4-(2-((2-amino-2,4-dimetylpentyl)oksy)pyrimidin-5-yl)pyridin-2-yl)karbamat; (S)-2,4-dimetyl-1-((2',4,6-trimetyl-[2,4'-bipyridin]-5-yl)oksy)pentan-2-amin;(S)-metyl(5-((2-amino-2,4-dimetylpentyl)oksy)-4,6-dimetyl-[2,4'-bipyridin]-2'-yl)karbamat;(S)-2,4-dimetyl-1-(4-(kinazolin-4-yl)-2-(trifluormetyl)fenoksy)pentan-2-amin;(S)-1-(4-(3,6-dihydro-2H-pyran-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-2,4-dimetyl-1-(4-(2-metylkinolin-4-yl)-2-(trifluormetyl)fenoksy)pentan-2-amin; (S)-1-(4-(6-klorkinolin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-1-((5-(5,7-difluorkinolin-4-yl)-3-(trifluormetyl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-2,4-dimetyl-1-((5-(kinolin-4-yl)-3-(trifluormetyl)pyridin-2-yl)oksy)pentan-2-amin; (S)-metyl (6-((2-amino-2,4-dimetylpentyl)oksy)-5-(trifluormetyl)-[3,4'-bipyridin]-2'-yl)karbamat;(S)-2,4-dimetyl-1-((2'-metyl-5-(trifluormetyl)-[3,4'-bipyridin]-6-yl)oksy)pentan-2-amin; (S)-1-((5-(6-klorkinolin-4-yl)-3-metylpyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((5-(6-fluorkinolin-4-yl)-3-metylpyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((5-(5,7-difluorkinolin-4-yl)-3-metylpyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((5-(7-klorkinolin-4-yl)-3-metylpyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((6-(5,7-difluorkinolin-4-yl)-4-metylpyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((6-(7-fluorkinolin-4-yl)-4-metylpyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2',4-dimetyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((6-(6-klorkinolin-4-yl)-4-metylpyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((6-(6-fluorkinolin-4-yl)-4-metylpyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((6-(7-klorkinolin-4-yl)-4-metylpyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((6-(7-fluorkinolin-4-yl)-4-metylpyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((4-klor-6-(5,7-difluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((4-klor-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-klor-6-(6-fluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-klor-6-(kinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-metyl-(5-((2-amino-2,4-dimetylpentyl)oksy)-4-klor-[2,4'-bipyridin]-2'-yl)karbamat; (S)-1-((4-klor-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-klor-6-(6-klorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((2',4-diklor-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-klor-6-(7-fluorkinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-klor-6-(7-(trifluormetyl)kinolin-4-yl)pyridin-3-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((4-klor-2',3'-dimetyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((5-(difluormetyl)-2'-metyl-[3,4'-bipyridin]-6-yl)oksy)-2,4-dimetylpentan-2-amin; (R)-metyl (6-((2-amino-2,4-dimetylpentyl)oksy)-5-(difluormetyl)-[3,4'-bipyridin]-2'-yl)karbamat;(R)-1-((3-(difluormetyl)-5-(kinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin; (R)-1-((3-(difluormetyl)-5-(2-metylpyrimidin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;(R)-1-((3-(difluormetyl)-5-(5,7-difluorkinolin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin; og(R)-1-((5-(7-klorkinolin-4-yl)-3-(difluormetyl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin;eller et farmasøytisk akseptabelt salt derav.7. Forbindelse ifølge krav 6 valgt blant(S)-1-(4-(2-(difluormetyl)pyridin-4-yl)-2-(trifluormetyl)fenoksy)-2,4-dimetylpentan-2-amin;(S)-2,4-dimetyl-1-(4-(2-metylpyridin-4-yl)-2-(trifluormetyl)fenoksy)pentan-2-amin; (S)-metyl (5-((2-amino-2,4-dimetylpentyl)oksy)-6-metyl-[2,4'-bipyridin]-2'-yl)karbamat; (S)-1-((4-(difluormetyl)-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-1-((2',6-bis(difluormetyl)-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; (S)-2,4-dimetyl-1-((2'-metyl-4-(trifluormetyl)-[2,4'-bipyridin]-5-yl)oksy)pentan-2-amin; (S)-1-((4-(difluormetyl)-3'-fluor-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((6-(difluormetyl)-3'-fluor-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin;(S)-1-((3-(difluormetyl)-5-(2-metylpyrimidin-4-yl)pyridin-2-yl)oksy)-2,4-dimetylpentan-2-amin; og(S)-1-((4-klor-2'-metyl-[2,4'-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; eller et farmasøytisk akseptabelt salt derav.8. Forbindelse med formel (II)eller et farmasøytisk akseptabelt salt derav, hvori:A er valgt blanthvori "" betegner festepunktet til B;B er valgt blant fenyl og pyridinyl;R1 er valgt blant hydrogen, difluormetyl, halogen, metoksy, metyl, -NHC(O)CH3, -NHCO2CH3, og trifluormetyl;R2 er valgt blant hydrogen, -CH2OH og halogen;R3 er valgt blant hydrogen, cyano, syklopropyl, difluormetyl, halogen, hydroksymetyl, metoksy, metyl, trifluormetoksy, trifluormetyl, og en fem-leddet aromatisk ring som inneholder ett, to eller tre heteroatomer valgt blant nitrogen, oksygen og svovel;R4 er valgt blant hydrogen, halogen og metyl; ogR5 er valgt blant hydrogen, etyl, fluormetyl, difluormetyl, metyl og trifluormetyl.9. Forbindelse ifølge krav 7, som er (S)-1-((2’,6-bis(difluormetyl)-[2,4’-bipyridin]-5-yl)oksy)-2,4-dimetylpentan-2-amin; eller et farmasøytisk akseptabelt salt derav. 10. Sammensetning som omfatter en farmasøytisk akseptabel mengde av en forbindelse ifølge et hvilket som helst av kravene 1 til 9, eller et farmasøytisk akseptabelt salt derav og en farmasøytisk akseptabel bærer.11. Forbindelse ifølge et hvilket som helst av kravene 1 til 9, eller et farmasøytisk akseptabelt salt derav for anvendelse i behandling eller håndtering av en sykdom eller en forstyrrelse mediert av AAK1-aktivitet.12. Forbindelsen eller det farmasøytisk akseptable saltet derav for anvendelse ifølge krav 11, hvori sykdommen eller forstyrrelsen er valgt blant Alzheimers sykdom, bipolar lidelse, smerte, Parkinsons sykdom og schizofreni.13. Forbindelsen eller det farmasøytisk akseptable saltet derav for anvendelse ifølge krav 12, hvori smerten er nevropatisk smerte.14. Forbindelsen eller det farmasøytisk akseptable saltet derav for anvendelse ifølge krav 13, hvori den nevropatiske smerten er fibromyalgi eller perifer nevropati.
Hva betyr A1, B, B1, C osv? info
Innehaver i EP:
Bristol-Myers Squibb Company
Route 206 and Province Line Road Princeton, NJ 08543 US
c/o Bristol-Myers Squibb Company5 Research Parkway Wallingford, Connecticut 06492 US
c/o Bristol-Myers Squibb CompanyRoute 206 and Province Line Road Princeton, New Jersey 08648 US
c/o Bristol-Myers Squibb Company5 Research Parkway Wallingford, Connecticut 06492 US
c/o Bristol-Myers Squibb Company5 Research Parkway Wallingford, Connecticut 06492 US
c/o Bristol-Myers Squibb CompanyRoute 206 and Province Line Road Princeton, New Jersey 08543 US
c/o Bristol-Myers Squibb Company5 Research Parkway Wallingford, Connecticut 06492 US
Fullmektig i Norge:
ZACCO NORWAY AS
Postboks 488 0213 OSLO NO ( OSLO kommune, Oslo fylke )

Org.nummer: 982702887
Din referanse: V6616NO00
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Kilde: Brønnøysundregistrene
Fullmektig i EP:
Kling, Edouard
Swords Laboratories, Ireland Swiss Branch, Steinhausen Hinterbergstrasse 16 6312 Steinhausen CH

2014.04.02, US 201461973942 P

2014.10.08, US 201462061591 P

US-A1- 2014 038 999 (B1)

WO-A2-2013/134336 (B1)

WO-A1-2004/041810 (B1)

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04-01 Via Altinn-sending EP Varsel om betaling av første årsavgift (3319) (PTEP3126351)
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05-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Utgående EP Registreringsbrev (3210) (PTEP3126351)
03-01 Brev UT EP Registreringsbrev (3210) (PTEP3126351)
Innkommende, AR289539575 Søknadsskjema Patent
01-01 Søknadsskjema Patent Søknadsskjema Patent
01-02 Fullmakt Fullmakt
01-03 EP oversettelse EP krav
Innkommende EP Publiseringsdokument fra EPO
02-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO

Til betaling:

Betalingshistorikk:

Liste av betalinger
Beskrivelse / Fakturanummer Betalingsdato Beløp Betaler Status
Årsavgift 11. avg. år (EP) expand_more 2025.04.09 4550,0 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 10. avg. år (EP) 2024.04.09 4160 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 9. avg. år (EP) 2023.04.12 2850 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 8. avg. år (EP) 2022.04.11 2550 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 7. avg. år (EP) 2021.04.09 2200 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 6. avg. år (EP) 2020.04.14 2000 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 5. avg. år (EP) 2019.04.09 1650 CPA GLOBAL LIMITED Betalt og godkjent
31819652 expand_more 2018.12.27 5500 TANDBERG INNOVATION AS Betalt
Denne oversikten kan mangle informasjon, spesielt for eldre saker, om tilbakebetaling, internasjonale varemerker og internasjonale design.

Lenker til publikasjoner og Norsk Patenttidende (søkbare tekstdokumenter)

Allment tilgjengelig patentsøknad
Hva betyr A1, B, B1, C osv? info
Kapitler uten data er fjernet. Melding opprettet: 01.05.2025 08:11:37