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Tittel COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS
Status
Hovedstatus
Detaljstatus 		I kraft info EP patent gjort gjeldende i Norge EP patent besluttet gjeldende i Norge
Patentnummer NO/EP2948461
Europeisk (EP) publiserings nummer EP2948461
EP levert
EP søknadsnummer 14702642.1
EP meddelt
Prioritet 2013.01.23, US 201361755537 P, .... se mer/flere nedenfor
Sakstype Europeisk
Løpedag
Utløpsdato
Allment tilgjengelig
Validert i Norge
Innehaver Entasis Therapeutics Limited (GB)
Oppfinner BASARAB, Gregory, Steven (US) .... se mer/flere nedenfor
Fullmektig ZACCO NORWAY AS (NO)
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Patentkrav1. Forbindelse eller farmasøytisk akseptabelt salt derav, hvori forbindelsen har strukturen i formel (I):hvori:X er fluor eller klor;R1 velges fra gruppen bestående av hydrogen, fenyl, -C=N, tetrahydropyranyl, N-metyl-1,2,4-triazolyl, pyrimidinyl, pyridinyl, pyrazinyl, syklopropyl, -C=CH, -CH=CH2 og C1-C3 alkyl, hvor C1-C3 alkyl eventuelt substitueres med én eller flere av: -OR10, halogen, -C≡N, -N3, -SO2CH3, -SCH3, -CH=CH2, -CH=NOR11 og fenyl;R2 velges fra gruppen bestående av hydrogen, -C=N, pyridinyl, C1-C3 alkyl, hvor C1-C3 alkyl eventuelt substitueres med én eller flere av: halogen, -OR20 og -CH=NOR21;R3 er hydrogen eller C1-C3 alkyl;R10 velges i hvert tilfelle uavhengig fra gruppen bestående av hydrogen, C1-C4 alkyl og -(CH2)2OCH3; ogR11, R20 og R21 er i hvert tilfelle uavhengig hydrogen eller C1-C4 alkyl.2. Forbindelsen eller farmasøytisk akseptabelt salt derav, ifølge krav 1, hvori R10 er hydrogen, metyl, etyl eller -(CH2)2OCH3.3. Forbindelsen eller farmasøytisk akseptabelt salt derav, ifølge krav 1 eller 2, hvori R11 er hydrogen eller metyl.4. Forbindelsen eller farmasøytisk akseptabelt salt derav, ifølge hvilket som helst av kravene 1– 3, hvori R20 er hydrogen, metyl eller etyl.5. Forbindelsen eller farmasøytisk akseptabelt salt derav, ifølge hvilket som helst av kravene krav 1–4, hvori R21 er hydrogen eller metyl.6. Forbindelsen eller farmasøytisk akseptabelt salt derav, ifølge hvilket som helst av kravene krav 1–5, hvori R1 velges fra gruppen bestående av hydrogen, metyl, etyl, fenyl, -CH2-fenyl, -CH2F, -CH2OCH3, -CH2CH=CH2, tetrahydropyranyl, -(CH2)3OH, -(CH2)3F, -(CH2)3OH, -(CH2)3F, -CH=CH2, -C≡N, -CH=NOCH3, -CH2SCH3, -CH2SO2CH3, -CH2N3, -CH2OCH2CH3, -CH2O(CH2)2OCH3,syklopropyl, pyridinyl, -CH(CH3)OCH3, pyrimidinyl, pyrazinyl, -C≡CH, N-metyl-1,2,4-triazolyl, -CH(OH)CH3, -CH=NOH og -CH2OH.7. Forbindelsen eller farmasøytisk akseptabelt salt derav, ifølge hvilket som helst av kravene krav 1–6, hvori R2 velges fra gruppen bestående av hydrogen, metyl, etyl, -CH2F, -CH2OCH3, -CH2OH, -CH=NOH, pyridinyl, -C≡N og -CH=NHOCH3.8. Forbindelsen eller farmasøytisk akseptabelt salt derav, ifølge hvilket som helst av kravene krav 1–7, hvori R3 er hydrogen eller metyl.9. Forbindelsen eller farmasøytisk akseptable salter derav, ifølge hvilket som helst av kravene 1– 8, hvori forbindelsen velges fra gruppen bestående av:(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-(2-okso-1,3-oksazolidin-3-yl)-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion; (2R,4S,4aS)-11 -fluor-2,4-dimetyl-8-[(4R)-4-metyl-2-okso-1,3-oksazolidin-3-yl]-1,2,4,4atetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11 -fluor-2,4-dimetyl-8-[(5S)-5-metyl-2-okso-1,3-oksazolidin-3-yl]-1,2,4,4atetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11 -fluor-2,4-dimetyl-8-[(5R)-5-metyl-2-okso-1,3-oksazolidin-3-yl]-1,2,4,4atetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11 -fluor-2,4-dimetyl-8-[(4S)-4-metyl-2-okso-1,3-oksazolidin-3-yl]-1,2,4,4atetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-8-[(4S)-4-etyl-2-okso-1,3-oksazolidin-3-yl]-11-fluor-2,4-dimetyl-1,2,4,4atetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-8-[(4R)-4-etyl-2-okso-1,3-oksazolidin-3-yl]-11-fluor-2,4-dimetyl-1,2,4,4atetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion);(2R,4S,4aS)-11 -fluor-2,4-dimetyl-8-[(4R)-2-okso-4-phenyl-1,3-oksazolidin-3-yl]-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11 -fluor-2,4-dimetyl-8-[(4S)-2-okso-4-phenyl-1,3-oksazolidin-3-yl]-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-8-[(4R)-4-Benzyl-2-okso-1,3-oksazolidin-3-yl]-11-fluor-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion; (2R,4S,4aS)-8-[(4S)-4-Benzyl-2-okso-1,3-oksazolidin-3-yl]-11-fluor-2,4-dimetyl-1,2,4,4atetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-8-(5,5-dimetyl-2-okso-1,3-oksazolidin-3-yl)-11-fluor-2,4-dimetyl-1,2,4,4atetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion; (2R,4S,4aS)-8-[(5S)-5-etyl-2-okso-1,3-oksazolidin-3-yl]-11-fluor-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-8-[(5R)-5-etyl-2-okso-1,3-oksazolidin-3-yl]-11-fluor-2,4-dimetyl-1,2,4,4atetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-8-[(4R)-4-(fluormetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-8-[(4S)-4-(fluormetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-8-[(4S)-4-(metoksymetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-8-[(4R)-4-(metoksymetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-8-((S)-5-(fluormetyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-klor-8-[(5S)-4-(metoksymetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion; (2R,4S,4aS)-11 -klor-8-[(5R)-4-(metoksymetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;((2R,4S,4aS)-11-klor-2,4-dimetyl-8-((R)-5-metyl-2-oksooksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-8-((4S,5R)-4,5-dimetyl-2-oksooksazolidin-3-yl)-11-fluor-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-8-((4R,5S)-4,5-dimetyl-2-oksooksazolidin-3-yl)-11-fluor-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-8-((S)-4-allyl-2-oksooksazolidin-3-yl)-11-fluor-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-8-((S)-5-(hydroksymetyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;((2R,4S,4aS)-11-fluor-2,4-dimetyl-8-[(4R-(tetrahydro-2H-pyran-4-yl)-2-okso-1,3-oksazolidin-3-yl]-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-[(4S-(tetrahydro-2H-pyran-4-yl) -2-okso-1,3-oksazolidin-3-yl]-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion; (2R,4S,4aS)-11-fluor-8-((S)-4-(3-hydroksypropyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion; (2R,4S,4aS)-11-fluor-8-((S)-4-(3-fluorpropyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-8-((S)-4-(2-hydroksyetyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-klor-8-((S)-5-(fluormetyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-chor-8-((S)-4-(3-hydrokspropyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-chor-8-((S)-4-(3-fluorpropyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-8-[(5S)-4-(metoksymetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-8-[(5R)-4-(metoksymetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-8-[(5R)-5-(hydroksymetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-8-[(5R)-5-(fluormetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion; (2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((S)-2-okso-4-vinyloksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-8-{(5R)-5-[(hydroksyimino)metyl]-2-okso-1,3-oksazolidin-3-yl}-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(4S)-3-[(2R,4S,4aS)-11-fluor-2,4-dimetyl-2’,4’,6’-triokso-1,1’,2,3’,4,4’,4a,6’-oktahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-8-yl]-2-okso-1,3-oksazolidin-4-karbonitril;(2R,4S,4aS)-11-fluor-8-{(4S)-4-[(metoksyimino)metyl]-2-okso-1,3-oksazolidin-3-yl}-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-8-{(5R)-5-(metoksyimino)metyl]-2-okso-1,3-oksazolidin-3-yl}-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((R)-4-((metyltio)metyl)-2-oksooksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((R)-4-((metylsulfonyl)metyl)-2-oksooksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-8-((R)-4-(azidometyl)-2-oksooksazolidin-3-yl)-11-fluor-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-8-((S)-4-(azidometyl)-2-oksooksazolidin-3-yl)-11-fluor-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion; (2R,4S,4aS)-8-[(4S)-4-(etoksymetyl)-2-okso-1,3-oksazolidin-3-yl]-11-fluor-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-8-{(4S)-4-[(2-metoksyetoksy)metyl]-2-okso-1,3-oksazolidin-3-yl}-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-8-((R)-4-(difluormetyl)-2-oksooksazolidin-3-yl)-11-fluor-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-8-((S)-4-syklopropyl-2-oksooksazolidin-3-yl)-11-fluor-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((R)-2-okso-5-(pyridin-2-yl)oksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((S)-2-okso-5-(pyridin-2-yl)oksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((R)-2-okso-4-(pyridin-2-yl)oksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((S)-2-okso-4-(pyridin-2-yl)oksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((R)-2-okso-4-(pyridin-4-yl)oksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion; (2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((S)-2-okso-4-(pyridin-4-yl)oksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-8-((R)-4-((R)-1-metoksyetyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-8-((R)-4-((S)-1-metoksyetyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((R)-2-okso-4-(pyrazin-2-yl)oksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((S)-2-okso-4-(pyrazin-2-yl)oksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((R)-2-okso-4-(pyrimidin-2-yl)oksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((S)-2-okso-4-(pyrimidin-2-yl)oksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-8-((S)-4-etynyl-2-oksooksazolidin-3-yl)-11-fluor-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-klor-2,4-dimetyl-8-((S)-4-metyl-2-oksooksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion; (2R,4S,4aS)-11-fluor-8-[(4S)-4-(metoksymetyl)-2-okso-1,3-oksazolidin-3-yl]-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((S)-4-(1-metyl-1H-1,2,4-triazol-5-yl)-2-oksooksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-2,4-dimetyl-8-((R)-4-(1-metyl-1H-1,2,4-triazol-5-yl)-2-oksooksazolidin-3-yl)-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion; (2R,4S,4aS)-11-fluor-8-((R)-4-((S)-1-hydroksyetyl)-2-oksooksazolidin-3-yl)-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;{(4S)-3-[(2R,4S,4aS)-11-fluor-2,4-dimetyl-2’,4’,6’-triokso-1,1’,2,3’,4,4’,4a,6’-oktahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-8-yl]-2-okso-1,3-oksazolidin-4-yl}acetonitril;(2R,4S,4aS)-8-((R)-4-((R)-1,2-dihydroksyetyl)-2-oksooksazolidin-3-yl)-11-fluor-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-8-((R)-4-((S)-1,2-dihydroksyetyl)-2-oksooksazolidin-3-yl)-11-fluor-2,4-dimetyl-2,4,4a,6-tetrahydro-1H,1’H-spiro[isoksazolo[4,5-g][1,4]oksazino[4,3-a]quinolin-5,5’-pyrimidin]-2’,4’,6’(3’H)-trion;(2R,4S,4aS)-11-fluor-8-{(4S)-4-[(hydroksyimino)metyl]-2-okso-1,3-oksazolidin-3-yl}-2,4-dimetyl-1,2,4,4a-tetrahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-2’,4’,6’(1’H,3’H)-trion;(5R)-3-[(2R,4S,4aS)-11-fluor-2,4-dimetyl-2’,4’,6’-triokso-1,1’,2,3’,4,4’,4a,6’-oktahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-8-yl]-2-okso-1,3-oksazolidin-5-karbonitril; og (5S)-3-[(2R,4S,4aS)-11-fluor-2,4-dimetyl-2’,4’,6’-triokso-1,1’,2,3’,4,4’,4a,6’-oktahydro-2’H,6H-spiro[1,4-oksazino[4,3-a][1,2]oksazolo[4,5-g]quinolin-5,5’-pyrimidin]-8-yl]-2-okso-1,3-oksazolidin-5-karbonitril eller et akseptabelt salt derav.10. Forbindelsen eller farmasøytisk akseptable salter derav, ifølge hvilket som helst av kravene 1– 8, hvori forbindelsen representeres med følgende strukturell formel:eller et farmasøytisk akseptabelt salt derav.11. Farmasøytisk sammensetning omfattende en forbindelse ifølge hvilket som helst av kravene 1–10 og et farmasøytisk akseptabelt salt derav, og et farmasøytisk akseptabelt hjelpestoff eller fortynner.12. Forbindelse ifølge hvilket som helst av kravene 1–10 eller et farmasøytisk akseptabelt salt derav, til anvendelse ved behandling av en bakteriell infeksjon.13. Forbindelse ifølge hvilket som helst av kravene 1–10 eller et farmasøytisk akseptabelt salt derav, til anvendelse for å hemme bakterielt DNA-gyrase.
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Entasis Therapeutics Limited
3rd Floor 1 Ashley Road AltrinchamCheshire WA14 2DT GB

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BASARAB, Gregory, Steven
AstraZeneca R&D Boston35 Gatehouse Drive Waltham, Massachusetts 02451 US
GOWRAVARAM, Madhusudhan, Reddy
c/o Astrazeneca Intellectual PropertyAstraZeneca R&D Boston35 Gatehouse Drive Waltham, Massachusetts 02451 US
HAUCK, Sheila, Irene
c/o Astrazeneca Intellectual PropertyAstraZeneca R&D Boston35 Gatehouse Drive Waltham, Massachusetts 02451 US
ZHOU, Fei
AstraZeneca R&D Boston35 Gatehouse Drive Waltham, Massachusetts 02451 US

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Fullmektig i Norge:
ZACCO NORWAY AS
Postboks 488 0213 OSLO NO ( OSLO kommune, Oslo fylke )

Org.nummer: 982702887
Din referanse: P62000403NO00E
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Kilde: Brønnøysundregistrene
Fullmektig i EP:
Potter Clarkson
The Belgrave Centre Talbot Street Nottingham NG1 5GG GB

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2013.01.23, US 201361755537 P

2013.07.30, US 201361859910 P

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WO-A1-2004/031195 (B1)

WO-A2-2006/120563 (B1)

WO-A1-2010/043893 (B1)

WO-A1-2007/072151 (B1)

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Hva betyr A1, B, B1, C osv? info
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