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Tittel NEW DIHYDROQUINOLINE-2-ONE DERIVATIVES
Status
Hovedstatus
Detaljstatus 		I kraft info EP patent gjort gjeldende i Norge EP patent besluttet gjeldende i Norge
Patentnummer NO/EP2755963
Europeisk (EP) publiserings nummer EP2755963
EP levert
EP søknadsnummer 12756741.0
EP meddelt
Prioritet 2011.09.15, WO PCT/CN11/079673
Sakstype Europeisk
Løpedag
Utløpsdato
Allment tilgjengelig
Validert i Norge
Innehaver F. Hoffmann-La Roche AG (CH)
Oppfinner AEBI, Johannes (CH) .... se mer/flere nedenfor
Fullmektig PLOUGMANN VINGTOFT NUF (NO)
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PATENTKRAV1. Forbindelser med formel (I)hvoriR1 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl;R2 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl;R3 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl;R4 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl; eller R3 og R4 sammen med karbonatomene som de er festet til, danner en dobbeltbinding;R5 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl;R6 er R8;R7 er H, halogen, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl; eller R1 og R7 sammen med nitrogen- og karbonatomene som de er festet til, danner et heterosykloalkyl substituert med én til tre substituenter uavhengig valgt fra H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl;R8 er -Om-(CR9R10)n-(CR11R12)p-(CR13R14)q-NR15R16, -NmR17-(CR9R10)n-(CR11R12)p-(CR13R14)q-NR15R16 eller -Sm(O)r-(CR9R10)n-(CR11R12)p-(CR13R14)q-NR15R16;R9 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl;R10 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl;R11 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl; eller R10 og R11 sammen med karbonatomene som de er festet til, danner en dobbeltbinding;R12 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl; eller R11 og R12 sammen med karbonatomet som de er festet til, danner et sykloalkyl eller et heterosykloalkyl;R13 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl; R14 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl; eller R10 og R14 sammen danner -(CH2)t-;R15 er H, alkyl, halogenalkyl, sykloalkyl, halogensykloalkyl, alkoksyalkyl, halogenalkoksyalkyl eller hydroksyalkyl;R16 er H, alkyl, halogenalkyl, sykloalkyl, halogensykloalkyl, hydroksyalkyl, alkoksyalkyl, halogenalkoksyalkyl, fenylalkyl, substituert fenylalkyl, aryl, substituert aryl, heterosykloalkyl, substituert heterosykloalkyl, heteroaryl, substituert heteroaryl, -S(O)2R18, -S(O)R18, -S(O)2OR18, -S(O)2NR18R19,-C(O)R18, -C(O)OR18 eller -C(O)NR18R19, hvori substituert fenylalkyl, substituert aryl, substituert heterosykloalkyl og substituert heteroaryl substitueres med én til tre substituenter uavhengig valgt fra alkyl, hydroksyalkyl, halogenalkyl, sykloalkyl, alkylsykloalkyl, halogensykloalkyl, alkylsykloalkylalkyl, halogensykloalkylalkyl, sykloalkylalkyl, sykloalkylalkoksy, sykloalkoksy, sykloalkoksyalkyl, sykloalkylalkoksyalkyl, alkoksy, alkoksyalkyl, halogenalkoksy, halogenalkoksyalkyl, alkoksyalkoksy, alkoksyalkoksyalkyl, alkoksykarbonyl, halogen, hydroksy, okso, cyano, triazolylalkyl, tetrazolylalkyl, amino, substituert amino, aminoalkyl, substituert aminoalkyl, aminokarbonyl, substituert aminokarbonyl, alkylkarbonylamino, sykloalkylkarbonylamino, alkylkarbonylaminoalkyl og sykloalkylkarbonylaminoalkyl, hvori substituert amino, substituert aminoalkyl og substituert aminokarbonyl substitueres på nitrogenatomet med én til to substituenter uavhengig valgt fra alkyl, sykloalkyl, alkylsykloalkyl, sykloalkylalkyl, alkylsykloalkylalkyl, hydroksyalkyl og alkoksyalkyl, hvori i tilfelle R15 er H eller alkyl og R16 er H eller alkyl, da er summen av n, p og q minst 1;eller R15 og R16 sammen med nitrogenatomet som de er festet til, danner et substituert heterosykloalkyl eller et substituert heteroaryl, hvori substituert heterosykloalkyl og substituert heteroaryl substitueres med R23, R24 og R25; eller R13 og R15 sammen med nitrogen- og karbonatomene som de er festet til, danner et substituert heterosykloalkyl, hvori substituert heterosykloalkyl substitueres med R23, R24 og R25;eller R11 og R15 sammen med nitrogen- og karbonatomene som de er festet til, danner et substituert heterosykloalkyl, hvori substituert heterosykloalkyl substitueres med R23, R24 og R25;eller R9 og R15 sammen med nitrogen- og karbonatomene som de er festet til, danner et substituert heterosykloalkyl, hvori substituert heterosykloalkyl substitueres med R23, R24 og R25;R17 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl;R18 er alkyl, sykloalkyl, halogenalkyl, halogensykloalkyl, hydroksyalkyl, halogenhydroksyalkyl, alkoksyalkyl, halogenalkoksyalkyl, alkylkarbonyloksyalkyl, aryl, substituert aryl, heterosykloalkyl, substituert heterosykloalkyl, heteroaryl, substituert heteroaryl, hvori substituert aryl, substituert heterosykloalkyl og substituert heteroaryl substitueres med én til tre substituenter uavhengig valgt fra alkyl, hydroksyalkyl, halogenalkyl, sykloalkyl, alkylsykloalkyl, halogensykloalkyl, alkylsykloalkylalkyl, halogensykloalkylalkyl, sykloalkylalkyl, sykloalkylalkoksy, sykloalkoksy, sykloalkoksyalkyl, sykloalkylalkoksyalkyl, alkoksy, alkoksyalkyl, halogenalkoksy, halogenalkoksyalkyl, alkoksyalkoksy, alkoksyalkoksyalkyl, alkoksykarbonyl, halogen, hydroksy, okso, cyano, triazolylalkyl, tetrazolylalkyl, amino, substituert amino, aminoalkyl, substituert aminoalkyl, aminokarbonyl, substituert aminokarbonyl, alkylkarbonylamino, sykloalkylkarbonylamino, alkylkarbonylaminoalkyl og sykloalkylkarbonylaminoalkyl, hvori substituert amino, substituert aminoalkyl og substituert aminokarbonyl substitueres på nitrogenatomet med én til to substituenter uavhengig valgt fra alkyl, sykloalkyl, alkylsykloalkyl, sykloalkylalkyl, alkylsykloalkylalkyl, hydroksyalkyl og alkoksyalkyl;R19 er H, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl;A1 er CR20;A2 er CR21;A3 er CR22 R20 er H, halogen, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl; R21 er H, halogen, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl; R22 er H, halogen, alkyl, halogenalkyl, sykloalkyl eller halogensykloalkyl; R23, R24 og R25 hver er valgt uavhengig blant H, alkyl, hydroksyalkyl, halogenalkyl, sykloalkyl, alkylsykloalkyl, halogensykloalkyl, alkylsykloalkylalkyl, halogensykloalkylalkyl, sykloalkylalkyl, sykloalkylalkoksy, sykloalkoksy, sykloalkoksyalkyl, sykloalkylalkoksyalkyl, alkoksy, alkoksyalkyl, halogenalkoksy, halogenalkoksyalkyl, alkoksyalkoksy, alkoksyalkoksyalkyl, alkoksykarbonyl, −S(O)2R18, −C(O)R18, halogen, hydroksy, okso, cyano, triazolylalkyl, tetrazolylalkyl, amino, substituert amino, aminoalkyl, substituert aminoalkyl, aminokarbonyl, substituert aminokarbonyl, alkylkarbonylamino, sykloalkylkarbonylamino, alkylkarbonylaminoalkyl og sykloalkylkarbonylaminoalkyl, hvori substituert amino, substituert aminoalkyl og substituert aminokarbonyl substitueres på nitrogenatomet med én til to substituenter uavhengig valgt fra alkyl, sykloalkyl, alkylsykloalkyl, sykloalkylalkyl, alkylsykloalkylalkyl, hydroksyalkyl og alkoksyalkyl;hvori i tilfelle m er null og R9 og R15, eller R11 og R15 eller R13 og R15 eller R15 og R16 sammen med nitrogen- og karbonatomene som de er festet til, danner et substituert heterosykloalkyl eller et substituert heteroaryl, da er minst ett av R23, R24, R25 og R16 forskjellig fra H, alkyl, halogenalkyl, alkoksy, halogenalkoksy, halogen, hydroksy, cyano, amino, substituert amino, aminokarbonyl, substituert aminokarbonyl, hvori substituert amino og substituert aminokarbonyl substitueres på nitrogenatomet med ett til to alkyl, og -C(O)R18, -S(O)2R18, hvori R18 er alkyl, halogenalkyl, hydroksyalkyl, halogenhydroksyalkyl, alkoksyalkyl eller halogenalkoksyalkyl;m er null eller 1, hvori i tilfelle m er 1, da er summen av n og p 2, 3 eller 4;n er null, 1 eller 2;p er null, 1 eller 2;q er null, 1 eller 2;r er null, 1 eller 2, hvori i tilfelle m er null, da er r null; t er null, 1 eller 2;eller farmasøytisk akseptable salter eller estere.2. Forbindelse ifølge krav 1, hvori R1 er alkyl.3. Forbindelse ifølge et hvilket som helst av kravene 1 til 2, hvori R8 er -Om-(CR9R10)n-(CR11R12)p-(CR13R14)q-NR15R16.4. Forbindelse ifølge et hvilket som helst av kravene 1 til 3, hvori R16 er -C(O)R18.5. Forbindelse ifølge et hvilket som helst av kravene 1 til 4, hvori R15 er alkyl.6. Forbindelse ifølge et hvilket som helst av kravene 1 til 5, hvori R18 er heteroaryl substituert med én til tre substituenter uavhengig valgt fra alkyl og halogen.7. Forbindelse ifølge et hvilket som helst av kravene 1 til 6, valgt blant etansulfonsyre [5-(1-methyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-amid;eddiksyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylkarbamoyl]-metylester;2-hydroksy-N-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-acetamid;6-[5-(2-hydroksy-etylamino)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-2-hydroksymetyl-pyrrolidin-1-yl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((R)-2-hydroksymetyl-pyrrolidin-1-yl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-2-hydroksymetyl-pyrrolidin-1-ylmetyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-2-hydroksymetyl-5-okso-pyrrolidin-1-ylmetyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-2-etylaminometyl-pyrrolidin-1-yl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-2-metoksymetyl-pyrrolidin-1-yl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on; 1-metyl-6-[5-((S)-2-[1,2,4]triazol-1-ylmetyl-pyrrolidin-1-yl)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;6-(5-benzylamino-pyridin-3-yl)-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-2-hydroksymetyl-5-okso-pyrrolidin-1-yl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;1-metyl-6-[5-(2-okso-pyrrolidin-1-yl)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;etansulfonsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyre [5-(1,4,4-trimetyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;1-metyl-6-[5-(2-okso-pyrrolidin-1-ylmetyl)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;1-metyl-6-[5-(2-okso-piperidin-1-ylmetyl)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;6-[5-(1,1-diokso-1λ6-tiomorfolin-4-ylmetyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-2-metoksymetyl-pyrrolidin-1-ylmetyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;(S)-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-pyrrolidin-2-karboksylsyremetylester;1-metyl-6-{5-[(S)-2-(2,2,2-trifluor-etoksymetyl)-pyrrolidin-1-ylmetyl]-pyridin-3-yl}-3,4-dihydro-1H-kinolin-2-on;6-[6-(2-hydroksy-etylamino)-pyrazin-2-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-(6-benzylamino-pyrazin-2-yl)-1-metyl-3,4-dihydro-1H-kinolin-2-on;7-fluor-6-[6-(2-hydroksy-etylamino)-pyrazin-2-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-(6-benzylamino-pyrazin-2-yl)-7-fluor-1-metyl-3,4-dihydro-1H-kinolin-2-on; 6-[6-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyrazin-2-yl]-2,6-diaza-spiro[3.3]heptan-2-karboksylsyre tert-butylester; 6-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-2,6-diaza-spiro[3.3]heptan-2-karboksylsyre tert-butylester; 6-[5-((R)-1-hydroksymetyl-2-metyl-propylamino)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[6-((R)-1-hydroksymetyl-2-metyl-propylamino)-pyrazin-2-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-(5-aminometyl-pyridin-3-yl)-1-metyl-3,4-dihydro-1H-kinolin-2-on;N-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-propionamid;Propan-2-sulfonsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;{2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-etyl}-karbaminsyre tert-butylester;3-metoksy-isoksazol-5-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid; syklopropankarboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;6-[5-(2-amino-etoksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on-hydroklorid;N-{2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-etyl}-propionamid;6-[5-(1,1-diokso-1λ6-[1,2]tiazinan-2-ylmetyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;og farmasøytisk akseptable salter derav.8. Forbindelse ifølge et hvilket som helst av kravene 1 til 6, valgt blant (S)-2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksymetyl]-azetidin-1-karboksylsyre tert-butylester;(R)-3-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-pyrrolidin-1-karboksylsyre tert-butylester;3-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-azetidin-1-karboksylsyre tert-butylester; (S)-3-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-pyrrolidin-1-karboksylsyre tert-butylester;(S)-3-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-piperidin-1-karboksylsyre tert-butylester;4-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-piperidin-1-karboksylsyre tert-butylester;(S)-2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksymetyl]-pyrrolidin-1-karboksylsyre tert-butylester;(S)-3-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-pyrrolidin-1-karboksylsyre tert-butylester;(R)-3-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-pyrrolidin-1-karboksylsyre tert-butylester;(R)-2-metyl-propan-2-sulfinsyre {3-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-oksetan-3-yl}-amid; etansulfonsyre [5-(2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;(R)-2-metyl-propan-2-sulfinsyre {(S eller R)-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;(R) 2-metyl-propan-2-sulfinsyre {(R eller S)-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;{(trans)-4-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-sykloheksyl}-karbaminsyre tert-butylester;6-[5-(1-amino-syklopropyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;1-metyl-6-[5-((S)-pyrrolidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on hydroklorid;1-metyl-6-[5-((S)-piperidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;1-metyl-6-[5-(piperidin-4-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on hydroklorid;6-[5-((S)-1-azetidin-2-ylmetoksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S eller R)-1-amino-etyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on hydroklorid; 6-[5-((R eller S)-1-amino-etyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on hydroklorid;1-metyl-6-[5-((S)-1-pyrrolidin-2-ylmetoksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on hydroklorid;7-fluor-1-metyl-6-[5-((R)-pyrrolidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on hydroklorid;1-metyl-6-[5-((R)-pyrrolidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on hydroklorid;6-[5-(3-amino-oksetan-3-yl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on hydroklorid;6-[5-(azetidin-3-yloksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on hydroklorid;6-[5-((trans)-4-amino-sykloheksyloksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on hydroklorid;6-[5-(1-amino-1-metyl-etyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-(5-aminometyl-pyridin-3-yl)-7-fluor-1-metyl-3,4-dihydro-1H-kinolin-2-on;3,5-dimetyl-isoksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;6-[5-((S)-1-syklopropankarbonyl-pyrrolidin-3-yloksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;3-metyl-N-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-butyramid;3,3,3-trifluor-N-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-propionamid;2-hydroksy-2-metyl-N-[5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-propionamid;5-metyl-[1,3,4]oksadiazol-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;1-metyl-6-[5-((S)-1-propionyl-piperidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;2-metoksy-pyrimidin-5-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid, 1-metyl-1H-imidazol-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;5-trifluormetyl-furan-3-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;pyridazin-3-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;pyrimidin-5-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;1-metyl-1H-pyrazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;1-metyl-6-[5-(1-propionyl-piperidin-4-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;pyridazin-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;1-metyl-6-[5-((S)-1-propionyl-pyrrolidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-1-syklopropankarbonyl-azetidin-2-ylmetoksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;3-metyl-isoksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;4-fluor-2,6-dimetyl-N-[5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-benzamid;1-metyl-6-[5-((S)-1-propionyl-azetidin-2-ylmetoksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;3,6-diklor-pyridazin-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-syklopropyl-1-(2,2,2-trifluor-etyl)-1H-pyrazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;pyridin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;1,3-dimetyl-1H-pyrazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid; pyrimidin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;6-metoksy-pyridazin-3-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;5-metyl-isoksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3,5-dimetyl-isoksazol-4-karboksylsyre {2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-etyl}-amid;1-metyl-1H-pyrazol-4-karboksylsyre {2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-etyl}-amid;6-klor-pyridazin-3-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-klor-6-metyl-pyridazin-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;1-metyl-6-[5-((S)-1-propionyl-pyrrolidin-2-ylmetoksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;5-syklopropyl-isoksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;2-metyl-5-trifluormetyl-oksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid; 2-metyl-oksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;5-syklopropyl-oksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;2,5-dimetyl-oksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;5-metyl-oksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3,5-dimetyl-isoksazol-4-karboksylsyre {1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-syklopropyl}-amid; 6-klor-pyridin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-metyl-pyridin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid; 3,6-diklor-pyridin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;6-metyl-pyridin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-klor-pyridin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-fluor-pyridin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;5-klor-3-metyl-pyridin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;1-metyl-6-[5-((R)-1-propionyl-pyrrolidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;7-fluor-1-metyl-6-[5-((S)-1-propionyl-pyrrolidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;5-trifluormetyl-pyrimidin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;5-metyl-pyrazin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;5-klor-pyrazin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;5-trifluormetyl-pyrazin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3,5-dimetyl-isoksazol-4-karboksylsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;1-metyl-6-[5-((R)-1-propionyl-pyrrolidin-2-ylmetoksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;1-metyl-6-[5-(1-propionyl-azetidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;N-{3-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-oksetan-3-yl}-propionamid;3-klor-pyridin-2-karboksylsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3,6-diklor-pyridazin-4-karboksylsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid; 7-fluor-1-metyl-6-[5-((R)-1-propionyl-pyrrolidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;5-klor-3-metoksy-pyrazin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3,5-dimetyl-isoksazol-4-karboksylsyre {(R eller S)-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid; 3-metyl-5-trifluormetyl-isoksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid; 3-klor-pyridin-2-karboksylsyre {1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-syklopropyl}-amid;3-klor-pyridin-2-karboksylsyre {1-metyl-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;3,5-dimetyl-isoksazol-4-karboksylsyre {1-metyl-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid; 3-klor-pyridin-2-karboksylsyre [5-(2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;3,5-dimetyl-isoksazol-4-karboksylsyre [5-(2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-klor-pyridin-2-karboksylsyre {1-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-syklopropyl}-amid; 3-metyl-pyridin-2-karboksylsyre {1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-syklopropyl}-amid;N-{(trans)-4-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-sykloheksyl}-propionamid;5-trifluormetyl-isoksazol-4-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;7-fluor-1-metyl-6-[5-((S)-pyrrolidin-3-yloksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;(R)-2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksymetyl]-pyrrolidin-1-karboksylsyre tert-butylester;1-metyl-6-[5-((R)-1-pyrrolidin-2-ylmetoksy)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on-hydroklorid;6-(5-aminometyl-pyridin-3-yl)-3,4-dihydro-1H-kinolin-2-on; 6-[5-(1-amino-syklopropyl)-pyridin-3-yl]-7-fluor-1-metyl-3,4-dihydro-1H-kinolin-2-on;etansulfonsyre {2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-etyl}-amid;3-klor-N-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-benzensulfonamid;6-metoksy-pyridin-3-sulfonsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3,5-dimetyl-isoksazol-4-sulfonsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid; syklopropansulfonsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;3,4-diklor-N-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-benzensulfonamid;1-metyl-1H-imidazol-4-sulfonsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;6-klor-pyridin-3-sulfonsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;1-metyl-1H-pyrazol-4-sulfonsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;6-[5-((S)-1-etansulfonyl-piperidin-3-yloksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-(1-etansulfonyl-piperidin-4-yloksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;2,2,2-trifluor-etansulfonsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;C,C,C-trifluor-N-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-metansulfonamid;6-[5-((S)-1-etansulfonyl-pyrrolidin-3-yloksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-1-etansulfonyl-azetidin-2-ylmetoksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;etansulfonsyre {1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-syklopropyl}-amid; 6-[5-((S)-1-etansulfonyl-pyrrolidin-2-ylmetoksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((R)-1-etansulfonyl-pyrrolidin-3-yloksy)-pyridin-3-yl]-7-fluor-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((R)-1-etansulfonyl-pyrrolidin-3-yloksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-(1-etansulfonyl-azetidin-3-yloksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;etansulfonsyre {1-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-yl]-syklopropyl}-amid;etansulfonsyre {(trans)-4-[5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-yloksy]-sykloheksyl}-amid; etansulfonsyre {(R eller S)-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid; etansulfonsyre {(S eller R)-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;1-metyl-1H-pyrazol-4-karboksylsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;(ras.)-etansulfonsyre {2-metyl-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-propyl}-amid;(ras.)-etansulfonsyre {syklopropyl-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-metyl}-amid;(ras.)-etansulfonsyre {1-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;6-[5-(1,1-diokso-1λ6-isotiazolidin-2-ylmetyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;(ras.)-etansulfonsyre {1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-yl]-propyl}-amid;etansulfonsyreetyl-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyremetyl-[5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyre {1-metyl-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-yl]-etyl}-amid; etansulfonsyreisopropyl-[5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyre (2-etoksy-etyl)-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;(ras.)-etansulfonsyremetyl-{1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;(ras.)-etansulfonsyreetyl-{1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;3,5-dimetyl-isoksazol-4-karboksylsyremetyl-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;6-{5-[2-(1,1-diokso-1λ6-isotiazolidin-2-yl)-etoksy]-pyridin-3-yl}-1-metyl-3,4-dihydro-1H-kinolin-2-on;etansulfonsyre {(R eller S)-1-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid; etansulfonsyre {(S eller R)-1-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid; etansulfonsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-4-metyl-pyridin-3-ylmetyl]-amid;etansulfonsyre [4-klor-5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyre [4-metyl-5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyremetyl-{2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-yloksy]-etyl}-amid;3-klor-pyridin-2-karboksylsyremetyl-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;N-metyl-N-{2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-etyl}-propionamid;1-metyl-1H-pyrazol-4-karboksylsyremetyl-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-metyl-pyridin-2-karboksylsyremetyl-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-klor-pyridin-2-karboksylsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-metyl-amid; 3-klor-pyridin-2-karboksylsyremetyl-{1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-syklopropyl}-amid; 1-metyl-1H-pyrazol-4-karboksylsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-metyl-amid; etansulfonsyre [5-(8-klor-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-klor-pyridin-2-karboksylsyre [5-(8-klor-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3,5-dimetyl-isoksazol-4-karboksylsyre [5-(8-klor-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;6-{5-[(3-etyl-oksetan-3-ylamino)-metyl]-pyridin-3-yl}-1-metyl-3,4-dihydro-1H-kinolin-2-on;etansulfonsyre [5-(7-klor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyre [5-(8-fluor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyre [5-(8-klor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyre [5-(5-fluor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-metyl-amid;N-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-propionamid;(ras.)-N-{1-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-propionamid;(S)-3-[5-(2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-pyrrolidin-1-karboksylsyre tert-butylester;3-klor-pyridin-2-karboksylsyremetyl-[5-(2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-klor-pyridin-2-karboksylsyre [5-(8-klor-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-metyl-amid;(R)-2-metyl-propan-2-sulfinsyre [4-klor-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid; 6-(5-aminometyl-4-klor-pyridin-3-yl)-1-metyl-3,4-dihydro-1H-kinolin-2-on-hydroklorid;3,5-dimetyl-isoksazol-4-karboksylsyre [4-klor-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-klor-pyridin-2-karboksylsyre [4-klor-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;(R)-2-metyl-propan-2-sulfinsyre [4-metyl-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;6-(5-aminometyl-4-metyl-pyridin-3-yl)-1-metyl-3,4-dihydro-1H-kinolin-2-on-hydroklorid;3,5-dimetyl-isoksazol-4-karboksylsyre [4-metyl-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid; 3-klor-pyridin-2-karboksylsyre [4-metyl-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;(R)-2-metyl-propan-2-sulfinsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-4-metyl-pyridin-3-ylmetyl]-amid; 6-(5-aminometyl-4-metyl-pyridin-3-yl)-7-fluor-1-metyl-3,4-dihydro-1H-kinolin-2-on-hydroklorid;3-klor-pyridin-2-karboksylsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-4-metyl-pyridin-3-ylmetyl]-amid;3-klor-pyridin-2-karboksylsyre [4-klor-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-metyl-amid;3-klor-pyridin-2-karboksylsyremetyl-[4-metyl-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;3-klor-pyridin-2-karboksylsyre {(R eller S)-1-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;5'-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-5,6-dihydro-4H-[3,3']bipyridinyl-1-karboksylsyre tert-butylester;{2-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-etyl}-karbaminsyre tert-butylester;3-klor-pyridin-2-karboksylsyre {2-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-etyl}-amid; etansulfonsyre [5-(4-okso-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]kinolin-8-yl)-pyridin-3-ylmetyl]-amid; etansulfonsyre [5-(3-okso-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]kinolin-9-yl)-pyridin-3-ylmetyl]-amid;3-klor-pyridin-2-karboksylsyre [5-(4-okso-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]kinolin-8-yl)-pyridin-3-ylmetyl]-amid;3-klor-pyridin-2-karboksylsyremetyl-[5-(4-okso-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]kinolin-8-yl)-pyridin-3-ylmetyl]-amid;6-[5-(2-amino-etoksy)-pyridin-3-yl]-7-fluor-1-metyl-3,4-dihydro-1H-kinolin-2-on-hydroklorid;(R)-2-metyl-propan-2-sulfinsyre {(R eller S)-1-[4-metyl-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;6-[5-((R eller S)-1-amino-etyl)-4-metyl-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on-hydroklorid;3-klor-pyridin-2-karboksylsyre {(R eller S)-1-[4-metyl-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid; 3,5-dimetyl-isoksazol-4-karboksylsyre {(R eller S)-1-[4-metyl-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;etansulfonsyre {2-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-yloksy]-etyl}-amid;3-klor-pyridin-2-karboksylsyre {2-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-etyl}-amid;N-{(trans)-4-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-sykloheksyl}-metansulfonamid;3,5-dimetyl-isoksazol-4-karboksylsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-4-metyl-pyridin-3-ylmetyl]-amid; 5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-3',6'-dihydro-2'H-[3,4']bipyridinyl-1'-karboksylsyre tert-butylester; etansulfonsyre {2-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-yloksy]-etyl}-metyl-amid;(R)-2-metyl-propan-2-sulfinsyre {(R eller S)-1-[4-klor-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid; 6-[5-((R eller S)-1-amino-etyl)-4-klor-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on-hydroklorid;3-klor-pyridin-2-karboksylsyre {(R eller S)-1-[4-klor-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid; (R)-2-metyl-propan-2-sulfinsyre {(R eller S)-1-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-4-metyl-pyridin-3-yl]-etyl}-amid;6-[5-((R eller S)-1-amino-etyl)-4-metyl-pyridin-3-yl]-7-fluor-1-metyl-3,4-dihydro-1H-kinolin-2-on-hydroklorid;6-[5-((S)-1-acetyl-pyrrolidin-3-yloksy)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;1-metyl-6-{5-[(S)-1-(1-metyl-1H-pyrazol-4-karbonyl)-pyrrolidin-3-yloksy]-pyridin-3-yl}-3,4-dihydro-1H-kinolin-2-on;(S)-3-[5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-pyrrolidin-1-karboksylsyreetylester;3,5-dimetyl-isoksazol-4-karboksylsyre {(R eller S)-1-[4-klor-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yl]-etyl}-amid;3-klor-pyridin-2-karboksylsyre {(R eller S)-1-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-4-metyl-pyridin-3-yl]-etyl}-amid;5-metyl-isoksazol-4-karboksylsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-4-metyl-pyridin-3-ylmetyl]-amid; 5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-3',4',5',6'-tetrahydro-2'H-[3,4']bipyridinyl-1'-karboksylsyre tert-butylester; N-{(R eller S)-1-[4-klor-5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-yl]-etyl}-propionamid;6-[5-(1-amino-syklopropyl)-pyridin-3-yl]-1-metyl-1H-kinolin-2-on; etansulfonsyre [5-(8-fluor-1-metyl-2-okso-1,2-dihydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;N-{(R eller S)-1-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-4-metyl-pyridin-3-yl]-etyl}-propionamid;N-[4-klor-5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-propionamid; N-{(R eller S)-1-[4-metyl-5-(1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-yl]-etyl}-propionamid;3,5-dimetyl-isoksazol-4-karboksylsyre {2-[5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-yloksy]-etyl}-amid; og farmasøytisk akseptable salter derav.9. Forbindelse ifølge et hvilket som helst av kravene 1 til 8, valgt blant 6-[5-(2-hydroksy-etylamino)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-2-hydroksymetyl-pyrrolidin-1-yl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-2-hydroksymetyl-pyrrolidin-1-ylmetyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;6-[5-((S)-2-hydroksymetyl-5-okso-pyrrolidin-1-ylmetyl)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;etansulfonsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid;etansulfonsyre [5-(7-fluor-1-metyl-2-okso-1,2,3,4-tetrahydrokinolin-6-yl)-pyridin-3-ylmetyl]-amid;1-metyl-6-[5-(2-okso-pyrrolidin-1-ylmetyl)-pyridin-3-yl]-3,4-dihydro-1H-kinolin-2-on;6-[5-((R)-1-hydroksymetyl-2-metyl-propylamino)-pyridin-3-yl]-1-metyl-3,4-dihydro-1H-kinolin-2-on;og farmasøytisk akseptable salter derav.10. Forbindelse ifølge et hvilket som helst av kravene 1 til 7 og 9, hvori forbindelsen er 3-klor-pyridin-2-karboksylsyre [5-(1-metyl-2-okso-1,2,3,4-tetrahydro-kinolin-6-yl)-pyridin-3-ylmetyl]-amid.11. Forbindelse ifølge et hvilket som helst av kravene 1 til 10 for anvendelse som terapeutisk aktivt stoff.12. Farmasøytisk sammensetning omfattende en forbindelse ifølge et hvilket som helst av kravene 1 til 10 og en terapeutisk inert bærer. 13. Forbindelse ifølge et hvilket som helst av kravene 1 til 10 for behandling eller profylakse av kronisk nyresykdom, kongestiv hjertesvikt, hypertensjon, primær hyperaldosteronisme og Cushings syndrom.
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Grenzacherstrasse 124 4070 Basel CH

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AEBI, Johannes
Im Kugelfang 27 CH-4102 Binningen CH
AMREIN, Kurt
Lettenweg 8 CH-4452 Itingen CH
HORNSPERGER, Benoit
9 rue des Sources F-68130 Altkirch FR
KNUST, Henner
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KUHN, Bernd
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MAERKI, Hans P.
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MAYWEG, Alexander V.
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MOHR, Peter
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LIU, Yongfu
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TAN, Xuefei
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ZHOU, Mingwei
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Fullmektig i Norge:
PLOUGMANN VINGTOFT NUF
C. J. Hambros plass 2 0164 OSLO NO ( OSLO kommune, Oslo fylke )

Org.nummer: 986406263
Din referanse: P70720NO01
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Kilde: Brønnøysundregistrene
Fullmektig i EP:
Bernard, Guillaume
F. Hoffmann-La Roche AG Patent Department Grenzacherstrasse 124 4070 Basel CH

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2011.09.15, WO PCT/CN11/079673

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SIMON LUCAS ET AL: "Fine-Tuning the Selectivity of Aldosterone Synthase Inhibitors: Structure-Activity and Structure-Selectivity Insights from Studies of Heteroaryl Substituted 1,2,5,6-Tetrahydropyrrolo[3,2,1- ij ]quinolin-4-one Derivatives", JOURNAL OF MEDICINAL CHEMISTRY, vol. 54, no. 7, 14 April 2011 (2011-04-14) , pages 2307-2319, XP55040241, ISSN: 0022-2623, DOI: 10.1021/jm101470k (B1)

US-A1- 2011 112 067 (B1)

US-A- 4 710 507 (B1)

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