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Tittel MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
Status
Hovedstatus
Detaljstatus 		I kraft info EP patent gjort gjeldende i Norge EP patent besluttet gjeldende i Norge
Patentnummer NO/EP3507289
Europeisk (EP) publiserings nummer EP3507289
EP levert
EP søknadsnummer 17777380.1
EP meddelt
Prioritet 2016.09.02, IN 201641030062, .... se mer/flere nedenfor
Sakstype Europeisk
Løpedag
Utløpsdato
Allment tilgjengelig
Validert i Norge
Innehaver Suven Life Sciences Limited (IN)
Oppfinner NIROGI, Ramakrishna (IN) .... se mer/flere nedenfor
Fullmektig Nordic Patent Service A/S (DK)
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PATENTKRAV1. Forbindelse av formel (I),R1 velges fra gruppen som består av:Ra er OH;X1 velges uavhengig fra CH2 eller O;a er 0 eller 1;R2 er -(C6-10)-aryl eller -(C5-10)-heteroaryl; hver av disse substitueres eventuelt med én eller flere substituenter valgt fra halogen, -O-(C1-4)-alkyl, -S-(C1-4)-alkyl, -N(CH3)2, -(C1-4)alkyl, -(C3-6)-sykloalkyl, halogen-(C1-4)-alkyl, -OH, -NH2, -CN eller R2a;R2a er -(C6-10)-aryl eller (C5-10)-heteroaryl; hver av disse substitueres eventuelt med én eller flere substituenter valgt fra gruppen som består av halogen, -OH, -NH2, -CN,-O-(C1-2)-alkyl, -S-(C1-2)-alkyl, -(C1-2)-alkyl eller (C3-6)-sykloalkyl;R3 er -(C1-4)-alkyl, -(C3-6)-sykloalkyl, -(C1-4)-alkyl-(C3-6)-sykloalkyl, halogen(C1-4)-alkyl og hydrogen; ogR4 er hydrogen, -(C1-4)-alkyl og halogen-(C1-4)-alkyl;eller en isotopisk form, en stereoisomer, en tautomer eller et farmasøytisk akseptabelt salt derav.2. Forbindelsen av formel (I) ifølge krav 1, hvori:R2 velges fra gruppen som består av:A3 er N eller CH;A4 er CH eller CF;Rb ved hver forekomst velges uavhengig fra halogen, -O-(C1-4)-alkyl, -S-(C1-4)-alkyl, -N(CH3)2, -(C1-4)-alkyl, -(C3-6)-sykloalkyl, halogen-(C1-4)-alkyl, -OH, -NH2, -CN, fenyl, pyridyl, pyrazolyl, tiazolyl og oksazolyl; hvori fenyl, pyridyl, pyrazolyl, tiazolyl og oksazolyl eventuelt substitueres med én eller flere substituenter valgt fra gruppen som består av halogen, -OH, -NH2, -CN, -O-(C1-2)-alkyl, -S-(C1-2)-alkyl, -(C1-2)-alkyl eller -(C3-6)-sykloalkyl;Rc er hydrogen eller -(C1-4)-alkyl;X2 velges uavhengig fra NH, -N-(C1-2)-alkyl, O eller S;X3 velges uavhengig fra CH eller N;b er 0, 1 eller 2;« » representerer festepunktet.3. Forbindelsen av formel (I) ifølge krav 1, hvori:ring A velges fraR2 velges fra gruppen som består av:A3 er N eller CH;A4 er CH eller CF;Rb ved hver forekomst velges uavhengig fra halogen, -O-(C1-4)-alkyl, -S-(C1-4)-alkyl, -N(CH3)2, -(C1-4)-alkyl, -(C3-6)-sykloalkyl, halogen-(C1-4)-alkyl, -OH,-NH2, -CN, fenyl, pyridyl, pyrazolyl, tiazolyl og oksazolyl; hvori fenyl, pyridyl, pyrazolyl, tiazolyl og oksazolyl eventuelt substitueres med én eller flere substituenter valgt fra gruppen som består av halogen, -OH, -NH2, -CN, -O-(C1-2)-alkyl, -S-(C1-2)-alkyl, -(C1-2)-alkyl eller -(C3-6)-sykloalkyl;Rc er hydrogen eller -(C1-4)-alkyl;X2 velges uavhengig fra NH, -N-(C1-2)-alkyl, O eller S;X3 velges uavhengig fra CH eller N;b er 0, 1 eller 2;« » representerer festepunktet;R3 er -(C1-4)-alkyl, halogen-(C1-4)-alkyl eller hydrogen; ogR4 er hydrogen, -(C1-4)-alkyl og halogen-(C1-4)-alkyl;eller en isotopisk form, en stereoisomer, en tautomer eller et farmasøytisk akseptabelt salt derav.4. Forbindelsen ifølge et hvilket som helst av krav 1 til 3, hvori forbindelsen velges fra gruppen som består av:N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-fluorpyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-metoksypyridin-5-ylmetyl)-1-metyl-1Hpyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-fluorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-tiazol-4-ylbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-pyrazol-1-ylbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-[4-(1-metyl-1H-pyrazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-[2-fluor-4-(1-metyl-1H-pyrazol-4-yl)benzyl]-1-metyl- 1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-metylpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-klorpyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2,5-difluorpyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(benzotiazol-6-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2'-fluor-[2,5]bipyridinyl-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(pyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-[2-(1-metyl-1H-pyrazol-4-yl)pyridin-5-ylmetyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2,3-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-metylpyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(lS,2S)-2-hydroksysykloheksyl]-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-metylsulfanylpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-[4-(2-metylpyridin-3-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(1-metyl-1H-benzimidazol-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-klorpyridin-5-ylmetyl)-1-(2-fluoretyl)-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-(2-hydroksy-2-metylpropyl)-4-[4-(tiazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(3-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-(1-hydroksysyklopentylmetyl)-4-[4-(tiazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(pyridin-3-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-syklopropylpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-fluorpyridin-4-ylmetyl)-1-etyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-fluorpyridin-4-ylmetyl)-1-isopropyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2,3-difluorfenylmetyl)-1,3-dimetyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3b]pyridin-6-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-fluorpyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-fluorpyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-fluorpyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(3,4-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(3,4-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(3,4-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(2,3-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(2,3-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(2,3-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(2,3-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(2,3-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(2,3-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-fluorpyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(2- fluorpyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-fluorpyridin-4-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-klorpyridin-5-ylmetyl)-1metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-klorpyridin-5-ylmetyl-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(3,4-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(3,4-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(3,4-difluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(1-metyl-1H-pyrazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(1-metyl-1H-pyrazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(1-metyl-1H-pyrazol-4-yl)benzyl]-1metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(1-metyl-1H-pyrazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(1-metyl-1H-pyrazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(1-metyl-1H-pyrazol-4-yl)benzyl]-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(3-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(3-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(3-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(3-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(3-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(3-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3b]pyridin-6-karboksamid (Isomer-I);cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(2-metylpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(2-metylpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(2-metylpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(2-metylpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamidtrans-N-(4-hydroksytetrahydropyran-3-yl)-4-(2-metylpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(2-metylpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-II);(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-1-metyl-1Hpyrrolo[2,3-b]pyridin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-4-(2-metylpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-klorpyridin-5-ylmetyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-fluorpyridin-4-ylmetyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-fluorpyridin-5-ylmetyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-1-metyl-(6-metylpyridin-3-ylmetyl)-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-fluorbenzyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-metoksybenzyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2'-fluor-[2,5]bipyridinyl-5-ylmetyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2,3-difluorbenzyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-metyl-4-pyridinylmetyl)-l-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid (Isomer-I);cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid(Isomer-II);Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-metoksybenzyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-metoksybenzyl)-1-metyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-4-(2-metylpyridin-5-ylmetyl)-1-metyl2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-klorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-klorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(3-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(3-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-[4-(1-metyl-1H-pyrazol-4-yl)-benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-[4-(1-metyl-1H-pyrazol-4-yl)-benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-fluorpyridin-5-ylmetyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-fluorpyridin-5-ylmetyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-metoksybenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-metoksybenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-fluorpyridin-4-ylmetyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(2-fluorpyridin-4-ylmetyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-fluorbenzyl)-7-metyl-5,6,7,8tetrahydro[1,7]naftyridin-2-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-(4-fluorbenzyl)-7-etyl-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-II)Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-I);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin- 2-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-[4-(tiazol-4-yl)benzyl]-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-II);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-I);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-II);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-I);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-II);cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-I);cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-II);Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;Racemisk trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-I);trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-II);Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-I);cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-II);Racemisk trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid;trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-I);trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-fluorbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-II);Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-I);cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-II);Racemisk trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid;trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-I);trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamidhydroklorid (Isomer-II);Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin- 2-karboksamid;cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-I);cis-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-II);Racemisk trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin- 2-karboksamid;trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-I);trans-N-(4-hydroksytetrahydropyran-3-yl)-4-(4-pyrazol-1-ylbenzyl)-5,6,7,8-tetrahydro[1,7]naftyridin-2-karboksamid (Isomer-II);N-[(1S,2S)-2-hydroksysykloheksyl]-8-(4-fluorbenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(4-metoksybenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(2-klorpyridin-5-ylmetyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-[4-(1-metyl-1H-pyrazol-4-yl)-benzyl]-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(2,3-difluorbenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(1-metyl-1H-pyrazol-4-ylmetyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-[4-(pyrazol-1-yl)benzyl]-2,3-dihydro[1,4]dioksino[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(2-metylpyridin-5-ylmetyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(2-fluorpyridin-5-ylmetyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(2-fluorpyridin-4-ylmetyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid (Isomer-II);cis-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid (Isomer-I);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid (Isomer-I);(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-8-(4-metoksybenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-8-(4-fluorbenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-8-(2-klorpyridin-5-ylmetyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-8-(2-metylpyridin-5-ylmetyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-8-(4-fluorbenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-8-(4-metoksybenzyl)-2,3-dihydro-[1,4]dioksino[2,3-b]pyridin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(4-fluorbenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(3-fluorbenzyl)-4-metyl-2H-pyrido[3,2b][1,4]oksazin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-[4-(1-metyl-1H-pyrazol-4-yl)benzyl]-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(2-fluorpyridin-4-ylmetyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid (Isomer-II);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid (Isomer-I);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-fluorbenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid (Isomer-II);trans-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-metoksybenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-metoksybenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-metoksybenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid (Isomer-I);Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-metoksybenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-metoksybenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-8-(4-metoksybenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid (Isomer-II);N-[(1S,2S)-2-hydroksysykloheksyl]-8-(2-klorpyridin-5-ylmetyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(4-metoksybenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-(2-metylpyridin-5-ylmetyl)-4-metyl-2Hpyrido[3,2-b][1,4]oksazin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-8-[4-pyrazol-1-ylbenzyl]-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-4-metyl-8-(1-metyl-1H-pyrazol-4-ylmetyl)-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-8-(4-fluorbenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-8-(4-metoksybenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-8-(4-fluorbenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-8-(4-metoksybenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-8-(4-pyrazol-1-ylbenzyl)-4-metyl-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-4-metyl-8-(1-metyl-1H-pyrazol-4-ylmetyl)-2H-pyrido[3,2-b][1,4]oksazin-6-karboksamid;N-[(1S,2S)-2-hydroksysykloheksyl]-7-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[3,2-b]pyridin-5-karboksamid;Racemisk cis-N-(3-hydroksytetrahydropyran-4-yl)-7-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[3,2-b]pyridin-5-karboksamid;cis-N-(3-hydroksytetrahydropyran-4-yl)-7-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[3,2-b]pyridin-5-karboksamid (Isomer-I);cis-N-(3-hydroksytetrahydropyran-4-yl)-7-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[3,2-b]pyridin-5-karboksamid (Isomer-II);Racemisk trans-N-(3-hydroksytetrahydropyran-4-yl)-7-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[3,2-b]pyridin-5-karboksamid;trans-N-(3-hydroksytetrahydropyran-4-yl)-7-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[3,2-b]pyridin-5-karboksamid (Isomer-I);trans-N-(3-hydroksytetrahydropyran-4-yl)-7-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[3,2-b]pyridin-5-karboksamid (Isomer-II);N-[(1S,2S)-2-hydroksysykloheksyl]-7-(2-klorpyridin-5-ylmetyl)-1-metyl-1H-pyrrolo[3,2-b]pyridin-5-karboksamid;Racemisk cis-N-(4-hydroksytetrahydropyran-3-yl)-7-(4-metoksybenzyl)-1-metyl-1Hpyrrolo[3,2-b]pyridin-5-karboksamid;(3S, 4S)-N-(4-hydroksytetrahydropyran-3-yl)-7-(4-fluorbenzyl)-1-metyl-1H-pyrrolo[3,2-b]pyridin-5-karboksamid; og(3S,4S)-N-(4-hydroksytetrahydropyran-3-yl)-7-(4-metoksybenzyl)-1-metyl-1H-pyrrolo[3,2-b]pyridin-5-karboksamid;eller et farmasøytisk akseptabelt salt derav.5. Farmasøytisk sammensetning omfattende forbindelsen av formel (I) eller et farmasøytisk akseptabelt salt derav ifølge et hvilket som helst av krav 1 til 4 og farmasøytisk akseptable hjelpestoffer.6. Den farmasøytiske sammensetningen ifølge krav 5 for anvendelse i behandlingen av sykdom eller lidelse mediert av muskarin M1-reseptor, hvori sykdommen eller lidelsen velges fra gruppen som består av kognitive lidelser, smerte eller søvnlidelse.7. Kombinasjon omfattende forbindelsen ifølge et hvilket som helst av krav 1 til 4 med ett eller flere terapeutiske midler valgt fra acetylkolinesteraseinhibitorer og NMDA-reseptorantagonist.8. Kombinasjonen ifølge krav 7, hvori de terapeutiske midlene velges fra galantamin, rivastigmin, donepezil, takrin og memantin.9. Forbindelse av formel (I) eller et farmasøytisk akseptabelt salt derav ifølge et hvilket som helst av kravene 1 til 4 for anvendelse i en fremgangsmåte for behandling av sykdom eller lidelse mediert av muskarin M1-reseptor, hvori sykdommen eller lidelsen velges fra gruppen som består av kognitive lidelser, smerte eller søvnlidelse.10. Forbindelsen for anvendelse ifølge krav 9, hvori den kognitive lidelsen velges fra gruppen som består av demens ved Alzheimers sykdom, demens ved Parkinsons sykdom, demens ved Huntingtons sykdom, demens assosiert med Downs syndrom, demens assosiert med Tourettes syndrom, demens assosiert med postmenopause, frontotemporal demens, demens med Lewy-legemer, vaskulær demens, demens ved HIV, demens ved Creutzfeldt-Jakobs sykdom, stoffindusert vedvarende demens, demens ved Picks sykdom, demens ved schizofreni, senil demens og demens ved generelle medisinske tilstander. 11. Forbindelsen av formel (I) ifølge et hvilket som helst av krav 1 til 4, for anvendelse ved behandling av sykdom eller lidelse valgt fra kognitive lidelser, smerte og søvnlidelse.
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Innehaver i EP:
Suven Life Sciences Limited
5th Floor Serene Chambers Road No. 5 Off Avenue 7 Banjara Hills Hyderabad, Telangana 500034 IN

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NIROGI, Ramakrishna
Suven Life Sciences LimitedSerene Chambers Road-5 Avenue 7Banjara Hills HyderabadTelangana 500034 IN
SHINDE, Anil Karbhari
Suven Life Sciences LimitedSerene Chambers Road-5 Avenue 7Banjara Hills HyderabadTelangana 500034 IN
MOHAMMED, Abdul Rasheed
Suven Life Sciences LimitedSerene Chambers Road-5 Avenue 7Banjara Hills HyderabadTelangana 500034 IN
BADANGE, Rajesh Kumar
Suven Life Sciences LimitedSerene Chambers Road-5 Avenue 7Banjara Hills HyderabadTelangana 500034 IN
JAYARAJAN, Pradeep
Suven Life Sciences LimitedSerene Chambers Road-5 Avenue 7Banjara Hills HyderabadTelangana 500034 IN
BHYRAPUNENI, Gopinadh
Suven Life Sciences LimitedSerene Chambers Road-5 Avenue 7Banjara Hills HyderabadTelangana 500034 IN
JASTI, Venkateswarlu
Suven Life Sciences LimitedSerene Chambers Road-5 Avenue 7Banjara Hills HyderabadTelangana 500034 IN

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Fullmektig i Norge:
Nordic Patent Service A/S
Bredgade 30 1260 KØBENHAVN K DK
Din referanse: V2009-051-NO
Fullmektig i EP:
HGF
1 City Walk Leeds LS11 9DX GB

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2016.09.02, IN 201641030062

2017.04.13, IN 201741013343

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WO-A1-2011/084368 (B1)

WO-A1-2011/159554 (B1)

WO-A1-2017/143041 (B1)

WO-A1-2016/029454 (B1)

WO-A1-2015/110370 (B1)

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