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Tittel COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF ENDOSOMAL TOLL-LIKE RECEPTORS
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Detaljstatus 		I kraft info EP patent gjort gjeldende i Norge EP patent besluttet gjeldende i Norge
Patentnummer NO/EP3510033
Europeisk (EP) publiserings nummer EP3510033
EP levert
EP søknadsnummer 17777966.7
EP meddelt
Prioritet 2016.09.09, US 201662385726 P
Sakstype Europeisk
Løpedag
Utløpsdato
Allment tilgjengelig
Validert i Norge
Innehaver Novartis AG (CH)
Oppfinner ALPER, Phillip (US) .... se mer/flere nedenfor
Fullmektig ZACCO NORWAY AS (NO)
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Patentkrav1. Forbindelse som har strukturen i formel (A) eller farmasøytisk akseptabelt salt av denne:L er -CH2- eller -CH2CH2-;Y1 er -CH2- eller -CH2CH2-;Y2 er -CH2- eller -CH2CH2-;Y3 er -CH2-, -XCH2- eller -CH2X-;X er -CH2- eller O;R1 er -NHC(=O)R6, -NHC(=O)(CH2)nR6, -NH(CH2)nC(=O)R6, -NHC(=O)(CH2)mNHR5, -NHC(=O)(CH2)mN(R5)2, -NHC(=O)(CHR9)mNHR5, -NHC(=O)(CH2)mNH2, -NHC(=O)(CH2)nOR9, -NHC(=O)OR9, -NH(CH2)mC(=O)N(R5)2, -NH(CHR9)nC(=O)R6, NHC(=O)(CHR9)nR6, -NHC(=O)(CHR9)nN(R8)2, -NHC(=O)(CHR9)nNHR8, -NH(CHR9)nC(=O)N(R8)2, -NH(CHR9)mC(=O)R6, -NHR6, -NR5R6, -NH2, -N(R5)2, -NHR5, -NHR8, -N(R6R8), -NH(C(R9)2)nR10, -NR9C(=O)OR11, -NH(CH2)nR6, -NH(CHR9)nR6, N(R6)2, -NHC(=O)(CH2)nN(CD3)2, -NH(CHR9)nCH2OR9, -NHCH2(CHR9)nOR9, -NH(CHR9)nOR9, -NR9(CH2)nOR9, -NHCH2(C(R9)2)nOR9, -OR9, -NR9C(=O)R5, -NR9C(=O)(CH2)nR5, -NR9C(=O)OR5, -NHS(=O)2R5, -NHC(=O)(CH2)nNR9C(=O)R5, -NHC(=O)(CH2)nNR9S(=O)2R5, et 8-oksa-3-azabisyklo[3.2.1]oktanyl, et 5-6-leddet heteroaryl som har 1 til 3 ringelementer som er uavhengig valgt blant N, O og S, eller et 4–6-leddet heterosykloalkyl som har 1 til 2 ringelementer som er uavhengig valgt blant N, NH, NR16 og O som er usubstituert eller er substituert med 1–2 R7-grupper;R2 er H, C1–C6-alkyl, C1–C6-halogenalkyl eller C1–C6-alkyl som er substituert med 1–2 R15-grupper;R3 er H, C1–C6-alkyl, -CD3 eller benzyl som er substituert med 1–2 R10-grupper;R4 er H, NH2, C1–C6-alkyl, halogen eller et fenyl som er substituert med 0–2 R18-grupper; hver R5 er uavhengig valgt blant C1–C6-alkyl, -CD3 og -(CH2)nOR9;R6 er et C3–C6-sykloalkyl, et oksa-3-azabisyklo[3.2.1]oktan eller et 4–6-leddet heterosykloalkyl som har 1 til 2 ringelementer som er uavhengig valgt blant N, NH, NR16 og O som er usubstituert eller er substituert med 1–2 R12-grupper;hver R7 er uavhengig valgt blant C1–C6-alkyl, halogen, hydroksyl, okso og et C1–C6-alkyl som er substituert med 1 til 3 -OH;hver R8 er uavhengig valgt blant C1–C6-halogenalkyl, -(C(R9)2)nOR9 og et C1–C6-alkyl som er substituert med 1 til 3 -OH;hver R9 er uavhengig valgt blant H og C1–C6-alkyl;R10 er C1–C6-alkoksy eller C3–C6-sykloalkyl;R11 er et C3–C6-sykloalkyl som er usubstituert eller er substituert med 1 til 3 C1–C6-alkylgrupper;hver R12 er uavhengig valgt blant C1–C6-alkyl, hydroksyl, halogen og et C1–C6-alkyl som er substituert med 1 til 3 -OH;R13 er H eller C1–C6-alkyl;R14 er H eller C1–C6-alkyl;R15 er -NHC(=O)(CH2)mNHR5, -NHC(=O)(CH2)mN(R5)2, -NHC(=O)(CH2)mNH2, -NHC(=O)(CHR9)nR6, -NHC(=O)(CHR9)nN(R8)2, -NHC(=O)(CHR9)nNHR8, -NH(CHR9)nC(=O)N(R8)2, -NH(CHR9)nC(=O)R6, -NHR6, -NH2, -N(R5)2, -NHR8, -N(R6R8), -NH(C(R9)2)nR10, -NR9C(=O)OR11, -NH(CHR9)nR6, -N(R6)2, -N(CD3)2, -NH(CHR9)nOR9 eller -NHCH2(C(R9)2)nOR9;hver R16 er C1–C6-alkyl;hver R17 er uavhengig valgt blant H og C1–C6-alkyl;hver R18 er uavhengig valgt blant halogen, -CN, C1–C6-alkoksy og C1–C6-alkyl;m er 1, 2, 3, 4, 5 eller 6, ogn er 1, 2, 3, 4, 5 eller 6.2. Forbindelse ifølge krav 1 som har strukturen i formel (I) eller formel (II), eller farmasøytisk akseptabelt salt av dette:der Y1, Y2, Y3, L, R1, R2 og RA er som definert i krav 1.3. Forbindelse ifølge krav 1 eller krav 2, der forbindelsen på formelen (A) eller forbindelsen på formelen (I) har strukturen i formel (Ia), formel (Ib), formel (Ic), formel (Id), formel (Ie), formel (If), formel (Ig), formel (Ih), formel (Ii), formel (Ij) eller formel (Ik), eller farmasøytisk akseptabelt salt av dette:der Y1, Y2, Y3, L, R1, R2, R3, R4, R13 og R14 er som definert i krav 1.4. Forbindelse ifølge krav 1 eller krav 2, der forbindelsen på formelen (A) eller forbindelsen på formelen (II) har strukturen i formel (IIa), formel (IIb), formel (IIc), formel (IId), formel (IIe), formel (IIf), formel (IIg), formel (IIh), formel (IIi), formel (IIj) eller formel (IIk), eller farmasøytisk akseptabelt salt av dette:der Y1, Y2, Y3, L, R1, R2, R3, R4, R13 og R14 er som definert i krav 1.5. Forbindelse ifølge et av kravene 1 til 4; eller farmasøytisk akseptabelt salt av dette, der: R1 er -NHC(=O)R6, -NHC(=O)(CH2)nR6, -NH(CH2)nC(=O)R6, -NHC(=O)(CH2)mNHR5, -NHC(=O)(CH2)mN(R5)2, -NHC(=O)(CHR9)mNHR5, -NHC(=O)(CH2)mNH2, -NHC(=O)(CH2)nOR9, -NHC(=O)OR9, -NH(CH2)mC(=O)N(R5)2, -NH(CHR9)mC(=O)R6, -NHR6, -NR5R6, -NH2, -N(R5)2, -NHR5, -NHR8, -NR9C(=O)OR11, -NH(CH2)nR6, -N(R6)2, -NHC(=O)(CH2)nN(CD3)2, -NH(CHR9)nCH2OR9, -NHCH2(CHR9)nOR9, -NH(CHR9)nOR9, -NR9(CH2)nOR9, -NHCH2(C(R9)2)nOR9, -OR9, -NR9C(=O)R5, -NR9C(=O)OR5, -NHS(=O)2R5, -NHC(=O)(CH2)nNR9C(=O)R5, eller -NHC(=O)(CH2)nNR9S(=O)2R5.6. Forbindelse ifølge et av kravene 1 til 4, eller farmasøytisk akseptabelt salt av dette, der: R1 er -NHC(=O)R6, -NHC(=O)(CH2)nR6, -NH(CH2)nC(=O)R6, -NHC(=O)(CH2)mNHR5, -NHC(=O)(CH2)mN(R5)2, -NHC(=O)(CHR9)mNHR5, -NHC(=O)(CH2)mNH2, -NH(CH2)mC(=O)N(R5)2, -NH(CHR9)nC(=O)R6, -NHR6, -NH2, -N(R5)2, -NHR5, -NHR8, -NH(CHR9)nOR9 eller -NHCH2(C(R9)2)nOR9.7. Forbindelse ifølge et av kravene 1 til 4, eller farmasøytisk akseptabelt salt av dette, der: R1 er -NHC(=O)R6, -NHC(=O)(CHR9)nR6, -NH(CHR9)nC(=O)R6 eller -NHR6.8. Forbindelse ifølge et av kravene 1 til 4, eller farmasøytisk akseptabelt salt av dette, der: L er -CH2- eller -CH2CH2-;Y1 er -CH2- eller -CH2CH2-;Y2 er -CH2- eller -CH2CH2-;Y3 er -CH2- eller -XCH2-;X er -CH2- eller O;R1 er -NH(CH2)nC(=O)R6, -NH(CH2)mC(=O)N(R5)2, -NH(CHR9)nC(=O)R6, -NH(CHR9)nC(=O)N(R8)2, -NH(CHR9)mC(=O)R6, -NH(C(R9)2)nR10, -NH(CH2)nR6, -NH(CHR9)nR6, -NH(CHR9)nCH2OR9, -NHCH2(CHR9)nOR9, -NH(CHR9)nOR9, -NR9(CH2)nOR9 eller -NHCH2(C(R9)2)nOR9;R2 er H, C1–C6-alkyl eller C1–C6-halogenalkyl;R3 er H, C1–C6-alkyl eller -CD3;R4 er H, NH2, C1–C6-alkyl eller halogen;hver R5 uavhengig er C1–C6-alkyl, -CD3 eller -(CH2)nOR9;R6 er et C3–C6sykloalkyl eller et 4-6-leddet heterosykloalkyl som har 1 til 2 ringelementer som er uavhengig valgt blant N, NH, NR16 og O som er usubstituert eller er substituert med 1–2 R12-grupper;hver R8 er uavhengig valgt blant C1–C6-halogenalkyl, -(C(R9)2)nOR9 og et C1–C6-alkyl som er substituert med 1 til 3 -OH;hver R9 er uavhengig valgt blant H og C1–C6-alkyl;R10 er C1–C6-alkoksy eller C3–C6-sykloalkyl; hver R12 er uavhengig valgt blant C1–C6-alkyl, hydroksyl, halogen og et C1–C6-alkyl som er substituert med 1 til 3 -OH;R13 er H eller C1–C6-alkyl;R14 er H eller C1–C6-alkyl;hver R16 er C1–C6-alkyl;hver R17 uavhengig er H eller C1–C6-alkyl;hver R18 uavhengig er halogen, -CN, C1–C6-alkoksy eller C1–C6-alkyl;m er 1, 2, 3, 4, 5 eller 6, ogn er 1, 2, 3, 4, 5 eller 6.9. Forbindelse ifølge et av kravene 1 til 4, eller farmasøytisk akseptabelt salt av dette, der: L er -CH2- eller -CH2CH2-;Y1 er -CH2- eller -CH2CH2-;Y2 er -CH2- eller -CH2CH2-;Y3 er -CH2- eller -XCH2-;X er -CH2- eller O;R1 er -NHR6, -NR5R6, -NH2, -N(R5)2, -NHR5, -NHR8, -N(R6R8) eller -N(R6)2;R2 er H, C1–C6-alkyl eller C1–C6-halogenalkyl;R3 er H, C1–C6-alkyl eller -CD3;R4 er H, NH2, C1–C6-alkyl eller halogen;hver R5 uavhengig er C1–C6-alkyl, -CD3 eller -(CH2)nOR9;R6 er et C3–C6-sykloalkyl eller et 4–6-leddet heterosykloalkyl som har 1 til 2 ringelementer som er uavhengig valgt blant N, NH, NR16 og O som er usubstituert eller er substituert med 1–2 R12-grupper;hver R8 er uavhengig valgt blant C1–C6-halogenalkyl, -(C(R9)2)nOR9 og et C1–C6-alkyl som er substituert med 1 til 3 -OH;hver R12 er uavhengig valgt blant C1–C6-alkyl, hydroksyl, halogen og et C1–C6-alkyl som er substituert med 1 til 3 -OH;R13 er H eller C1–C6-alkyl;R14 er H eller C1–C6-alkyl;hver R16 er C1–C6-alkyl;hver R17 uavhengig er H eller C1–C6-alkyl;hver R18 uavhengig er halogen, -CN, C1–C6-alkoksy eller C1–C6-alkyl; m er 1, 2, 3, 4, 5 eller 6, ogn er 1, 2, 3, 4, 5 eller 6.10. Forbindelse ifølge et av kravene 1 til 9, eller farmasøytisk akseptabelt salt av dette, der R6 er et usubstituert 4–6-leddet heterosykloalkyl som har 1 til 2 ringelementer som er uavhengig valgt blant N, NH og O.11. Forbindelse ifølge et av kravene 1 til 9, eller farmasøytisk akseptabelt salt av dette, der R6 er syklobutyl, oksetanyl, piperidinyl, pyrrolidinyl, morfolinyl eller azetadinyl.12. Forbindelse ifølge krav 1, eller farmasøytisk akseptabelt salt av dette, valgt blant:4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((3-metyl-5-(6-metyl-1H-pyrazol[3,4-b]pyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((3-metyl-5-(2-metyl-1,7-naftyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((3-metyl-5-(2-metyl-7H-pyrrol[2,3-d]pyrimidin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((5-(1,6-dimetyl-1H-pyrrol[2,3-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)oksetan-3-amin;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(dimetylamino)acetamid; (S)-N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin-3-karboksamid;(R)-N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin-3-karboksamid;6-(4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-oksa-6-azaspiro[3.3]heptan; 4-(1-((4-aminobisyklo[2.2.2]oktan-1-yl)metyl)-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1-metyl-1H-pyrazol[3,4-d]pyrimidin-6-amin; 4-(2-((4-aminobisyklo[2.2.2]oktan-1-yl)metyl)-6,7-dihydro-2H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1-metyl-1H-pyrazol[3,4-d]pyrimidin-6-amin;4-(1-((4-aminobisyklo[2.2.2]oktan-1-yl)metyl)-3-metyl-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1-metyl-1H-pyrazol[3,4-d]pyrimidin-6-amin;4-(2-((4-aminobisyklo[2.2.2]oktan-1-yl)metyl)-3-metyl-6,7-dihydro-2H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1-metyl-1H-pyrazol[3,4-d]pyrimidin-6-amin;4-((5-(5-klor-1-metyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;1,6-dimetyl-4-(3-metyl-1-((4-(pyrrolidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1H-pyrazol[3,4-d]pyrimidin;1,3,5-trimetyl-7-(3-metyl-1-((4-(pyrrolidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1H-pyrazol[4,3-d]pyrimidin;N-(2-metoksyetyl)-4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin; 4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-d]pyrimidin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin;2-(etylamino)-N-(4-((3-metyl-5-(6-metyl-1H-pyrazol[3,4-d]pyrimidin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)acetamid;4-(4-((3-metyl-5-(6-metyl-1H-pyrazol[3,4-d]pyrimidin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin;2-(etylamino)-N-(4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)acetamid;4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-(oksetan-3-ylmetyl)bisyklo[2.2.2]oktan-1-amin; 3-(dimetylamino)-N-(4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)propanamid;4-(4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin;4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;N-syklobutyl-4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin; N,N-disyklobutyl-4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;6-metyl-4-(3-metyl-1-((4-(piperidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1H-pyrazol[3,4-d]pyrimidin;6-metyl-4-(3-metyl-1-((4-(pyrrolidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1H-pyrazol[3,4-d]pyrimidin;(3-(((4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)amino)metyl)oksetan-3-yl)metanol;N-(4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)azetidin-3-karboksamid;(S)-N-(4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin-3-karboksamid; (S)-N-(4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin-2-karboksamid; (R)-N-(4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin-3-karboksamid; (R)-N-(4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin-2-karboksamid; 3,6-dimetyl-4-(3-metyl-1-((4-morfolinbisyklo[2.2.2]oktan-1-yl)metyl)-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)isoksazol[5,4-d]pyrimidin;1,3,5-trimetyl-7-(3-metyl-1-((4-(piperidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1H-pyrazol[4,3-d]pyrimidin;1,6-dimetyl-4-(3-metyl-1-((4-(piperidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1H-pyrazol[3,4-d]pyrimidin;4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N,N-bis(trideuterometyl)bisyklo[2.2.2]oktan-1-amin; 4-((3-metyl-5-(1H-pyrazol[3,4-b]pyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((3-metyl-5-(1H-pyrazol[3,4-b]pyridin-4-yl)-4,5,6,7-tetrahydro-2H-pyrazol[4,3-c]pyridin-2-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N,N-dimetylbisyklo[2.2.2]oktan-1-amin; 4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.1]heptan-1-amin;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-(trifluormetyl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-ol;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)acetamid;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)metansulfonamid;tert-butyl(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)(metyl)karbamat;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-metylbisyklo[2.2.2]oktan-1-amin;1-metylsyklopropyl(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)karbamat;3-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-2H-pyrazol[4,3-c]pyridin-2-yl)metyl)bisyklo[1.1.1]pentan-1-amin;4-((5-(1-(4-metoksybenzyl)-6-metyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;N-syklobutyl-4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-isopropylbisyklo[2.2.2]oktan-1-amin;2-((4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)amino)propan-1-ol;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-etylbisyklo[2.2.2]oktan-1-amin;5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-1-((4-(pyrrolidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin;4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin; 4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-7,7-dimetyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;N-(2,2-difluoretyl)-4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;-((3-metyl-5-(2-metylkinolin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((3-metyl-5-(2-fenylpyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;1-((4-(azetidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-7,7-dimetyl-4,5,6,7-tetrahydro-2H-pyrazol[4,3-c]pyridin-2-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)tiomorfolin-1,1-dioksid;5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-1-((4-(piperidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin;1-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)azetidin-3-ol;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-(2-metoksyetyl)bisyklo[2.2.2]oktan-1-amin;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N,N-bis(2-metoksyetyl)bisyklo[2.2.2]oktan-1-amin; 4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-(2-etoksyetyl)bisyklo[2.2.2]oktan-1-amin;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N,N-bis(2-etoksyetyl)bisyklo[2.2.2]oktan-1-amin; 4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-(2-metoksyetyl)-N-metylbisyklo[2.2.2]oktan-1-amin; (3S,4R)-1-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)pyrrolidin-3,4-diol;(S)-1-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)pyrrolidin-3-ol; 2-((4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)amino)-N,N-dimetylacetamid; N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-N-metyloksetan-3-amin; 4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-isopropyl-N-metylbisyklo[2.2.2]oktan-1-amin; N-syklobutyl-4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-metylbisyklo[2.2.2]oktan-1-amin; (3S,4S)-1-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)pyrrolidin-3,4-diol;1-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-2-oksabisyklo[2.2.2]oktan-4-amin;5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-1-((4-(pyrrolidin-1-yl)-2-oksabisyklo[2.2.2]oktan-1-yl)metyl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin;4-((5-(6-(4-fluorfenyl)-1-metyl-1H-pyrazol[3,4-d]pyrimidin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-(4-(1-((4-aminobisyklo[2.2.2]oktan-1-yl)metyl)-3-metyl-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)pyridin-2-yl)benzonitril;3-metyl-5-(2-fenylpyridin-4-yl)-1-((4-(pyrrolidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin;2-metyl-4-(3-metyl-1-((4-(pyrrolidin-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-6,7-dihydro-1H-pyrazol[4,3-c]pyridin-5(4H)-yl)-1,7-naftyridin;4-((5-(2-(4-fluorfenyl)pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((5-(2-(2-fluor-4-metylfenyl)pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((5-(2-(4-metoksyfenyl)pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((3-metyl-5-(2-(p-tolyl)pyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-(2-(5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)etyl)bisyklo[2.2.2]oktan-1-amin; 4-((5-(2,8-dimetyl-1,7-naftyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((3-metyl-5-(2-metyl-6-fenylpyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-((5-([2,2'-bipyridin]-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-1-((4-(piperidin-1-yl)-2-oksabisyklo[2.2.2]oktan-1-yl)metyl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-(1-metoksypropan-2-yl)bisyklo[2.2.2]oktan-1-amin; 4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-etyl-N-metylbisyklo[2.2.2]oktan-1-amin;1-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N,N-dimetyl-2-oksabisyklo[2.2.2]oktan-4-amin;2-((4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)amino)-1-(piperidin-1-yl)etanon;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(pyrrolidin-1-yl)acetamid; 4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-(2-metoksy-2-metylpropyl)bisyklo[2.2.2]oktan-1-amin;1-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-N-(2-metoksyetyl)-2-oksabisyklo[2.2.2]oktan-4-amin; 4-((5-(2-klor-5,7-dihydrofuro[3,4-d]pyrimidin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-1-metylpiperazin-2-on;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-3-(dimetylamino)propanamid; 2-((4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)amino)-1-(pyrrolidin-1-yl)etanon; (R)-4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-metylmorfolin;1-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-4-metylpiperazin-2-on;(S)-4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-metylmorfolin;(2S,6R)-4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2,6-dimetylmorfolin;(2S,6S)-4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2,6-dimetylmorfolin;N-(syklobutylmetyl)-1-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-2-oksabisyklo[2.2.2]oktan-4-amin;(2R,6R)-4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2,6-dimetylmorfolin;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(etylamino)acetamid;3-amino-N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)propanamid;6-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-oksa-6-azaspiro[3.3]heptan; (R)-N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(metylamino)propanamid; (S)-N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(metylamino)propanamid; 1-((4-(1H-imidazol-1-yl)bisyklo[2.2.2]oktan-1-yl)metyl)-5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin;(1R,5S)-3-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-8-oksa-3-azabisyklo[3.2.1]oktan;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(metylamino)acetamid; N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-4-metylmorfolin-3-karboksamid;1-((4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)amino)-2-metylpropan-2-ol; 2-(etylamino)-N-(4-((3-metyl-5-(5-metyl-1H-pyrazol[4,3-b]pyridin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)acetamid;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin-2-karboksamid;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-3-(etylamino)propanamid; N-etyl-4-((3-metyl-5-(2-fenylpyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;(S)-4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-3-metylmorfolin;(R)-4-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-3-metylmorfolin;N-(2-metoksyetyl)-4-((3-metyl-5-(2-fenylpyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)azetidin-3-karboksamid;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(etyl(metyl)amino)acetamid; N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(3-fluorazetidin-1-yl)acetamid;2-(bis(trideuterometyl)amino)-N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)acetamid;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-hydroksyacetamid; N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(3-hydroksyazetidin-1-yl)acetamid;(3-(((4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)amino)metyl)oksetan-3-yl)metanol;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(N-metylmetylsulfonamido)acetamid;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(N-metylacetamido)acetamid 4-((3-metyl-5-(6-metyl-1-(trideuterometyl)-1H-pyrazol[3,4-b]pyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;(S)-N-(4-((5-(1-etyl-6-metyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin-3-karboksamid; N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-3-(metylamino)propanamid; N-syklobutyl-1-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)-2-oksabisyklo[2.2.2]oktan-4-amin;N-syklobutyl-4-((3-metyl-5-(2-fenylpyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin;tert-butyl(4-((5-(1-etyl-6-metyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)karbamat; tert-butyl(4-((3-metyl-5-(2-metyl-7H-pyrrol[2,3-d]pyrimidin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)karbamat;tert-butyl(4-((3-metyl-5-(2-metyl-1,7-naftyridin-4-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)karbamat;tert-butyl(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.1]heptan-1-yl)karbamat;4-((5-(1,6-dimetyl-1H-pyrazol[3,4-d]pyrimidin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin og4-((5-(1-etyl-6-metyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-amin. 13. Forbindelse ifølge krav 1, eller farmasøytisk akseptabelt salt av dette, valgt blant:N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)oksetan-3-amin;N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-(dimetylamino)acetamid; (S)-N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin-3-karboksamid;(R)-N-(4-((5-(1,6-dimetyl-1H-pyrazol[3,4-b]pyridin-4-yl)-3-metyl-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)morfolin-3-karboksamid og 6-(4-((3-metyl-5-(1,3,5-trimetyl-1H-pyrazol[4,3-d]pyrimidin-7-yl)-4,5,6,7-tetrahydro-1H-pyrazol[4,3-c]pyridin-1-yl)metyl)bisyklo[2.2.2]oktan-1-yl)-2-oksa-6-azaspiro[3.3]heptan.14. Farmasøytisk sammensetning som omfatter en terapeutisk effektiv mengde av en forbindelse ifølge et av kravene 1 til 13, eller et farmasøytisk akseptabelt salt av dette, og en farmasøytisk akseptabel bærer.15. Forbindelse ifølge et av kravene 1 til 13, eller farmasøytisk akseptabelt salt av dette, til bruk for å behandle en autoimmun sykdom.16. Forbindelse til bruk ifølge krav 15, eller farmasøytisk akseptabelt salt av dette, der den autoimmune sykdommen er systemisk lupus erythematosus, kutan lupus, diskoid lupus, blandet bindevevssykdom, primær biliær cirrhose, immunologisk trombocytopeni, hidradenitis suppurativa, dermatomyositt, polymyositt, Sjögrens syndrom, artritt, revmatoid artritt eller psoriasis.17. Kombinasjon som omfatter en terapeutisk effektiv mengde av en forbindelse ifølge et av kravene 1 til 13, eller et farmasøytisk akseptabelt salt av dette, og ett eller flere ytterligere terapeutiske midler, der det ytterligere terapeutiske middelet er uavhengig valgt blant betennelseshemmende midler, immunmodulerende midler, immunsupprimerende midler, cytokiner, ikke-steroide betennelsesdempende midler (NSAID-er), antimalariamidler, antirevmatiske midler, hemmere for B-celleaktiverende faktor (BAFF), hemmere for B-lymfocyttstimulator (BLyS), og steroidhormoner.
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Novartis AG
Lichtstrasse 35 4056 Basel CH

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ALPER, Phillip
Novartis Institute for Functional Genomics Inc.DBA Genomics Institute of the NovartisResearch Foundation10675 John Jay Hopkins Drive San Diego, California 92121 US
DEANE, Jonathan
Novartis Institute for Functional Genomics Inc.DBA Genomics Institute of the NovartisResearch Foundation10675 John Jay Hopkins Drive San Diego, California 92121 US
JIANG, Songchun
Novartis Institute for Functional Genomics Inc.DBA Genomics Institute of the NovartisResearch Foundation10675 John Jay Hopkins Drive San Diego, California 92121 US
JIANG, Tao
Novartis Institute for Functional Genomics Inc.DBA Genomics Institute of the NovartisResearch Foundation10675 John Jay Hopkins Drive San Diego, California 92121 US
KNOEPFEL, Thomas
Novartis Pharma AGSt. JohannPostfach 4002 Basel CH
MICHELLYS, Pierre-Yves
Novartis Institute for Functional Genomics Inc.DBA Genomics Institute of the NovartisResearch Foundation10675 John Jay Hopkins Drive San Diego, California 92121 US
MUTNICK, Daniel
Novartis Institutes for Biomedical Research Inc.5300 Chiron Way Emeryville, California 94608 US
PEI, Wei
Novartis Institute for Functional Genomics Inc.DBA Genomics Institute of the NovartisResearch Foundation10675 John Jay Hopkins Drive San Diego, California 92121 US
SYKA, Peter
Novartis Institute for Functional Genomics Inc.DBA Genomics Institute of the NovartisResearch Foundation10675 John Jay Hopkins Drive San Diego, California 92121 US
ZHANG, Guobao
c/o 279 Wenjing roadMinhang District Shanghai 200245 CN
ZHANG, Yi
171 School Street Belmont, Massachusetts 02478 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: V352464NO00
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Kilde: Brønnøysundregistrene
Fullmektig i EP:
Brennan, Méabh Bridget
Novartis Pharma AG Patent Department Postfach 4002 Basel CH

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2016.09.09, US 201662385726 P

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WO-A1-2013/117615 (B1)

WO-A1-2007/022280 (B1)

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Kapitler uten data er fjernet. Melding opprettet: 21.05.2025 05:36:11