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Tittel SOMATOSTATIN MODULATORS AND USES THEREOF
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Detaljstatus 		I kraft info EP patent gjort gjeldende i Norge EP patent besluttet gjeldende i Norge
Patentnummer NO/EP3484865
Europeisk (EP) publiserings nummer EP3484865
EP levert
EP søknadsnummer 17828375.0
EP meddelt
Prioritet 2016.07.14, US 201662362493 P, .... se mer/flere nedenfor
Sakstype Europeisk
Løpedag
Utløpsdato
Allment tilgjengelig
Validert i Norge
Innehaver Crinetics Pharmaceuticals, Inc. (US)
Oppfinner ZHAO, Jian (US) .... se mer/flere nedenfor
Fullmektig BRYN AARFLOT AS (NO)
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Patentkrav1. Forbindelse som har følgende struktur, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav:hvori:hver Ra er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -CH2OH eller -CH2CH2OH;hver Rb er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3 eller -OCF3;m er 1 eller 2; n er 0, 1 eller 2;hver Rc er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2CH3, -CH2CH2CH3, -CH(CH3)2, -CH2CH2CH2CH3, -CH2CH(CH3)2, -CH(CH3)(CH2CH3), -C(CH3)3, -CH2OH, -CH2CN, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCH2CH3, -OCF3, -CO2H, -CO2CH3, -CO2CH2CH3, -CH2CO2H, -CH2CO2CH3, -CH2CO2CH2CH3, -C(=O)NH2, -C(=O)NHCH3, -C(=O)NHOCH3, -C(=O)N(CH3)2, -SO2N(CH3)2, -C(=NOCH3)H, -CH2C(=O)NH2, -CH2C(=O)NHCH3, -CH2C(=O)N(CH3)2, -NH2, -NHCH3, -N(CH3)2, -NHCO2CH3, -NHSO2CH3, -CH2NH2, -CH2NHCH3, -CH2N(CH3)2, -CH(CF3)NH2, azetidinyl eller pyrrolidinyl;hver Rd er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2CH3, -CH2CH2CH3, -CH(CH3)2, -CH2CH2CH2CH3, -CH2CH(CH3)2, -CH(CH3)(CH2CH3), -C(CH3)3, -CH2OH, -CH2CN, -CH2F, -CHF2, -CF3, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, -CN, -OH, -OCH3, -OCH2CH3, -OCF3, -OCH2OCH3, -OCH2OCH2CH3, -OCH2CH2OH, -C(=O)NHOCH3, -C(=NOH)H, -C(=NOCH3)H, -CH2C(=O)NH2, -NH2, -NHCO2CH3, -NHSO2CH3, -NH(C=O)NHCH3, -NH(C=O)NHOCH3 eller -CH(CF3)NH2; eller dersom en Rc og en Rd er på tilstøtende atomer av RB, blir de tilstøtende Rc- og Rd-gruppene tatt sammen med de mellomliggende atomene som de er festet til for å danne en 5-eller 6-leddet monosyklisk heterosyklisk ring;p er 1 eller 2; q er 0, 1 eller 2;X er CRf eller N;Y er CRf eller N;Z er CRf eller N;Re er hydrogen, F, Cl, Br, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCH2CH3 eller -OCF3;hver Rf er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCH2CH3 eller -OCF3;R1 er hydrogen;R2 er hydrogen, metyl, etyl, 2-fluoretyl, 2-hydroksyetyl, 2-metoksyetyl, n-propyl, ipropyl, syklopropyl, 3-fluorpropyl, 3-metoksypropyl, n-butyl, i-butyl, sek-butyl, syklobutyl, tert-butyl eller oksetanyl;R5 er hydrogen, F, Cl, Br, -OH, -OCH3, -NH2, -NHCH3, -N(CH3)2, -OCH2CH3, -OCF3, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -C(=O)OCH3, -C(=O)NH2, -C(=O)NHCH3 eller -C(=O)N(CH3)2;eller R2 og R5 blir tatt sammen med de mellomliggende atomene som de er festet til for å danne et azetidinyl, pyrrolidinyl, piperidinyl, morfolinyl, tiomorfolinyl, piperazinyl eller azepanyl.2. Forbindelsen ifølge krav 1, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav, hvori:hver Ra er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -CH2OH eller -CH2CH2OH;hver Rb er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3 eller -OCF3;hver Rc er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -NH2, -C(=O)NH2, -C(=NOCH3)H, -SO2N(CH3)2, azetidinyl eller pyrrolidinyl;hver Rd er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -OCH2OCH3, -CH2OH, -OCH2CH2OH, -C(=O)NHOCH3, -NH2, -NHCO2CH3, -NH(C=O)NHOCH3 eller -CH2C(=O)NH2; eller hvis en Rc og en Rd er på tilstøtende atomer av RB, blir de tilstøtende Rc- og Rd-gruppene tatt sammen med de mellomliggende atomene som de er festet til for å danne 5-leddet monosyklisk heterosyklisk ring.3. Forbindelsen ifølge krav 1 eller krav 2, hvori forbindelsen har følgende struktur, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav:.4. Forbindelsen ifølge et hvilket som helst av kravene 1 til 3, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav, hvori: hver Ra er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -CH2OH eller -CH2CH2OH;hver Rb er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3 eller -OCF3;hver Rc er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -NH2, -C(=O)NH2, -C(=NOCH3)H, -SO2N(CH3)2, azetidinyl eller pyrrolidinyl;hver Rd er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -OCH2OCH3, -CH2OH, -OCH2CH2OH, -C(=O)NHOCH3, -NH2, -NHCO2CH3, -NH(C=O)NHOCH3 eller -CH2C(=O)NH2;Re er hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3 eller -OCF3; hver Rf er hydrogen;R1 er hydrogen;R2 er hydrogen;R5 er hydrogen, F, Cl, Br, -OH, -OCH3, -NH2, -NHCH3, -N(CH3)2, -OCH2CH3, -OCF3, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -C(=O)OCH3, -C(=O)NH2, -C(=O)NHCH3 eller -C(=O)N(CH3)2; eller R2 og R5 blir tatt sammen med de mellomliggende atomene som de er festet til for å danne et piperidinyl, morfolinyl, tiomorfolinyl eller piperazinyl.5. Forbindelsen ifølge et hvilket som helst av kravene 1 til 4, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav, hvori: hver Ra er uavhengig hydrogen, F, Cl, -CH3, -CF3, -CN, -OH, -OCH3, -OCF3, -CH2OH eller -CH2CH2OHhver Rb er uavhengig hydrogen, F, Cl, -CH3, -CF3, -CN, -OH, -OCH3 eller -OCF3; hver Rc er uavhengig hydrogen, F, Cl, -CH3, -CF3, -CN, -OH, -OCH3 eller -OCF3; hver Rd er uavhengig hydrogen, F, Cl, -CH3, -CF3, -CN, -OH, -OCH3, -OCF3 eller -NH2; X er CRf; Y er CRf; og Z er CRf;eller X er N; Y er CRf; og Z er CRf;eller X er CRf; Y er N; og Z er CRf;eller X er CRf; Y er CRf; og Z er N;Re er hydrogen, F eller Cl;hver Rf er hydrogen;R1 er hydrogen;R2 er hydrogen;R5 er hydrogen;eller R2 og R5 blir tatt sammen med de mellomliggende atomene som de er festet til for å danne et morfolinyl.6. Forbindelsen ifølge et hvilket som helst av kravene 1 til 3, hvori forbindelsen har følgende struktur av formel (AVb), eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav:Formel (AVb)hvori: R1 er hydrogen;R2 er hydrogen, metyl, etyl, 2-fluoretyl, 2-hydroksyetyl, 2-metoksyetyl, n-propyl, ipropyl, syklopropyl, 3-fluorpropyl, 3-metoksypropyl, n-butyl, i-butyl, sek-butyl, syklobutyl, tert-butyl eller oksetanyl;R5 er hydrogen, F, Cl, Br, -OH, -OCH3, -NH2, -NHCH3, -N(CH3)2, -OCH2CH3, -OCF3, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -C(=O)OCH3, -C(=O)NH2, -C(=O)NHCH3 eller -C(=O)N(CH3)2;eller R2 og R5 blir tatt sammen med de mellomliggende atomene som de er festet til for å danne et azetidinyl, pyrrolidinyl, piperidinyl, morfolinyl, tiomorfolinyl, piperazinyl eller azepanyl.7. Forbindelsen ifølge krav 6, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav, hvori:Ra er hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -CH2OH eller -CH2CH2OH;Rb er hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3 eller -OCF3; hver Rc er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -NH2, -C(=O)NH2, -C(=NOCH3)H, -SO2N(CH3)2, azetidinyl eller pyrrolidinyl;hver Rd er uavhengig hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -OCH2OCH3, -CH2OH, -OCH2CH2OH, -C(=O)NHOCH3, -NH2, -NHCO2CH3, -NH(C=O)NHOCH3 eller -CH2C(=O)NH2;Re er hydrogen, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3 eller -OCF3; R1 er hydrogen;R2 er hydrogen;R5 er hydrogen, F, Cl, Br, -OH, -OCH3, -NH2, -NHCH3, -N(CH3)2, -OCH2CH3, -OCF3, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -C(=O)OCH3, -C(=O)NH2, -C(=O)NHCH3 eller -C(=O)N(CH3)2;eller R2 og R5 blir tatt sammen med de mellomliggende atomene som de er festet til for å danne et piperidinyl, morfolinyl, tiomorfolinyl eller piperazinyl. 8. Forbindelsen ifølge krav 6 eller krav 7, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav, hvori:Ra er hydrogen, F, Cl, -CH3, -CF3, -CN, -OH, -CH2OH, -CH2CH2OH, -OCH3 eller -OCF3;Rb er hydrogen, F, Cl, -CH3, -CF3, -CN, -OH, -OCH3 eller -OCF3;hver Rc er uavhengig hydrogen, F, Cl, -CH3, -CF3, -CN, -OH, -NH2, -OCH3, -OCF3, -CONH2 eller -C(=NOCH3)H;hver Rd er uavhengig hydrogen, F, Cl, -CH3, -CF3, -CN, -OH, -NH2, -OCH3 eller -OCF3; R1 er hydrogen;R2 er hydrogen;R5 er hydrogen;eller R2 og R5 blir tatt sammen med de mellomliggende atomene som de er festet til for å danne et morfolinyl.9. Forbindelsen ifølge krav 1, hvori forbindelsen er:1-1: 3-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3,5-dimetylfenyl)cinnolin-6-yl]-5-fluorbenzamid;1-2: 3-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3,5-dimetylfenyl)cinnolin-6-yl]-2-hydroksybenzonitril;1-4: 3-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3-fluor-5-metylfenyl)cinnolin-6-yl]-5-fluorbenzamid;1-5: 3-{4-[trans-4-amino-3-fluorpiperidin-1-yl]-7-klor-3-(3-fluor-5-metylfenyl)cinnolin-6-yl}-5-fluorbenzamid;1-6: 3-{4-[cis-4-amino-3-fluorpiperidin-1-yl]-7-klor-3-(3-fluor-5-metylfenyl)cinnolin-6-yl}-5-fluorbenzamid;1-7: 3-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3-fluor-5-metylfenyl)cinnolin-6-yl]-2-hydroksybenzonitril;1-8: 5-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3-fluor-5-metylfenyl)cinnolin-6-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-on;1-9: 4-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3-fluor-5-metylfenyl)cinnolin-6-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-on;1-10: 3-{4-[trans-4-amino-3-metoksypiperidin-1-y1]-7-klor-3-(3-fluor-5-metylfenyl)cinnolin-6-yl}-5-fluorbenzamid; 1-11: 3-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3,5-diklorfenyl)cinnolin-6-yl]-2-hydroksybenzonitril;1-12: 3-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3-klor-5-metylfenyl)cinnolin-6-yl]-5-fluor-2-hydroksybenzonitril;1-13: 3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)cinnolin-6-yl]-5-fluorbenzamid;1-14: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)cinnolin-6-yl]-5-fluorbenzamid;1-16: 5-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)cinnolin-6-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-on;1-17: 3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)cinnolin-6-yl]-2-hydroksybenzonitril;1-18: 3-[4-(4-aminopiperidin-1-yl)-3-(3-klor-5-metylfenyl)cinnolin-6-yl]-2-hydroksybenzonitril;1-19: 3-[4-(4-aminopiperidin-1-yl)-3-(3-klor-5-fluorfenyl)cinnolin-6-yl]-2-hydroksybenzonitril;1-20: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)cinnolin-6-yl]-2-hydroksybenzonitril;1-21: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-diklorfenyl)cinnolin-6-yl]-2-hydroksybenzonitril;1-22: 3-[4-(4-aminopiperidin-1-yl)-3-(3-klor-5-metylfenyl)cinnolin-6-yl]-5-fluor-2-hydroksybenzonitril;1-23: 6-[4-(4-aminopiperidin-1-yl)-3-(3-klor-5-metylfenyl)cinnolin-6-yl]-4-fluor-2,3-dihydro-1H-1,3-benzodiazol-2-on;1-24: 4-[4-(4-aminopiperidin-1-yl)-3-(3-klor-5-metylfenyl)cinnolin-6-yl]-6-fluor-2,3-dihydro-1H-1,3-benzodiazol-2-on;1-25: 3-[7-klor-3-(3-fluor-5-metylfenyl)-4-{4-[(2-fluoretyl)amino]piperidin-1-yl}cinnolin-6-yl]-5-fluorbenzamid;1-26: 3-{4-[trans-4-amino-3-hydroksypiperidin-1-yl]-7-klor-3-(3-fluor-5-metylfenyl)cinnolin-6-yl}-5-fluorbenzamid;1-27: 3-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3,5-diklorfenyl)cinnolin-6-yl]-5-fluor-2-hydroksybenzonitril;1-28: 6-[4-(4-aminopiperidin-1-yl)-3-(3,5-diklorfenyl)cinnolin-6-yl]-4-fluor-2,3-dihydro-1H-1,3-benzodiazol-2-on;1-29: 2-[4-(4-aminopiperidin-1-yl)-3-(3-klor-5-metylfenyl)cinnolin-6-yl]-6-fluorfenol; 1-30: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-diklorfenyl)cinnolin-6-yl]-5-fluorbenzamid;1-31: 3-[3-(3,5-diklorfenyl)-4-{4-[(oksetan-3-yl)amino]piperidin-1-yl}cinnolin-6-yl]-5-fluorbenzamid;1-33: 3-[3-(3,5-diklorfenyl)-4-{4-[(2-fluoretyl)amino]piperidin-1-yl}cinnolin-6-yl]-5-fluorbenzamid;1-35: 3-[7-klor-3-(3-klor-5-metylfenyl)-4-{4-[(2-fluoretyl)amino]piperidin-1-yl}cinnolin-6-yl]-5-fluorbenzamid;1-36: 3-[7-klor-3-(3-klor-5-metylfenyl)-4-{4-[(2-fluoretyl)amino]piperidin-1-yl}cinnolin-6-yl]-5-fluor-2-hydroksybenzonitril;1-38: 3-[7-klor-3-(3-klor-5-metylfenyl)-4-{4-[(oksetan-3-yl)amino]piperidin-1-yl}cinnolin-6-yl]-5-fluorbenzamid;1-39: 3-[7-klor-3-(3-klor-5-metylfenyl)-4-{4-[(oksetan-3-yl)amino]piperidin-1-yl}cinnolin-6-yl]-5-fluor-2-hydroksybenzonitril;1-40: 3-[3-(3-klor-5-metylfenyl)-4-{4-[(oksetan-3-yl)amino]piperidin-1-yl}cinnolin-6-yl]-5-fluor-2-hydroksybenzonitril;1-41: 3-{4-[trans-4-amino-3-fluorpiperidin-1-yl]-7-klor-3-(3-klor-5-metylfenyl)cinnolin-6-yl}-5-fluorbenzamid;1-42: 6-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3-klor-5-metylfenyl)cinnolin-6-yl]pyridin-2-karboksamid;1-43: 6-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3-klor-5-metylfenyl)cinnolin-6-yl]-5-klorpyridin-2-karboksamid;1-44: 2-[4-(4-aminopiperidin-1-yl)-7-klor-3-(3-klor-5-metylfenyl)cinnolin-6-yl]pyridin-4-karboksamid;1-45: 2-[4-(4-aminopiperidin-1-yl)-3-(3-klor-5-metylfenyl)cinnolin-6-yl]-6-fluor-3-metylfenol;1-48: 3-{4-[cis-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-klor-5-metylfenyl)cinnolin-6-yl}-5-fluorbenzamid;1-49: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-klor-5-metylfenyl)cinnolin-6-yl}-5-fluorbenzamid;1-51: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-diklorfenyl)cinnolin-6-yl}-2-hydroksybenzonitril;1-52: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-klor-5-metylfenyl)cinnolin-6-yl}-2-hydroksybenzonitril; 1-53: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metylfenyl)cinnolin-6-yl}-2-hydroksybenzonitril;1-54: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)cinnolin-6-yl}-2-hydroksybenzonitril;1-55: 5-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)cinnolin-6-yl}-4-aminopyridin-3-karbonitril;1-56: 5-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metylfenyl)cinnolin-6-yl}-4-aminopyridin-3-karbonitril;1-57: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)cinnolin-6-yl}-3-aminopyridin-4-karbonitril;1-58: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metylfenyl)cinnolin-6-yl}-3-aminopyridin-4-karbonitril;eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav.10. Forbindelsen ifølge krav 1, hvori forbindelsen er:2-1: 3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-2-hydroksybenzonitril;2-2: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-2-hydroksybenzonitril;2-3: 3-{4-[trans-4-amino-3-metoksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-hydroksybenzonitril;2-4: 3-{4-[trans-4-amino-3-metoksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}benzonitril;2-5: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]benzonitril;2-6: 2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]fenol;2-7: 6-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]pyridin-2-karboksamid;2-8: 4-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-on;2-9: 5-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-on;2-10: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-5-fluor-2-hydroksybenzonitril; 2-16: 3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-fluor-2-hydroksybenzonitril;2-19: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-hydroksybenzonitril;2-20: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl }-2-hydroksybenzonitril;2-58: 3-{4-[cis-4-amino-3-hydroksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-(metoksymetoksy)benzonitril;2-59: 3-{4-[(3R,4R)-4-amino-3-fluorpiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-hydroksybenzonitril;2-60: 3-{4-[cis-4-amino-3-hydroksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-hydroksybenzonitril;2-61: 3-{4-[(3S,4R)-4-amino-3-metoksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-hydroksybenzonitril;2-62: 3-{4-[(3R,4S)-4-amino-3-metoksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-(metoksymetoksy)benzonitril;2-63: 3-{4-[cis-4-amino-3-hydroksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-5-fluor-2-hydroksybenzonitril;2-65: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-2-(2-hydroksyethoksy)benzonitril;2-66: 3-{4-[(3R,4S)-4-amino-3-metoksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-hydroksybenzonitril;2-75: 5-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-6-(azetidin-1-yl)pyridin-3-karbonitril;2-76: 5-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-6-(azetidin-1-yl)pyridin-3-karboksamid;2-77: 2-amino-3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]benzonitril;2-78: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-2-(metoksymetoksy)benzonitril;2-80: 6-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-fluor-2,3-dihydro-1H-1,3-benzodiazol-2-on;2-81: 2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-6-[-(metoksyimino)metyl]fenol; 2-83: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4,6-difluorfenyl}karbamat;2-84: 3-{4-[trans-4-amino-3-metoksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-(metoksymetoksy)benzonitril;2-85: 6-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}pyridin-2-karboksamid;2-86: N-{2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4,6-difluorfenyl}metansulfonamid;2-92: trans-4-amino-1-[6-(3-cyano-2-hydroksyfenyl)-3-(3,5-difluorfenyl)kinolin-4-yl]piperidin-3-karbonitril;2-94: cis-4-amino-1-[6-(3-cyano-2-hydroksyfenyl)-3-(3,5-difluorfenyl)kinolin-4-yl]piperidin-3-karbonitril;2-99: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4,5-difluor-2-hydroksybenzonitril;2-100: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4,5-difluor-2-hydroksybenzonitril;2-102: 3-{4-[trans-4-amino-3-metoksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4,5-difluor-2-hydroksybenzonitril;2-103: 3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-4,5-difluor-2-hydroksybenzonitril;2-104: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl}-4,5-difluor-2-hydroksybenzonitril;2-106: 3-{4-[trans-4-amino-3-metoksypiperidin-1-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl}-4,5-difluor-2-hydroksybenzonitril;2-107: 3-{4-[cis-4-amino-3-hydroksypiperidin-1-yl]-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl}-4,5-difluor-2-hydroksybenzonitril;2-108: 2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4,6-difluor-3-metylfenol;2-109: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4,6-difluor-3-metylfenol;2-111: 2-{4-[trans-4-amino-3-metoksypiperidin-1-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4,6-difluor-3-metylfenol;2-112: 2-{4-[trans-4-amino-3-metoksypiperidin-1-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl}-4,6-difluor-3-metylfenol; 2-113: cis-4-amino-1-[6-(3,5-difluor-2-hydroksy-6-metylfenyl)-3-(3-fluor-5-metoksyfenyl)kinolin-4-yl]piperidin-3-ol;2-114: 2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4-fluor-6-[(metoksyimino)metyl]fenol;2-115: 2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-6-[(metoksyimino)metyl]fenol;2-116: 2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-4-fluor-6-[(metoksyimino)metyl]fenol;2-117: 2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-3,4-difluor-6-[(metoksyimino)metyl]fenol;2-118: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl}-4-fluor-6-[(1E)-(metoksyimino)metyl]fenol;2-119: trans-4-amino-1-[6-(3-cyano-5,6-difluor-2-hydroksyfenyl)-3-(3,5-difluorfenyl)kinolin-4-yl]piperidin-3-karbonitril;2-120: cis-4-amino-1-[6-(3-cyano-5,6-difluor-2-hydroksyfenyl)-3-(3,5-difluorfenyl)kinolin-4-yl]piperidin-3-karbonitril;2-121: trans-4-amino-1-[6-(3-cyano-5,6-difluor-2-hydroksyfenyl)-3-(3-fluor-5-metylfenyl)kinolin-4-yl]piperidin-3-karbonitril;2-122: cis-4-amino-1-[6-(3-cyano-5,6-difluor-2-hydroksyfenyl)-3-(3-fluor-5-metylfenyl)kinolin-4-yl]piperidin-3-karbonitril;2-123: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-3,4,6-trifluorfenyl}karbamat;2-124: metyl-N-{3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-5-fluorpyridin-4-yl}karbamat;2-125: metyl-N-{3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-5-cyanopyridin-4-yl}karbamat;2-126: 1-[3-(3,5-difluorfenyl)-6-{3-fluor-2-[(hydroksyimino)metyl]fenyl}kinolin-4-yl]piperidin-4-amin;2-127: 1-(6-{3-klor-2-[(hydroksyimino)metyl]fenyl}-3-(3,5-difluorfenyl)kinolin-4-yl)piperidin-4-amin;2-128: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-2-[(hydroksyimino)metyl]benzonitril;2-129: 1-[3-(3,5-difluorfenyl)-6-{3-fluor-2-[(metoksyimino)metyl]fenyl}kinolin-4-yl]piperidin-4-amin; 2-130: 1-(6-{3-klor-2-[(metoksyimino)metyl]fenyl}-3-(3,5-difluorfenyl)kinolin-4-yl)piperidin-4-amin;2-131: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-2-[(1E)-(metoksyimino)metyl]benzonitril;2-132: 1-{6-[3-(1-amino-2,2,2-trifluoretyl)fenyl]-3-(3,5-difluorfenyl)kinolin-4-yl}piperidin-4-amin;2-133: 1-{6-[2-(1-amino-2,2,2-trifluoretyl)-3-fluorfenyl]-3-(3,5-difluorfenyl)kinolin-4-yl}piperidin-4-amin;2-134: 2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-6-klor-3,4-difluorfenol;2-135: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-6-klor-3,4-difluorfenol;2-136: 2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-6-klor-4-fluorfenol;2-137: 2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-6-klorfenol; 2-138: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-6-klorfenol;2-139: 1-{2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4,6-difluorfenyl}-3-metoksyurea;2-140: 1-(2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4,6-difluorfenyl)-3-metoksyurea;2-141: 6-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4-klor-2,3-dihydro-1H-1,3-benzodiazol-2-on;2-142: 5-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-2,3-dihydro-1,3-benzoksazol-2-on;2-143: metyl-trans-4-amino-1-[6-(3-cyano-2-hydroksyfenyl)-3-(3,5-difluorfenyl)kinolin-4-yl]piperidin-3-karboksylat;2-144: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-6-fluorfenol;2-146: trans-4-amino-1-[6-(3-cyano-2-hydroksyfenyl)-3-(3,5-difluorfenyl)kinolin-4-yl]piperidin-3-karboksamid;2-147: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-5-klor-4-fluor-2-hydroksybenzonitril; 2-148: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-6-cyanofenyl}karbamat;2-149: trans-4-amino-1-[6-(3-cyano-2-hydroksyfenyl)-3-(3,5-difluorfenyl)kinolin-4-yl]-N-metylpiperidin-3-karboksamid;2-150: 2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-3,4,6-trifluorfenol;2-151: trans-4-amino-1-[6-(3-cyano-2-hydroksyfenyl)-3-(3,5-difluorfenyl)kinolin-4-yl]-N,N-dimetylpiperidin-3-karboksamid;2-152: 1-[3-(3,5-difluorfenyl)-6-{5-fluor-4-[(hydroksyimino)metyl]pyridin-3-yl}kinolin-4-yl]piperidin-4-amin;2-153: N-[(2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-6-fluorfenyl)metyliden]hydroksylamin;2-154: N-[(2-{4-[(trans)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4,6-difluorfenyl)metyliden]hydroksylamin;2-155: N-[(2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl}-6-fluorfenyl)metyliden]hydroksylamin;2-156: 4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-[3-fluor-2-(1H-imidazol-2-yl)fenyl]-3-(3-fluor-5-metoksyfenyl)kinolin;2-157: 4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-[3-fluor-2-(1H-imidazol-5-yl)fenyl]-3-(3-fluor-5-metoksyfenyl)kinolin;2-158: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl}-4,5-difluor-2-hydroksybenzonitril;2-159: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl}-4,5-difluor-2-hydroksybenzonitril;2-160: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl}-3,4,6-trifluorfenol;2-161: 1-[3-(3-fluor-5-metoksyfenyl)-6-(2,3,5-trifluor-6-hydroksyfenyl)kinolin-4-yl]piperidin-4-ol;2-162: 1-{3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-5-hydroksypyridin-4-yl}-3-metoksyurea;2-163: 1-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl]-6-klorfenyl}-3-metoksyurea;2-164: 1-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl]-4,6-difluorfenyl}-3-metoksyurea; 2-165: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl]-4,6-difluorfenyl}karbamat;2-166: 1-(6-{3-fluor-2-[(hydroksyimino)metyl]fenyl}-3-(3-fluor-5-metoksyfenyl)kinolin-4-yl)piperidin-4-amin;2-167: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl]-6-cyanofenyl}karbamat;2-168: 1-(6-{5-fluor-4-[(hydroksyimino)metyl]pyridin-3-yl}-3-(3-fluor-5-metylfenyl)kinolin-4-yl)piperidin-4-amin;2-169: 3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-fluorpyridin-4-amin;2-170: metyl-(trans)-4-amino-1-[6-(3-cyano-2-hydroksyfenyl)-3-(3,5-difluorfenyl)kinolin-4-yl]piperidin-3-karboksylat;2-171: metyl-N-{3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-fluorpyridin-4-yl}karbamat;2-172: 1-{3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-fluorpyridin-4-yl}-3-metoksyurea;2-173: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl]-6-fluorfenyl}karbamat;2-174: 1-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metoksyfenyl)kinolin-6-yl]-6-fluorfenyl}-3-metoksyurea;2-176: 1-(6-{5-fluor-4-[(hydroksyimino)metyl]pyridin-3-yl}-3-[3-fluor-5-(trifluormetyl)fenyl]kinolin-4-yl)piperidin-4-amin;2-177: 4-amino-5-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]pyridin-3-karbonitril;2-178: 3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-fluorpyridin-2-amin;2-179: 2-amino-3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4,5-difluorbenzonitril;2-180: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-6-cyano-3,4-difluorfenyl}karbamat;2-181: 3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-klorpyridin-4-amin;2-182: metyl-N-{3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-fluorpyridin-2-yl}karbamat; 2-183: 1-{3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-fluorpyridin-2-yl}-3-metoksyurea;2-184: metyl-N-{3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-klorpyridin-4-yl}karbamat;2-185: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4-cyanofenyl}karbamat;2-186: 1-{3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-klorpyridin-4-yl}-3-metoksyurea;2-187: 4-amino-5-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]pyridin-3-karbonitril;2-189: 1-{2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4-cyanofenyl}-3-metoksyurea;2-190: 3-{4-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-hydroksybenzonitril;2-192: 1-(6-{5-klor-4-[(hydroksyimino)metyl]pyridin-3-yl}-3-(3,5-difluorfenyl)kinolin-4-yl)piperidin-4-amin;2-193: 3-{4-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-2-hydroksybenzonitril;2-194: 3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-5-fluor-2-(metoksymetoksy)benzonitril;2-195: 1-[3-(3,5-difluorfenyl)-6-{3-[(hydroksyimino)metyl]pyridin-2-yl}kinolin-4-yl]piperidin-4-amin;2-196: 1-[3-(3,5-difluorfenyl)-6-{2-[(hydroksyimino)metyl]pyridin-3-yl}kinolin-4-yl]piperidin-4-amin;2-197: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-4,6-difluorfenyl}karbamat;2-200: 1-[3-(3,5-difluorfenyl)-6-{6-[(hydroksyimino)metyl]pyridin-2-yl}kinolin-4-yl]piperidin-4-amin;2-202: 1-[3-(3,5-difluorfenyl)-6-{3-fluor-2-[(hydroksyimino)metyl]-6-metylfenyl}kinolin-4-yl]piperidin-4-amin;2-205: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-6-cyano-3,4-difluorfenyl}karbamat;2-207: 1-(2-{4-[cis-4-amino-3-metoksypiperidin-1-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl}-4,6-difluorfenyl)-3-metoksyurea; 2-208: 1-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-6-cyano-3,4-difluorfenyl}-3-metylurea;2-209: metyl-N-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-6-fluorfenyl}karbamat;2-213: 4-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-2-[(metoksyimino)metyl]fenol;2-215: 1-{3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-4-metylpyridin-2-yl}-3-metoksyurea;2-217: trans-1-(6-{3-fluor-2-[(hydroksyimino)metyl]fenyl}-3-(3-fluor-5-metylfenyl)kinolin-4-yl)-3-metoksypiperidin-4-amin;2-218: metyl-N-(2-{4-[trans-4-amino-3-metoksypiperidin-1-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl}-6-cyanofenyl)karbamat;2-219: cis-3-{4-[4-amino-3-hydroksypiperidin-1-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl}-5-fluor-2-hydroksybenzonitril;2-221: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl}-6-[(metoksyimino)metyl]fenol;2-222: 1-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-4-cyanofenyl}-3-metoksyurea;2-223: 1-{3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-5-fluorfenyl}-3-metoksyurea;2-226: 1-{3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]pyridin-2-yl}-3-metoksyurea;2-227: cis-4-amino-1-(6-{3-fluor-2-[(hydroksyimino)metyl]fenyl}-3-(3-fluor-5-metylfenyl)kinolin-4-yl)piperidin-3-ol;2-235: metyl-N-(2-{4-[trans-4-amino-3-metoksypiperidin-1-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl}-4,6-difluorfenyl)karbamat;2-236: 1-(2-{4-[trans-4-amino-3-metoksypiperidin-1-yl]-3-(3-fluor-5-metylfenyl)kinolin-6-yl}-4,6-difluorfenyl)-3-metoksyurea;2-237: 1-{2-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-4-cyano-6-fluorfenyl}-3-metoksyurea;2-239: 1-{3-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]-6-metylpyridin-2-yl}-3-metoksyurea;2-240: 1-{4-[4-(4-aminopiperidin-1-yl)-3-(3-fluor-5-metylfenyl)kinolin-6-yl]fenyl}-3-metoksyurea; 2-241: 2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-6-brom-3,4-difluorfenol;2-243: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-6-[(1E)-(metoksyimino)metyl]fenol;2-244: 5-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-aminopyridin-3-karbonitril;2-246: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}pyridin-2-amin;2-247: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-metylpyridin-3-amin;2-248: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}pyridin-2-ol;2-250: 2-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorfenyl)kinolin-6-yl]-4-metylpyridin-3-amin;2-251: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-3-hydroksypyridin-4-karbonitril;2-254: 5-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-hydroksypyridin-3-karbonitril;2-256: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-5-fluorpyridin-4-ol;2-258: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-metylpyridin-3-ol;2-259: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-5-fluorpyridin-2-ol;2-261: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-3-fluorpyridin-4-karbonitril;2-262: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-3-aminopyridin-4-karbonitril;2-263: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}pyridin-3-ol;2-264: N-[(3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}pyridin-2-yl)metyliden]hydroksylamin;2-265: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-5-fluorpyridin-3-amin; 2-266: 3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-5-[(metoksyimino)metyl]pyridin-4-amin;2-269: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-[(metoksyimino)metyl]pyridin-3-amin;2-273: 1-(3-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}pyridin-2-yl)-3-metoksyurea;2-275: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-klorpyridin-3-amin;2-283: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}pyridin-3-amin;2-284: 2-{4-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-metoksypyridin-3-amin;2-285: 2-{4-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-6-[(metoksyimino)metyl]fenol;2-286: 2-{4-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-6-[(metoksyimino)metyl]fenol;2-287: 2-{4-[(4aR,8aR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-[(metoksyimino)metyl]pyridin-3-amin;2-288: 2-{4-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-[(metoksyimino)metyl]pyridin-3-amin;2-289: 2-{4-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-3-aminopyridin-4-karbonitril;2-290: 2-{4-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-3-aminopyridin-4-karbonitril;2-291: (5-{4-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-aminopyridin-3-karbonitril;2-292: (5-{4-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-aminopyridin-3-karbonitril;2-293: 3-{4-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}pyridin-2-amin;2-294: 3-{4-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}pyridin-2-amin;2-295: 2-{4-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-metylpyridin-3-amin; 2-296: 2-{4-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-metylpyridin-3-amin;2-297: 2-{4-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-metylpyridin-3-ol;2-298: 2-{4-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-4-metylpyridin-3-ol;2-299: 3-{4-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-5-fluor-2-hydroksybenzonitril;2-300: 3-{4-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-3-(3,5-difluorfenyl)kinolin-6-yl}-5-fluor-2-hydroksybenzonitril;eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav.11. Forbindelsen ifølge krav 1, hvori forbindelsen er:3-1: 3-[8-(4-aminopiperidin-1-yl)-7-(3-fluor-5-metylfenyl)-1,5-naftyridin-2-yl]-5-fluorbenzamid;3-2: 3-[8-(4-aminopiperidin-1-yl)-7-(3-fluor-5-metylfenyl)-1,5-naftyridin-2-yl]-5-fluor-2-hydroksybenzonitril;3-3: 4-[8-(4-aminopiperidin-1-yl)-7-(3-fluor-5-metylfenyl)-1,5-naftyridin-2-yl]-6-fluor-2,3-dihydro-1H-1,3-benzodiazol-2-on;3-4: 5-[8-(4-aminopiperidin-1-yl)-7-(3-fluor-5-metylfenyl)-1,5-naftyridin-2-yl]-2,3-dihydro-1H-1,3-benzodiazol-2-on;3-5: 6-[8-(4-aminopiperidin-1-yl)-7-(3-fluor-5-metylfenyl)-1,5-naftyridin-2-yl]-4-fluor-2,3-dihydro-1H-1,3-benzodiazol-2-on;3-6: 3-[8-(4-aminopiperidin-1-yl)-7-(3-klor-5-metylfenyl)-1,5-naftyridin-2-yl]-5-fluor-2-hydroksybenzonitril;3-7: 3-[8-(4-aminopiperidin-1-yl)-7-(3-fluor-5-metylfenyl)-1,5-naftyridin-2-yl]-2-hydroksybenzonitril;3-8: 2-[8-(4-aminopiperidin-1-yl)-7-(3-fluor-5-metylfenyl)-1,5-naftyridin-2-yl]-6-fluorfenol;3-9: 6-[8-(4-aminopiperidin-1-yl)-7-(3,5-difluorfenyl)-1,5-naftyridin-2-yl]-4-fluor-2,3-dihydro-1H-1,3-benzodiazol-2-on;3-10: 6-{8-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-7-(3,5-difluorfenyl)-1,5-naftyridin-2-yl}-4-fluor-2,3-dihydro-1H-1,3-benzodiazol-2-on; 3-11: 4-{8-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-7-(3-fluor-5-metylfenyl)-1,5-naftyridin-2-yl}-6-fluor-2,3-dihydro-1H-1,3-benzodiazol-2-on;3-12: 4-{8-[trans-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-7-(3,5-difluorfenyl)-1,5-naftyridin-2-yl}-1H,2H,3H-imidazo[4,5-c]pyridin-2-on;eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav.12. Forbindelsen ifølge krav 1, hvori forbindelsen er:4-1: 3-[5-(4-aminopiperidin-1-yl)-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl]-2-hydroksybenzonitril;4-2: 3-[5-(4-aminopiperidin-1-yl)-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl]-2-hydroksybenzonitril;4-3: 3-[5-(4-aminopiperidin-1-yl)-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl]-5-fluor-2-hydroksybenzonitril;4-4: 3-[5-(4-aminopiperidin-1-yl)-6-(3-klor-5-metylfenyl)-1,8-naftyridin-3-yl]-2-hydroksybenzonitril;4-5: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-6: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-7: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl}-5-fluor-2-hydroksybenzonitril;4-8: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl}-5-fluor-2-hydroksybenzonitril;4-9: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl}-5-fluor-2-hydroksybenzonitril;4-10: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl}-5-fluor-2-hydroksybenzonitril;4-11: 2-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl}-3-aminopyridin-4-karbonitril;4-12: 2-{5-[(4aS,8aS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl}-3-aminopyridin-4-karbonitril;4-13: 5-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl}-4-aminopyridin-3-karbonitril; 4-14: 5-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b]morfolin-6-yl]-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl}-4-aminopyridin-3-karbonitril;4-15: 2-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl}-3-aminopyridin-4-karbonitril;4-16: 2-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl}-3-aminopyridin-4-karbonitril;4-17: 2-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-fluorfenyl)-1,8-naftyridin-3-yl}-3-aminopyridin-4-karbonitril;4-18: 2-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-fluorfenyl)-1,8-naftyridin-3-yl}-3-aminopyridin-4-karbonitril;4-19: 2-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-metylfenyl)-1,8-naftyridin-3-yl}-3-aminopyridin-4-karbonitril;4-20: 2-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-metylfenyl)-1,8-naftyridin-3-yl}-3-aminopyridin-4-karbonitril;4-21: 2-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl}-4-[(metoksyimino)metyl]pyridin-3-amin;4-22: 2-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl}-4-[(metoksyimino)metyl]pyridin-3-amin;4-23: 2-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-metylfenyl)-1,8-naftyridin-3-yl}-4-[(metoksyimino)metyl]pyridin-3-amin;4-24: 2-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-metylfenyl)-1,8-naftyridin-3-yl}-4-[(metoksyimino)metyl]pyridin-3-amin;4-25: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-26: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-27: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-fluorfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-28: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-fluorfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-29: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-fluor-5-metoksyfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-30: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-fluor-5-metoksyfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril; 4-31: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-metylfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-32: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-metylfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-33: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3,5-diklorfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-34: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3,5-diklorfenyl)-1,8-naftyridin-3-yl}-2-hydroksybenzonitril;4-35: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-36: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3,5-difluorfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-37: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-38: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-fluor-5-metylfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-39: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-fluor-5-metoksyfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-40: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-fluor-5-metoksyfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-41: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-fluorfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-42: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-fluorfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-43: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-metylfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-44: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3-klor-5-metylfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-45: 3-{5-[(4αR,8αR)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3,5-diklorfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;4-46: 3-{5-[(4αS,8αS)-oktahydro-1H-pyrido[3,4-b][1,4]oksazin-6-yl]-6-(3,5-diklorfenyl)-1,8-naftyridin-3-yl}pyridin-2-amin;eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav. 13. Forbindelsen ifølge krav 1, hvori forbindelsen har følgende struktur:eller et farmasøytisk akseptabelt salt eller solvat derav.14. Farmasøytisk sammensetning omfattende en forbindelse ifølge et hvilket som helst av kravene 1 til 12, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav, og minst én farmasøytisk akseptabel eksipiens.15. Farmasøytisk sammensetning omfattende en forbindelse ifølge krav 13, eller et farmasøytisk akseptabelt salt, eller solvat derav, og minst én farmasøytisk akseptabel eksipiens.16. Den farmasøytiske sammensetningen ifølge krav 14 eller krav 15, hvori den farmasøytiske sammensetningen er i form av en tablett, en pille eller en kapsel.17. Forbindelse ifølge et hvilket som helst av kravene 1 til 12, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav, for anvendelse som en medisin.18. Forbindelse ifølge krav 13, eller et farmasøytisk akseptabelt salt, eller solvat derav, for anvendelse som en medisin.19. Forbindelse ifølge et hvilket som helst av kravene 1 til 12, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav, for anvendelse i behandlingen av akromegali, en nevroendokrin svulst, en oftalmisk sykdom eller tilstand, nevropati, nefropati, en respiratorisk sykdom eller tilstand, kreft, smerte, en nevrodegenerativ sykdom eller tilstand, en inflammatorisk sykdom eller tilstand, en psykiatrisk sykdom eller tilstand, eller kombinasjoner derav. 20. Forbindelse ifølge krav 13, eller et farmasøytisk akseptabelt salt, eller solvat derav, for anvendelse i behandlingen av akromegali, en nevroendokrin svulst, en oftalmisk sykdom eller tilstand, nevropati, nefropati, en respiratorisk sykdom eller tilstand, kreft, smerte, en nevrodegenerativ sykdom eller tilstand, en inflammatorisk sykdom eller tilstand, en psykiatrisk sykdom eller tilstand, eller kombinasjoner derav.21. Farmasøytisk sammensetning ifølge et hvilket som helst av kravene 14 til 16 for anvendelse i behandlingen av akromegali, en nevroendokrin svulst, en oftalmisk sykdom eller tilstand, nevropati, nefropati, en respiratorisk sykdom eller tilstand, kreft, smerte, en nevrodegenerativ sykdom eller tilstand, en inflammatorisk sykdom eller tilstand, en psykiatrisk sykdom eller tilstand, eller kombinasjoner derav.22. Forbindelse ifølge et hvilket som helst av kravene 1 til 12, eller et farmasøytisk akseptabelt salt, solvat, diastereomerblanding eller individuelle enantiomerer derav, for anvendelse i behandlingen av akromegali, en nevroendokrin svulst eller kombinasjoner derav.23. Forbindelse ifølge krav 13, eller et farmasøytisk akseptabelt salt, eller solvat derav, for anvendelse i behandlingen av akromegali, en nevroendokrin svulst eller kombinasjoner derav.24. Farmasøytisk sammensetning ifølge et hvilket som helst av kravene 14 til 16 for anvendelse i behandlingen av akromegali, en nevroendokrin svulst eller kombinasjoner derav.
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Crinetics Pharmaceuticals, Inc.
10222 Barnes Canyon Road, Building No. 2 San Diego, CA 92121 US

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ZHAO, Jian
10222 Barnes Canyon Road Building 2 San Diego, California 92121 US
HAN, Sangdon
10222 Barnes Canyon Road Building 2 San Diego, California 92121 US
KIM, Sun Hee
10222 Barnes Canyon Road Building 2 San Diego, California 92121 US
WANG, Shimiao
10222 Barnes Canyon Road Building 2 San Diego, California 92121 US
ZHU, Yunfei
10222 Barnes Canyon Road Building 2 San Diego, California 92121 US

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BRYN AARFLOT AS
Stortingsgata 8 0161 OSLO NO ( OSLO kommune, Oslo fylke )

Org.nummer: 979993269
Din referanse: 142022 LBA
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2016.07.14, US 201662362493 P

2016.10.21, US 201662411338 P

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EP-A1- 2 871 179 (B1)

KR-A- 20160 062 023 (B1)

Scott E. Wolkenberg ET AL: "Design, Synthesis, and Evaluation of Novel 3,6-Diaryl-4-aminoalkoxyquinolines as Selective Agonists of Somatostatin Receptor Subtype 2", Journal of Medicinal Chemistry, vol. 54, no. 7, 14 April 2011 (2011-04-14) , pages 2351-2358, XP055569581, US ISSN: 0022-2623, DOI: 10.1021/jm101501b (B1)

WO-A2-2008/051272 (B1)

US-A1- 2015 232 478 (B1)

WO-A1-2010/041054 (B1)

US-A1- 2003 153 553 (B1)

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