Nøkkelinformasjon info chevron_right

Viktig informasjon i saken hentes i sanntid direkte fra EPO sitt register (European Patent Register), slik at du enkelt og raskt får oversikt i saken.
Beskrivelse Verdi
Saken / databasen er sist oppdatert info  
Tittel USE OF INHIBITORS OF THE ACTIVITY OR FUNCTION OF PI3K
Status
Hovedstatus
Detaljstatus 		I kraft info EP patent gjort gjeldende i Norge EP patent besluttet gjeldende i Norge
Patentnummer NO/EP2790705
Europeisk (EP) publiserings nummer EP2790705
EP levert
EP søknadsnummer 12818825.7
EP meddelt
Prioritet 2011.12.15, US 201161576194 P
Sakstype Europeisk
Løpedag
Utløpsdato
Allment tilgjengelig
Validert i Norge
Innehaver Novartis AG (CH)
Oppfinner COOKE, Nigel Graham (CH) .... se mer/flere nedenfor
Fullmektig ZACCO NORWAY AS (NO)
Lenke til European patent Register Informasjon i saken, dokumenter og patentfamilie
Patentfamilie Se i Espacenet

Sammendrag og figur info chevron_right

EPO translation logo


Se forsidefigur og sammendrag i Espacenet

Beskrivelse og krav info chevron_right

T3

Beskrivelse

(74) Agent or Attorney ZACCO NORWAY AS, Postboks 2003 Vika, 0125 OSLO, Norge

(54) Title USE OF INHIBITORS OF THE ACTIVITY OR FUNCTION OF PI3K

(56) References

Cited: WO-A1-2008/012326, WO-A1-2009/058361, WO-A1-2010/036908, WO-A2-2010/129816, WO-A1-2012/004299, WO-A2-2005/086814, WO-A2-2008/157191, WO-A1-2010/120991

Enclosed is a translation of the patent claims in Norwegian. Please note that as per the Norwegian Patents Acts, section 66i the patent will receive protection in Norway only as far as there is agreement between the translation and the language of the application/patent granted at the EPO. In matters concerning the validity of the patent, language of the application/patent granted at the EPO will be used as the basis for the decision. The patent documents published by the EPO are available through Espacenet (http://worldwide.espacenet.com) or via the search engine on our website here: https://search.patentstyret.no/

Krav

Patentkrav1. PI3K-inhibitor, hvori inhibitoren har en inhiberende virkning på PI3K isoform delta, for anvendelse i behandling av en immunpatologi hos et individ som lider av en sykdom eller en lidelse valgt fra akutt og cerebral malaria, via funksjonell inhibering av TLR9 hos det infiserte individet, hvori PI3K-inhibitoren er valgt fra tetrahydro-pyrido-pyrimidin-forbindelser med formel (I) og/eller tautomerer o /eller N-oksider o /eller farmasøytisk akseptable salter derav,hvoriY er valgt fra O eller NR3;R1 er valgt fra fenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,2,3-triazinyl, 1,2,4-triazinyl, 1,3,5-triazinyl,eller-C(O)-R4hvoriR4 er valgt fra C1-C8-alkyl, halo-C1-C8-alkyl, hydroksy-C1-C8-alkyl, C1-C8-alkoksy-C1-C8-alkyl, C1-C8-alkyl-sulfonyl-C1-C8-alkyl, heterosyklyl, heterosyklyl-oksy, heterosyklyl-C1-C8-alkyl, C3-C12-sykloalkyl, C3-C12-sykloalkyl-C1-C8-alkyl, heteroaryl, heteroaryl-oksy, heteroaryl-C1-C8-alkyl, hydroksy, C1-C8-alkoksy, amino, N-C1-C8-alkylamino eller N,N-di-C1-C8-alkyl-amino,hvori 'C1-C8-alkyl' i N-C1-C8-alkyl-amino og N,N-di-C1-C8-alkyl-amino kan være usubstituert eller substituert med halogen, hydroksy eller C1-C4-alkoksy;hvori 'C3-C12-sykloalkyl' i C3-C12-sykloalkyl og C3-C12-sykloalkyl-C1-C8-alkyl kan være usubstituert eller substituert med 1-5 substituenter uavhengig valgt fra okso, halogen, C1-C8-alkyl, halo-C1-C8-alkyl, hydroksy-C1-C8-alkyl, hydroksyl, C1-C8-alkoksy, C1-C8-alkoksy-C1-C8-alkyl, amino, N-C1-C8-alkyl-amino, N,N-di-C1-C8-alkylamino, C1-C8-alkyl-karbonyl, halo-C1-C8-alkyl-karbonyl, hydroksy-C1-C8-alkyl-karbonyl eller C1-C8-alkoksy-C1-C8-alkyl-karbonyl;hvori 'heterosyklyl' er valgt fra oksiranyl, aziridinyl, oksetanyl, tietanyl, acetitinyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrotiofenyl, 2,3-dihydrofuranyl, 2,5-dihydrofuranyl, 2,3-dihydrotiofenyl, 1-pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl, tetrahydropyranyl, piperidinyl, tetrahydrotiopyranyl, morfolinyl, tiomorfolinyl, piperazinyl, azepanyl, tiepanyl eller oksepanyl; der hver av disse er usubstituert eller substituert med 1-5 substituenter uavhengig valgt fra okso, halogen, C1-C8-alkyl, halo-C1-C8-alkyl, hydroksy-C1-C8-alkyl, hydroksyl, C1-C8-alkoksy, C1-C8-alkoksy-C1-C8-alkyl, amino, N-C1-C8-alkyl-amino, N,N-di-C1-C8-alkyl-amino, C1-C8-alkylkarbonyl, halo-C1-C8-alkyl-karbonyl, hydroksy-C1-C8-alkyl-karbonyl eller C1-C8-alkoksy-C1-C8-alkyl-karbonyl;hvori 'heterosyklyl' kan være festet til et heteroatom eller et karbonatom, og hvor N- og/eller S-heteroatomene eventuelt også kan være oksidert til ulike oksidasjonstilstander;hvori 'heteroaryl' er valgt frafuranyl, tiofenyl, pyrrolyl, imidazolyl, pyrazolyl, tiazolyl, isotiazolyl, oksazolyl, isoksazolyl, 1,2,5-oksadiazolyl, 1,2,4-oksadiazolyl, 1,2,3-oksadiazolyl,1,3,4-oksadiazolyl, 1,2,5-tiadiazolyl, 1,2,4-tiadiazolyl, 1,2,3-tiadiazolyl,1,3,4-tiadiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,5-triazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,2,3-triazinyl, 1,2,4-triazinyl eller 1,3,5-triazinyl; der hver av disse er usubstituert eller substituert med 1-5 substituenter uavhengig valgt fra halogen, C1-C8-alkyl, halo-C1-C8-alkyl, hydroksy-C1-C8-alkyl, hydroksyl, C1-C8-alkoksy, C1-C8-alkoksy-C1-C8-alkyl, amino, N-C1-C8-alkyl-amino, N,N-di-C1-C8-alkyl-amino, C1-C8-alkyl-karbonyl, halo-C1-C8-alkyl-karbonyl, hydroksy-C1-C8-alkyl-karbonyl eller C1-C8-alkoksy-C1-C8-alkyl-karbonyl; hvori 'heteroaryl' kan være festet til et heteroatom eller et karbonatom, og hvor N- og/eller S-heteroatomene eventuelt også kan være oksidert til ulike oksidasjonstilstander; R2 er valgt fra fenyl, naftyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, kinolinyl eller isokinolinyl, der hver av disse er usubstituert eller substituert med 1-5 substituenter uavhengig valgt fra halogen, cyano, nitro, C1-C8-alkyl, halo-C1-C8-alkyl, hydroksy-C1-C8-alkyl, hydroksyl, C1-C8-alkoksy, C1-C8-alkoksy-C1-C8-alkyl, amino, N-C1-C8-alkyl-amino, N,N-di-C1-C8-alkyl-amino, C1-C8-alkyl-karbonyl, halo-C1-C8-alkyl-karbonyl, hydroksy-C1-C8-alkylkarbonyl eller C1-C8-alkoksy-C1-C8-alkyl-karbonyl;R3 er valgt fra H, C1-C4-alkyl eller halo-C1-C4-alkyl; ogm er valgt fra 0 eller 1.2. PI3K-inhibitor, hvori inhibitoren har en inhiberende virkning på PI3K isoform delta, for anvendelse ifølge krav 1 med formel (Id') og/eller tautomerer og/eller N-oksider og/eller farmasøytisk akseptable salter derav.3. PI3K-inhibitor, hvori inhibitoren har en inhiberende virkning på PI3K isoform delta, for anvendelse ifølge krav 1 med formel (Ie')og/eller tautomerer og/eller N-oksider og/eller farmasøytisk akseptable salter derav.4. PI3K-inhibitor, hvori inhibitoren har en inhiberende virkning på PI3K isoform delta, for anvendelse ifølge et hvilket som helst av kravene 1 til 3, hvoriR2 er valgt fra naftyl, pyridyl eller pyrimidinyl; der hver av disse er usubstituert eller substituert med 1–3 substituenter uavhengig valgt fra halogen, cyano, nitro, C1-C8-alkyl, halo-C1-C8-alkyl, hydroksy-C1-C8-alkyl, hydroksyl, C1-C8-alkoksy, C1-C8-alkoksy-C1-C8-alkyl, amino, N-C1-C8-alkyl-amino, N,N-di-C1-C8-alkyl-amino, C1-C8-alkyl-karbonyl, halo-C1-C8-alkyl-karbonyl, hydroksy-C1-C8-alkyl-karbonyl eller C1-C8-alkoksy-C1-C8-alkyl-karbonyl.5. PI3K-inhibitor, hvori inhibitoren har en inhiberende virkning på PI3K isoform delta, for anvendelse ifølge et hvilket som helst av kravene 1 til 4, hvori R1, hvis den er til stede, er -C(O)-R4, hvoriR4 er valgt fra heterosyklyl, C4-C8-sykloalkyl eller heteroaryl;hvori 'C3-C12-sykloalkyl' kan være usubstituert eller substituert med 1–3 substituenter uavhengig valgt fra fluor, C1-C4-alkyl, hydroksyl, C1-C4-alkoksy; hvori 'heterosyklyl' er valgt fra pyrrolidinyl, tetrahydropyranyl, piperidinyl, tetrahydrotiopyranyl, morfolinyl eller piperazinyl; der hver av disse er usubstituert eller substituert med 1–3 substituenter uavhengig valgt fra okso, halogen, C1-C4-alkyl, hydroksyl, C1-C4-alkyl-karbonyl; hvori 'heterosyklyl' kan være festet til et heteroatom eller et karbonatom, og hvor N- og/eller S-heteroatomene eventuelt også kan være oksidert til ulike oksidasjonstilstander;hvori 'heteroaryl' er valgt frafuranyl, imidazolyl, pyrazolyl, tiazolyl, oksazolyl, isoksazolyl, 1,3,4-oksadiazyolyl, pyridyl, pyrazinyl; der hver av disse er usubstituert eller substituert med 1–3 substituenter uavhengig valgt fra C1-C4-alkyl, hydroksyl;hvori 'heteroaryl' kan være festet til et heteroatom eller et karbonatom, og hvor N- og/eller S-heteroatomene eventuelt også kan være oksidert til forskjellige oksideringstilstander.6. PI3K-inhibitor, hvori inhibitoren har en inhiberende virkning på PI3K isoform delta, for anvendelse ifølge et hvilket som helst av kravene 1 til 4, hvori R1, hvis den er til stede, er -C(O)-R4, ogR4 er valgt fra C1-C8-alkyl, C1-C8-alkoksy-C1-C8-alkyl, C1-C8-alkoksy eller N,N-di-C1-C8-alkyl-amino,hvori 'C1-C8-alkyl' i N,N-di-C1-C8-alkyl-amino kan være usubstituert eller substituert med halogen, hydroksy eller C1-C4-alkoksy.7. PI3K-inhibitor, hvori inhibitoren har en inhiberende virkning på PI3K isoform delta, for anvendelse ifølge krav 1, hvori PI3K-inhibitoren er valgt fra gruppen bestående av{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon;{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon;{(S)-3-[6-(2,4-Dimetoksy-pyrimidin-5-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon;{3-[6-(2,4-Dimetoksy-pyrimidin-5-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon;2-Metoksy-5-{4-[(S)-1-(tetrahydro-pyran-4-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;2-Metoksy-5-{4-[1-(tetrahydro-pyran-4-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;1-{(S)-3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-propan-1-on; 1-{3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-propan-1-on;{(S)-3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon;{3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon;2-Amino-5-{4-[(S)-1-(tetrahydro-pyran-4-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;2-Amino-5-{4-[1-(tetrahydro-pyran-4-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;(S)-(3-(6-(5-Fluor-6-metoksypyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon;(3-(6-(5-Fluor-6-metoksypyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon;(S)-2-Metoksy-5-(4-(1-(2-metoksyacetyl)pyrrolidin-3-yloksy)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)nikotinonitril;2-Metoksy-5-(4-(1-(2-metoksyacetyl)pyrrolidin-3-yloksy)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)nikotinonitril;(S)-5-(4-(1-(Syklopentankarbonyl)pyrrolidin-3-yloksy)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)-2-metoksynikotinonitril;5-(4-(1-(Syklopentankarbonyl)pyrrolidin-3-yloksy)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)-2-metoksynikotinonitril;(2,4-Dimetyl-oksazol-5-yl)-{(S)-3-[6-(6-metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;(2,4-Dimetyl-oksazol-5-yl)-{3-[6-(6-metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;Furan-3-yl-{(S)-3-[6-(6-metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;Furan-3-yl-{3-[6-(6-metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;Furan-3-yl-{(S)-3-[6-(6-metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;Furan-3-yl-{3-[6-(6-metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(3-metyl-3H-imidazol-4-yl)-metanon; {3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(3-metyl-3H-imidazol-4-yl)-metanon; {(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(2-metyl-oksazol-4-yl)-metanon;{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(2-metyl-oksazol-4-yl)-metanon;(3-Metoksy-syklobutyl)-{(S)-3-[6-(6-metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;(3-Metoksy-syklobutyl)-{3-[6-(6-metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;({(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-oksazol-4-yl-metanon;({3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-oksazol-4-yl-metanon;1-(4-{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-karbonyl}-piperidin-1-yl)-etanon;1-(4-{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-karbonyl}-piperidin-1-yl)-etanon;{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(4-metyl-oksazol-5-yl)-metanon;{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(4-metyl-oksazol-5-yl)-metanon;5-{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-karbonyl}-1H-pyridin-2-on;5-{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-karbonyl}-1H-pyridin-2-on;{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(1-metyl-1H-imidazol-4-yl)-metanon; {3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(1-metyl-1H-imidazol-4-yl)-metanon; {(S)-3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-oksazol-4-yl-metanon;{3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-oksazol-4-yl-metanon;{(S)-3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-oksazol-5-yl-metanon; {3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-oksazol-5-yl-metanon;{(S)-3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(2-metyl-oksazol-4-yl)-metanon;{3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(2-metyl-oksazol-4-yl)-metanon;{(S)-3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(2,2-dimetyl-tetrahydro-pyran-4-yl)-metanon;{3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(2,2-dimetyl-tetrahydro-pyran-4-yl)-metanon;{(S)-3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(2,4-dimetyl-oksazol-5-yl)-metanon; {3-[6-(5,6-Dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(2,4-dimetyl-oksazol-5-yl)-metanon;(4,4-Difluor-sykloheksyl)-{(S)-3-[6-(5,6-dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;(4,4-Difluor-sykloheksyl)-{3-[6-(5,6-dimetoksy-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;2-Metoksy-5-{4-[(S)-1-(2-tetrahydro-pyran-4-yl-acetyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;2-Metoksy-5-{4-[1-(2-tetrahydro-pyran-4-yl-acetyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;5-{4-[(S)-1-(2,4-Dimetyl-oksazol-5-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-2-metoksy-nikotinonitril;5-{4-[1-(2,4-Dimetyl-oksazol-5-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-2-metoksy-nikotinonitril;5-{4-[(S)-1-(2,2-Dimetyl-tetrahydro-pyran-4-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-2-metoksy-nikotinonitril;5-{4-[1-(2,2-Dimetyl-tetrahydro-pyran-4-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-2-metoksy-nikotinonitril;{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(5-metyl-oksazol-4-yl)-metanon;{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(5-metyl-oksazol-4-yl)-metanon;{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(5-metyl-isoksazol-4-yl)-metanon; {3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(5-metyl-isoksazol-4-yl)-metanon;{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(3-metyl-isoksazol-4-yl)-metanon;{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(3-metyl-isoksazol-4-yl)-metanon;{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(3-metyl-isoksazol-4-yl)-metanon;{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(3-metyl-isoksazol-4-yl)-metanon;Isoksazol-3-yl-{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;Isoksazol-3-yl-{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;Isoksazol-5-yl-{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;Isoksazol-5-yl-{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;2-Metoksy-5-{4-[(S)-1-(tiazol-4-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;2-Metoksy-5-{4-[1-(tiazol-4-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;2-Metoksy-5-{4-[(S)-1-(1-metyl-1H-pyrazol-4-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;2-Metoksy-5-{4-[1-(1-metyl-1H-pyrazol-4-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;2-Metoksy-5-{4-[(S)-1-(1-metyl-1H-pyrazol-3-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;2-Metoksy-5-{4-[1-(1-metyl-1H-pyrazol-3-karbonyl)-pyrrolidin-3-yloksy]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-nikotinonitril;(2,2-Dimetyl-tetrahydro-pyran-4yl)-{(S)-3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon; (2,2-Dimetyl-tetrahydro-pyran-4yl)-{3-[6-(6-Metoksy-5-metyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon; (1,1-Diokso-heksahydro-1lambda*6*-tiopyran-4-yl)-{(S)-3-[6-(6-metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon; (1,1-Diokso-heksahydro-1lambda*6*-tiopyran-4-yl)-{3-[6-(6-metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-metanon;(S)-(2,4-Dimetyloksazol-5-yl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)metanon; (2,4-Dimetyloksazol-5-yl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)metanon; (S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(tiazol-5-yl)metanon; (3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(tiazol-5-yl)metanon;(S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(1-metyl-1H-pyrazol-5-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(1-metyl-1H-pyrazol-5-yl)metanon;4-((S)-3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-karbonyl)pyrrolidin-2-on; 4-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-karbonyl)pyrrolidin-2-on;(S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(pyridin-3-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(pyridin-3-yl)metanon;(S)-(1H-Imidazol-4-yl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)metanon;(1H-Imidazol-4-yl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)metanon;5-((S)-3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-karbonyl)pyrrolidin-2-on; 5-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-karbonyl)pyrrolidin-2-on;(S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(pyridin-4-yl)metanon; (3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(pyridin-4-yl)metanon;(S)-(1,3-Dimetyl-1H-pyrazol-4-yl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)metanon; (1,3-Dimetyl-1H-pyrazol-4-yl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)metanon; (S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(1H-pyrazol-4-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(1H-pyrazol-4-yl)metanon;(S)-(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(5-metyl-1,3,4-oksadiazol-2-yl)metanon;(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(5-metyl-1,3,4-oksadiazol-2-yl)metanon; (S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(pyrazin-2-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(pyrazin-2-yl)metanon;(S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(1-metyl-1H-imidazol-4-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(1-metyl-1H-imidazol-4-yl)metanon;{(S)-3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(1-metyl-1H-pyrazol-4-yl)-metanon;{3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(1-metyl-1H-pyrazol-4-yl)-metanon; {(S)-3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-tiazol-4-yl-metanon;{3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-tiazol-4-yl-metanon;{(S)-3-[6-(5-Klor-6-metoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon; {3-[6-(5-Klor-6-metoksy-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon;(S)-(3-(6-(6-Amino-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon;(3-(6-(6-Amino-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)azetidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon;{(S)-3-[6-(2-Metoksy-pyrimidin-5-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon;{3-[6-(2-Metoksy-pyrimidin-5-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon;[(S)-3-(6-Kinolin-3-yl-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy)-pyrrolidin-1-yl]-(tetrahydro-pyran-4-yl)-metanon;[3-(6-Kinolin-3-yl-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy)-pyrrolidin-1-yl]-(tetrahydro-pyran-4-yl)-metanon;(S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon;(S)-1-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)-3,3-dimetylbutan-1-on;1-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)-3,3-dimetylbutan-1-on;1-{(S)-3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-propan-1-on;1-{3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-propan-1-on;2-Metoksy-5-[4-((S)-1-propionyl-pyrrolidin-3-yloksy)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-nikotinonitril;2-Metoksy-5-[4-(1-propionyl-pyrrolidin-3-yloksy)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-nikotinonitril;(S)-6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-4-(1-(pyridin-2-yl)pyrrolidin-3-yloksy)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine; 6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-4-(1-(pyridin-2-yl)pyrrolidin-3-yloksy)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine;(S)-6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-4-(1-(pyrimidin-2-yl)pyrrolidin-3-yloksy)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine;6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-4-(1-(pyrimidin-2-yl)pyrrolidin-3-yloksy)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine;(S)-1-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)propan-1-on;1-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)propan-1-on;(S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon; (S)-2-Metoksy-5-(4-(1-(tetrahydro-2H-pyran-4-karbonyl)pyrrolidin-3-ylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)nikotinonitril;2-Metoksy-5-(4-(1-(tetrahydro-2H-pyran-4-karbonyl)pyrrolidin-3-ylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)nikotinonitril;(S)-1-(4-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-karbonyl)piperidin-1-yl)etanon;1-(4-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-karbonyl)piperidin-1-yl)etanon;(2,2-Dimetyltetrahydro-2H-pyran-4-yl)((S)-3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)metanon;(2,2-Dimetyltetrahydro-2H-pyran-4-yl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)metanon;(S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(oksazol-5-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(oksazol-5-yl)metanon; ((S)-3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)((1s,4R)-4-metoksysykloheksyl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)((1s,4R)-4-metoksysykloheksyl)metanon; ((S)-3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)((1r,4S)-4-metoksysykloheksyl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)((1r,4S)-4-metoksysykloheksyl)metanon; ((1s,4R)-4-Hydroksysykloheksyl)((S)-3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)metanon;((1s,4R)-4-Hydroksysykloheksyl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)metanon; ((1r,4S)-4-Hydroksysykloheksyl)((S)-3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)metanon;((1r,4S)-4-Hydroksysykloheksyl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)metanon; (S)-(3-(6-(6-Metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(1-metyl-1H-imidazol-4-yl)metanon;(3-(6-(6-Metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(1-metyl-1H-imidazol-4-yl)metanon;(S)-(3-(6-(6-Metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(oksazol-5-yl)metanon;(3-(6-(6-Metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(oksazol-5-yl)metanon;(S)-(3-(6-(6-Metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(oksazol-4-yl)metanon;(3-(6-(6-Metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(oksazol-4-yl)metanon;(2,2-Dimetyltetrahydro-2H-pyran-4-yl)((S)-3-(6-(6-metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)metanon; (2,2-Dimetyltetrahydro-2H-pyran-4-yl)(3-(6-(6-metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)metanon; (S)-1-(3-(6-(6-Metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)propan-1-on;1-(3-(6-(6-Metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)propan-1-on;(S)-(3-(6-(5-Klor-6-metoksypyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon; (3-(6-(5-Klor-6-metoksypyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon;(S)-(3-(6-(6-Metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon; (3-(6-(6-Metoksy-5-metylpyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)(tetrahydro-2H-pyran-4-yl)metanon; (Tetrahydro-pyran-4-yl)-{(S)-3-{6-(5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl}-metanon;(Tetrahydro-pyran-4-yl)-{3-{6-(5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl}-metanon;(S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(4-metylpiperazin-1-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(4-metylpiperazin-1-yl)metanon;(S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(morfolino)metanon; (3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(morfolino)metanon;(S)-(4-Hydroksypiperidin-1-yl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)metanon; 4-Hydroksypiperidin-1-yl)(3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)metanon; (S)-N-(2-Hydroksyetyl)-3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)-N-metylpyrrolidin-1-karboksamide; N-(2-Hydroksyetyl)-3-(6-(6-metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)-N-metylpyrrolidin-1-karboksamide; (S)-1-(4-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-karbonyl)piperazin-1-yl)etanon; 1-(4-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-karbonyl)piperazin-1-yl)etanon;(S)-2-Metoksy-5-(4-(1-(morfolin-4-karbonyl)pyrrolidin-3-yloksy)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)nikotinonitril;2-Metoksy-5-(4-(1-(morfolin-4-karbonyl)pyrrolidin-3-yloksy)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)nikotinonitril;(S)-(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(oksazol-4-yl)metanon;(3-(6-(6-Metoksy-5-(trifluormetyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl)(oksazol-4-yl)metanon;1-(4-{(S)-3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-karbonyl}-piperidin-1-yl)-etanon; 1-(4-{3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-karbonyl}-piperidin-1-yl)-etanon; {(S)-3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(3-metyl-3H-imidazol-4-yl)-metanon;{3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-(3-metyl-3H-imidazol-4-yl)-metanon; {(S)-3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-oksazol-5-yl-metanon;{3-[6-(6-Metoksy-5-trifluormetyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-yloksy]-pyrrolidin-1-yl}-oksazol-5-yl-metanon;{(S)-3-[6-(6-Metoksy-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon; og{3-[6-(6-Metoksy-pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yloksy)pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-metanon.8. PI3K-inhibitor, hvori inhibitoren har en inhiberende virkning på PI3K isoform delta, for anvendelse ifølge et hvilket som helst av kravene 1 til 7 i form av et salt valgt fraa) citrat, fumarat eller napadisylat; ellerb) fosfat, hydroklorid eller hippurat. 9. Farmasøytisk sammensetning omfattende en PI3K-inhibitor, hvori inhibitoren har en inhiberende virkning på PI3K isoform delta, eller farmasøytisk akseptable salter eller solvater derav, hvori PI3K-inhibitoren er som definert i hvilke som helst av kravene 1 til 8, for anvendelse i behandling av en immunpatologi hos et individ som lider av en sykdom eller en lidelse valgt fra akutt og cerebral malaria, via funksjonell inhibering av TLR9 hos det infiserte individet.10. Kombinasjon omfattende en PI3K-inhibitor, hvori inhibitoren har en inhiberende virkning på PI3K isoform delta, eller farmasøytisk akseptable salter eller solvater derav, hvori PI3K-inhibitoren er som definert i hvilke som helst av kravene 1 til 8, for anvendelse i behandling av en immunpatologi hos et individ som lider av en sykdom eller en lidelse valgt fra akutt og cerebral malaria, via funksjonell inhibering av TLR9 hos det infiserte individet, og ett eller flere ytterligere aktive ingredienser.
Hva betyr A1, B, B1, C osv? info

Klasser info chevron_right

Innehaver(e) info chevron_right

Innehaver i EP:
Novartis AG
Lichtstrasse 35 4056 Basel CH

Oppfinner(e) info chevron_right

COOKE, Nigel Graham
Novartis Pharma AGPostfach CH-4002 Basel CH
FERNANDES GOMES DOS SANTOS, Paulo Antonio
Novartis Pharma AGWerk KlybeckPostfach CH-4002 Basel CH
FURET, Pascal
Novartis Pharma AGWerk KlybeckPostfach CH-4002 Basel CH
HEBACH, Christina
Novartis Pharma AGPostfach CH-4002 Basel CH
HÖGENAUER, Klemens
Novartis Pharma AGPostfach CH-4002 Basel CH
HOLLINGWORTH, Gregory
Novartis Pharmaceuticals UK LimitedWimblehurst Road HorshamSussex RH12 5AB GB
KALIS, Christoph
Novartis Pharma AGPostfach CH-4002 Basel CH
LEWIS, Ian
Novartis Pharma AGPostfach CH-4002 Basel CH
SMITH, Alexander Baxter
Novartis Pharma AGPostfach CH-4002 Basel CH
SOLDERMANN, Nicolas
Novartis Pharma AGWerk KlybeckPostfach CH-4002 Basel CH
STAUFFER, Frédéric
Novartis Pharma AGWerk KlybeckPostfach CH-4002 Basel CH
STRANG, Ross
Novartis Pharma AGPostfach CH-4002 Basel CH
STOWASSER, Frank
Novartis Pharma Stein AGPostfach CH-4332 Stein CH
TUFILLI, Nicola
Novartis Pharma AGPostfach CH-4002 Basel CH
VON MATT, Anette
Novartis Pharma AGPostfach CH-4002 Basel CH
WOLF, Romain
Novartis Pharma AGPostfach CH-4002 Basel CH
ZECRI, Frédéric
Novartis Institutes for BioMedical Research Inc.100 Technology Square Cambridge, MA 02139 US

Fullmektig info chevron_right

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

Org.nummer: 982702887
Din referanse: P61704497NO00E
  • Foretaksnavn:
  • Foretaksform:
  • Næring:
  • Forretningsadresse:
     

Kilde: Brønnøysundregistrene
Fullmektig i EP:
Marti, Christiane
Novartis Pharma AG Patent Department 4002 Basel CH

Prioritet info chevron_right

2011.12.15, US 201161576194 P

Anførte dokumenter info chevron_right

WO-A1-2008/012326 (B1)

WO-A1-2009/058361 (B1)

WO-A1-2010/036908 (B1)

WO-A2-2010/129816 (B1)

WO-A1-2012/004299 (B1)

WO-A2-2005/086814 (B1)

WO-A2-2008/157191 (B1)

WO-A1-2010/120991 (B1)

Sakshistorikk info chevron_right

Statushistorie

Liste over statusendringer i sakshistorikk
Hovedstatus Beslutningsdato, detaljstatus
EP patent gjort gjeldende i Norge EP patent besluttet gjeldende i Norge
EP under behandling Forespørsel om å gjøre EP patent gyldig er mottatt

Korrespondanse

expand_more file_download  
Liste over sakshistorikk og korrespondanse
Dato Type korrespondanse Journal beskrivelse
Innkommende EP Publiseringsdokument fra EPO
17-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
16-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
15-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
14-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
13-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
12-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
11-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
10-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
09-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
08-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
07-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
06-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
05-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Innkommende EP Publiseringsdokument fra EPO
04-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Utgående EP Registreringsbrev (3210)
03-01 Brev UT EP Registreringsbrev (3210)
Innkommende Søknadsskjema Patent
01-01 Søknadsskjema Patent Søknadsskjema Patent
01-02 Fullmakt Fullmakt
01-03 EP oversettelse EP krav
01-04 Hovedbrev EP søknadsskjema
Innkommende EP Publiseringsdokument fra EPO
02-01 EP Publiseringsdokument fra EPO EP Publiseringsdokument fra EPO
Informasjon om ikke tilgjengelige dokumenter

Betaling info chevron_right

Til betaling:

Neste fornyelse/årsavgift:

Betalingshistorikk:

Liste av betalinger
Beskrivelse / Fakturanummer Betalingsdato Beløp Betaler Status
Årsavgift 13. avg. år (EP) 2024.12.19 5460 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 12. avg. år (EP) 2023.12.19 3850 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 11. avg. år (EP) 2022.12.20 3500 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 10. avg. år (EP) 2021.12.21 3200 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 9. avg. år (EP) 2020.12.18 2850 CPA GLOBAL LIMITED Betalt og godkjent
Årsavgift 8. avg. år (EP) 2019.12.27 2550 1/IPAN GMBH Betalt og godkjent
Årsavgift 7. avg. år (EP) 2018.12.11 2200 CPA GLOBAL LIMITED Betalt og godkjent
31803263 expand_more 2018.03.09 5500 ZACCO NORWAY AS Betalt
Årsavgift 6. avg. år (EP) 2017.12.27 2000 CPA GLOBAL LIMITED Betalt og godkjent
Denne oversikten kan mangle informasjon, spesielt for eldre saker, om tilbakebetaling, internasjonale varemerker og internasjonale design.

Publikasjon(er) info chevron_right

Lenker til publikasjoner og Norsk Patenttidende (søkbare tekstdokumenter)

Oversettelse av europeisk patentskrift
Allment tilgjengelig patentsøknad
Norsk Patenttidende - ved meddelelse
Nye digitale Norske Tidende, nyhet om tjenesten ved lansering
Om Norske Tidende
Hva betyr A1, B, B1, C osv? info
Kapitler uten data er fjernet. Melding opprettet: 15.05.2025 07:22:43