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DK3013798T3 - Kondenserede tricykliske urinstofforbindelser som RAF-kinase- og/eller RAF-kinase-dimerhæmmere - Google Patents

Kondenserede tricykliske urinstofforbindelser som RAF-kinase- og/eller RAF-kinase-dimerhæmmere Download PDF

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DK3013798T3
DK3013798T3 DK14818636.4T DK14818636T DK3013798T3 DK 3013798 T3 DK3013798 T3 DK 3013798T3 DK 14818636 T DK14818636 T DK 14818636T DK 3013798 T3 DK3013798 T3 DK 3013798T3
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optionally substituted
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heterocyclyl
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Changyou Zhou
Guoliang Zhang
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Claims (24)

1. Forbindelse med formlen (I):
eller en stereoisomer deraf eller et farmaceutisk acceptabelt salt deraf, hvor: Q er valgt blandt C og N; R1, R2, R3 og R4, som kan være det samme eller forskellige, hver især er valgt blandt hydrogen, halogen, alkyl, alkenyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, alkynyl, -CN, -NR6R7, -OR6,-COR6, -CO2R6, -CONR6R7, -C(=NR6)NR7R8, -NR6COR7, -NR6CONR7R8, -NR6CO2R7, -SO2R6, -NR6SO2NR7R8, -NR6SO2R7 og -NR6SO2-aryl, hvor al kyl, alkenyl, alkynyl, cycloalkyl, heteroaryl, aryl og heterocyclyl uafhængigt eventuelt er substitueret med mindst en substituent R9, eller (R1 og R2), og/eller (R3 og R4), sammen med den ring, hvortil de er bundet, danner en kondenseret ring, som er valgt blandt heterocyclyl- og hetero-arylringe, der eventuelt er substitueret med mindst en substituent R9; forudsat at R1 er fraværende, når Q er N; R5 er valgt blandt alkyl-, cycloalkyl-, heterocyclyl-, aryl-, heteroarylringe, hvoraf hver eventuelt er substitueret med mindst en substituent R9; R6, R7og R8, som kan være det samme eller forskellige, hver især er valgt blandt H, al kyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl og heteroaryl; eller (R6 og R7), og/eller (R7 og R8) sammen med atomet/atomerne, hvortil de er bundet, hver især danner en ring, som er valgt blandt heterocyclyl- og heteroarylringe, der eventuelt er substitueret med mindst en substituent R9; R9 er valgt blandt halogen, halogenalkyl, alkyl, alkenyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, alkynyl, oxo, -alkyl-NR'R", -CN, -OR', -NR'R", -COR', -CO2R', -CONR'R",-C(=NR')NR"R'", nitro, -NR'COR", -NR'CONR'R", -NR'CO2R", -SO2R', -SO2-aryl,-NR'SO2NR"R'", NR'SO2R" og -NR'SO2-aryl, hvor cycloalkyl-, aryl-, heteroaryl- eller heterocyclylgruppen hver især uafhængigt eventuelt er substitueret med en, to eller tre substituenter, der er valgt blandt halogen, alkyl og halogenalkyl, hvor R', R" og R'" uafhængigt valgt blandt H, halogenalkyl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl og heteroaryl, eller (R' og R"), og/eller (R" og R'") sammen med atomerne, hvortil
de er bundet, danner en ring, som er valgt blandt heterocyclyl, eventuelt substitueret med halogen og alkyl, og heteroarylringe, eventuelt substitueret med halogen og al kyl.
2. Forbindelse ifølge krav 1, hvor Q er C.
3. Forbindelse ifølge krav 1 eller 2, hvor R1 og R2, der kan være det samme eller forskellige, hver især er valgt blandt hydrogen, halogen og alkyl, eventuelt substitueret med mindst en substituent R9.
4. Forbindelse ifølge et af kravene 1 til 3, hvor R3 og R4, der kan være det samme eller forskellige, hver især er valgt blandt hydrogen, halogen, alkyl, eventuelt substitueret med mindst en substituent R9, -NR6R7 og -CONR6R7, hvor R6 og R7 hver især er valgt blandt hydrogen eller alkyl.
5. Forbindelse ifølge et af kravene 1 til 3, hvor R3 er -NR6R7 eller -CONR6R7, og R4 er hydrogen, hvor R6 og R7 hver især er valgt blandt hydrogen eller alkyl.
6. Forbindelse ifølge et af kravene 1 til 3, hvor R3 og R4 sammen med den ring, hvortil de er bundet, danner en kondenseret ring, som er valgt blandt naphthy-ridinyl, pyridooxazinyl, pyridopyrimidinyl og purinyl, hvor ringen eventuelt er substitueret med oxo.
7. Forbindelse ifølge et af kravene 1 til 3, hvor R3 og R4 sammen med den ring, hvortil de er bundet, danner en kondenseret ring, som er valgt blandt heterocyclyl- og heteroarylringe, eventuelt substitueret med mindst en substituent R9, der er repræsenteret ved
hvor R1 og R2 er defineret som i formlen (I), og X er valgt blandt -O-, -NR'- og -CR'R", hvor R' og R" uafhængigt er valgt blandt H, halogenalkyl eller alkyl.
8. Forbindelse ifølge et af kravene 1 til 3, hvor R3 og R4 sammen med den ring, hvortil de er bundet, danner en kondenseret ring, som er valgt blandt hetero-cvclvl- oq heteroarylringe, der er repræsenteret ved
9. Forbindelse ifølge et af kravene 1 til 8, hvor R5 er methyl, ethyl, propyl, isppopyl, butyl, tert-butyl, pentyl, neopentyl, hexyl, octyl, nonyl eller decyl, hvoraf hver eventuelt er substitueret med et eller to eller tre halogener.
10. Forbindelse ifølge et af kravene 1 til 8, hvor R5 er phenyl eller naphthyl, hvoraf hver eventuelt er substitueret med en eller to eller tre substituenter R9 som defineret i formlen (I) ifølge krav 1.
11. Forbindelse ifølge et af kravene 1 til 8, hvor R5 er phenyl eller naphthyl, hvoraf hver eventuelt er substitueret med en eller to eller tre substituenter R9, der er valgt blandt halogen, halogenalkyl, alkyl, alkenyl, alkynyl, -alkyl-NR'R", -CN, -OR', -NR'R" og nitro, hvor R' og R" uafhængigt er valgt blandt H, halogenalkyl og alkyl, eller (R' og R") sammen med det nitrogenatom, hvortil de er bundet, danner en ring, som er valgt blandt heterocyclyl, eventuelt substitueret med halogen og alkyl.
12. Forbindelse ifølge et af kravene 1 til 8, hvor R5 er pyridinyl or pyrimidinyl, hvoraf hver eventuelt er substitueret med en eller to eller tre substituenter R9 som defineret i formlen (I) ifølge krav 1.
13. Forbindelse ifølge et af kravene 1 til 8, hvor R5 er pyridinyl eller pyrimidinyl, hvoraf hver eventuelt er substitueret med en eller to eller tre substituenter R9, der er valgt blandt halogen, halogenalkyl, alkyl, alkenyl, alkynyl, -alkyl-NR'R", -CN, -OR', -NR'R" og nitro, hvor R' og R" uafhængigt er valgt blandt H, halogenalkyl og alkyl, eller (R' og R") sammen med det nitrogenatom, hvortil de er bundet, danner en ring, der er valgt blandt heterocyclyl, eventuelt substitueret med halogen og alkyl.
14. Forbindelse ifølge et af kravene 1 til 8, hvor R5 er tetrahydropyranyl or piperidinyl, hvoraf hver eventuelt er substitueret med en eller to eller tre substituenter R9 som defineret i formlen (I) ifølge krav 1.
15. Forbindelse ifølge et af kravene 1 til 8, hvor R5 er tetrahydropyranyl eller piperidinyl, hvoraf hver eventuelt er substitueret med en eller to eller tre substituenter R9, der er valgt blandt halogen, halogenalkyl, alkyl, alkenyl, alkynyl, -alkyl-NR'R", -CN, -OR', -NR'R" og nitro, hvor R' og R" uafhængigt er valgt blandt H, halogenalkyl og alkyl, eller (R' og R") sammen med det nitrogenatom, hvortil de er bundet, danner en ring, der er valgt blandt heterocyclyl, eventuelt substitueret med halogen og al kyl.
16. Forbindelse ifølge et af kravene 1 til 8, hvor R5 er en monocyklisk eller bicyklisk cycloalkylgruppe, hvoraf hver eventuelt er substitueret med en eller to eller tre substituenter R9 som defineret i formlen (I) ifølge krav 1.
17. Forbindelse ifølge et af kravene 1 til 8, hvor R5 er en monocyklisk cycloalkylgruppe, der er valgt blandt cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl og cyclooctyl; eller en bicyklisk cycloalkylgruppe, der er valgt blandt dem, der er anbragt som en bicyklisk ring, valgt blandt [4,4]-, [4,5]-, [5,5]-, [5,6]- og [6,6]-ringsystemer, hvoraf hver eventuelt er substitueret med en eller to eller tre substituenter R9, der er valgt blandt halogen, halogenalkyl, alkyl, alkenyl, alkynyl, -alkyl-NR'R", - CN, -OR', -NR'R" og nitro, hvor R' og R" uafhængigt er valgt blandt H, halogenalkyl og alkyl, eller (R' og R") sammen med nitrogenatomet, hvortil de er bundet, form en ring, som er valgt blandt heterocyclyl, eventuelt substitueret med halogen og alkyl.
18. Forbindelse ifølge krav 7, der er i en af de følgende konfigurationer:
eller
19. Forbindelse ifølge krav 1, med formlen (III):
eller en stereoisomer deraf eller et farmaceutisk acceptabelt salt deraf, hvor: R1 og R2, der kan være det samme eller forskellige, hver især er valgt blandt hydrogen, halogen og alkyl, eventuelt substitueret med mindst en substituent R9; R5 er valgt blandt alkyl-, cycloalkyl-, heterocyclyl-, aryl-, heteroarylringe, hvoraf hver eventuelt er substitueret med mindst en substituent R9; R9 er valgt blandt halogen, halogenalkyl, alkyl, alkenyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, alkynyl, oxo, -alkyl-NR'R", -CN, -OR', -NR'R", -COR', -CO2R', -CONR'R",-C(=NR')NR"R'", nitro, -NR'COR", -NR'CONR'R", -NROO2R", , -SO2-aryl,-NR'SO2NR"R"', NR'SO2R" og -NR'SO2-aryl, hvor cycloalkyl-, aryl-, heteroaryl- eller heterocyclylgruppen hver især uafhængigt eventuelt er substitueret med en, to eller tre substituenter, der er valgt blandt halogen, alkyl og halogenalkyl, hvor R', R" og R'" uafhængigt valgt blandt H, halogenalkyl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl og heteroaryl, eller (R' og R"), og/eller (R" og R'") sammen med atomerne, hvortil de er bundet, danner en ring, som er valgt blandt heterocyclyl, eventuelt substitueret med halogen og alkyl, og heteroarylringe, eventuelt substitueret med halogen og alkyl.
20. Forbindelse ifølge krav 19, hvor R5 er phenyl, eventuelt substitueret med en eller to eller tre substituenter R9, der er valgt blandt halogen, halogenalkyl, alkyl, alkenyl, alkynyl, -alkyl-NR'R",-CN, -OR', -NR'R" og nitro, hvor R' og R" uafhængigt er valgt blandt H, halogenalkyl og alkyl, eller (R' og R") sammen
med det nitrogenatom, hvortil de er bundet, danner en ring, der er valgt blandt heterocyclyl, eventuelt substitueret med halogen og alkyl.
21. Forbindelse ifølge krav 1, der er
eller en stereoisomer deraf eller et farmaceutisk acceptabelt salt deraf.
22. Farmaceutisk sammensætning omfattende mindst en farmaceutisk acceptabel bærer og som en aktiv bestanddel en terapeutisk virksom mængde af en forbindelse ifølge et af kravene 1 -21 eller en stereoisomer deraf eller et farmaceutisk acceptabelt salt deraf.
23. Forbindelse ifølge et af kravene 1-21 eller en stereoisomer deraf eller et farmaceutisk acceptabelt salt deraf til anvendelse ved behandling af cancer, som reagerer på inhibering af Raf-kinase- og/eller Raf-kinase-dimer.
24. Forbindelse ifølge et af kravene 1-21 eller en stereoisomer deraf eller et farmaceutisk acceptabelt salt deraf til anvendelse ved behandling eller forebyggelse af cancer, der valgt blandt gruppen bestående af melanomer og skjoldbruskkirtelcancer, Barrets adenokarcinom, brystcancer, livmoderhalscancer, kolorektal cancer, mavecancer, lungecancer, æggestokcancer, cancer
i bugspytkirtlen, prostatacancer, hæmatologiske cancertyper, cancer i galdegangen, non-samll-celle-lungecancer, endometriumcancer, blodcancer, tyk-tarmskarcinom, histiocytisk lymfom og lungeadenokarcinom.
DK14818636.4T 2013-06-28 2014-06-27 Kondenserede tricykliske urinstofforbindelser som RAF-kinase- og/eller RAF-kinase-dimerhæmmere DK3013798T3 (da)

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WO2014206343A1 (en) * 2013-06-28 2014-12-31 Beigene, Ltd. Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors
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