DK2576541T3 - Aminopyrimidinderivater som lrrk2-modulatorer - Google Patents

Aminopyrimidinderivater som lrrk2-modulatorer Download PDF

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DK2576541T3
DK2576541T3 DK11724168.7T DK11724168T DK2576541T3 DK 2576541 T3 DK2576541 T3 DK 2576541T3 DK 11724168 T DK11724168 T DK 11724168T DK 2576541 T3 DK2576541 T3 DK 2576541T3
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ylamino
pyrimidin
methoxy
methylamino
chloro
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Daniel Jon Burdick
Mark Chambers
Bryan K Chan
Huifen Chen
Anthony Estrada
Janet L Gunzner
Daniel Shore
Shumei Wang
Guiling Zhao
Charles Baker-Glenn
Zachary Kevin Sweeney
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Hoffmann La Roche
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Claims (23)

1. Forbindelse med formel I:
I eller farmaceutisk acceptable salte deraf, hvor: m er fra 0 til 3; X er: -NRa-; og Ra er hydrogen eller Ci-6alkyl; R1 er: Ci-ealkyl; C2-ealkenyl; C2-ealkynyl; halo-Ci-ealkyl; Ci-ealkoxy-Ci-ealkyl; hydroxy-C2-ealkenyl; amino-Ci-ealkyl; Ci-ealkylsulfonyl-Ci-ealkyl; C3-ecycloalkyl eventuelt substitueret med Ci-ealkyl; Cs-ecycloalkyl-Ci-ealkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; tetrahydropyranyl; tetrahydropyranyl-Ci-ealkyl, oxetanyl; eller oxetan-Ci-ealkyl; eller R1 og Ra sammen med de atomer til hvilke de er bundet kan danne en tre- til seks-leddet ring der eventuelt kan omfatte et yderligere heteroatom valgt fra O, N og S, og som er substitueret med oxo, halo eller Ci-6alkyl; R2 er: halo; Ci-ealkoxy; cyano; C2-ealkynyl; C2-ealkenyl; halo-Ci-ealkyl; halo-Ci-6alkoxy; C3-6cycloalkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-ealkyl; Cs-ecycloalkyl-Ci-ealkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; acetyl; oxetanyl; eller oxetan-Ci-6alkyl; R3 er: -OR4; halo; cyano; Ci-ealkyl; halo-Ci-ealkyl; C3-6cycloalkyl eventuelt substitueret med Ci-ealkyl; Cs-ecycloalkyl-Ci-ealkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; oxetanyl; eller oxetan-Ci-6alkyl; R4 er: hydrogen, Ci-ealkyl; halo-Ci-ealkyl; Ci-ealkoxy-Ci-ealkyl; C3-6cycloalkyl eventuelt substitueret med Ci-6alkyl eller halo; C3-6cycloalkyl-Ci-6alkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl eller halo; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; oxetanyl; eller oxetan-Ci-6alkyl; R5 er: hydrogen; eller Ci-6alkyl; n er 0 eller 1; R6 er: hydrogen; Ci-6alkyl; Ci-6alkoxy-Ci-6alkyl; hydroxy-Ci-6alkyl; amino-Ci-ealkyl; C3-6cycloalkyl; Cs-ecycloalkyl-Ci-ealkyl; heterocyclyl; eller heterocyclyl-Ci-ealkyl; hvor C3-6cycloalkyl, Cs-ecycloalkyl-Ci-ealkyl, heterocyclyl og heterocyclyl-Ci-6alkyl hver eventuelt kan være substitueret med en, to, tre eller fire grupper uafhængigt valgt fra: Ci-6alkyl; halo-Ci-6alkyl; Ci-6alkoxy; halo-Ci-6alkoxy; hydroxy; hydroxy-Ci-6alkyl; halo; nitril; Ci-ealkyl-carbonyl; Ci-ealkyl-sulfonyl; C3-ecycloalkyl; Cs-ecycloalkyl-Ci-ealkyl; C3-6cycloalkyl-carbonyl; amino; eller heterocyclyl; eller to af grupperne sammen med de atomer til hvilke de er bundet kan danne en fem- eller seks-leddet ring; eller R5 og R6 sammen med det nitrogenatom til hvilket de er bundet danner en tre- til syv-leddet ring der eventuelt omfatter et yderligere heteroatom valgt fra O, N og S(0)n, og som eventuelt er substitueret med en- to, tre eller fire grupper uafhængigt valgt fra: Ci-6alkyl; halo-Ci-6alkyl; Ci-ealkoxy; halo-Ci-ealkoxy; hydroxy; hydroxy-Ci-ealkyl; halo, nitril; Ci-ealkyl-carbonyl; Ci-ealkyl-sulfonyl; C3-ecycloalkyl; Cs-ecycloalkyl-Ci-ealkyl; C3-6cycloalkyl-carbonyl; amino; Ci-ealkyl-heterocyclyl, Ci-ealkoxy-Ci-ealkyl eller heterocyclyl; eller to af grupperne sammen med de atomer til hvilke de er bundet kan danne en fem- eller seks-leddet ring; og R7 er: halo; Ci-6alkyl; Ci-6alkoxy; halo-Ci-6alkyl; eller halo-Ci-6alkoxy.
2. Forbindelse med formel I ifølge krav 1:
I eller farmaceutisk acceptable salte deraf, hvor: m er fra 0 til 3; X er: -NRa-; og Ra er hydrogen eller Ci-6alkyl; R1 er: Ci-ealkyl; C2-ealkenyl; C2-ealkynyl; halo-Ci-ealkyl; Ci-ealkoxy-Ci-ealkyl; hydroxy-C2-6alkenyl; amino-Ci-ealkyl; Ci-ealkylsulfonyl-Ci-ealkyl; C3-ecycloalkyl eventuelt substitueret med Ci-ealkyl; Cs-ecycloalkyl-Ci-ealkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; oxetanyl; eller oxetan-Ci-ealkyl; eller R1 og Ra sammen med de atomer til hvilke de er bundet kan danne en tre- til seks-leddet ring der eventuelt kan omfatte et yderligere heteroatom valgt fra O, N og S, og som er substitueret med oxo, halo eller Ci-6alkyl; R2 er: halo; Ci-ealkoxy; cyano; C2-ealkynyl; C2-ealkenyl; halo-Ci-ealkyl; halo-Ci-6alkoxy; C3-6cycloalkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-ealkyl; Cs-ecycloalkyl-Ci-ealkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; acetyl; oxetanyl; eller oxetan-Ci-6alkyl; R3 er: -OR4; halo; cyano; Ci-ealkyl; halo-Ci-ealkyl; C3-6cycloalkyl eventuelt substitueret med Ci-6alkyl; C3-6cycloalkyl-Ci-6alkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; oxetanyl; eller oxetan-Ci-6alkyl; R4 er: Ci-ealkyl; halo-Ci-ealkyl; Ci-ealkoxy-Ci-ealkyl; C3-6cycloalkyl eventuelt substitueret med Ci-6alkyl eller halo; C3-6cycloalkyl-Ci-6alkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl eller halo; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; oxetanyl; eller oxetan-Ci-ealkyl; R5 er: hydrogen; eller Ci-6alkyl; n er 0 eller 1; R6 er: hydrogen; Ci-6alkyl; Ci-6alkoxy-Ci-6alkyl; hydroxy-Ci-6alkyl; amino-Ci-ealkyl; C3-6cycloalkyl; Cs-ecycloalkyl-Ci-ealkyl; heterocyclyl; eller heterocyclyl-Ci-ealkyl; hvor C3-6cycloalkyl, Cs-ecycloalkyl-Ci-ealkyl, heterocyclyl og heterocyclyl-Ci-6alkyl hver eventuelt kan være substitueret med en, to, tre eller fire grupper uafhængigt valgt fra: Ci-6alkyl; halo-Ci-6alkyl; Ci-6alkoxy; halo-Ci-6alkoxy; hydroxy; hydroxy-Ci-6alkyl; halo; nitril; Ci-ealkyl-carbonyl; Ci-ealkyl-sulfonyl; C3-ecycloalkyl; Cs-ecycloalkyl-Ci-ealkyl; C3-6cycloalkyl-carbonyl; amino; eller heterocyclyl; eller to af grupperne sammen med de atomer til hvilke de er bundet kan danne en fem- eller seks-leddet ring; eller R5 og R6 sammen med det nitrogenatom til hvilket de er bundet danner en tre- til syv-leddet ring der eventuelt omfatter et yderligere heteroatom valgt fra O, N og S(0)n, og som eventuelt er substitueret med en- to, tre eller fire grupper uafhængigt valgt fra: Ci-6alkyl; halo-Ci-6alkyl; Ci-ealkoxy; halo-Ci-ealkoxy; hydroxy; hydroxy-Ci-ealkyl; halo, nitril; Ci-ealkyl-carbonyl; Ci-ealkyl-sulfonyl; C3-ecycloalkyl; Cs-ecycloalkyl-Ci-ealkyl; C3-6cycloalkyl-carbonyl; amino; eller heterocyclyl; eller to af grupperne sammen med de atomer til hvilke de er bundet kan danne en fem- eller seks-leddet ring; og R7 er: halo; Ci-6alkyl; Ci-6alkoxy; halo-Ci-6alkyl; eller halo-Ci-6alkoxy.
3. Forbindelse ifølge et af kravene 1-2, hvor forbindelsen er ifølge formel II:
II eller et farmaceutisk acceptabelt salt deraf, hvor: m er fra 0 til 3; X er: -NRa-; og Ra er hydrogen eller Ci-6alkyl; R1 er: Ci-ealkyl; C2-ealkenyl; C2-ealkynyl; halo-Ci-ealkyl; Ci-ealkoxy-Ci-ealkyl; hydroxy-C2-ealkenyl; amino-Ci-ealkyl; Ci-ealkylsulfonyl-Ci-ealkyl; C3-ecycloalkyl eventuelt substitueret med Ci-ealkyl; Cs-ecycloalkyl-Ci-ealkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; oxetanyl; eller oxetan-Ci-ealkyl; R2 er: halo; Ci-ealkoxy; cyano; C2-ealkynyl; C2-ealkenyl; halo-Ci-ealkyl; halo-Ci-6alkoxy; C3-6cycloalkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-ealkyl; Cs-ecycloalkyl-Ci-ealkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; oxetanyl; eller oxetan-Ci-6alkyl; R3 er: -OR4; halo; cyano; C3-6cycloalkyl eventuelt substitueret med Ci-ealkyl; C3-6cycloalkyl-Ci-6alkyl hvor C3-6cycloalkyldelen eventuelt er substitueret med Ci-6alkyl; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; oxetanyl; eller oxetan-Ci-6alkyl; R4 er: Ci-ealkyl; halo-Ci-ealkyl; Ci-ealkoxy-Ci-ealkyl; C3-ecycloalkyl eventuelt substitueret med Ci-ealkyl; Cs-ecycloalkyl-Ci-ealkyl hvor C3-ecycloalkyldelen eventuelt er substitueret med Ci-6alkyl; tetrahydrofuranyl; tetrahydrofuranyl-Ci-6alkyl; oxetanyl; eller oxetan-Ci-6alkyl; R5 er: hydrogen; eller Ci-6alkyl; R6 er: hydrogen; Ci-ealkyl; Ci-ealkoxy-Ci-ealkyl; amino-Ci-ealkyl; C3-ecycloalkyl; Cs-ecycloalkyl-Ci-ealkyl; heterocyclyl; eller heterocyclyl-Ci-ealkyl; hvor C3-6cycloalkyl, Cs-ecycloalkyl-Ci-ealkyl, heterocyclyl og heterocyclyl-Ci-6alkyl hver eventuelt kan være substitueret med en, to eller tre grupper uafhængigt valgt fra: Ci-6alkyl; halo-Ci-6alkyl; Ci-6alkoxy; halo-Ci-ealkoxy; hydroxy; hydroxy-Ci-ealkyl; halo; nitril; Ci-ealkyl-carbonyl; Ci-ealkyl-sulfonyl; C3-ecycloalkyl; Cs-ecycloalkyl-Ci-ealkyl; C3-6cycloalkyl-carbonyl; amino; eller heterocyclyl; eller to af grupperne sammen med de atomer til hvilke de er bundet kan danne en fem- eller seks-leddet ring; eller R5 og R6 sammen med det nitrogenatom til hvilket de er bundet danner en tre- til syv-leddet ring der eventuelt omfatter et yderligere heteroatom valgt fra O, N og S(0)n, og som eventuelt er substitueret med en, to eller tre grupper uafhængigt valgt fra: Ci-6alkyl; halo-Ci-6alkyl; Ci-6alkoxy; halo-Ci-6alkoxy; hydroxy; hydroxy-Ci-6alkyl; halo, nitril; Ci-6alkyl-carbonyl; Ci-6alkyl-sulfonyl; C3-6Cycloalkyl; C3-6Cycloalkyl-Ci-6alkyl; C3-6cycloalkyl-carbonyl; amino; eller heterocyclyl; eller to af grupperne sammen med de atomer til hvilke de er bundet kan danne en fem- eller seks-leddet ring; og R7 er: halo; Ci-6alkyl; Ci-6alkoxy; halo-Ci-6alkyl; eller halo-Ci-6alkoxy.
4. Forbindelse ifølge krav 3, hvor m er 0 eller 1.
5. Forbindelse ifølge krav 3, hvor R1 er Ci-6alkyl.
6. Forbindelse ifølge krav 3, hvor R2 er: halo; halo-Ci-6alkyl; eller cyano.
7. Forbindelse ifølge krav 3, hvor R2 er: chlor, trifluormethyl eller cyano.
8. Forbindelse ifølge krav 3, hvor R3 er: halo; eller -OR4.
9. Forbindelse ifølge krav 3, hvor R3 er: halo; Ci-6alkoxy; eller halo-Ci-6alkoxy.
10. Forbindelse ifølge krav 3, hvor R3 er: methoxy; chlor; eller fluor.
11. Forbindelse ifølge krav 3 hvor m er 1 og R7 er halo eller methoxy.
12. Forbindelse ifølge krav 3, hvor R5 og R6 sammen med det nitrogenatom til hvilket de er bundet danner en tre- til seks-leddet ring der eventuelt omfatter et yderligere heteroatom valgt fra O, N og S, og som eventuelt er substitueret med en, to eller tre grupper uafhængigt valgt fra Ci-6alkyl, halo-Ci-6alkyl, Ci-6alkoxy, halo-Ci-ealkoxy, hydroxy, hydroxy- Ci-ealkyl, halo, nitril, Ci-ealkyl-carbonyl, Ci-ealkyl-sulfonyl, C3-6cycloalkyl, Cs-ecycloalkyl-Ci-ealkyl, C3-6cycloalkyl-carbonyl, amino, eller heterocyclyl, eller to af grupperne sammen med de atomer til hvilke de er bundet kan danne en fem- eller seks-leddet ring.
13. Forbindelse ifølge krav 3, hvor R5 og R6 sammen med det nitrogenatom til hvilket de er bundet danner en morpholinylgruppe der eventuelt er substitueret én eller to gange med grupper uafhængigt valgt fra Ci-6alkyl, halo-Ci-6alkyl, Ci-6alkoxy, halo-Ci-6alkoxy, hydroxy, hydroxy-Ci-6alkyl, halo, nitril, Ci-6alkyl-carbonyl, Ci-ealkyl-sulfonyl, C3-6cycloalkyl, Cs-ecycloalkyl-Ci-ealkyl, C3-6cycloalkyl-carbonyl, amino, eller heterocyclyl, eller de to grupper sammen med de atomer til hvilke de er bundet kan danne en fem- eller seks-leddet ring.
14. Forbindelse ifølge krav 3 hvor forbindelsen er ifølge formel III
III hvor: p er fra O til 2; Y er: -0-; -S(0)n-; -NR10; eller -CRnR12- når p er 1 eller 2; og Y er -CRnR12- når p er 0; R8 og R9 hver uafhængigt er: hydrogen; Ci-ealkyl; halo-Ci-6alkyl; Ci-6alkoxy; halo-Ci-6alkoxy; hydroxy; hydroxy-Ci-6alkyl; halo; nitril; Ci-6alkyl-carbonyl; Ci-ealkyl-sulfonyl; C3-6cycloalkyl; Cs-ecycloalkyl-Ci-ealkyl; C3-6cycloalkyl-carbonyl; amino; eller heterocyclyl; eller R8 og R9 sammen med de atomer til hvilke de er bundet danner en fem- eller seks-leddet ring; R10 er: hydrogen; Ci-ealkyl; hydroxy-Ci-ealkyl; halo-Ci-ealkyl; hydroxy-Ci-ealkyl; Ci-ealkyl-carbonyl; Ci-ealkyl-sulfonyl; C3-6cycloalkyl; C3-6cycloalkyl-Ci-ealkyl; C3-6cycloalkyl-carbonyl; heterocyclyl; eller heterocyclyl-Ci-ealkyl; eller en af R8 og R9 sammen med R10 og atomerne til hvilket de er bundet danner en fem- eller seks-leddet ring; R11 er: hydrogen; Ci-6alkyl; eller halo; R12 er: hydrogen; Ci-ealkyl; halo-Ci-ealkyl; Ci-ealkoxy; halo-Ci-ealkoxy; hydroxy; hydroxy-Ci-6alkyl; halo; nitril; Ci-6alkyl-carbonyl; Ci-6alkyl-sulfonyl; C3-6cycloalkyl; C3-6cycloalkyl-Ci-6alkyl; C3-6cycloalkyl-carbonyl; amino; heterocyclyl; eller heterocyclyl-Ci-6alkyl; eller R11 og R12 sammen med the atom til hvilket de er bundet kan danne en tre- til seks-leddet ring der eventuelt omfatter et heteroatom valgt fra O, N og S; eller en af R8 og R9 sammen med R10 og atomerne til hvilket de er bundet danner en fem- eller seks-leddet ring; eller en af R8 og R9 sammen med R12 og atomerne til hvilket de er bundet danner en fem- eller seks-leddet ring; og m, η, X, R1, R2, R3 og R7 er som defineret heri.
15. Forbindelse ifølge krav 3, hvor p er 1.
16. Forbindelse ifølge krav 3, hvorY er-O-; -NR10; eller -CRnR12-.
17. Forbindelse ifølge krav 3, hvor Y er -O-.
18. Forbindelse ifølge et hvilket som helst af kravene 1 til 17, valgt fra the grupperne bestående af 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-N-(2-hydroxy-ethyl)-2- methoxy-benzamid, 5-chlor-N-cyclopropyl-2-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2- ylamino)-benzamid, ((2S,6R)-2,6-dimethylmorpholino)(2-fluor-5-methoxy-4-(4-(methylamino)-5- (trifluormethyl)pyrimidin-2-ylamino)phenyl)methanon, (15.45) -2-oxa-5-azabicyclo[2.2.1]heptan-5-yl(2-fluor-3-methoxy-4-(4-(methylamino)-5-(trifluormethyl)pyrimidin-2-ylamino)phenyl)methanon, (15.45) -2-oxa-5-azabicyclo[2.2.1]heptan-5-yl(4-(4-(ethylamino)-5-(trifluormethyl)pyrimidin-2-ylamino)-2-fluor-3-methoxyphenyl)methanon, (2,6-diimethyl-morpholin-4-yl)-[3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-phenyl]-methanon, (2-ethoxy-5-fluor-4-(4-(methylamino)-5-(trifluormethyl)pyrimidin-2- ylamino)phenyl)(morpholino)methanon, (2-fluor-3-isopropoxy-4-(4-(methylamino)-5-(trifluormethyl)pyrimidin-2- ylamino)phenyl)(morpholino)methanon, (2-fluor-3-isopropoxy-4-(4-(methylamino)-5-(trifluormethyl)pyrimidin-2- ylamino)phenyl)(morpholino)methanon, (2-fluor-5-methoxy-4-(4-(methylamino)-5-(trifluormethyl)pyrimidin-2- ylamino)phenyl)(3-methoxypyrrolidin-l-yl)methanon, (3-methoxy-4-(5-methoxy-4-(methylamino)pyrimidin-2-ylamino)phenyl) (morpholino)methanon, (4-(4-(ethylamino)-5-(trifluormethyl)pyrimidin-2-ylamino)-2-fluor-3- methoxyphenyl)(morpholino)methanon, (4-(4-(ethylamino)-5-(trifluormethyl)pyrimidin-2-ylamino)-2-fluor-3- isopropoxyphenyl)(morpholino)methanon, (4-(4-(ethylamino)-5-(trifluormethyl)pyrimidin-2-ylamino)-3- (trifluormethoxy)phenyl)(morpholino)methanon, (4-(4-(ethylamino)-5-(trifluormethyl)pyrimidin-2-ylamino)-3- (trifluormethoxy)phenyl)(morpholino)methanon, (4-(4-(ethylamino)-5-(trifluormethyl)pyrimidin-2-yl-amino)-3- isopropoxyphenyl)(morpholino)methanon, (4-(4-(ethylamino)-5-(trifluormethyl)pyrimidin-2-ylamino)-3- isopropoxyphenyl)(morpholino)methanon, (4-(4-(ethylamino)-5-(trifluormethyl)pyrimidin-2-ylamino)-5-fluor-2- methoxyphenyl)(morpholino)methanon, (4-(4-(methylamino)-5-(trifluormethyl)pyrimidin-2-ylamino)-3- (trifluormethoxy)phenyl)(morpholino)methanon, (4-(5-chlor-4-(methylamino)pyrimidin-2-ylamino)-3- methylphenyl)(morpholino)methanon, (4-(5-chlor-4-(methylamino)pyrimidin-2-ylamino)-3-methylphenyl)(4- hydroxypiperidin-l-yl)methanon, (4-(5-cyclopropyl-4-methoxypyrimidin-2-ylamino)-3- methoxyphenyl)(morpholino)methanon, (4-{5-chlor-4-[(tetrahydro-furan-2-ylmethyl)-amino]-pyrimidin-2-ylamino}-3- methoxy-phenyl)-morpholin-4-yl-methanon, (4-{5-chlor-4-[(tetrahydro-furan-3-ylmethyl)-amino]-pyrimidin-2-ylamino}-3- methoxy-phenyl)-morpholin-4-yl-methanon, (4-diimethylamino-piperidin-l-yl)-[3-methoxy-4-(4-methylamino-5- trifluormethyl-pyrimidin-2-ylamino)-phenyl]-methanon, (4-tert-butyl-piperidin-l-yl)-[4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3- methoxyphenyl]-methanon, (5-chlor-2-methoxy-4-(4-(methylamino)-5-(trifluormethyl)pynmidin-2- ylamino)phenyl)(perdeuteromorpholino)methanon, (5-chlor-2-methoxy-4-(4-(methylamino)-5-(trifluormethyl)pyrimidin-2- ylamino)phenyl)(3-methoxypyrrolidin-l-yl)methanon, (5-chlor-4-(5-chlor-4-(methylamino)pyrimidin-2-ylamino)-2- methoxyphenyl)(morpholino)methanon, (5-fluor-2-methoxy-4-(4-(methylamino)-5-(trifluormethyl)pynmidin-2- ylamino)phenyl)(morpholino)methanon, [2-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-5-methoxy-phenyl]- morpholin-4-yl-methanon, [2-chlor-5-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [2-fluor-3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [2-fluor-5-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [2-fluor-5-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-((S)-2-methoxymethyl-pyrrolidin-l-yl)-methanon, [3-(2-fluor-ethoxy)-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [3-brom-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-phenyl]- morpholin-4-yl-methanon, [3-brom-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-phenyl]-morpholin-4-yl- methanon, [3-chlor-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-phenyl]- morpholin-4-yl-methanon, [3-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-phenyl]-morpholin-4-yl- methanon, [3-cyclobutoxy-4-(4-methylamino-5-trifliiormethyl-pyrimidin-2-ylamino)-phenyl]- morpholin-4-yl-methanon, [3-cyclobutylmethoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [3-cyclopropyl-4-(4-methylamino-5-trifluormethyl-pynmidin-2-ylamino)-phenyl]- morpholin-4-yl-methanon, [3-cyclopropylmethoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [3-ethoxy-4-(4-methylamino-5-trifluormethyl-pynmidin-2-ylamino)-phenyl]- morpholin-4-yl-methanon, [3-isopropoxy-4-(4-methylamino-5-trifluormethyl-pynmidin-2-ylamino)-phenyl]- morpholin-4-yl-methanon, [3-methoxy-4-(4-methylamino-5-prop-l-ynyl-pyrimidin-2-ylamino)-phenyl]- morpholin-4-yl-methanon, [3-methoxy-4-(4-methylamino-5-trifluormethyl-pynmidin-2-ylamino)-phenyl]- morpholin-4-yl-methanon, [3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-phenyl]-(8- oxa-3-aza-bicyclo[3.2.1]oct-3-yl)-methanon, [3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-phenyl]-(2- oxa-5-aza-bicyclo[2.2.1]hept-5-yl)-methanon, [3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-phenyl]- pyrrolidin-l-yl-methanon, [3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-phenyl]-[4- (2,2,2-trifluor-ethyl)-piperazin-l-yl]-methanon, [3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-phenyl]-(4- methoxy-piperidin-l-yl)-methanon, [4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-2-fluor-5-methoxy- phenyl]-morpholin-4-yl-methanon, [4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-2-fluor-5-methoxy- phenyl]-((S)-2-methoxymethyl-pyrrolidin-l-yl)-methanon, [4-(5-brom-4-methoxy-pyrimidin-2-ylamino)-2-chlor-5-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-brom-4-methoxy-pyrimidin-2-ylamino)-3-cyclopropoxy-phenyl]-morpholin- 4-yl-methanon, [4-(5-brom-4-methoxy-pyrimidin-2-ylamino)-3-methoxy-phenyl]-((S)-2,2-di- deutero-3-methyl-morpholin-4-yl)-methanon, [4-(5-brom-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-morpholin- 4-yl-methanon, [4-(5-brom-4-methylamino-pynmidin-2-ylamino)-3-methoxy-phenyl]-[4-(l- hydroxy-l-methyl-ethyl)-piperidin-l-yl]-methanon, [4-(5-brom-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3- trifluormethyl-pyrrolidin-l-yl)-methanon, [4-(5-brom-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4- cyclobutyl-piperazin-l-yl)-methanon, [4-(5-brom-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-[4-(2,2,2- trifluor-ethyl)-piperazin-l-yl]-methanon, [4-(5-brom-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4- methoxy-piperidin-l-yl)-methanon, [4-(5-brom-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-((R)-3- hydroxy-pyrrolidin-l-yl)-methanon, [4-(5-brom-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4-oxetan- 3- yl-piperazin-l-yl)-methanon, [4-(5-brom-4-methylamino-pyrimidin-2-ylamino)-5-chlor-2-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-cyclobutylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-cyclohexylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-cyclopentylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-ethylamino-pyrimidin-2-ylamino)-2-fluor-5-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-ethylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-morpholin-4- yl-methanon, [4-(5-chlor-4-isobutylamino-pynmidin-2-ylamino)-3-methoxy-phenyl]-morpholin- 4- yl-methanon, [4-(5-chlor-4-isopropylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-fluor-5-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-(2,2,2-trifliior-ethoxy)- phenyl]-morpholin-4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-(oxetan-3-yloxy)-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-cyclobutoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-cyclopentyloxy-phenyl]-(2- oxa-6-aza-spiro[3.3]hept-6-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-cyclopentyloxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-cyclopropoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-cyclopropyl-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-difluormethoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-difluormethoxy-phenyl]-(4- hydroxy-piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-ethoxy-phenyl]-morpholin-4- yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-hydroxy-phenyl]-morpholin-4- yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-isopropoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-morpholin- 4-yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4-hydroxy- piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(octahydro- pyrido[l,2-a]pyrazin-2-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(2-hydroxy- piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4,4- dimethyl-piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3,5- dimethyl-piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-[4-(l- hydroxy-l-methyl-ethyl)-piperidin-l-yl]-methanon, [4-(5-chlor-4-methylamino-pynmidin-2-ylamino)-3-methoxy-phenyl]-(3-hydroxy- pyrrolidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4-methyl- piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-piperidin-l- yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4,4-difluor- piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3-methyl- piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4-methoxy- piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3,3-difluor- piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4-fluor- piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3-methoxy- piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4-ethyl- piperazin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3- trifluormethyl-piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-[4-(2- hydroxy-ethyl)-piperazin-l-yl]-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(2-methyl- pyrrolidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4- hydroxymethyl-piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(2-methyl- piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-pyrrolidin-l- yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4- methansulfonyl-piperazin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3- trifluormethyl-pyrrolidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-[4-(2,2,2- trifluor-ethyl)-piperazin-l-yl]-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(2-methyl- morpholin-4-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(2,6- dimethyl-morpholin-4-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(2,2-diethyl- morpholin-4-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3- hydroxymethyl-morpholin-4-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(2-isobutyl- morpholin-4-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(2- hydroxymethyl-morpholin-4-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3,3- dimethyl-morpholin-4-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4-methyl- piperazin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4- isopropyl-piperazin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-piperazin-l- yl-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3-oxa-8- aza-bicyclo[3.2.1]oct-8-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-((S)-3- methyl-morpholin-4-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(2-oxa-5- aza-bicyclo[2.2.1]hept-5-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(8-oxa-3- aza-bicyclo[3.2.1]oct-3-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-((R)-3- methyl-morpholin-4-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4- cyclopropanecarbonyl-piperazin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3- morpholin-4-yl-azetidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-[4-(l- methyl-piperidin-4-yl)-piperazin-l-yl]-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(3,3-difluor- azetidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4- dimethylamino-piperidin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4-piperidin- 4-yl-piperazin-l-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(2-oxa-6- aza-spiro[3.3]hept-6-yl)-methanon, [4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-tnfluormethoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-chlor-4-propylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-morpholin-4- yl-methanon, [4-(5-cyclobutyl-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-cyclopropyl-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-cyclopropyl-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]- morpholin-4-yl-methanon, [4-(5-fluor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-morpholin- 4-yl-methanon, [4-(5-fluor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-(4-hydrc>xy- piperidin-l-yl)-methanon, [4-(5-iod-4-methylamino-pynmidin-2-ylamino)-3-methoxy-phenyl]-morpholin-4- yl-methanon, [4-[5-chlor-4-(2-methoxy-ethylamino)-pyrimidin-2-ylamino]-3-(2,2,2-trifluor- ethoxy)-phenyl]-morpholin-4-yl-methanon, [5-chlor-2-ethoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [5-chlor-2-methoxy-4-(4-methylamino-5-trifliiormethyl-pyrimidin-2-ylamino)- phenyl]-piperazin-l-yl-methanon, [5-chlor-2-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-(2,6-dimethyl-morpholin-4-yl)-methanon, [5-chlor-2-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [5-chlor-4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-2-methoxy- phenyl]-morpholin-4-yl-methanon, [5-chlor-4-(5-chlor-4-ethylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]- morpholin-4-yl-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]- morpholin-4-yl-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]- (4,4-difluor-piperidin-l-yl)-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]- piperazin-l-yl-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]-(4- dimethylamino-piperidin-l-yl)-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]-(3- hydroxy-pyrrolidin-l-yl)-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]- pyrrolidin-l-yl-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]-(4- hydroxy-piperidin-l-yl)-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]-(2- hydroxymethyl-morpholin-4-yl)-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]- [l,4]oxazepan-4-yl-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]- ((2R,6S)-2,6-dimethyl-morpholin-4-yl)-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]-(3- hydroxy-azetidin-l-yl)-methanon, [5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-phenyl]- ((3R,5S)-dimethyl-piperazin-l-yl)-methanon, [5-ethoxy-2-fluor-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [5-ethoxy-4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-2-fluor-phenyl]- morpholin-4-yl-methanon, {4-[5-brom-4-(2-methoxy-ethylamino)-pyrimidin-2-ylamino]-2-fluor-5-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-brom-4-(2-methoxy-ethylamino)-pyrimidin-2-ylamino]-3-ethoxy-phenyl}- morpholin-4-yl-methanon, {4-[5-brom-4-(2-methoxy-ethylamino)-pyrimidin-2-ylamino]-3-isopropoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-brom-4-(2-methoxy-ethylamino)-pyrimidin-2-ylamino]-3-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(l-methyl-cyclobutylamino)-pyrimidin-2-ylamino]-3-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(2,2,2-trifluor-ethylamino)-pyrimidin-2-ylamino]-3-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(2,2-difluor-ethylamino)-pyrimidin-2-ylamino]-3-methoxy-phenyl}- morpholin-4-yl-methanon, {4-[5-chlor-4-(2-cyclopropyl-ethylamino)-pyrimidin-2-ylamino]-3-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(2-methansulfonyl-ethylamino)-pyrimidin-2-ylamino]-3-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(2-methoxy-ethylamino)-pyrimidin-2-ylamino]-3-cyclobutoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(2-methoxy-ethylamino)-pyrimidin-2-ylamino]-3-methoxy-phenyl}- morpholin-4-yl-methanon, {4-[5-chlor-4-(2-methoxy-prc>pylamino)-pyrimidin-2-ylamino]-3-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(cyclobutylmethyl-amino)-pyrimidin-2-ylamino]-3-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(cyclopentylmethyl-amino)-pyrimidin-2-ylamino]-3-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(cyclopropylmethyl-amino)-pyrimidin-2-ylamino]-3-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(tetrahydro-furan-3-ylamino)-pyrimidin-2-ylamino]-3-methoxy- phenyl}-morpholin-4-yl-methanon, {4-[5-chlor-4-(tetrahydro-pyran-3-ylamino)-pyrimidin-2-ylamirio]-3-rnethoxy- phenyl}-morpholin-4-yl-methanon, l-[2-fluor-5-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- benzoyl]-pyrrolidin-3-carbonitril, l-[3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-benzoyl]- piperidin-4-carbonitril, l-[4-(5-brom-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-benzoyl]- piperidin-4-carbonitril, l-[4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-benzoyl]- piperidin-4-carbonitril, l-[5-chlor-2-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- benzoyl]-pyrrolidin-3-carbonitril, l-[5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-benzoyl]- piperidin-4-carbonitril, l-[5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-benzoyl]- pyrrolidin-3-carbonitril, 1- {2-[2-methoxy-4-(morpholin-4-carbonyl)-phenylamino]-4-methylamino-pyrimidin-5-yl}-ethanon, 1- {4-[4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-benzoyl]-piperazin-l-yl}-ethanon, 2- (2-methoxy-4-(2,2,6,6-tetrafluormorpholin-4-carbonyl)phenylamino)-4-(methylamino)pyrimidin-5-carbonitril, 2-(2-methoxy-4-(morpholin-4-carbonyl)phenylamino)-4-(methylamino)pyrimidin- 5-carbonitril, 2-(4-((3S,4S)-3,4-difluorpyrrolidin-l-carbonyl)-2-methoxyphenylamino)-4- (methylamino)pyrimidin-5-carbonitril, 2-(4-(4,4-difluorpiperidin-l-carbonyl)-2-methoxyphenylamino)-4- (methylamino)pyrimidin-5-carbonitril, 2-[2,5-diimethoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-l-morpholin-4-yl-ethanon, 2-[2-methoxy-4-(morpholin-4-carbonyl)-phenylamino]-4-methylamino-pyrimidin- 5-carbonitril, 2-[2-methoxy-4-(piperidin-l-carbonyl)-phenylamino]-4-methylamino-pyrimidin-5- carbonitril, 2-[2-methoxy-4-(pyrrolidin-l-carbonyl)-phenylamino]-4-methylamino-pyrimidin- 5-carbonitril, 2-[3-methoxy-4-(4-methylamino-5-trifluormethyl-pynmidin-2-ylamino)-phenyl]- 1- morpholin-4-yl-ethanon, 2- [4-((2R,6S)-2,6-diimethyl-morpholin-4-carbonyl)-5-fluor-2-methoxy-phenylamino]-4-methylamino-pyrimidin-5-carbonitnl, 2-[4-((2R,6S)-2,6-diimethyl-morpholin-4-carbonyl)-5-fluor-2-methoxy-phenylamino]-4-ethylamino-pyrimidin-5-carbonitnl, 2- [4-((R)-3 -fluor-pyrrolidin-l-carbonyl)-2-methoxy-phenylamino]-4-methylamino-pyrimidin-5-carbonitril, 2-[4-((S)-3-fluor-pyrrolidin-l-carbonyl)-2-methoxy-phenylamino]-4- methylamino-pyrimidin-5-carbonitril, 2-[4-(3,3-diifluor-azetidin-l-carbonyl)-2-methoxy-phenylamino]-4-methylamino- pyrimidin-5-carbonitril, 2-[4-(3,3-diifluor-pyrrolidin-l-carbonyl)-2-methoxy-phenylamino]-4- methylamino-pyrimidin-5-carbonitril, 2-[4-(3-fluor-azetidin-l-carbonyl)-2-methoxy-phenylamino]-4-methylamino- pyrimidin-5-carbonitril, 2-[4-(5-brom-4-methylamino-pyrimidin-2-ylamino)-2,5-dimethoxy-phenyl]-l- morpholin-4-yl-ethanon, 2-[4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2,5-dimethoxy-phenyl]-l- morpholin-4-yl-ethanon, 2-[4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-phenyl]-l- morpholin-4-yl-ethanon, 2-[4-(azetidin-l-carbonyl)-2-methoxy-phenylamino]-4-methylamino-pyrimidin-5- carbonitril, 2-[5-fluor-2-methoxy-4-(morpholin-4-carbonyl)-phenylamino]-4-methylamino- pyrimidin-5-carbonitril, 2-fluor-5-methoxy-N-(2-methoxy-ethyl)-N-methyl-4-(4-methylamino-5- trifluormethyl-pyrimidin-2-ylamino)-benzamid, 2-fluor-5-methoxy-N-methyl-4-(4-methylamino-5-trifluormethyl-pyrimidin-2- ylamino)-benzamid, 2- fluor-N-(2-hydroxy-2-methylprc>pyl)-5-methoxy-N-methyl-4-(4-(methylamino)-5-(trifluormethyl)pyrimidin-2-ylamino)benzamid, 3- methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-N-oxetan-3-yl-benzamid, 3-methoxy-4-(4-methylamino-5-trifliiormethyl-pyrimidin-2-ylamino)-N-(l-methyl- piperidin-4-yl)-benzamid, 3-methoxy-N-(2-methoxy-ethyl)-4-(4-methylamino-5-trifluormethyl-pyrimidin-2- ylamino)-benzamid, 3- methoxy-N-(2-methoxy-ethyl)-N-methyl-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-benzamid, 4- (4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-2-fluor-5-methoxy-N-(2-methoxy-ethyl)-N-methyl-benzamid, 4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-3-methoxy-phenyl]- morpholin-4-yl-methanon, 4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-3-methoxy-N-(2-methoxy- ethyl)-N-methyl-benzamid, 4-(5-chlor-4-(methylamino)pyrimidin-2-ylamino)-N,N,3-trimethylbenzamid, 4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-benzamid, 4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-N-(tetrahyd ro-pyran- 3-yl)-benzamid, 4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-N,N-dimethyl- benzamid, 4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-N-methyl-benzamid, 4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-N-oxetan-3-yl- benzamid, 4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-N-cycloprc>pyl-3-methoxy- benzamid, 4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-N-ethyl-3-methoxy-benzamid, 4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-N-isoprc>pyl-3-methoxy- benzamid, 4-(5-cyano-4-ethylamino-pyrimidin-2-ylamino)-2-fluor-5-methoxy-N,N-dimethyl- benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-2-fluor-5-methoxy-N,N- dimethyl-benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-N,N-dimethyl- benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-N-methyl-benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-N-(2,2-difluor-ethyl)-3- methoxy-benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-N-(3,3-difluor-cyclobutyl)-3- methoxy-benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-N,N-diethyl-3-methoxy- benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-N-cyclopropylmethyl-3- methoxy-benzamid, 4-(5-cyano-4-methylamino-pynmidin-2-ylamino)-N-ethyl-3-methoxy-benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-N-ethyl-3-methoxy-N-methyl- benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-N-ethyl-N-isopropyl-3-methoxy- benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-N-isoprc>pyl-3-methoxy- benzamid, 4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-N-isopropyl-3-methoxy-N- methyl-benzamid, 4-ethylamino-2-[5-fluor-2-methoxy-4-(morpholin-4-carbonyl)-phenylamino]- pyrimdine-5-carbonitril, 5-chlor-2-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-N- (l-methyl-piperidin-4-yl)-benzamid, 5-chlor-2-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-N- oxetan-3-yl-benzamid, 5-chlor-2-methoxy-N,N-dimethyl-4-(4-methylamino-5-trifluormethyl-pyrimidin-2- ylamino)-benzamid, 5-chlor-4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-2-methoxy-N-(2- methoxyethyl)-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-N,N- dimethyl-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-N-(2- methoxy-ethyl)-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-N-methyl- benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-N-oxetan-3- yl-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-N-(l-methyl- piperidin-4-yl)-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-N-(2- methoxy-ethyl)-N-methyl-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-N-(l- methylcyclobutyl)-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-N-(l-cyano-cyclopropyl)- 2-methoxy-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-N-(2-hydroxy-2-methyl- propyl)-2-methoxy-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-N-(2-hydroxy-ethyl)-2- methoxy-N-methyl-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-N-(2-hydroxy-propyl)-2- methoxy-benzamid, 5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-N-cyclopropyl-2- methoxy-benzamid, 5-chlor-N-(l-cyano-cyclopropyl)-2-methoxy-4-(4-methylamino-5-trifluormethyl- pyrimidin-2-ylamino)-benzamid, 5-chlor-N-(l-cyano-cyclopropyl)-2-methoxy-4-(4-methylamino-5-trifluormethyl- pyrimidin-2-ylamino)-benzamid, 5-chlor-N-(2-hydroxy-2-methyl-propyl)-2-methoxy-4-(4-methylamino-5- trifluormethyl-pyrimidin-2-ylamino)-benzamid, 5-chlor-N-(2-hydroxy-2-methyl-propyl)-2-methoxy-N-methyl-4-(4-methylamino- 5-trifluormethyl-pyrimidin-2-ylamino)-benzamid, 5-chlor-N-cyclopropyl-4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-2- methoxy-benzamid, azetidin-l-yl-[4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy- phenyl]-methanon, N-(3,3-diifluor-cyclobutyl)-3-methoxy-4-(4-methylamino-5-trifluormethyl- pyrimidin-2-ylamino)-benzamid, N-(3-aminopropyl)-4-(5-chlor-4-(methylamino)pyrimidin-2-ylamino)-3- methoxybenzamid, N-(3-amino-propyl)-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-3-methoxy- benzamid, N-(3-amino-propyl)-5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2- methoxy-benzamid, N-(4,4-diifluor-cyclohexyl)-3-methoxy-4-(4-methylamino-5-trifluormethyl- pyrimidin-2-ylamino)-benzamid, N,N-diiethyl-3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- benzamid, N-ethyl-2-fluor-5-methoxy-N-(2-methoxy-ethyl)-4-(4-methylamino-5- trifluormethyl-pyrimidin-2-ylamino)-benzamid, N-ethyl-3-methoxy-N-methyl-4-(4-methylamino-5-trifluormethyl-pyrimidin-2- ylamino)-benzamid, N-ethyl-4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-2-fluor-5- methoxy-N-(2-methoxy-ethyl)-benzamid, N-tert-butyl-4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-benzamid, and N-tert-butyl-5-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-2-methoxy-benzamid, eller et farmaceutisk acceptabelt salt deraf.
19. Forbindelse ifølge et hvilket som helst af kravene 1 til 18, valgt fra grupperne bestående af [3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-phenyl]- morpholin-4-yl-methanon, (5-chlor-2-methoxy-4-(4-(methylamino)-5-(trifluormethyl)pyrimidin-2- ylamino)phenyl)(perdeuteromorpholino)methanon, (5-fluor-2-methoxy-4-(4-(methylamino)-5-(trifluormethyl)pyrimidin-2- ylamino)phenyl)(morpholino)methanon, [2-fluor-3-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [3-chlor-4-(5-chlor-4-methylamino-pyrimidin-2-ylamino)-phenyl]-morpholin-4-yl- methanon, [3-isopropoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)-phenyl]- morpholin-4-yl-methanon, [4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-2-fluor-5-methoxy- phenyl]-morpholin-4-yl-methanon, [5-chlor-2-methoxy-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, [5-chlor-4-(4-ethylamino-5-trifluormethyl-pyrimidin-2-ylamino)-2-methoxy- phenyl]-morpholin-4-yl-methanon, [5-ethoxy-2-fluor-4-(4-methylamino-5-trifluormethyl-pyrimidin-2-ylamino)- phenyl]-morpholin-4-yl-methanon, 2-(2-methoxy-4-(morpholin-4-carbonyl)phenylamino)-4-(methylamino)pyrimidin-5-carbonitril, and N-tert-butyl-4-(5-cyano-4-methylamino-pyrimidin-2-ylamino)-3-methoxy-benzamid, eller et farmaceutisk acceptabelt salt deraf.
20. Sammensætning omfattende: (a) en farmaceutisk acceptabel bærer; og (b) en forbindelse ifølge krav 1.
21. Forbindelse med formel I ifølge et hvilket som helst af kravene 1-19 til anvendelse som terapeutisk aktivt stof.
22. Anvendelse af en forbindelse med formel I ifølge et hvilket som helst af kravene 1-19 til fremstillingen af et medikament til terapeutisk og/eller profylaktisk behandling af Parkinson's sygdom.
23. Forbindelse med formel I ifølge kravene 1-19 til anvendelsen som terapeutisk aktivt stof til terapeutisk og/eller profylaktisk behandling af Parkinson's sygdom.
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