DK3109240T3 - Triazinforbindelse og anvendelse deraf til medicinske formål - Google Patents

Triazinforbindelse og anvendelse deraf til medicinske formål Download PDF

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DK3109240T3
DK3109240T3 DK15751885.3T DK15751885T DK3109240T3 DK 3109240 T3 DK3109240 T3 DK 3109240T3 DK 15751885 T DK15751885 T DK 15751885T DK 3109240 T3 DK3109240 T3 DK 3109240T3
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alkyl
mmol
compound
mixture
chloro
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Hironobu Nagamori
Ikuo Mitani
Masaki Yamashita
Takahiro Hotta
Yuichi Nakagawa
Masatoshi Ueda
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Japan Tobacco Inc
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Claims (19)

1. Forbindelse repræsenteret ved formlen [I] eller et farmaceutisk acceptabelt salt deraf;
hvor Xer CH eller N, ring Cy er formlen:
eller formlen:
{hvor R1 er (1) halogen, (2) C1-6 alkyl, (3) cyano eller
(4) haloCi-4 alkyl, R2 er (1) halogen, (2) hydroxy, (3) carboxy, (4) C1-6 alkyl, (5) C1-6 alkoxy, (6) haloCi-4 alkoxy, (7) haloCi-4 alkyl, (8) C1-6 alkyl-carbonyl, (9) -C(O)NRa1 Ra2 (Ra1 og Ra2 hver uafhængigt er hydrogen eller C1-6 alkyl) eller (10) -(CnH2n)-Rb (n er 1,2, 3 eller 4, -(CnH2n)- kan være en lige eller forgrenet kæde, og Rb er (a) hydroxy, (b) carboxy, (c) C1-6 alkoxy, (d) C1-6 alkyl-carbonyloxy, (e) -C(O)NRb1Rb2 (Rb1 og Rb2 hver uafhængigt er hydrogen eller Ci-e alkyl), (f) -OC(O)NRb3Rb4 (Rb3 og Rb4 hver uafhængigt er hydrogen eller C1-6 alkyl), (g) -NRb5C(O)NRb6Rb7 (Rb5, Rb6 og Rb7 hver uafhængigt er hydrogen eller C1-6 alkyl), (h) -NRb8Rb9 (Rb8 og Rb9 hver uafhængigt er hydrogen, C1-6 alkyl eller haloCi-4 alkyl), (i) -NRb10S(O)2Rb11 (Rb1° og Rb11 hver uafhængigt er hydrogen, C1-6 alkyl eller C3-7 cycloalkyl), (j) -NRb12C(O)ORb13 (Rb12 er hydrogen eller C1-6 alkyl, og Rb13 er C1-6 alkyl), (k) -NRb14C(O)Rb15 (Rb14 er hydrogen eller C1-6 alkyl, og Rb15 er (i) Ce-io aryl, (11) C1-8 alkyl (hvilket C1-8 alkyl eventuelt er substitueret med 1,2 eller 3 substi-tuenter udvalgt fra gruppen bestående af hydroxy, haloCi-4 alkyl, C1-6 alkoxy og Ce-io aryl), (iii) adamantyl eller (iv) C3-7 cycloalkyl (hvilket C3-7-cycloalkyl eventuelt er substitueret med 1,2, 3 eller 4 substituenter udvalgt fra gruppen bestående af C1-6 alkyl, halogen, hydroxyl C1-6 alkyl og halo C1-4 alkyl, og/eller eventuelt danner en fusioneret ring med en benzenring), eller Rb14 og Rb15 eventuelt danner et 4-, 5- eller 6-leddet lactam sammen med nitrogenatomet, som Rb14 er bundet til, og carbonatomet, som Rb15 er bundet til (hvor lactamet eventuelt er substitueret med 1, 2 eller 3 C1-6 alkyler og/eller eventuelt danner en fusioneret ring med en benzenring)), (l) formlen:
hvor m2 og m3 hver uafhængigt er 1,2 eller 3, m4 er 0, 1,2, 3 eller 4, Rb16 er C1-6 alkyl eller C1-6 alkoxy, og, når m4 er 2, 3 eller 4, hvert Rb16 er udvalgt uafhængigt, eller (m) formlen:
hvor m5 og m6 hver uafhængigt er 1,2 eller 3, ogRb17 er C1-6 alkyl eller C1-6 alkoxy), R3 er (1) halogen, (2) hydroxy, (3) C1-6 alkyl eller (4) -ORC {Rc er C1-6 alkyl eventuelt substitueret med 1, 2 eller 3 substituenter udvalgt fra gruppen bestående af de følgende (a) til (f); (a) halogen, (b) hydroxy, (c) C1-6 alkoxy, (d) -C(O)NRc1Rc2 (Rc1 og Rc2 hver uafhængigt er hydrogen eller C1-6 alkyl), (e) Ce-io aryl (hvilket Ce-io aryl eventuelt er substitueret med 1,2 eller 3 substituenter udvalgt fra gruppen bestående af
(i) halogen, (ii) hydroxy, (iii) C1-6 alkyl, (iv) C1-6 alkoxy og (v) haloCi-4 alkyl) og (f) 5- eller 6-leddet heteroaryl indeholdende 1, 2 eller 3 nitrogenatomer, oxygenatomer eller svovlatomer (hvilket heteroaryl eventuelt er substitueret med 1,2 eller 3 substituenter udvalgt fra gruppen bestående af (i) halogen, (ii) hydroxy, (iii) C1-6 alkyl, (iv) C1-6 alkoxy og (v) haloCi-4 alkyl)} og R4 er (1) hydrogen, (2) halogen, (3) C1-6 alkyl eller (4) C1-6 alkoxy}, R5 er (1) halogen, (2) hydroxy, (3) C1-6 alkylsulfanyl, (4) C1-6 alkyl (hvilket Ci-e alkyl eventuelt er substitueret med 1,2 eller 3 substituenter udvalgt fra gruppen bestående af halogen, Ce-io aryl og Ci-e alkoxy), (5) C3-7 cycloalkyl, (6) -ORd {Rd er (a) C2-6 alkynyl, (b) C3-7 cycloalkyl, eventuelt substitueret med 1,2 eller 3 C1-6 alkyler eller (c) C1-8 alkyl (hvilket C1-8 alkyl eventuelt er substitueret med 1,2 eller 3 substituenter udvalgt fra gruppen bestående af de følgende (i) til (v); (i) halogen, (ii) Ce-io aryl, (iii) C1-6 alkoxy, (iv) C3-7 cycloalkyl (hvilket C3-7 cycloalkyl eventuelt er substitueret med 1, 2 eller 3 substituenter udvalgt fra gruppen bestående af Ci-e alkyl og haloCi-4 alkyl), og (v) 4-, 5- eller 6-leddet mættet heterocyclyl, der indeholder 1, 2 eller 3 nitrogenatomer, oxygenatomer eller svovlatomer (hvor det mættede heterocyclyl eventuelt er substitueret med 1,2 eller 3 substituenter udvalgt fra gruppen bestående af C1-6 alkyl og haloCi-4 alkyl))} eller (7) formlen: » hvor Re er (a) C1-6 alkyl, (b) C3-7 cycloalkyl, (c) 5- eller 6-leddet heteroaryl, der indeholder 1,2 eller 3 nitrogenatomer, oxygenatomer eller svovlatomer eller (d) Ce-io aryl (hvilket Ce-io aryl eventuelt er substitueret med 1,2 eller 3 substituenter udvalgt fra gruppen bestående af (i) halogen, (ii) C1-6 alkyl, (iii) haloCi-4 alkyl, (iv) C1-6 alkoxy og (v) haloCi-4 alkoxy) og m1 er 0, 1,2 eller 3, og, når m1 er 2 eller 3, hvert R5 er udvalgt uafhængigt, med undtagelse af 4,6-bis-(2,5-dimethyl-phenyl)-1,3,5-triazin-2-ol.
2. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, hvor ring Cy er formlen:
hvor R1, R2 og R3 4 er som defineret i krav 1.
3. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, hvor ring Cy er formlen:
hvor R1, R3 og R4 er som defineret i krav 1.
4. Forbindelse ifølge et af kravene 1 til 3 eller et farmaceutisk acceptabelt salt deraf, hvor X er CH.
5. Forbindelse ifølge et af kravene 1 til 3 eller et farmaceutisk acceptabelt salt deraf, hvor X er N.
6. Forbindelse ifølge et af kravene 1 til 5 eller et farmaceutisk acceptabelt salt deraf, hvor R1 er (1) chlor, (2) methyl, (3) cyano eller (4) trifluormethyl.
7. Forbindelse ifølge et af kravene 1 til 6 eller et farmaceutisk acceptabelt salt deraf, hvor R4 er hydrogen.
8. Forbindelse ifølge et af kravene 1,2 og 4 til 7 eller et farmaceutisk acceptabelt salt deraf, hvor R2 er -(CnH2n)-Rb (n er 1 eller 2, -(CnH2n)- kan være en lige eller forgrenet kæde, og Rb er (a) -C(O)NRb1Rb2, (b) -NRb5C(O)NRb6Rb7, (c) -NRb10S(O)2Rb11 eller (d) -NRb14C(0)Rb15 (Rb1, Rb2, Rb5, Rb6, Rb7, Rb1°, Rb11, Rb14 og Rb15 er som defineret i krav 1)).
9. Forbindelse ifølge krav 8 eller et farmaceutisk acceptabelt salt deraf, hvor R2 er -CH2-Rb (Rb er som defineret i krav 8).
10. Forbindelse ifølge et af kravene 1 og 3 til 9 eller et farmaceutisk acceptabelt salt deraf, hvor R3 er (1) halogen, (2) hydroxy, (3) Ci-e alkyl eller (4) -ORC {Rc er Ci-e alkyl, som eventuelt er substitueret med 1,2 eller 3 substituenter udvalgt fra gruppen bestående af de følgende (a) til (f) (a) halogen, (b) hydroxy, (c) Ci-e alkoxy, (d) -C(O)NRc1Rc2 (Rc1 og Rc2 hver uafhængigt er hydrogen eller Ci-e alkyl), (e) phenyl (hvilket phenyl eventuelt er substitueret med 1,2 eller 3 substituenter udvalgt fra gruppen bestående af (i) halogen, (ii) hydroxy, (iii) Ci-e alkyl, (iv) C1-6 alkoxy og (v) haloCi-4 alkyl) og (f) pyridyl (hvilket pyridyl eventuelt er substitueret med 1,2 eller 3 substituenter udvalgt fra gruppen bestående af (i) halogen, (ii) hydroxy, (iii) Ci-e alkyl, (iv) C1-6 alkoxy og (v) haloCi-4 alkyl)}.
11. Forbindelse ifølge et af kravene 1 til 10 eller et farmaceutisk acceptabelt salt deraf, hvor m1 er 1, og R5 er formlen:
hvor Re er som defineret i krav 1.
12. Forbindelse ifølge krav 1 udvalgt blandt de følgende formler:
eller et farmaceutisk acceptabelt salt deraf.
13. Farmaceutisk sammensætning omfattende forbindelsen ifølge et af kravene 1 til 12 eller et farmaceutisk acceptabelt salt deraf og et farmaceutisk acceptabelt bærestof.
14. En mPGES-1 -inhibitor omfattende forbindelsen ifølge etaf kravene 1 til 12 eller et farmaceutisk acceptabelt salt deraf.
15. Terapeutisk eller profylaktisk middel til anvendelse ved behandling af smerte, reumatisme, feber, osteoartrose, arteriosklerose, Alzheimers sygdom, multipel sklerose, glaukom, okulær hypertension, iskæmisk retinal sygdom, systemisk sklerodermi eller kræft omfattende forbindelsen ifølge et af kravene 1 til 12 eller et farmaceutisk acceptabelt salt deraf.
16. Terapeutisk eller profylaktisk middel til anvendelse ved behandling af glaukom eller okulær hypertension, omfattende forbindelsen ifølge et af kravene 1 til 12 eller et farmaceutisk acceptabelt salt deraf og en eller flere typer af andre terapeutiske midler mod glaukom i kombination.
17. Forbindelse ifølge et af kravene 1 til 12 eller et farmaceutisk acceptabelt salt deraf til anvendelse ved inhibering af mPGES-1.
18. Forbindelse ifølge et af kravene 1 til 12 eller et farmaceutisk acceptabelt salt deraf til anvendelse ved behandling eller forebyggelse af smerte, reumatisme, feber, osteoartrose, arteriosklerose, Alzheimers sygdom, multipel sklerose, glaukom, okulær hypertension, iskæmisk retinal sygdom, systemisk skle-rodermi eller kræft.
19. Forbindelse til anvendelse ifølge krav 18, som er til anvendelse ved behandling eller forebyggelse af glaukom eller okulær hypertension, hvor anvendelsen yderligere omfatter indgivelse af en farmaceutisk virksom mængde af en eller flere typer af andre terapeutiske midler mod glaukom.
DK15751885.3T 2014-02-20 2015-02-19 Triazinforbindelse og anvendelse deraf til medicinske formål DK3109240T3 (da)

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