ME02203B - Hinolin i hinoksalin derivati kao inhibitori kinaza - Google Patents

Hinolin i hinoksalin derivati kao inhibitori kinaza

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Publication number
ME02203B
ME02203B MEP-2015-120A MEP12015A ME02203B ME 02203 B ME02203 B ME 02203B ME P12015 A MEP12015 A ME P12015A ME 02203 B ME02203 B ME 02203B
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Montenegro
Prior art keywords
pyrido
trifluoroethyl
quinolin
pyrimidin
compound according
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MEP-2015-120A
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Andrew Harry Parton
Mezher Hussein Ali
Daniel Christopher Brookings
Julien Alistair Brown
Daniel James Ford
Richard Jeremy Franklin
Barry John Langham
Judi Charlotte Neuss
Joanna Rachel Quincey
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Ucb Biopharma Sprl
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Priority claimed from GBGB1014963.1A external-priority patent/GB201014963D0/en
Priority claimed from GBGB1101128.5A external-priority patent/GB201101128D0/en
Application filed by Ucb Biopharma Sprl filed Critical Ucb Biopharma Sprl
Publication of ME02203B publication Critical patent/ME02203B/me

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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Claims (38)

1. Jedinjenje formule (I) ili njegov N-oksid, ili njegova farmaceutski prihvatljiva so ili solvat:gdeU predstavlja -CF3, -CHF2 ili -CH2F;Q predstavlja kiseonik, sumpor, N-R4 ili kovalentnu vezu;Z predstavlja opciono supstituisanu bicikličnu heteroaril grupu koja se sastoji od dva kuplovana šesto-člana aromatična prstena, heteroaril grupa Z sadrži najmanje jedan atom azota koji je za ostatak molekula vezan preko atoma ugljenika;M predstavlja aril ili heteroaril grupu, od kojih svaka može biti opciono supstituisana sa jednim ili više supstituenata;W predstavlja C-R5 ili N;R1, R2 i R3 nezavisno predstavljaju vodonik, halogen, cijano, nitro, C1-6 alkil, trifluorometil, C3-7 cikloalkil(C1-6)alkil, C3-7heterocikloalkil(C1-6)alkil, aril(C1-6)-alkil, heteroaril(C1-6)alkil, hidroksi, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio, C1-6 alkilsulfinil, C1-6 alkilsulfonil, amino, C1-6 alkilamino, di(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksikarbonilamino, C1-6 alkilsulfonilamino, formil, C2-6 alkilkarbonil, karboksi, C2-6 alkoksikarbonil, aminokarbonil, C1-6 alkilaminokarbonil, di(C1-6) alkilaminokarbonil, aminosulfonil, C1- 6 alkilaminosulfonil ili di(C1-6) alkilaminosulfonil;R4 predstavlja vodonik ili C1-6 alkil; iR5 predstavlja vodonik, halogen, C1-6 alkil ili C1-6 alkoksi.
2. N-oksid derivat jedinjenja formule (I) kako je definisano u patentnom zahtevu 1, ili njegova farmaceutski prihvatljiva so ili solvat.
3. Jedinjenje prema patentnom zahtevu 1 ili zahtevu 2, naznačeno time što U predstavlja -CF3.
4. Jedinjenje prema zahtevu 3, naznačeno time što atom ugljenika za koji su -KZ i -CF3 grupe direktno vezane, ima (R) konfiguraciju.
5. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što Q predstavlja N-R4.
6. Jedinjenje prema patentnom zahtevu 5 naznačeno time što R4 predstavlja vodonik ili metil.
7. Jedinjenje prema bilo kom od prethodnih zahteva naznačeno time što Z predstavlja hinolinil, izohinolinil, cinolinil, hinazolinil, hinoksalinil, ftalazinil, naftiridinil, pirido-pirimidinil ili pteridinil grupe koje su sve vezane za ostatak molekula preko atoma ugljenika, i od kojih svaka grupa može biti opciono supstituisana sa jednim ili više supstituenata nezavisno izabranih između: halogen, cijano, nitro, C1-6 alkil, trifluorometil, hidroksi, okso, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio , C1-6 alkilsulfinil, C1-6 alkilsulfonil, amino, C1-6 alkilamino, di(C1-6) alkilamino, arilamino, C1-6 alkoksiaril(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksi karbonilamino, C1-6 alkilsulfonilamino, formil, C2-6 alkilkarbonil, C3-6 cikloalkilkarbonil, C3-6 heterocikloalkilkarbonil, (C1-6)alkil-(C3-6) heterocikloalkilkarbonil, karboksi, C2-6 alkoksikarbonil, aminokarbonil, C1-6 alkilaminokarbonil, di(C1-6) alkilaminokarbonil, aminosulfonil, C1-6 alkilaminosulfonil i di(C1-6)alkilaminosulfonil.
8. Jedinjenje prema patentnom zahtevu 7, naznačeno time što Z predstavlja pirido[3,2-d]-pirimidin-4-il.
9. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što M predstavlja fenil, pirolil, furil, tienil, imidazolil, oksazolil, izoksazolil, tiazolil, izotiazolil, pirazolil, triazolil, oksadiazolil, tiadiazolil, piridinil, pirimidinil, piridazinil, pirazinil, tetrazolil ili triazinil, od kojih svaka grupa može biti opciono supstituisana sa jednim ili više supstituenata izabranih od: halogena, cijano, nitro, C1-6 alkil, trifluorometil, hidroksi, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio, C1-6 alkilsulfinil, C1-6 alkilsulfonil, amino, C1-6 alkilamino, di(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksikarbonilamino, C1-6 alkilsulfonilamino, formil, C2 -6 alkilkarbonil, karboksi, C2-6 alkoksikarbonil, aminokarbonil, C1-6 alkilaminokarbonil, di(C1-6)alkilaminokarbonil, aminosulfonil, C1-6 alkilaminosulfonil, di(C1-6)alkilamino sulfonil, C3-7cikloalkil, C3-6 heterocikloalkil, (C1-6)alkil(C3-6) heterocikloalkil, monociklični aril i monociklični heteroaril.
10. Jedinjenje prema patentnom zahtevu 9, naznačeno time što M predstavlja fenil, piridinil ili pirazinil, od kojih svaka grupa može biti opciono supstituisana sa jednim ili više supstituenata koji su nezavisno izabrani od: halogena, C1-6 alkil i C1-6 alkoksi.
11. Jedinjenje prema patentnom zahtevu 10 naznačeno time što M predstavlja piridinil.
12. Jedinjenje prema patentnom zahtevu 10 naznačeno time što M predstavlja metilpiridinil.
13. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time što W predstavlja C-R5.
14. Jedinjenje prema patentnom zahtevu 13, naznačeno time što R5 predstavlja vodonik.
15. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što R3 predstavlja vodonik.
16. Jedinjenje prema patentnom zahtevu 1 predstavljeno formulom (IIA); ili njegova farmaceutski prihvatljiva so ili solvat: gde su R1 i R2 kao što je definisano u zahtevu 1; X predstavlja N ili CH; R16 i R17 nezavisno predstavljaju vodonik, halogen, cijano, C1-6 alkil, trifluorometil, amino, C1-6 alkilamino ili di(C1-6)alkilamino; i R18 i R19 nezavisno predstavljaju vodonik, halogen, cijano, C1-6 alkil, trifluorometil ili aminokarbonil.
17. Jedinjenje prema patentnom zahtevu 16 naznačeno time što R19 predstavlja vodonik.
18. Jedinjenje prema patentnom zahtevu 17 predstavljeno formulom (IIb), ili njegova farmaceutski prihvatljiva so ili solvat gde su R1 i R2 kao što je definisano u patentnom zahtevu 1; i X, R16, R17 i R18 su kao što je definisano u patentnom zahtevu 16.
19. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 18 naznačeno time što X predstavlja N.
20. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 19 naznačeno time što R16 predstavlja vodonik.
21. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 20 naznačeno time što R17 predstavlja vodonik.
22. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 21 naznačeno time što R18 predstavlja vodonik ili C1-6 alkil.
23. Jedinjenje prema patentnom zahtevu 22, naznačeno time što R18 predstavlja vodonik.
24. Jedinjenje prema patentnom zahtevu 22, naznačeno time što R18 predstavlja metil.
25. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time što R1 predstavlja vodonik, halogen, C1-6 alkil, trifluorometil ili C1-6 alkilsulfonil.
26. Jedinjenje prema patentnom zahtevu 25, naznačeno time što R1 predstavlja hloro.
27. Jedinjenje prema patentnom zahtevu 25, naznačeno time što R1 predstavlja trifluorometil.
28. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što R2 predstavlja vodonik, halogen ili C1-6 alkil.
29. Jedinjenje prema patentnom zahtevu 28, naznačeno time što R2 predstavlja vodonik.
30. Jedinjenje prema patentnom zahtevu 1 izabrano od sledećeg: N-{(R)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-[(R)-1-(8-hloro-2-fenilhinolin-3-il) -2,2,2-trifluoroetil] pirido [3,2-d] pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(4-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(4-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(2-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(2-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(5-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(5-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(pyrazin-2-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(6-metoksipirazin-2-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(6-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[8-hloro-2-(6-metil-1-oksipiridin-3-il)hinolin-3-y]]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[8-metil-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-amin; N-{(R)-1-[8-metil-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(2-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(2-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(5-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(5-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[2-(piridin-3-il)-8-(trifluorometil)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[2-(1-oksipiridin-3-il)-8-(trifluorometil)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[2-(6-metilpiridin-3-il)-5,6,8-trifluorohinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[2-(6-metil-1-oksipiridin-3-il)-5,6,8-trifluorohinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-N-metil-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-N-(1-oksipirido-[3,2-d]pirimidin-4-il) amin; N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-N-(1-oksi-pirido[3,2-d]pirimidin-4-il)amin; N-{(S)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(S)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(R)-1-[2-(piridin-3-il) hinolin-3-il]-2,2,2-trifluoroetil} pirido [3,2-d] pirimidin-4-amin; N-{(R)-1-[2-(1-oksipiridin-3-il) hinolin-3-il] -2,2,2-trifluoroetil} pirido [3,2-d] -pirimidin-4-amin ; N-{(R)-1-[8-hloro-2-(6-hloropiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[2-(2-metil-1-oksipiridin-3-il)-8-(trifluorometil)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[8-(Metansulfonil)-2-(2-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin -4-amin; N-{(R)-1-[8-(metansulfonil)-2-(2-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; i N-{(R)-1-[8-(metansulfonil)-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin.
31. Jedinjenje formule (I) kako je definisano u zahtevu 1 ili njegov N-oksid, ili njegova farmaceutski prihvatljiva so ili solvat, za upotrebu u terapiji.
32. Jedinjenje formule (I) kako je definisano u zahtevu 1 ili njegov N-oksid, ili njegova farmaceutski prihvatljiva so ili solvat, za upotrebu u lečenju i/ili prevenciji poremećaja za koje je indikovna administracija selektivnog PI3K inhibitora.
33. Farmaceutska kompozicija koja sadrži jedinjenje formule (I) kako je definisano u zahtevu 1 ili njegov N-oksid, ili njegovu farmaceutski prihvatljivu so ili solvat, zajedno sa farmaceutski prihvatljivim nosačem.
34. Upotreba jedinjenja formule (I) kako je definisano u zahtevu 1 ili njegovog N-oksida, ili njegove farmaceutski prihvatljive soli ili solvata, za proizvodnju medikamenta za lečenje i/ili prevenciju poremećaja za koje je indikovana administracija selektivnog PI3K inhibitora.
35. N-{(R)-1-[8-Hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-il amin prema patentnom zahtevu 1.
36. N-{(R)-1-[8-Hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin prema zahtevu 1, za upotrebu u lečenju i/ili prevenciji zapaljenskih, autoimunih, kardiovaskularnih, neurodegenerativnih, metaboličkih, onkoloških, noiceptivnih ili oftalmičkih stanja.
37. Farmaceutska kompozicija prema patentnom zahtevu 33, koja sadrži N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin zajedno sa farmaceutski prihvatljivim nosačem.
38. Upotreba N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-ilamina za proizvodnju medikamenta za lečenje i/ili prevenciju inflamatornih, autoimunih, kardiovaskularnih, neurodegenerativnih, metaboličkih, onkoloških, noiceptivnih ili oftalmičkih stanja. 2
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