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HRP20231048T1 - Derivati bipirazola kao jak inhibitori - Google Patents

Derivati bipirazola kao jak inhibitori Download PDF

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HRP20231048T1
HRP20231048T1 HRP20231048TT HRP20231048T HRP20231048T1 HR P20231048 T1 HRP20231048 T1 HR P20231048T1 HR P20231048T T HRP20231048T T HR P20231048TT HR P20231048 T HRP20231048 T HR P20231048T HR P20231048 T1 HRP20231048 T1 HR P20231048T1
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Yun-Long Li
Jincong Zhuo
Ding-Quan Qian
Song MEI
Ganfeng Cao
Yongchun Pan
Qun Li
Zhongjiang JIA
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Incyte Holdings Corporation
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Claims (23)

1. Spoj Formule I, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u postupku za liječenje astme, sistemskog eritemskog lupusa, akneformnog osipa, ili ulceroznog kolitisa: [image] gdje: Cy1 je fenil, piridil, pirimidinil, pirazinil, ili piridazinil, od kojih je svaki opcionalno supstituiran s 1, 2, 3, ili 4 skupine koje se neovisno biraju od R3, R4, R5, i R6; Y je N ili CH; R1 je C1-6 alkil, C1-6 haloalkil, C3-7 cikloalkil, C3-7 cikloalkil-C1-3 alkil-, 4-7-člani heterocikloalkil, 4-7-člani heterocikloalkil-C1-3 alkil, fenil, fenil-C1-3 alkil, 5-6-člani heteroaril, ili 5-6-člani heteroaril-C1-3 alkil, od kojih je svaki opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od fluoro, kloro, C1-3 alkil, -OH, -O(C1-3 alkil), -CN, -CF3, -CHF2, -CH2F, -NH2, -NH(C1-3 alkil), -N(C1-3alkil)2, -C(=O)N(C1-3 alkil)2, -C(=O)NH(C1-3 alkil), -C(=O)NH2, -C(=O)O(C1-3 alkil), -S(=O)2(C1-3 alkil), -S(=O)2(C3-6 cikloalkil), -C(=O)(C3-6 cikloalkil), i -C(=O)(C1-3 alkil); R2 je H ili C1-3 alkil; pri čemu je navedeni C1-3 alkil opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od fluoro, kloro, -OH, -O(C1-3 alkil), -CN, -CF3, -CHF2, -CH2F, -NH2, -NH(C1-3 alkil), i -N(C1-3 alkil)2; ili R1 i R2 zajedno s atomom dušika s kojim su vezani, tvore 4-člani, 5-člani, ili 6-člani heterocikloalkil prsten koji je opcionalno suspstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od F, Cl, -OH, -O(C1-3 alkil), -CN, C1-3 alkil, C1-3 haloalkil, -NH2, -NH(C1-3 alkil), -N(C1-3 alkil)2, -CH2CN, i -CH2OH; R3 je H, F, Cl, -CN, C1-3 alkil, C1-3 fluoroalkil, -O(C1-3 alkil), ili -O(C1-3 fluoroalkil); R4 je H, F, Cl, -CN, C1-3 alkil, C1-3 fluoroalkil, -O(C1-3 alkil), ili -OC(C1-3 fluoroalkil); R5 je H, F, Cl, -CN, C1-3 alkil, C1-3 fluoroalkil, -O(C1-3 alkil), ili -OC(C1-3 fluoroalkil); R6 je H, F, Cl, -CN, C1-3 alkil, C1-3 fluoroalkil, -O(C1-3 alkil), ili -OC(C1-3 fluoroalkil); R7 je H, F, Cl, C1-3 alkil, C1-3 haloalkil, -NR17R17a, -NHC(=O)R17b, -C(=O)NR17aR17b, -NHS(=O)2R17b, ili -S(=O)2NR17aR17b, pri čemu je navedeni C1-3 alkil opcionalno supstituiran s 1, 2 ili 3 supstituenta odabrana od F, Cl, -CN, -CF3, -CHF2, -CH2F, -NH2, -NH(CH3), -N(CH3)2, OH, -OCH3, -OCF3, -OCHF2, i -OCH2F; R8 je H, F, Cl, C1-3 alkil, ili C1-3 haloalkil; R9 je H, F, Cl, C1-3 alkil, C1-3 haloalkil, ciklopropil, -CN, -NH2, -NH(C1-3 alkil), ili -N(C1-3 alkil)2, pri čemu je navedeni C1-3 alkil opcionalno supstituiran s 1, 2 ili 3 supstituenta odabrana od F, kloro, -CN, -CF3, -CHF2, -CH2F, -NH2, i OH; R10 je H, F, Cl, C1-3 alkil, C1-3 haloalkil, ciklopropil, -CN, -NH2, -NH(C1-3 alkil), ili -N(C1-3 alkil)2, pri čemu je navedeni C1-3 alkil opcionalno supstituiran s 1, 2 ili 3 supstituenta odabrana od F, kloro, -CN, -CF3, -CHF2, -CH2F, -NH2, i OH; R17 je C1-6alkil, fenil ili 5-6-člani heteroaril, od kojih je svaki opcionalno supstituiran s 1, 2, 3 ili 4 neovisno odabrana R27 supstituenta; R17a je H ili C1-3 alkil; R17b je C1-3 alkil opcionalno supstituiran s 1, 2 ili 3 supstituenta odabrana od F, kloro, -CN, -CF3, -CHF2, -CH2F, -NH2, -NH(CH3), -N(CH3)2, OH, -OCH3, -OCF3, -OCHF2, i -OCH2F; i svaki R27 je neovisno odabran od sljedećih: halogen, -OH, -NO2, -CN, C1-3 alkil, C2-3 alkenil, C2-3 alkinil, C1-3 haloalkil, cijano-C1-3 alkil, HO-C1-3 alkil, CF3-C1-3 hidroksialkil, C1-3 alkoksi-C1-3 alkil, C3-7 cikloalkil, C1-3 alkoksi, C1-3 haloalkoksi, H2N-, (C1-3 alkil)NH-, (C1-3 alkil)2N-, HS-, C1-3 alkil-S-, C1-3 alkil-S(=O)-, C1-3 alkil-S(=O)2-, karbamil, C1-3 alkilkarbamil, di(C1-3 alkil)karbamil, karboksi, C1-3 alkil-C(=O)-, C1-4 alkoksi-C(=O)-, C1-3 alkil-C(=O)O-, C1-3 alkil-C(=O)NH-, C1-3 alkil-S(=O)2NH-, H2N-SO2-, C1-3 alkil-NH-S(=O)2-, (C1-3 alkil)2-N-S(=O)2-, H2N-S(=O)2NH-, C1-3 alkil-NHS(=O)2NH-, (C1-3 alkil)2N-S(=O)2NH-, H2N-C(=O)NH-, C1-3 alkil-NHC(=O)NH-, i (C1-3 alkil)2-N-C(=O)NH-.
2. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj Formule I je spoj Formule Ia: [image] ili njegova farmaceutski prihvatljiva sol, gdje X je N ili CR4; i W je N ili CR6.
3. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj Formule I je spoj Formule Ia: [image] ili njegova farmaceutski prihvatljiva sol, gdje: X je N ili CR4; W je N ili CR6; Y je N ili CH; R1 je C1-6 alkil, C1-6 haloalkil, C3-6 cikloalkil, C3-6 cikloalkil-C1-3 alkil-, 4-6-člani heterocikloalkil, ili 4-6-člani heterocikloalkil-C1-3 alkil, od kojih je svaki opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od fluoro, kloro, C1-3 alkil, -OH, -O(C1-3 alkil), -CN, -CF3, -CHF2, -CH2F, -NH2, -NH(C1-3 alkil), -N(C1-3 alkil)2, -C(=O)N(C1-3 alkil)2, -C(=O)NH(C1-3 alkil), -C(=O)NH2, -C(=O)O(C1-3 alkil), -S(=O)2(C1-3 alkil), -S(=O)2(C3-6 cikloalkil), -C(=O)(C3-6cikloalkil), i -C(=O)(C1-3 alkil); R2 je H ili C1-3 alkil; pri čemu je navedeni C1-3 alkil opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od fluoro, kloro, -OH, -O(C1-3 alkil), -CN, -CF3, -CHF2, -CH2F, -NH2, -NH(C1-3 alkil), i -N(C1-3 alkil)2; ili R1 i R2 zajedno s atomom dušika s kojim su vezani, tvore 4-člani, 5-člani, ili 6-člani heterocikloalkil prsten koji je opcionalno suspstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od fluoro, -OH, -O(C1-3 alkil), -CN, C1-3 alkil, C1-3 haloalkil, -NH2, -NH(C1-3 alkil), -N(C1-3 alkil)2, i -CH2CN; R3 je H, F, Cl, -CN, C1-3 alkil, -OCF3, -CF3, ili -O(C1-3 alkil); R4 je H, F, Cl, -CN, C1-3 alkil, ili -O(C1-3 alkil); R5 je H, F, Cl, -CN, C1-3 alkil, ili -O(C1-3 alkil); R6 je H, F, Cl, -CN, ili C1-3 alkil; R7 je H, F, Cl, C1-3 alkil, C1-3 haloalkil, -NR17R17a, -NHC(=O)R17b, -C(=O)NR17aR17b, -NHS(=O)2R17b, ili -S(=O)2NR17aR17b, pri čemu je navedeni C1-3 alkil opcionalno supstituiran s 1, 2 ili 3 supstituenta odabrana od F, Cl, -CN, -CF3, -CHF2, -CH2F, -NH2, i OH; R8 je H, F, Cl, C1-3 alkil, ili C1-3 haloalkil; R9 je H, F, Cl, C1-3 alkil, C1-3 haloalkil, ciklopropil, -CN, -NH2, -NH(C1-3 alkil), ili -N(C1-3 alkil)2, pri čemu je navedeni C1-3 alkil opcionalno supstituiran s 1, 2 ili 3 supstituenta odabrana od F, kloro, -CN, -CF3, -CHF2, -CH2F, -NH2, i OH; R10 je H, F, Cl, C1-3 alkil, C1-3 haloalkil, ciklopropil, -CN, -NH2, -NH(C1-3 alkil), ili -N(C1-3 alkil)2, pri čemu je navedeni C1-3 alkil opcionalno supstituiran s 1, 2 ili 3 supstituenta odabrana od F, kloro, -CN, -CF3, -CHF2, -CH2F, -NH2, i OH; R17 je C1-6 alkil, fenil ili 5-6-člani heteroaril, od kojih je svaki opcionalno supstituiran s 1, 2, 3 ili 4 supstituenta neovisno odabrana od R27; R17a je H ili C1-3 alkil; R17b je C1-3 alkil opcionalno supstituiran s 1, 2 ili 3 supstituenta odabrana od F, kloro, -CN, -CF3, -CHF2, -CH2F, -NH2, i OH; i svaki R27 je neovisno odabran od sljedećih: halogen, -OH, -NO2, -CN, C1-3 alkil, C2-3 alkenil, C2-3 alkinil, C1-3 haloalkil, cijano-C1-3 alkil, HO-C1-3 alkil, CF3-C1-3 hidroksialkil, C1-3 alkoksi-C1-3 alkil, C3-7 cikloalkil, C1-3 alkoksi, C1-3 haloalkoksi, H2N-, (C1-3 alkil)NH-, (C1-3 alkil)2N-, HS-, C1-3 alkil-S-, C1-3 alkil-S(=O)-, C1-3 alkil-S(=O)2-, karbamil, C1-3 alkilkarbamil, di(C1-3 alkil)karbamil, karboksi, C1-3 alkil-C(=O)-, C1-4 alkoksi-C(=O)-, C1-3 alkil-C(=O)O-, C1-3 alkil-C(=O)NH-, C1-3 alkil-S(=O)2NH-, H2N-SO2-, C1-3 alkil-NH-S(=O)2-, (C1-3 alkil)2-N-S(=O)2-, H2N-S(=O)2NH-, C1-3 alkil-NHS(=O)2NH-, (C1-3 alkil)2N-S(=O)2NH-, H2N-C(=O)NH-, C1-3 alkil-NHC(=O)NH-, i (C1-3 alkil)2N-C(=O)NH-.
4. Spoj ili sol za uporabu prema patentnom zahtjevu 3, naznačen time, da: R1 je C1-6 alkil, C1-6 haloalkil, C3-6 cikloalkil, ili C3-6 cikloalkil-C1-3 alkil, gdje je svaki navedeni C1-6 alkil, C3-6 cikloalkil, i C3-6 cikloalkil-C1-3 alkil, opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od fluoro, -CF3, i metila; R2 je H ili metil; R3 je H, F ili Cl; R4 je H ili F; R5 je H ili F; R6 je H ili F; R7 je H, metil, etil ili HO-CH2-; R8 je H ili metil; R9 je H, metil ili etil; i R10 je H, metil, etil ili HO-CH2-.
5. Spoj ili sol za uporabu prema bilo kojem od patentnih zahtjeva 2 do 4, naznačen time, da: a) Y je N; ili b) Y je CH.
6. Spoj ili sol za uporabu prema bilo kojem od patentnih zahtjeva 2 do 5, naznačen time, da: a) X je N; ili b) X je CR4; ili c) X je CR4 i R4 je H ili F.
7. Spoj ili sol za uporabu prema bilo kojem od patentnih zahtjeva 2 do 6, naznačen time, da: a) W je N; ili b) W je CR6; ili c) W je CR6 i R6 je H, F ili Cl; ili d) W je CR6 i R6 je H ili F; ili e) W je CR6 i R6 je H.
8. Spoj ili sol za uporabu prema bilo kojem od patentnih zahtjeva 2 do 7, naznačen time, da R3 je H ili F.
9. Spoj ili sol za uporabu prema bilo kojem od patentnih zahtjeva 2 do 8, naznačen time, da R5 je H ili F.
10. Spoj ili sol za uporabu prema bilo kojem od patentnih zahtjeva 1 do 9, naznačen time, da: a) R2 je H ili metil; ili b) R2 je H.
11. Spoj ili sol za uporabu prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time, da: a) R1 je C1-6 alkil, C1-6 haloalkil, C3-6 cikloalkil, ili C3-6 cikloalkil-C1-3 alkil, gdje je svaki navedeni C1-6 alkil, C3-6 cikloalkil, i C3-6 cikloalkil-C1-3 alkil, opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od fluoro, -CF3, i metila; ili b) R1 je izopropil, etil, 1-metilpropil, 2,2,2-trifluoro-1-metiletil, 1-ciklopropiletil, ciklopropil, 1-trifluorometilciklopropil, 1-ciklopropil-2,2,2-trifluoroetil, 2,2,2-trifluoroetil, ili 2,2-difluoroetil; ili c) R1 je izopropil, etil, 1-metilpropil, ili 2,2,2-trifluoro-1-metiletil.
12. Spoj ili sol za uporabu prema bilo kojem od patentnih zahtjeva 1 do 11, naznačen time, da R7 je H, metil, etil, ili HO-CH2-.
13. Spoj ili sol za uporabu prema bilo kojem od patentnih zahtjeva 1 do 4 i 6 do 12, naznačen time, da spoj Formule I je: a) spoj Formule II: [image] ili njegova farmaceutski prihvatljiva sol; ili b) spoj Formule III: [image] ili njegova farmaceutski prihvatljiva sol; ili c) spoj Formule IV: [image] ili njegova farmaceutski prihvatljiva sol; ili d) spoj Formule IIa: [image] ili njegova farmaceutski prihvatljiva sol; ili e) spoj Formule IIIa: [image] ili njegova farmaceutski prihvatljiva sol; ili f) spoj Formule IVa: [image] ili njegova farmaceutski prihvatljiva sol.
14. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da se spoj bira od sljedećih: 5-[3-(cijanometil)-3-(3'-metil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-N-[(1S)-2,2,2-trifluoro-1-metiletil]pirazin-2-karboksamid; 5-[3-(cijanometil)-3-(3'-metil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-N-izopropilpirazin-2-karboksamid; 4-[3-(cijanometil)-3-(3'-metil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-N-izopropilbenzamid; 4-[3-(cijanometil)-3-(3'-metil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamid; 4-[3-(1H,1'H-4,4'-bipirazol-1-il)-3-(cijanometil)azetidin-1-il]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamid; 5-[3-(cijanometil)-3-(3,3'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-N-izopropilpirazin-2-karboksamid; 4-[3-(cijanometil)-3-(3,5'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamid; 5-[3-(cijanometil)-3-(3',5'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-N-izopropilpirazin-2-karboksamid; 5-[3-(cijanometil)-3-(3',5'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-N-[(1S)-2,2,2-trifluoro-1-metiletil]pirazin-2-karboksamid; 5-[3-(cijanometil)-3-(3-metil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-N-izopropilpirazin-2-karboksamid; 5-[3-(cijanometil)-3-(3'-etil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-N-[(1S)-2,2,2-trifluoro-1-metiletil]pirazin-2-karboksamid; 4-{3-(cijanometil)-3-[3'-(hidroksimetil)-1H,1'H-4,4'-bipirazol-1-il]azetidin-1-il}-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamid; 4-{3-(cijanometil)-3-[3-(hidroksimetil)-3'-metil-1H,1'H-4,4'-bipirazol-1-il]azetidin-1-il}-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamid; ili njihova farmaceutski prihvatljiva sol.
15. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj je 4-[3-(cijanometil)-3-(3',5'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamid, ili njegova farmaceutski prihvatljiva sol.
16. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj ili sol je za uporabu u postupku za liječenje astme.
17. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj ili sol je za uporabu u postupku liječenja astme, i pri čemu spoj je 4-[3-(cijanometil)-3-(3',5'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamid, ili njegova farmaceutski prihvatljiva sol.
18. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj ili sol je za uporabu u postupku za liječenje sistemskog eritemskog lupusa.
19. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj ili sol je za uporabu u postupku za liječenje sistemskog eritemskog lupusa, i pri čemu spoj je 4-[3-(cijanometil)-3-(3',5'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamid, ili njegova farmaceutski prihvatljiva sol.
20. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj ili sol je za uporabu u postupku za liječenje akneformnog osipa.
21. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj ili sol je za uporabu u postupku za liječenje akneformnog osipa, i pri čemu spoj je 4-[3-(cijanometil)-3-(3',5'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamid, ili njegova farmaceutski prihvatljiva sol.
22. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj ili sol je za uporabu u postupku za liječenje ulceroznog kolitisa.
23. Spoj ili sol za uporabu prema patentnom zahtjevu 1, naznačen time, da spoj ili sol je za uporabu u postupku za liječenje ulceroznog kolitisa, i pri čemu spoj je 4-[3-(cijanometil)-3-(3',5'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamid, ili njegova farmaceutski prihvatljiva sol.
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