HRP20220362T1 - Biciklički kondenzirani heteroarilni ili arilni spojevi i njihova upotreba kao inhibitori irak4 - Google Patents

Biciklički kondenzirani heteroarilni ili arilni spojevi i njihova upotreba kao inhibitori irak4 Download PDF

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Publication number
HRP20220362T1
HRP20220362T1 HRP20220362TT HRP20220362T HRP20220362T1 HR P20220362 T1 HRP20220362 T1 HR P20220362T1 HR P20220362T T HRP20220362T T HR P20220362TT HR P20220362 T HRP20220362 T HR P20220362T HR P20220362 T1 HRP20220362 T1 HR P20220362T1
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HR
Croatia
Prior art keywords
methoxy
carboxamide
oxopyrrolidin
fluoro
compound
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HRP20220362TT
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English (en)
Inventor
David Randolph ANDERSON
Mark Edward Bunnage
Kevin Joseph Curran
Christoph Martin Dehnhardt
Lori Krim Gavrin
Joel Adam Goldberg
Seungil Han
David Hepworth
Horng-Chih Huang
Arthur Lee
Katherine Lin Lee
Frank Eldridge Lovering
Michael Dennis Lowe
John Paul Mathias
Nikolaos PAPAIOANNOU
Akshay PATNY
Betsy Susan PIERCE
Eddine Saiah
Joseph Walter Strohbach
John David TRZUPEK
Richard Vargas
Xiaolun Wang
Stephen Wayne Wright
Christoph Wolfgang ZAPF
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Pfizer Inc.
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Publication of HRP20220362T1 publication Critical patent/HRP20220362T1/hr

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    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
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Claims (27)

1. Spoj Formule III [image] , naznačen time što svaki od X i X′ je neovisno CR8 ili N; Y je neovisno N ili CR8′; uz uvjet da najmanje jedan od X, X′ ili Y nije N; R1 je C6-C6alkil ili C3-C6cikloalkil, gdje navedeni alkil ili cikloalkil može biti supstituiran s deuterijem, halogenom, OH, cijano, C1-C3alkilom, C3-C6cikloalkilom, C1-C6alkoksi ili C1-C6alkiltiolilom; svaki od R3a i R3b je neovisno vodik ili C1-C3alkil; R4 je za svaku pojavu (jedan, dva, tri, četiri ili pet) neovisno i izborno halogen, C1-C6alkil, C2-C6alkenil, -OR5, –(CR3aR3b)n-(3- do 6-eročlani cikloalkil), –(CR3aR3b)n-(4- do 6-eročlani heterocikloalkil), gdje je svaki od navedenog alkila, cikloalkila ili heterocikloalkila izborno i neovisno supstituiran s jednim do pet deuterija, halogena, OH, CN, -C(O)(CH2)tCN ili -C1-C6alkoksi; -NR11aR11b; dva R4 uzeta zajedno s odgovarajućim ugljicima na koje je svaki od njih vezan tvore ciklopropil, ciklobutil ili ciklopentil, gdje navedeni ciklopropil, ciklobutil ili ciklopentil može biti supstituiran s jednim do tri F, Cl, OH, metila, etila, propila, C1-C3fluoralkila, C1-C3difluoralkila, C1-C3trifluoralkila, C1-C3hidroksialkila, metoksi ili etoksi; R5 je vodik ili C1-C6alkil, gdje navedeni alkil može biti supstituiran s fluorom; R8 je neovisno vodik, halogen, cijano, -NR11aR11b, C1-C6alkil, 5- do 6-eročlani heteroaril ili aril, gdje navedeni alkil ili heteroaril ili aril može biti supstituiran s jednim, dva ili tri halogena, -NR11aR11b, C1-C3alkila ili okso; R8′ je vodik, deuterij, halogen ili cijano; svaki od R11a i R11b je neovisno vodik ili C1-C6alkil, gdje navedeni alkil može biti supstituiran s OH; n je neovisno 0 ili 1; i t je 1, 2 ili 3; ili farmaceutski prihvatljiva sol navedenog spoja, ili tautomer navedenog spoja ili navedene soli.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što Y je N; X i X′ su CR8; ili farmaceutski prihvatljiva sol navedenog spoja, ili tautomer navedenog spoja ili navedene soli.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što svaki od X i X′ je CR8, a Y je CR8′; ili farmaceutski prihvatljiva sol navedenog spoja, ili tautomer navedenog spoja ili navedene soli.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što su X i Y N, a X′ je CR8; ili njegova farmaceutski prihvatljiva sol, ili tautomer navedenog spoja ili navedene soli.
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je X N, X′ je CR8, a Y je CR8′; ili njegova farmaceutski prihvatljiva sol, ili tautomer navedenog spoja ili navedene soli.
6. Spoj u skladu s patentnih zahtjeva 1, 2, 3, 4 ili 5, naznačen time što je R1 C1-C3alkil, gdje navedeni alkil može biti supstituiran s jednim do tri deuterija, F, Cl ili C1-C3alkoksi; a svaki od R3a i R3b je neovisno vodik ili metil; ili farmaceutski prihvatljiva sol navedenog spoja, ili tautomer navedenog spoja ili soli.
7. Spoj u skladu s patentnim zahtjevom 6, naznačen time što je R4 za svaku pojavu neovisno i izborno F; Cl; OH; ili C1-C3alkil, izborno supstituiran s jednim do pet deuterija, Cl, F, OH, C1-C3alkila ili C1-C3alkoksi; ili dva R4 uzeta zajedno s ugljicima na koje su vezani tvore ciklopropil, ciklobutil ili ciklopentil, gdje navedeni ciklopropil, ciklobutil ili ciklopentil može biti supstituiran s jednim do tri Cl, F, OH, metila, etila, propila, C1-C3fluoralkila, C1-C3difluoralkila, C1-C3trifluoralkila, C1-C3hidroksialkila, metoksi ili etoksi; ili farmaceutski prihvatljiva sol navedenog spoja, ili tautomer navedenog spoja ili soli.
8. Spoj u skladu s patentnim zahtjevom 7, naznačen time što je R1 metil, etil, propil ili izopropil, gdje svaki od navedenih ostataka R1 može biti supstituiran deuterijem, fluorom ili s metoksi; ili farmaceutski prihvatljiva sol navedenog spoja, ili tautomer navedenog spoja ili navedene soli.
9. Spoj u skladu s patentnim zahtjevom 8, naznačen time što se svakog R4 neovisno i izborno bira između fluora, OH, metila, etila, propila, gdje navedeni metil, etil ili propil mogu biti supstituirani s jednim, dva ili tri fluora, OH ili metoksi; ili dva R4 uzeta zajedno s ugljicima na koje su vezani tvore ciklopropil, ciklobutil ili ciklopentil, gdje navedeni ciklopropil, ciklobutil ili ciklopentil mogu biti supstituirani s jednim do tri Cl, F, OH, metila, fluormetila, difluormetila, trifluormetila, etila, metoksimetila, propila, C1-C3fluoralkila, C1-C3difluoralkila, C1-C3trifluoralkila, C1-C3hidroksialkila, metoksi ili etoksi; i R8 je neovisno vodik, halogen ili C1-C6alkil, gdje navedeni alkil može biti supstituiran s fluorom; ili farmaceutski prihvatljiva sol navedenog spoja, ili tautomer navedenog spoja ili navedene soli.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira između: 5-{[(2S)-5-oksopirolidin-2-il]metoksi}-3-(propan-2-iloksi)naftalen-2-karboksamida; 1-{[(2S)-4,4-difluor-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 1-{[(2S,4S)-4-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 1-{[(2S,4S)-4-etil-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 1-{[(2S,4S)-4-fluor-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 1-{[(2S)-4,4-difluor-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,4S)-5-okso-4-(2,2,2-trifluoretil)pirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 1-{[(2S,3S,4R)-4-fluor-3-metil-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 3-metoksi-5-{[(2S)-5-oksopirolidin-2-il]metoksi}naftalen-2-karboksamida; 1-{[(2S,4S)-4-fluor-4-metil-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S)-4,4-difluor-3-metil-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 1-{[(2S,3S,4S)-4-fluor-3-metil-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 1-{[(2S,3S,4R)-4-fluor-3-metil-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S,4S)-4-fluor-3-metil-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 5-{[(2S,4S)-4-fluor-4-metil-5-oksopirolidin-2-il]metoksi}-3-metoksinaftalen-2-karboksamida; 1-{[(2R,3R,4S)-3-etil-4-fluor-3-hidroksi-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S)-3-etil-4,4-difluor-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 5-{[(2S,4R)-4-fluor-4-(hidroksimetil)-5-oksopirolidin-2-il]metoksi}-3-metoksinaftalen-2-karboksamida; 7-metoksi-1-{[(2S,3R)-3-metil-5-oksopirolidin-2-il]metoksi}izokinolin-6-karboksamida; 1-{[(2S,4S)-4-fluor-4-(fluormetil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 3-metoksi-5-{[(2S,3R)-3-metil-5-oksopirolidin-2-il]metoksi}naftalen-2-karboksamida; 5-{[(2S,3S,4S)-4-fluor-3-metil-5-oksopirolidin-2-il]metoksi}-3-metoksinaftalen-2-karboksamida; 8-fluor-5-{[(2S,3S,4S)-4-fluor-3-metil-5-oksopirolidin-2-il]metoksi}-3-metoksinaftalen-2-karboksamida; 5-{[(2S,4R)-4-fluor-5-okso-4-(2,2,2-trifluoretil)pirolidin-2-il]metoksil-3-metoksinaftalen-2-karboksamida; 1-{[(2S,3S)-3-etil-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3R)-3-etil-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 4-{[(2S,3S,4S)-4-fluor-3-metil-5-oksopirolidin-2-il]metoksi}-6-metoksikinolin-7-karboksamida; 1-{[(2S,3S)-3-etenil-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,4S)-4-fluor-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,4S)-4-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 4-{[(2S,4S)-4-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-6-metoksikinolin-7-karboksamida; 4-{[(2S,4S)-4-fluor-4-metil-5-oksopirolidin-2-il]metoksi}-6-(propan-2-iloksi)kinolin-7-karboksamida; 7-etoksi-1-{[(2S,3S,4S)-4-fluor-3-metil-5-oksopirolidin-2-il]metoksi}izokinolin-6-karboksamida; 7-etoksi-1-{[(2S,4S)-4-fluor-4-(fluormetil)-5-oksopirolidin-2-il]metoksi}izokinolin-6-karboksamida; 1-{[(2S,3S)-3-ciklopropil-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 7-metoksi-1-{[(2S,3R)-5-okso-3-propilpirolidin-2-il]metoksi}izokinolin-6-karboksamida; 4-{[(2S,3S,4S)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-6-metoksikinolin-7-karboksamida; 1-{[(2S,3S,4R)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S,4S)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-7-[(trideuterij)metiloksi]izokinolin-6-karboksamida; 4-{[(2S,3S,4S)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-6-metoksikinazolin-7-karboksamida; 1-{[(2S,3S,4R)-3-etil-4-metoksi-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S,4S)-3-(pentadeuterij)etil-4-fluor-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S)-3-etil-4,4-difluor-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3R,4R)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3R)-4,4-difluor-3-(metoksimetil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3R,4S)-4-fluor-3-(metoksimetil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 7-metoksi-1-{[(2S,3S,4R)-4-metoksi-3-metil-5-oksopirolidin-2-il]metoksi}izokinolin-6-karboksamida; 1-{[(2S,3R,4R)-4-fluor-3-(metoksimetil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S,4R)-3-etil-4-hidroksi-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S)-3-(2-fluoretil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S,4S)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 7-etoksi-1-{[(2S,3S,4S)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}izokinolin-6-karboksamida; 1-{[(2S,3S,4S)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-4-fluor-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S,4S)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-8-fluor-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3R)-3-etil-5-oksopirolidin-2-il]metoksi}-4-fluor-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3R)-3-etil-5-oksopirolidin-2-il]metoksi}-8-fluor-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3R)-3-(fluormetil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3R,4S)-4-fluor-3-(fluormetil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S,4S)-3-ciklopropil-4-fluor-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S,4R)-3-ciklopropil-4-fluor-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 1-{[(2S,3S,4S)-4-fluor-3-(2-fluoretil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 4-(1-metil-1H-imidazol-4-il)-1-{[(2S)-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 4-(1,2-dimetil-1H-imidazol-4-il)-1-{[(2S)-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 4-(2-metil-1H-imidazol-4-il)-1-{[(2S)-5-oksopirolidin-2-il]metoksi}-7-(propan-2-iloksi)izokinolin-6-karboksamida; 1-{[(2S,3S,4S)-3-etil-4-fluor-5-okso(3,4-bisdeuterij)pirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; 4-{[(2S,3S,4S)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-6-metoksikinolin-7-karboksamida; i 1-{[(2S,3R,4R)-4-fluor-3-(fluormetil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamida; ili farmaceutski prihvatljive soli navedenog spoja, ili tautomera navedenog spoja ili soli.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačen time što je namijenjen upotrebi u liječenju sisavca, uključujući čovjeka, koji ima bolest ili stanje kojeg se bira iz skupine koju čine autoimune bolesti; upalne bolesti; autoupalna stanja; bolna stanja; dišna, stanja dušnih puteva i plućna stanja; gastrointestinalni (GI) poremećaji; alergijske bolesti; bolesti uzrokovane infekcijom; stanja uzrokovana traumom i ozljedom tkiva; fibrotične bolesti; bolesti uzrokovane preosjetljivošću IL1-puteva; oftalmičke/očne bolesti; poremećaji zglobova, mišića i kostiju; kože/dermatološke bolesti; bubrežne bolesti; genetske bolesti; krvotvorne bolesti; bolesti jetre; oralne bolesti; metaboličke bolesti, uključujući dijabetes (primjerice tip II) i njegove komplikacije; proliferativne bolesti; kardiovaskularna stanja; vaskularna stanja; neuroupalna stanja; neurodegenerativna stanja; rak; sepsa; plućna upala i ozljeda pluća; i plućna hipertenzija.
12. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 11, naznačen time što je bolest ili stanje sistemni eritematozni lupus (SLE), lupozni nefritis, reumatoidni artritis, psorijaza, atopični dermatitis, giht, periodični sindrom povezan s kriopirinom (CAPS), difuzni limfom velikih B-stanica (DLBCL), kronična bolest bubrega ili akutna ozljeda bubrega, kronični opstruktivni plućni poremećaj (COPD), astma ili bronhospazam.
13. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 12, naznačen time što je bolest ili stanje sistemni eritematozni lupus (SLE), lupozni nefritis, reumatoidni artritis, psorijaza ili atopični dermatitis.
14. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 11, naznačen time što je bolest ili stanje gnojni hidradentis.
15. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegovu farmaceutski prihvatljivu sol, ili tautomer navedenog spoja ili navedene soli, te farmaceutski prihvatljivi vehikulum, razrjeđivač ili nosač.
16. Farmaceutska kombinacija, naznačena time što sadrži terapijski djelotvornu količinu pripravka koji sadrži: prvi spoj, gdje je prvi spoj spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegova farmaceutski prihvatljiva sol, ili tautomer navedenog spoja ili navedene soli; drugi spoj, gdje se drugi spoj bira iz skupine koju čine kortikosteroid, hidroksiklorokin, ciklofosfamid, azatioprin, mikofenolat mofetil, metotreksat, inhibitor janus kinaze, statin, kalcipotrien, inhibitor angiotenzin-konvertirajućeg enzima i blokator angiotenzinskog receptora; i izborni farmaceutski prihvatljivi nosač, pomoćno sredstvo ili razrjeđivači.
17. Farmaceutska kombinacija u skladu s patentnim zahtjevom 16, naznačena time što je drugi spoj inhibitor janus kinaze.
18. Farmaceutska kombinacija u skladu s patentnim zahtjevom 17, naznačena time što se inhibitor janus kinaze bira između ruksolitiniba, baricitiniba, tofacitiniba, decernotiniba, cerdulatiniba, JTE-052, peficitiniba, GLPG-0634, INCB-47986, INCB-039110, PF-04965842, XL-019, ABT-494, R-348, GSK-2586184, AC-410, BMS-911543 i PF-06263276.
19. Farmaceutska kombinacija u skladu s patentnim zahtjevom 18, naznačena time što je inhibitor janus kinaze tofacitinib.
20. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 1-{[(2S,3S,4S)-4-fluor-3-(2-fluoretil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamid, ili njegova farmaceutski prihvatljiva sol, ili tautomer navedenog spoja ili soli.
21. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 1-{[(2S,3R)-3-etil-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamid, ili njegova farmaceutski prihvatljiva sol, ili tautomer navedenog spoja ili soli.
22. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 1-{[(2S,3S,4S)-4-fluor-3-metil-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamid, ili njegova farmaceutski prihvatljiva sol, ili tautomer navedenog spoja ili soli.
23. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 1-{[(2S,3R,4S)-4-fluor-3-(fluormetil)-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamid, ili njegova farmaceutski prihvatljiva sol, ili tautomer navedenog spoja ili soli.
24. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 4-{[(2S,3S,4S)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-6-metoksikinazolin-7-karboksamid, ili njegova farmaceutski prihvatljiva sol, ili tautomer navedenog spoja ili soli.
25. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 1-{[(2S,3S,4R)-3-etil-4-fluor-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamid, ili njegova farmaceutski prihvatljiva sol, ili tautomer navedenog spoja ili soli.
26. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 1-{[(2R,3R,4S)-3-etil-4-fluor-3-hidroksi-5-oksopirolidin-2-il]metoksi}-7-metoksiizokinolin-6-karboksamid, ili njegova farmaceutski prihvatljiva sol, ili tautomer navedenog spoja ili soli.
27. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili 20 do 26, naznačen time što je namijenjen upotrebi kao medikament.
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