HRP20140892T1 - Novi hidroksi-6-heteroarilfenantridini i njihova uporaba kao inhibitora za pde4 - Google Patents

Novi hidroksi-6-heteroarilfenantridini i njihova uporaba kao inhibitora za pde4 Download PDF

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HRP20140892T1
HRP20140892T1 HRP20140892TT HRP20140892T HRP20140892T1 HR P20140892 T1 HRP20140892 T1 HR P20140892T1 HR P20140892T T HRP20140892T T HR P20140892TT HR P20140892 T HRP20140892 T HR P20140892T HR P20140892 T1 HRP20140892 T1 HR P20140892T1
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salt
compound
formula
oxide
treatment
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Ulrich Kautz
Beate Schmidt
Dieter Flockerzi
Armin Hatzelmann
Christof Zitt
Johannes Barsig
Degenhard Marx
Hans-Peter Kley
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Takeda Gmbh
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Claims (25)

1. Spoj, naznačen time, da ima formulu I [image] u kojoj R1 je metoksi, R2 je metoksi, etoksi, difluorometoksi ili 2,2-difluoroetoksi, R3 je vodik, R31 je vodik, R4 je -O-R41, gdje R41 je vodik, Har je supstituiran s R6 i R7, i to je piridinil, gdje R6 je okso, i R7 je metil, ili njegov enantiomer, njegova sol, njegov N-oksid ili sol od enantiomera ili N-oksid od toga spoja.
2. Spoj formule I prema zahtjevu 1, naznačen time, da R1 je metoksi, R2 je metoksi, etoksi, difluorometoksi ili 2,2-difluoroetoksi, R3 je vodik, R31 je vodik, R4 je -O-R41, gdje R41 je vodik, R5 je vodik, Har je 1-metil-1H-piridin-2-on-5-il, ili njegov enantiomer, njegova sol, njegov N-oksid ili sol od enantiomera ili N-oksid od toga spoja.
3. Spoj formule I prema zahtjevu 1, naznačen time, da R1 je metoksi, R2 je etoksi, etoksi, difluorometoksi ili 2,2-difluoroetoksi, R3 je vodik, R31 je vodik, R4 je -O-R41, gdje R41 je vodik, R5 je vodik, Har je 1-metil-1H-piridin-2-on-5-il, ili njegov enantiomer, njegova sol, njegov N-oksid ili sol od enantiomera ili N-oksid od toga spoja.
4. Spoj formule I prema zahtjevu 1, naznačen time, da je to 5-((2R,4aR,10bR)-9-etoksi-2-hidroksi-8-metoksi-1,2,3,4,4a,10b-heksahidro-fenantridin-6-il)-1-metil-1H-piridin-2-on ili sol toga spoja.
5. Spoj formule I prema zahtjevu 1, naznačen time, da je to 5-((2R,4aR,10bR)-9-etoksi-2-hidroksi-8-metoksi-1,2,3,4,4a,10b-heksahidro-fenantridin-6-il)-1-metil-1H-piridin-2-on.
6. Spoj formule I prema bilo kojem od zahtjeva 1 do 3, naznačen time, da ima konfiguraciju prikazanu u formuli I*, u odnosu na pozicije 4a i 10b, [image] ili njegova sol, njegov N-oksid ili sol od N-oksida toga spoja.;
7. Spoj formule I prema bilo kojem od zahtjeva 1 do 3, naznačen time, da ima konfiguraciju prikazanu u formuli I*, u odnosu na pozicije 2, 4a i 10b, [image] ili njegova sol, njegov N-oksid ili sol od N-oksida toga spoja.
8. Spoj formule I ili njegova sol prema zahtjevu 4, naznačen time, da se upotrebljava u liječenju bolesti.
9. Spoj formule I prema zahtjevu 5, naznačen time, da se upotrebljava u liječenju bolesti.
10. Farmaceutski sastav, naznačen time, da obuhvaća jedan ili više spojeva formule I ili njegov enantiomer, njegovu sol, njegov N-oksid ili sol od enantiomera ili od N-oksida toga ili od tih spojeva prema bilo kojem od zahtjeva 1 do 3, zajedno s uobičajenim farmaceutskim pomoćnim sredstvima i/ili nosačima.
11. Farmaceutski sastav, naznačen time, da obuhvaća spoj formule I ili njegovu sol prema zahtjevu 4, zajedno s uobičajenim farmaceutskim pomoćnim sredstvima i/ili nosačima.
12. Farmaceutski sastav, naznačen time, da obuhvaća spoj formule I prema zahtjevu 5, zajedno s uobičajenim farmaceutskim pomoćnim sredstvima i/ili nosačima.
13. Farmaceutski sastav, naznačen time, da obuhvaća jedan ili više spojeva formule I ili njegovu sol, njegov N-oksid ili sol od N-oksida toga ili tih spojeva prema bilo kojem od zahtjeva 6 ili 7, zajedno s uobičajenim farmaceutskim pomoćnim sredstvima i/ili nosačima.
14. Uporaba spoja formule I ili njegovog enantiomera, njegove soli, njegovog N-oksida ili soli od enantiomera ili od N-oksida toga spoja prema bilo kojem od zahtjeva 1 do 3, naznačena time, da je za proizvodnju farmaceutskih sastava za liječenje bronhijalne astme, COPD-a, psorijaze, atopičnog ekcema ili mellitus dijabetesa.
15. Uporaba spoja formule I ili njegove soli prema zahtjevu 4, naznačena time, da je za proizvodnju farmaceutskih sastava za liječenje bronhijalne astme, COPD-a, psorijaze ili atopičnog ekcema.
16. Uporaba spoja formule I ili njegove soli prema zahtjevu 4, naznačena time, da je za proizvodnju farmaceutskih sastava za liječenje mellitus dijabetesa.
17. Uporaba spoja formule I prema zahtjevu 5, naznačena time, da je za proizvodnju farmaceutskih sastava za liječenje bronhijalne astme, COPD-a, psorijaze ili atopičnog ekcema.
18. Uporaba spoja formule I prema zahtjevu 5, naznačena time, da je za proizvodnju farmaceutskih sastava za liječenje mellitus dijabetesa.
19. Uporaba spoja formule I ili njegove soli, njegovog N-oksida ili soli od N-oksida toga spoja prema bilo kojem od zahtjeva 6 ili 7, naznačena time, da je za proizvodnju farmaceutskih sastava za liječenje bronhijalne astme, COPD-a, psorijaze, atopičnog ekcema ili mellitus dijabetesa.
20. Spoj formule I ili njegov enantiomer, njegova sol, njegov N-oksid ili sol od enantiomera ili od N-oksida toga spoja prema bilo kojem od zahtjeva 1 do 3, naznačen time, da se upotrebljava za liječenje bronhijalne astme, COPD-a, psorijaze, atopičnog ekcema ili mellitus dijabetesa.
21. Spoj formule I ili njegova sol prema zahtjevu 4, naznačen time, da se upotrebljava za liječenje bronhijalne astme, COPD-a, psorijaze ili atopičnog ekcema.
22. Spoj formule I ili njegova sol prema zahtjevu 4, naznačen time, da se upotrebljava za liječenje mellitus dijabetesa.
23. Spoj formule I prema zahtjevu 5, naznačen time, da se upotrebljava za liječenje bronhijalne astme, COPD-a, psorijaze ili atopičnog ekcema.
24. Spoj formule I prema zahtjevu 5, naznačen time, da se upotrebljava za liječenje mellitus dijabetesa.
25. Spoj formule I ili njegova sol ili njegov N-oksid, ili sol od N-oksida toga spoja prema bilo kojem od zahtjeva 6 ili 7, naznačen time, da se upotrebljava za liječenje bronhijalne astme, COPD-a, psorijaze, atopičnog ekcema ili mellitus dijabetesa.
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