HRP20140350T1 - Organski spojevi - Google Patents

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HRP20140350T1
HRP20140350T1 HRP20140350AT HRP20140350T HRP20140350T1 HR P20140350 T1 HRP20140350 T1 HR P20140350T1 HR P20140350A T HRP20140350A T HR P20140350AT HR P20140350 T HRP20140350 T HR P20140350T HR P20140350 T1 HRP20140350 T1 HR P20140350T1
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Urs Baettig
Anne-Marie D'souza
Peter Hunt
Neil John Press
Simon James Watson
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Novartis Ag
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    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
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    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Claims (16)

1. Spoj, naznačen time, da ima formulu I [image] ili njegovi solvati, hidrati ili njegove farmaceutski prihvatljive soli, gdje R1 je H, 3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, 3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, (C1-C4 alkil)-3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, (C1-C4 alkil)-3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena, CN-skupinama ili OH-skupinama, C1-C6 alkoksi opcijski supstituiran s jednim ili više atoma halogena ili OH-skupinama, ili eter-skupina koja sadrži 2 do 10 atoma ugljika i 1 do 3 atoma kisika, pri čemu je eter-skupina opcijski supstituirana s jednim ili više supstituenata od kojih je svaki neovisno odabran od sljedećih: OH, halogen, 3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina. i 3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina; R2 je 3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, 3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, (C1-C4 alkil)-3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, (C1-C4 alkil)-3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena, CN-skupinama ili OH-skupinama, ili eter-skupina koja sadrži 2 do 10 atoma ugljika i 1 do 3 atoma kisika, pri čemu je eter-skupina opcijski supstituirana s jednim ili više supstituenata od kojih je svaki neovisno odabran od sljedećih: OH, halogen, 3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, i 3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, ili R1 i R2, zajedno s atomom ugljika na kojega su priključeni, tvore 3 do 10-članu karbocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina, ili 3 do 10-članu heterocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina; R3 je vodik, halogen ili cijano; R4 je H, C1-C8 alkil, C3-C8 cikloalkil, C6-C8 cikloalkenil ili (C1-C4 alkil)-R6, gdje je svaka alkil-skupina opcijski supstituirana s jednim ili više atoma halogena; R5 je C1-C8 alkil, C3-C8 cikloalkil, C5-C8 cikloalkenil, (C1-C4 alkil)-C3-C8 cikloalkil ili (C1-C4 alkil)-C5-C8 cikloalkenil, gdje je svaka alkil-skupina opcijski supstituirana s jednim ili više atoma halogena; ili R1 i R6, zajedno s atomima kisika i dušika na koje su priključeni, tvore 5 do 10-članu heterocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina; R6 je odabran od sljedećih: 3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, 3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, NR7R9, NR7(SO2)R9, (SO2)NR7R8, (SO2)R9, NR7C(O)R9, C(O)NR7R9, NR7C(O)NR8R9, NR7C(O)OR9, C(O)OR7, OC(O)R9, OC(O)NR7, C(O)R9, SR7, CN i NO2; R7 i R8 su svaki neovisno odabrani od sljedećih: H, C1-C6 alkil, C3-C10 cikloalkil, C5-C10 cikloalkenil i -(C1-C3 alkilen)-C3-C10 cikloalkil; R9 je odabran od sljedećih: H, C1-C6 alkil, -(C1-C3 alkilen)-C3-C10 cikloalkil, 3 do 10-člana karbociklička skupina, 3 do 10-člana heterociklička skupina, gdje je svaka od alkil-skupina i alkil-prstenastih sustava opcijski supstituiran(a) s OH, halo, C1-C3 alkil i C1-C3 alkoksi; X je CR14 ili N; Z je neovisno odabran od sljedećih: OH; 3 do 10-člana karbociklička skupina; 3 do 10-člana heterociklička skupina; benzil; C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena, CN-skupinama ili OH-skupinama; C1-C6 alkoksi opcijski supstituiran s jednim ili više atoma halogena, CN-skupinama ili OH-skupinama; -Oaril; -Obenzil; -O(CH2)aC(O)E; NR10(SO2)R12; (SO2)NR10R11; (SO2)R12;NR10C(O)R12; C(O)NR10R12; NR10C(O)NR11R12; NR10C(O)OR12; NR10R12; C(O)OR10; OC(O)R12; OC(O)NR10; C(O)R12; SR12; CN; NO2; i halogen; ili gdje postoje dva ili više Z supstituenta, ta dva Z supstituenta zajedno s atomima na koje su priključeni, opcijski tvore 5- do 7-člani karbociklički ili 4- do 7-člani heterociklički supstituent kondenziran na prstenasti sustav; a je 0, 1, 2, 3 ili 4, gdje je alkilen-skupina opcijski supstituirana s OH ili NH2, kada a je 1, 2, 3 ili 4; E je NR10R12 ili OR12; svaki od R10 i R11 su neovisno odabrani od sljedećih: H, C1-C6 alkil, C3-C10 cikloalkil, C5-C10 cikloalkenil i -(C1-C3alkilen)-C3-C10 cikloalkil; svaki R12 je odabran od sljedećih: H, C1-C6 alkil, -(C1-C3 alkilen)-C3-C10 cikloalkil, 3 do 10-člana karbociklička skupina i 3 do 10-člana heterociklička skupina, gdje je svaki od tih prstenastih sustava opcijski supstituiran s OH, halo, C1-C3 alkil i C1-C3 alkoksi; i R14 je H ili C1-C6 alkil.
2. Spoj prema zahtjevu 1, naznačen time, da R1 je H ili C1-C4 alkil.
3. Spoj prema zahtjevu 1 ili zahtjevu 2, naznačen time, da R1 je H ili C1-C4 alkil; R2 je C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena, CN-skupinama ili OH-skupinama, ili eter-skupina sadrži 2 do 10 atoma ugljika i 1 do 3 atoma kisika, 4 do 6-članu karbocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina, ili 4 do 6-članu heterocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina; ili R1 i R2, zajedno s atomom ugljika na koji su priključeni, tvore 4 do 6-članu karbocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina ili 4 do 6-članu heterocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina.
4. Spoj prema bilo kojem prethodnom zahtjevu, naznačen time, da R3 je halogen.
5. Spoj prema bilo kojem prethodnom zahtjevu, naznačen time, da R4 je H, C1-C4 alkil, C3-C6 cikloalkil ili (C1-C3 alkil)-C3-C6 cikloalkil.
6. Spoj prema bilo kojem prethodnom zahtjevu, naznačen time, da R5 je C1-C6 alkil.
7. Spoj prema bilo kojem prethodnom zahtjevu, naznačen time, da X je CH.
8. Spoj prema zahtjevu 1, naznačen time, da je spoj odabran između sljedećih: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema zahtjevu 1, naznačen time, da je taj spoj 6-kloro-3-[2-(1-etil-propilamino)-3,4-diokso-ciklobut-1-enilamino]-2-hidroksi-N-metoksi-N-metil-benzensulfonamid sljedeće strukture: [image] ili njegova farmaceutski prihvatljiva sol.
10. Spoj prema bilo kojem od zahtjeva 1 do 9, naznačen time, da se taj spoj u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, upotrebljava kao farmaceutsko sredstvo.
11. Uporaba spoja prema bilo kojem od zahtjeva 1 do 9, naznačena time, da se taj spoj u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, koristi u proizvodnji lijeka za liječenje upalnih ili alergijskih stanja ili bolesti.
12. Uporaba prema zahtjevu 11, naznačena time, da to stanje je COPD.
13. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 9, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, zajedno s farmaceutski prihvatljivim nosačem ili pomoćnim sredstvom.
14. Postupak proizvodnje spoja prema bilo kojem od zahtjeva 1 do 9, naznačen time, da taj postupak obuhvaća reakciju spoja formule II [image] gdje su R3, R4 i R5 određeni u zahtjevu 1, sa spojem formule III [image] gdje su X, R1 i R2 određeni u zahtjevu 1; a zatim izolaciju proizvoda.
15. Kombinacija spoja prema bilo kojem od zahtjeva 1 do 9, naznačena time, da se taj spoj u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, miješa s drugom ljekovitom tvari.
16. Kombinacija prema zahtjevu 15, naznačena time, da druga ljekovita tvar je protuupalna, bronhodilatacijska, antihistaminska ili antitusivna ljekovita tvar.
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