HRP20100542T1 - Derivati bifenila i njihova uporaba za liječenje hepatitisa c - Google Patents

Derivati bifenila i njihova uporaba za liječenje hepatitisa c Download PDF

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HRP20100542T1
HRP20100542T1 HR20100542T HRP20100542T HRP20100542T1 HR P20100542 T1 HRP20100542 T1 HR P20100542T1 HR 20100542 T HR20100542 T HR 20100542T HR P20100542 T HRP20100542 T HR P20100542T HR P20100542 T1 HRP20100542 T1 HR P20100542T1
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alkyl
pharmaceutically acceptable
acceptable salt
unsubstituted
group
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James Wheelhouse Christopher
James Floyd Thomas Alexander
John Bushnell David
Lumley James
Iain Salter James
Clive Carter Malcolm
Mathews Neil
John Pilkington Christopher
Martyn Angell Richard
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Arrow Therapeutics Limited
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Priority claimed from GB0610664A external-priority patent/GB0610664D0/en
Priority claimed from GB0610663A external-priority patent/GB0610663D0/en
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Publication of HRP20100542T1 publication Critical patent/HRP20100542T1/hr

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Abstract

Spoj koji je derivat bifenila formule (I), ili njegova farmaceutski prihvatljiva sol naznačen time da: R1 je dio-A1-L1-A1' pri čemu A1 je fenil, L1 je -CH2- i A1' je 4-[(C1-C4 alkil)sulfonil]piperazin-1-il; A je -CO-NH-;B je -NH-CO-NH-, -NH-CO- ili -CO-NH-; - R2 je C1-C4 alkil; - R3 je C1-C4 alkil, C1-C4 alkoksi, C1-C2 haloalkil, C1-C2 haloalkoksi ili halogen; - n i m su isti ili različiti i svaki predstavlja 0 ili 1; - R4 je C1-C5 alkilna skupina ili dio -A4, -A4-A4', -L4-A4, -A4-L4-A4', -A4-CO-A4' ili -L4-Het4-L4'; - svaki A4 dio je isti ili različit, te je fenil, furanil, imidazolil, pirazolil, pirolidinil, azetidinil, tetrahidrofuranil, piperazinil, piperidinil, pirolidin-2-onil, tiadiazolil, izotiazolil, C3-C8 cikloalkil, morfolinil, tienil, piridil, pirolil, S,S-diokso-tiomorfolinil, tetrahidropiranil, tiazolil, oksadiazolil ili indazolil skupina, svaki A4 dio može biti nesupstituiran ili supstituiran sa (a) jednostrukim nesupstituiranim -CONR'R"' supstituentom i/ili (b) 1 ili 2 nesupstituirana supstituenta odabrana od fluora, klora, broma, -NR'R"', C1-C4 alkila, C1-C2 alkoksi, C1-C2 haloalkila i cijano, pri čemu R' je vodik ili C1-C4 alkil i R"' predstavlja C1-C4 alkil; - svaki A4' dio je isti ili različit i predstavlja morfolinil, piperazinil, izoksazolil, pirolidinil, S,S-dioksothiomorfolinil, 2,6-dioksopiperidinil, triazolil, piperidinil, ciklopropil ili cikloheksilnu skupinu koja je nesupstituirana ili supstituirana sa (a) jednostrukim nesupstituiranim -SO2-(C1-C4 alkil) supstituentom i/ili (b) 1 ili 2 nesupstituirana supstituenta odabrana od klora, fluora, broma, C1-C2 alkila i C1-C2 haloalkila; - L4 predstavlja C1-C3 alkilen skupinu ili C1-C3 hidroksialkilen skupinu; - L4' predstavlja C1-C2 alkilnu skupinu; i- Het4 predstavlja -O- ili -NH-.Patent sadrži još 8 patetnih zahtjeva.

Claims (9)

1. Spoj koji je derivat bifenila formule (I), ili njegova farmaceutski prihvatljiva sol [image] naznačen time da: R1 je dio-A1-L1-A1' pri čemu A1 je fenil, L1 je -CH2- i A1' je 4-[(C1-C4 alkil)sulfonil]piperazin-1-il; A je -CO-NH-; B je -NH-CO-NH-, -NH-CO- ili -CO-NH-; - R2 je C1-C4 alkil; - R3 je C1-C4 alkil, C1-C4 alkoksi, C1-C2 haloalkil, C1-C2 haloalkoksi ili halogen; - n i m su isti ili različiti i svaki predstavlja 0 ili 1; - R4 je C1-C5 alkilna skupina ili dio -A4, -A4-A4', -L4-A4, -A4-L4-A4', -A4-CO-A4' ili -L4-Het4-L4'; - svaki A4 dio je isti ili različit, te je fenil, furanil, imidazolil, pirazolil, pirolidinil, azetidinil, tetrahidrofuranil, piperazinil, piperidinil, pirolidin-2-onil, tiadiazolil, izotiazolil, C3-C8 cikloalkil, morfolinil, tienil, piridil, pirolil, S,S-diokso-tiomorfolinil, tetrahidropiranil, tiazolil, oksadiazolil ili indazolil skupina, svaki A4 dio može biti nesupstituiran ili supstituiran sa (a) jednostrukim nesupstituiranim -CONR'R"' supstituentom i/ili (b) 1 ili 2 nesupstituirana supstituenta odabrana od fluora, klora, broma, -NR'R"', C1-C4 alkila, C1-C2 alkoksi, C1-C2 haloalkila i cijano, pri čemu R' je vodik ili C1-C4 alkil i R"' predstavlja C1-C4 alkil; - svaki A4' dio je isti ili različit i predstavlja morfolinil, piperazinil, izoksazolil, pirolidinil, S,S-dioksothiomorfolinil, 2,6-dioksopiperidinil, triazolil, piperidinil, ciklopropil ili cikloheksilnu skupinu koja je nesupstituirana ili supstituirana sa (a) jednostrukim nesupstituiranim -SO2-(C1-C4 alkil) supstituentom i/ili (b) 1 ili 2 nesupstituirana supstituenta odabrana od klora, fluora, broma, C1-C2 alkila i C1-C2 haloalkila; - L4 predstavlja C1-C3 alkilen skupinu ili C1-C3 hidroksialkilen skupinu; - L4' predstavlja C1-C2 alkilnu skupinu; i - Het4 predstavlja -O- ili -NH-.
2. Spoj prema zahtjevu 1, naznačen time da R4 je -A4 ili -A4-L4-A4'.
3. Spoj prema zahtjevu 2, naznačen time da kada R4 je A4 to je C3-C6 cikloalkil i/ili kada R4 je -A4-L4-A4', A4 je fenil, L4 je -CH2- i A4' je skupina [image]
4. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time da je 5'-(ciklopropankarbonil-amino)-2'-trifluorometoksi-bifenil-4-karboksilna kiselina {4-[4-(propan-1-sulfonil)-piperazin-1-ilmetil]-fenil}-amid, ili njegova farmaceutski prihvatljiva sol.
5. Derivat bifenila formule (I), kako je definiran u bilo kojem od prethodnih zahtjeva, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za liječenje ljudi ili životinja.
6. Uporaba derivata bifenila formule (I), kako je definiran u bilo kojem od zahtjeva 1 do 4, ili njegove farmaceutski prihvatljive soli, naznačena time da je za proizvodnju lijeka za upotrebu u liječenju ili ublažavanju HCV.
7. Farmaceutski pripravak naznačen time da sadrži derivat bifenila formule (I), kako je definiran u bilo kojem od zahtjeva 1 do 4, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljivo otapalo ili nosač.
8. Farmaceutski pripravak prema zahtjevu 7, naznačen time da nadalje sadrži interferon i/ili ribavirin.
9. Proizvod naznačen time da sadrži : a. derivat bifenila formule (I), kako je definiran u bilo kojem od zahtjeva 1 do 4, ili njegovu farmaceutski prihvatljivu sol; b. interferon i/ili ribavirin; i c. farmaceutski prihvatljiv nosač ili otapalo; za istovremenu, odvojenu ili uzastopnu upotrebu pri liječenju ljudi ili životinja.
HR20100542T 2005-09-16 2010-10-05 Derivati bifenila i njihova uporaba za liječenje hepatitisa c HRP20100542T1 (hr)

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Application Number Priority Date Filing Date Title
GBGB0518971.7A GB0518971D0 (en) 2005-09-16 2005-09-16 Chemical compounds
GB0610664A GB0610664D0 (en) 2006-05-30 2006-05-30 Chemical compounds
GB0610663A GB0610663D0 (en) 2006-05-30 2006-05-30 Chemical compounds
PCT/GB2006/003469 WO2007031791A1 (en) 2005-09-16 2006-09-18 Biphenyl derivatives and their use in treating hepatitis c

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EP (1) EP1940786B1 (hr)
JP (1) JP2009508835A (hr)
KR (1) KR20080050490A (hr)
AT (1) ATE478044T1 (hr)
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HR (1) HRP20100542T1 (hr)
IL (1) IL189694A0 (hr)
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