HRP20151338T1 - [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metoksi-etil)-4trifluorometoksi-1h-indol-3-il]metanon kao inhibitor triptaze mastocita - Google Patents

[4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metoksi-etil)-4trifluorometoksi-1h-indol-3-il]metanon kao inhibitor triptaze mastocita Download PDF

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HRP20151338T1
HRP20151338T1 HRP20151338TT HRP20151338T HRP20151338T1 HR P20151338 T1 HRP20151338 T1 HR P20151338T1 HR P20151338T T HRP20151338T T HR P20151338TT HR P20151338 T HRP20151338 T HR P20151338T HR P20151338 T1 HRP20151338 T1 HR P20151338T1
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crystalline form
compound according
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HRP20151338TT
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Yong Mi Choi-Sledeski
Nakyen Choy
Gregory Bernard Poli
John J. Shay
Patrick Wai-Kwok Shum
Adam W. Sledeski
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Sanofi
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Claims (15)

1. Spoj s formulom I: [image] ili njegova farmaceutski prihvatljiva sol, ili solvat od toga.
2. Spoj prema zahtjevu 1 naznačen time da je farmaceutski prihvatljiva sol odabrana od: hidroklorida, fumarata, bezilata, tozilata, sulfata, citrata, metansulfonata, tartrata, fosfata, glutamata i benzoata.
3. Spoj prema zahtjevu 2, naznačen time da sol je benzoat.
4. Kristalni oblik spoja prema zahtjevu 4, naznačen time da kristalni oblik ima XRPD vrhove uz postupak koji koristi Cu antikatodu kod, barem dva od 2 theta kutova: 7.75, 10.13, 17.03, 17.16, 18.39, 21.33, i 21.88.
5. Kristalni oblik spoja prema zahtjevu 5, naznačen time da kristalni oblik ima XRPD vrhove uz postupak koji koristi Cu antikatodu kod, barem tri od slijedećih kutova: 7.75, 10.13, 17.03, 17.16, 18.39, 21.33, i 21.88.
6. Kristalni oblik spoja prema zahtjevu 5, naznačen time da kristalni oblik ima XRPD vrhove uz postupak koji koristi Cu antikatodu kod, barem četiri od slijedećih kutova: 7.75, 10.13, 17.03, 17.16, 18.39, 21.33, i 21.88.
7. Kristalni oblik spoja prema zahtjevu 6, naznačen time da kristalni oblik ima XRPD vrhove uz postupak koji koristi Cu antikatodu kod, barem pet od slijedećih kutova: 7.75, 10.13, 17.03, 17.16, 18.39, 21.33, i 21.88.
8. Kristalni oblik spoja prema zahtjevu 3, naznačen time da se kristalni oblik tali kod 162 stupnja Celzija.
9. Spoj prema zahtjevu 1 naznačen time da je za uporabu u liječenju fiziološkog stanja koje je potrebno ublažiti inhibicijom triptaze, pri čemu je fiziološko stanje odabrano iz skupine koju čine upalna bolest, bolest destrukcije zglobne hrskavice, očni konjunktivitis, proljetni konjunktivitis, upalna crijevna bolest, astma, alergijski rinitis, intersticijska bolest pluća, fibroza, kronična opstruktivna plućna bolest, sklerodermija, plućna fibroza, ciroza jetre, fibroza miokarda, neurofibrom, hipertrofični ožiljak, dermatološko stanje, stanje povezano s pucanjem aterosklerotičnog plaka, periodontalna bolest, dijabetička retinopatija, rast tumora, anafilaksija, multipla skleroza, peptički ulkus, te sincicijska virusna infekcija.
10. Spoj prema zahtjevu 9 naznačen time da je za uporabu u liječenju fiziološkog stanja koje je potrebno ublažiti inhibicijom triptaze, pri čemu fiziološko stanje je KOPB.
11. Farmaceutski pripravak naznačen time da sadrži terapeutsku učinkovitu količinu spoja prema zahtjevu 1 i njihov farmaceutski prihvatljiv nosač.
12. Farmaceutski pripravak prema zahtjevu 11 naznačen time da dodatno sadrži terapeutsku učinkovitu količinu drugog spoja odabranog iz skupine koja sadrži beta adrenergični agonist, antikolinergik, protu-upalni kortikosteroid, antagonist receptora leukotriena, inhibitor lipoksigenaze, inhibitor fosfodiesterase-4, te protuupalno sredstvo.
13. Farmaceutski pripravak prema zahtjevu 12, naznačen time da je inhibitor fosfodiesteraze-4 odabran od roflumilasta i ciflumolasta.
14. Spoj naznačen time da ima formulu odabranu iz skupine koju čine: [image] [image] i [image]
15. Spoj naznačen time da ima formulu: [image]
HRP20151338TT 2008-08-22 2015-12-07 [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metoksi-etil)-4trifluorometoksi-1h-indol-3-il]metanon kao inhibitor triptaze mastocita HRP20151338T1 (hr)

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Application Number Priority Date Filing Date Title
US9101808P 2008-08-22 2008-08-22
US9101108P 2008-08-22 2008-08-22
EP09791693.6A EP2367812B1 (en) 2008-08-22 2009-08-20 [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4trifluoromethoxy-1h-indol-3-yl]methanone as an inhibitor of mast cell tryptase
PCT/US2009/054381 WO2010022196A2 (en) 2008-08-22 2009-08-20 [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase

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HRP20151338T1 true HRP20151338T1 (hr) 2016-01-15

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US (2) US8217178B2 (hr)
EP (1) EP2367812B1 (hr)
JP (1) JP5656834B2 (hr)
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CN (2) CN102149705B (hr)
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CL2009001759A1 (es) 2010-07-23
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CA2734877C (en) 2014-04-29
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