HRP20180116T1 - (2s)-n-[(1s)-1-cijano-2-feniletil]-1,4-oksazepan-2-karboksamidi kao inhibitori dipeptidil peptidaze i - Google Patents

(2s)-n-[(1s)-1-cijano-2-feniletil]-1,4-oksazepan-2-karboksamidi kao inhibitori dipeptidil peptidaze i Download PDF

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HRP20180116T1
HRP20180116T1 HRP20180116TT HRP20180116T HRP20180116T1 HR P20180116 T1 HRP20180116 T1 HR P20180116T1 HR P20180116T T HRP20180116T T HR P20180116TT HR P20180116 T HRP20180116 T HR P20180116T HR P20180116 T1 HRP20180116 T1 HR P20180116T1
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carboxamide
ethyl
cyano
phenyl
oxo
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Hans Roland Lönn
Stephen Connolly
Steven Swallow
Staffan PO KARLSSON
Carl-Johan Aurell
John Fritiof PONTÉN
Kevin James Doyle
Amanda Jane Van De Poël
Graham Peter Jones
David Wyn Watson
Jacqueline Anne Macritchie
Nicholas John Palmer
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Astrazeneca Ab
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    • A—HUMAN NECESSITIES
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Claims (11)

1. Spoj formule (I) [image] gdje R1 je [image] R2 je odabran iz vodika, F, Cl, Br, OSO2C1-3alkila, ili C1-3alkila; R3 je odabran iz vodika, F, Cl, Br, CN, CF3, SO2C1-3alkil, CONH2 ili SO2NR4R5, gde R4 i R5 zajedno s atomom dušika za koji su vezani formiraju azetidinski, pirolidinski ili piperidinski prsten; ili R1 je izabran između [image] [image] ili [image] X je izabran između O, S ili CF2; Y je izabran između O ili S; Q je izabran između CH ili N; R6 je izabran od C1-3alkila, pri čemu je navedeni C1-3alkil izborno supstituiran s 1, 2 ili 3 F i izborno s jednim supstituentom odabranim od OH, OC1-3alkila, N(C1-3alkila)2, ciklopropila ili tetrahidropirana; R7 je izabran između vodika, F, Cl ili CH3; ili njegova farmaceutski prihvatljiva sol.
2. Spoj sukladno patentnom zahtjevu 1 gdje R1 je [image] ili njegova farmaceutski prihvatljiva sol.
3. Spoj sukladno patentnom zahtjevu 1 ili patentnom zahtjevu 2 naznačeno time što X je O; R6 je C1-3alkil; i R7 je vodik; ili njegova farmaceutski prihvatljiva sol.
4. Spoj formule (I) sukladno patentnom zahtjevu 1 izabran između: (2S)-N-[(1S)-1-Cijano-2-(4’-cijanobifenil-4-il)etil]-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(3-metil-2-okso-2,3-dihidro-1,3-benzoksazol-5-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(3,7-dimetil-2-okso-2,3-dihidro-1,3-benzoksazol-5-il)fenil]etil}-1,4-oksazepan-2-karboksamida; 4’-[(2S)-2-Cijano-2-{[(2S)-1,4-oksazepan-2-ilkarbonil]amino}etil]bifenil-3-il metansulfonata; (2S)-N-{(1S-1-Cijano-2-[4-(3-metil-1,2-benzoksazol-5-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4’-(trifluorometil)bifenil-4-il]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-(3’,4’-difluorobifenil-4-il)etil]-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(6-cijanopiridin-3-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(4-metil-3-okso-3,4-dihidro-2H-1,4-benzotiazin-6-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-(1S)-1-Cijano-2-[4-(3-etil-7-metil-2-okso-2,3-dihidro-1,3-benzoksazol-5-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-{4-[3-(2-hidroksi-2-metilpropil)-2-okso-2,3-dihidro-1,3-benzoksazol-5-il]fenil}etil]-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-{4-[3-(2,2-difluoroetil)-7-fluoro-2-okso-2,3-dihidro-1,3-benzoksazol-5-il]fenil} etil]-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-(4-{3-[2-(dimetilamino)etil]-2-okso-2,3-dihidro-1,3-benzoksazol-5-il}fenil)etil]-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(3,3-difluoro-1-metil-2-okso-2,3-dihidro-1H-indol-6-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(7-fluoro-3-metil-2-okso-2,3-dihidro-1,3-benzoksazol-5-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(3-etil-2-okso-2,3-dihidro-1,3-benzoksazol-5-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-{4-[3-(ciklopropilmetil)-2-okso-2,3-dihidro-1,3-benzoksazol-5-il]fenil}etil]-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-{4-[3-(2-metoksietil)-2-okso-2,3-dihidro-1,3-benzotiazol-5-il]fenil}etil]-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-{4-[2-okso-3-(propan-2-il)-2,3-dihidro-1,3-benzoksazol-5-il]fenil}etil]-1,4-oksazepan- 2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(4-metil-3-okso-3,4-dihidro-2H-1,4-benzoksazin-6-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-{4-[3-(2-metoksietil)-2-okso-2,3-dihidro-1,3-benzoksazol-5-il]fenil}etil]-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(5-cijanotiofen-2-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-2-(4’-Karbamoil-3’-fluorobifenil-4-il)-1-cijanoetil]-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(1-metil-2-okso-1,2-dihidrohinolin-7-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-{4-[2-okso-3-(tetrahidro-2H-piran-4-ilmetil)-2,3-dihidro-1,3-benzoksazol-5-il]fenil}etil]-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-2-[4-(7-Hloro-3-metil-2-okso-2,3-dihidro-1,3-benzoksazol-5-il)fenil]-1-cijanoetil}-1,4-oksazepan- 2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-{4-[3-(2,2-difluoroetil)-2-okso-2,3-dihidro-1,3-benzoksazol-5-il]fenil}etil]-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-{4-[2-okso-3-(2,2,2-trifluoroetil)-2,3-dihidro-1,3-benzoksazol-5-il]fenil}etil]-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4-(3-metil-2-okso-2,3-dihidro-1,3-benzotiazol-5-il)fenil]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-1-Cijano-2-[4’-(metilsulfonil)bifenil-4-il]etil}-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-2-[4’-(Azetidin-1-ilsulfonil)bifenil-4-il]-1-cijanoetil}-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-(4’-fluorobifenil-4-il)etil]-1,4-oksazepan-2-karboksamida; (2S)-N-{(1S)-2-[4-(1,3-Benzotiazol-5-il)fenil]-1-cijanoetil}-1,4-oksazepan-2-karboksamida; (2S)-N-[(1S)-1-Cijano-2-(4’-cijanobifenil-4-il)etil]-1,4-oksazepan-2-karboksamida; i njihovih farmaceutski prihvatljivih soli.
5. Spoj sukladno patentnom zahtjevu 1 koje je (2S)-N-{(1S)-1-cijano-2-[4-(3-metil-2-okso-2,3-dihidro-1,3-benzoksazol- 5-il)fenil]etil}-1,4-oksazepan-2-karboksamid [image] ili njegova farmaceutski prihvatljiva sol.
6. Spoj sukladno patentnom zahtjevu 1 koje je (2S)-N-{(1S)-1-cijano-2-[4-(3-metil-2-okso-2,3-dihidro-1,3-benzoksazol- 5-il)fenil]etil}-1,4-oksazepan-2-karboksamid [image]
7. Farmaceutski pripravak koji sadrži spoj formule (I) sukladno bilo kojem od patentnih zahtjeva 1 do 6 i farmaceutski prihvatljiv ađuvant, razrjeđivač ili nosač.
8. Spoj formule (I) sukladno bilo kojem od patentnih zahtjeva 1 do 6 za terapiju.
9. Spoj formule (I) sukladno bilo kojem od patentnih zahtjeva 1 do 6, za liječenje opstruktivnih bolesti dišnih puteva: uključujući bilo koju od astme, uključujući bronhijalnu, alergijsku, intrinzičnu, ekstrinzičnu, indiciranu vježbanjem, indiciranu lijekom (uključujući aspirin i indiciran s NSAID) i astmu indiciranu prašinom, intermitetnu i perzistentnu i svih težina, i druge uzroke hiper-responsivnosti dišnih puteva; kroničnu opstruktivnu bolest pluća (COPD); bronhitis, uključujući infektivni i eozinofilni bronhitis; emfizem; bronhiektazu; cističnu fibrozu; sarkoidozu; deficijenciju alfa-1 antitripsina; pluća poljoprivrednika i srodne bolesti; hipersenzitivni pneumonitis; fibrozu pluća, uključujući kriptogeni fibrozni alveolitis, idiopatske intersticijalne pneumonije, fibrozu koju komplicira anti-neoplastična terapija i kronična infekcija, uključujući tuberkulozu i aspergilozu i druge gljivične infekcije; komplikacije transplantacije pluća; vaskulitis i trombotičke poremećaje vaskulature pluća, i plućnu hipertenziju; antitusivnu aktivnost uključujući tretman kroničnog kašlja povezanog s inflamatornim i sekretornim stanjima dišnih puteva, i jatrogeni kašalj; akutni i kronični rinitis uključujući rinitis medikamentozu, i vazomotorni rinitis; alergijski rinitis od višegodišnjih i sezonskih biljaka uključujući rinitis nervozu (peludnu groznicu); nazalnu polipozu; akutnu virusnu infekciju uključujući običnu prehladu, i infekciju kao posljedicu respiratornog sincicijalnog virusa, influencu, koronavirus (uključujući SARS) i adenovirus, akutnu povredu pluća, adultni respiratorni distres sindrom (ARDS), kao i pogoršanja svakog od gore navedenih stanja bolesti respiratornog trakta, naročito pogoršanja svih tipova astme ili COPD.
10. Spoj formule (I) za upotrebu sukladno patentnom zahtjevu 9 za liječenju astme ili kronične opstruktivne bolesti pluća.
11. Kombinacija spoja formule (I) sukladno bilo kojem od patentnih zahtjeva 1 do 6 i jednog ili više sredstava neovisno izabranih između: • nesteroidnog agonista receptora glukokoritokoida; • selektivnog agonista β2 adrenoceptora; • inhibitora fosfodiesteraze; • inhibitora proteaze; • glukokortikoida; • antikolinergičkog sredstva; • modulatora funkcije receptora za kemokin; i • inhibitora funkcije kinaze.
HRP20180116TT 2014-01-24 2018-01-22 (2s)-n-[(1s)-1-cijano-2-feniletil]-1,4-oksazepan-2-karboksamidi kao inhibitori dipeptidil peptidaze i HRP20180116T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461931090P 2014-01-24 2014-01-24
EP15701577.7A EP3097086B1 (en) 2014-01-24 2015-01-23 (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors
PCT/GB2015/050155 WO2015110826A1 (en) 2014-01-24 2015-01-23 (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors

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HRP20180116T1 true HRP20180116T1 (hr) 2018-03-23

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HRP20180116TT HRP20180116T1 (hr) 2014-01-24 2018-01-22 (2s)-n-[(1s)-1-cijano-2-feniletil]-1,4-oksazepan-2-karboksamidi kao inhibitori dipeptidil peptidaze i
HRP20201147TT HRP20201147T1 (hr) 2014-01-24 2020-07-23 (2s)-n-[(1s)-1-cijano-2-feniletil]-1,4-oksazepan-2-karboksamidi kao inhibitori dipeptidil peptidaze i

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US (16) US9522894B2 (hr)
EP (3) EP3744714A1 (hr)
JP (5) JP6469711B2 (hr)
KR (1) KR102417684B1 (hr)
CN (2) CN110483492B (hr)
AP (1) AP2016009322A0 (hr)
AR (1) AR099177A1 (hr)
AU (4) AU2015208932C1 (hr)
BR (1) BR112016016224B1 (hr)
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