ME02167B - Piridinil- i pirazinil-metiloksi-aril derivati korisni kao inhibitori tirozin kinaze slezine (syk) - Google Patents

Piridinil- i pirazinil-metiloksi-aril derivati korisni kao inhibitori tirozin kinaze slezine (syk)

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Publication number
ME02167B
ME02167B MEP-2015-102A MEP2015102A ME02167B ME 02167 B ME02167 B ME 02167B ME P2015102 A MEP2015102 A ME P2015102A ME 02167 B ME02167 B ME 02167B
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Montenegro
Prior art keywords
methyl
oxy
pyridinyl
tetrahydro
phenyl
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MEP-2015-102A
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English (en)
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Francis Louis Atkinson
Michael David Barker
John Liddle
David Matthew Wilson
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Glaxo Group Ltd
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Publication of ME02167B publication Critical patent/ME02167B/me

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Claims (28)

1.Jedinjenje formule (I):u kome:X je CR1 ili N;Y je CH, C ili N;R1 je vodonik, C1-6alkoksi ili C1-6alkil;R2 je vodonik, C1-6alkoksi, halo, -C(O)C1-6alkil, CN, halo-C1-6alkil ili C(O)NR4R5;R3 je vodonik ili C1-6alkoksi;R4 je vodonik ili C1-6alkil:R5 je vodonik ili C1-6alkil im i n su celi brojevi od kojih je svaki nezavisno izabran od 1 i 2; ilinjegova so.
2.Jedinjenje prema zahtevu 1, gde je jedinjenje jedinjenje formule (Ia) u kome X je CR1 ili N; Y je CH, C ili N; R1 je vodonik, C1-6alkoksi ili C1-6alkil; R2 je vodonik, C1-6alkoksi, halo ili -C(O)C1-6alkil, i m i n su celi brojevi od kojih je svaki nezavisno izabran od 1 i 2; ili njegova so.
3.Jedinjenje ili njegova so prema zahtevu 1 ili zahtevu 2, gde je X CR1.
4.Jedinjenje ili njegova so prema zahtevu 3, gde je R1 metil, metoksi ili vodonik.
5.Jedinjenje ili njegova so prema bilo kom od zahteva 1 do 4, gde je Y C.
6.Jedinjenje ili njegova so prema bilo kom od zahteva 1 do 5, gde je R2 vodonik, metoksi ili –C(O)CH3.
7.Jedinjenje ili njegova so prema bilo kom od patentnih zahteva 1 do 6, gde su m i n oba 2.
8.Jedinjenje prema patentom zahtevu 1, koje je izabrano od: 7-(3-{[(4-metil-2-piridinil)metil]oksi}-2-piridinil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 7-(2-(metiloksi)-6-{[(4-metil-2-piridihil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 7-(4-(metiloksi)-2-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 1-[4-{[(4-metil-2-piridinil)metil]oksi}-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)fenil]etanon; 1-[4-[(2-pirazinilmetil)oksi]-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)fenil]etanon; 7-(5-fluoro-2-{[(4-metil-2-piridinil)metil]oksi}fenil)-1,2,3,4-tetrahidroizohinolin; 7-[2-({[4-(metiloksi)-2-piridinil]metil}oksi)fenil]-2,3,4,5-tetrahidro-1H-3-benzazepin; 1-[4-[(2-piridinilmetil)oksi]-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)fenil]etanon; 7-(2-(metiloksi)-6-{[(4-metil-2-piridinil)metil]oksi}fenil)-1,2,3,4-tetrahidroizohinolin; 7-(5-(etiloksi)-2-{[(4-metil-2-piridinil)metil]oksi}fenil)-1,2,3,4-tetrahidroizohinolin; 7-{2-(metiloksi)-6-[(2-pirazinilmetil)oksi]fenil}-2,3,4,5-tetrahidro-1H-3-benzazepin; 4-{[(4-metil-2-piridinil)metil]oksi}-3-(1,2,3,4-tetrahidro-7-izohinolinil)benzonitril; 7-[2-{[(4-metil-2-piridinil)metil]oksi}-5-(trifluorometil)fenil]-1,2,3,4-tetrahidroizohinolin; 7-(5-(metiloksi)-2-{[(4-metil-2-piridinil)metil]oksi}fenil)-1,2,3,4-tetrahidroizohinolin; 7-{5-(metiloksi)-2-[(2-pirazinilmetil)oksi]fenil}-2,3,4,5-tetrahidro-1H-3-benzazepin; 7-[5-(metiloksi)-2-({[4-(metiloksi)-2-piridinil]metil}oksi)fenil]-2,3,4,5-tetrahidro-1H-3-benzazepin; 1-[4-({[4-(metiloksi)-2-piridinil]metil}oksi)-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)fenil]etanon; 7-[2-({[4-(metiloksi)-2-piridinil]metil}oksi)fenil]-2,3,4,5-tetrahidro-1H-3-benzazepin; 7-(5-fluoro-2-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 7-(5-(etiloksi)-2-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 7-(5-(metiloksi)-2-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 4-{[(4-metil-2-piridinil)metil]oksi}-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)benzonitril; 7-[2-{[(4-metil-2-piridinil)metil]oksi}-5-(trifluorometil)fenil]-2,3,4,5-tetrahidro-1H-3-benzazepin; 1-[4-{[(4-etil-2-piridinil)metil]oksi}-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)fenil]etanon; 1-[4-({[4-(etiloksi)-2-piridinil]metil}oksi)-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)fenil]etanon; 7-{5-(metiloksi)-2-[(2-piridinilmetil)oksi]fenil}-2,3,4,5-tetrahidro-1H-3-benzazepin; 1-[4-[(2-piridinilmetil)oksi]-3-(1,2,3,4-tetrahidro-7-izohinolinil)fenil]etanon; N-metil-4-{[(4-metil-2-piridinil)metil]oksi}-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)berizamid; 4-{[(4-metil-2-piridinil)metil]oksi}-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)benzamid; N,N-dimetil-4-{[(4-metil-2-piridinil)metil]oksi}-3-(1,2,3,4-tetrahidro-7-izohinolinil)benzamid; 4-{[(4-metil-2-piridinil)metil]oksi}-3-(1,2,3,4-tetrahidro-7-izohinolinil)benzamid; 7-(2,3-bis(metiloksi)-6-{[(4-metil-2-piridinil)metil]oksi}fenil)-1,2,3,4-tetrahidroizohinolin; 7-(2,3-bis(metiloksi)-6-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 7-(5-hloro-2-{[(4-metil -2- piridinil) metil] oksi}fenil)-2,3,4,5- tetrahidro-1H-3-benzazepin; 7-{5-hloro-2-[(2-piridinilmetil)oksi]fenil}-1,2,3,4-tetrahidroizohinolin; 7-(6-hloro-3-{[(4-metil-2-piridinil)metil]oksi}-2-piridinil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 7-(6-hloro-3-{[(4-metil-2-piridinil)metil]oksi}-2-piridinil)-1,2,3,4-tetrahidroizohinolin; 1-{3-(2,3-dihidro-1H-izoindol-5-il)-4-[(2-piridinilmetil)oksi]fenil}etanon; i 1-[4-[(2-piridinilmetil)oksi]-3-(1,2,3,4-tetrahidro-6-izohinolinil)fenil]etanon; ili njegova so.
9.Jedinjenje prema zahtevu 1, koje je izabrano od: 7-(3-{[(4-metil-2-piridinil)metil]oksi}-2-piridinil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 7-(2-(metiloksi)-6-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 7-(4-(metiloksi)-2-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; 1-[4-{[(4-metil-2-piridinil)metil]oksi}-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)fenil]etanon; 1-[4-[(2-pirazinilmetil)oksi]-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)fenil]etanon; 7-(5-fluoro-2-{[(4-metil-2-piridinil)metil]oksi}fenil)-1,2,3,4-tetrahidroizohinolin; 7-[2-({[4-(metiloksi)-2-piridinil]metil}oksi)fenil]-2,3,4,5-tetrahidro-1H-3-benzazepin; i 1-[4-[(2-piridinilmetil)oksi]-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)fenil]etanon, ili njegova so.
10.Jedinjenje prema zahtevu 1 koje je 1-[4-{[(4-metil-2-pindinil)metil]oksi}-3-(2,3,4,5-tetrahidro-1H-3-benzazepin-7-il)fenil]etanon; ili njegova so.
11.Jedinjenje prema zahtevu 1 koje je 7-(2-(metiloksi)-6-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; ili njegova so.
12.Jedinjenje prema patentom zahtevu 11 koje je 7-(2-(metiloksi)-6-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin mezilat.
13.Jedinjenje ili njegova so prema bilo kom od zahteva 1 do 11, gde je so farmaceutski prihvatljiva so.
14.Farmaceutska kompozicija koja sadrži jedinjenje formule (I) ili njegovu farmaceutski prihvatljivu so kao što je definisano prema zahtevu 13 i jedan ili više farmaceutski prihvatljivih nosača, razblaživača ili ekscipijenata.
15.Farmaceutska kompozicija prema zahtevu 14, u kojoj jedinjenje formule (I) je 7-(2-(metiloksi)-6-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; ili njegova farmaceutski prihvatljiva so.
16.Farmaceutska kompozicija prema zahtevu 15, gde je farmaceutski prihvatljiva so mezilat.
17.Farmaceutska kompozicija prema zahtevu 14, 15 ili 16, gde je kompozicija prilagođena za lokalno dermalno davanje.
18.Kombinacija koja sadrži jedinjenje formule (I) ili njegovu farmaceutski prihvatljivu so kao što je definisano prema zahtevu 13, zajedno sa jednim ili više drugih terapeutski aktivnih sredstava.
19.Kombinacija prema zahtevu 18, gde je jedinjenje formule (I) 7-(2-(metiloksi)-6-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; ili njegova farmaceutski prihvatljiva so.
20.Kombinacija prema zahtevu 19, gde je farmaceutski prihvatljiva so mezilat.
21.Jedinjenje formule (I) ili njegova farmaceutski prihvatljiva so kao što je definisano prema zahtevu 13, za primenu u terapiji.
22.Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu u terapiji prema zahtevu 21, gde je jedinjenje 7-(2-(metiloksi)-6-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; ili njegova farmaceutski prihvatljiva so.
23.Jedinjenje ili njegova farmaceutski prihvatljiva so za primenu u terapiji prema zahtevu 22, gde je farmaceutski prihvatljiva so mezilat.
24.Jedinjenje formule (I) ili njegova farmaceutski prihvatljiva so kao što je definisano u zahtevu 13, za upotrebu u inhibiciji tirozin kinaze slezine.
25.Jedinjenje ili njegova farmaceutski prihvatljiva so kao što je deifinisano prema zahtevu 13, za upotrebu u lečenju autoimunih stanja.
26.Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema zahtevu 25, gde je autoimuno stanje hronična idiopatska urtikarija sa i bez statusa auto-antitela.
27.Jedinjenje ili njegova farmaceutski prihavatljiva so za upotrebu prema zahtevu 26, gde je jedinjenje 7-(2-(metiloksi)-6-{[(4-metil-2-piridinil)metil]oksi}fenil)-2,3,4,5-tetrahidro-1H-3-benzazepin; ili njegova farmaceutski prihvatljiva so.
28.Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema zahtevu 27, gde je farmaceutski prihvatljiva so mezilat.
MEP-2015-102A 2011-03-11 2012-03-08 Piridinil- i pirazinil-metiloksi-aril derivati korisni kao inhibitori tirozin kinaze slezine (syk) ME02167B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1104153.0A GB201104153D0 (en) 2011-03-11 2011-03-11 Novel compounds
PCT/EP2012/053948 WO2012123311A1 (en) 2011-03-11 2012-03-08 Pyridinyl- and pyrazinyl -methyloxy - aryl derivatives useful as inhibitors of spleen tyrosine kinase (syk)
EP12707342.7A EP2683709B1 (en) 2011-03-11 2012-03-08 Pyridinyl- and pyrazinyl-methyloxy-aryl derivatives useful as inhibitors of spleen tyrosine kinase (syk)

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ME02167B true ME02167B (me) 2015-10-20

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UA109807C2 (xx) 2015-10-12
KR101564007B1 (ko) 2015-10-28
MX339123B (es) 2016-05-12
IL227873A (en) 2016-02-29
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MA35030B1 (fr) 2014-04-03
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DK2937344T3 (en) 2017-10-23
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ZA201306554B (en) 2017-05-31
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