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ME02053B - Oksazol supstituisani indazoli kao inhibitori pi3-kinaze - Google Patents

Oksazol supstituisani indazoli kao inhibitori pi3-kinaze

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Publication number
ME02053B
ME02053B MEP-2015-22A MEP2215A ME02053B ME 02053 B ME02053 B ME 02053B ME P2215 A MEP2215 A ME P2215A ME 02053 B ME02053 B ME 02053B
Authority
ME
Montenegro
Prior art keywords
oxazol
salt
methyl
compound
compound according
Prior art date
Application number
MEP-2015-22A
Other languages
English (en)
Inventor
David A Mareska
Julie Nicole Hamblin
Suzanne Elaine Keeling
Joelle Le
Charlotte Jane Mitchell
Nigel James Parr
Original Assignee
Glaxo Group Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of ME02053B publication Critical patent/ME02053B/me

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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Claims (23)

1.Jedinjenje formule (I):gdeR1 je 9- ili 10-člani biciklični heteroaril, pri čemu 9- ili 10-člani biciklični heteroaril sadrži od jedan do tri heteroatoma nezavisno izabrana od kiseonika i azota i opciono supstituisan sa C1-6alkil, C3-6cikloalkil, halo, -CN ili - NHSO2R5, ilipiridinil opciono supstituisan sa jednim ili dva supstituenta nezavisno izabrana od C1-6alkil, -OR6, halo i –NHSO2R7;R2 i R3, zajedno sa atomom azota za koji su vezani, obrazuju 6- ili 7-člani heterocikl pri čemu 6- ili 7-člani heterocikl opciono sadrži atom kiseonika ili drugi atom azota i opciono je supstituisan sa jednim ili dva supstituenta nezavisno izabrana od C1-6alkil;R4 je vodonik ili metil;R6 je vodonik C1-4alkil; iR5 i R7 su svaka nezavisno C1-6alkil, ili fenil opciono supstituisan sa jednim ili dva supstituenta nezavisno izabrana od halo;ili njegova so.
2.Jedinjenje prema zahtevu 1, ili njegova so, gde R1 je 9-člani biciklični heteroaril pri čemu 9-člani biciklični heteroatom sadrži jedan ili dva atoma azota, ili piridinil opciono supstituisan sa jednim ili dva supstituenta izabrana od -OR6 i-NHSO2R7.
3.Jedinjenje prema zahtevu 1 ili zahtevu 2, ili njegova so, gde je R1 indolil.
4.Jedinjenje prema zahtevu 1 ili zahtevu 2, ili njegova so, gde je R1 piridinil opciono supstituisan sa jednim ili dva supstituenta nazavisno izabrana od - OR6 i -NHSO2R7.
5.Jedinjenje prema bilo kom od prethodnih zahteva, ili njegova so, gde R2 i R3, zajedno sa atomom azota za koji su vezani, obrazuju 6-člani heterocikl pri čemu 6-člani heterocikl opciono sadrži atom kiseonika ili drugi atom azota i opciono je supstituisan sa jednim ili dva supstituenta nezavisno izabrana od C1-6 alkila.
6.Jedinjenje prema bilo kom od prethodnih zahteva, ili njegova so, gde R2 i R3, zajedno sa atomom azota za koji su vezani, obrazuju 6-člani heterocikl pri čemu 6-člani heterocikl sadrži atom kiseonika i opciono je supstituisan sa jednim ili dva supstituenta nezavisno izabrana od C1-4 alkila.
7.Jedinjenje prema bilo kom od zahteva 1 do 5, ili njegova so, gde R2 i R3, zajedno sa atomom azota za koji su vezani, obrazuju 6-člani heterocikl u kome 6-člani heterocikl sadrži drugi atom azota i opciono je supstituisan sa C1-4 alkil.
8.Jedinjenje prema bilo kom od prethodnih zahteva, ili njegova so, gde je R4 vodonik.
9.Jedinjenje prema zahtevu 1, koje je: N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamid; N-[5-[4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamid; N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]-2,4-difluorobenzensulfonamid; 2,4-difluoro-N-[5-[4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]benzensulfonamid; 4-((5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-6-(1H-indol-4-il)-1H-indazol; 6-((1H-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1H-indazol; 6-((1H-indol-4-il)-4-[5-(4-morfolinilmetil)-1,3-oksazol-2-il]-1H-indazol; N-[5-[4-(5-{[(2R,6R)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamid; 6-((1H-indol-4-il)-4-[5-(1-piperazinilmetil)-1,3-oksazol-2-il]-1H-indazol; ili njegova so.
10.Jedinjenje prema zahtevu 1, koje je: N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamid ili njegova so.
11.Jedinjenje prema zahtevu 1 koje je: 6-((1H-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1H-indazol ili njegova so.
12.Jedinjenje prema bilo kom od zahteva 1 do 11 u obliku njegove farmaceutski prihvatljive soli.
13.Jedinjenje prema zahtevu 11 u obliku soli sukcinata.
14.Jedinjenje prema zahtevu 1, koje je: N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1H-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamid
15.Jedinjenje prema zahtevu 1 koje je: 6-((1H-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1H-indazol
16.Farmaceutska kompozicija sadrži jedinjenje koje je definisano u bilo kom od patentnih zahteva 1 do 11, ili njegova farmaceutski prihvatljiva so, i jedan ili više farmaceutski prihvatljivih ekscipijenata.
17.Jedinjenje definisano prema bilo kom od zatheva 1 do 11, ili njegova farmaceutski prihvatljiva so, za upotrebu u medicinskoj terapiji.
18.Jedinjenje definisano prema bilo kom od zahteva 1 do 11, ili njegova farmaceutski prihvatljiva so, za upotrebu u lečenju poremećaja posredovanog neodgovarajućom aktivnošću PI-3-kinaze.
19.Upotreba jedinjenja kako je definisano prema bilo kom od patentnih zahteva 1 do 11, ili njegova farmaceutski prihvatljiva so u proizvodnji leka za upotrebu u lečenju poremećaja posredovanog neodgovarajućom aktivnošću PI3-kinaze.
20.Jedinjenje za upotrebu prema zahtevu 18, gde poremećaj posredovan neodgovarajućom aktivnošću PI3-kinaze je respiratorna bolest, virusna infekcija, nevirusna respiratorna infekcija, alergijska bolest, autoimuna bolest, inflamatorna bolest, kardiovaskularna bolest, hematološki malignitet, neurodegenerativna bolest, pankreatitis, višestruko otkazivanje organa, bolest bubrega, agregacija krvnih pločica, kancer, pokretljivost sperme, odbacivanje transplanta, odbacivanje grafta, povreda pluća ili bol.
21.Jedinjenje za upotrebu prema zahtevu 18, gde je poremećaj posredovan neodgovarajućom aktivnošću PI3-kinaze astma, hronična obstruktivna bolest pluća (COPD), idiopatska pulmonarna fibroza (IPF), virusne infekcije respiratornog trakta, virusno pogoršanje respiratornih bolesti, aspergiloza, lajšmanijaza, alergijski rinitis, atopični dermatitis, reumatoidni artritis, multipla skleroza, inflamatorna bolest creva, tromboza, ateroskleroza, hematološki malignitet, neurodegenerativna bolest, pankreatitis, višestruko otkazivanje organa, bolest bubrega, agregacija krvnih pločica, kancer, pokretnljivost sperme, odbacijavanje transplanta, odbacivanje grafta, povreda pluća, bol u vezi sa reumatoidnim artritisom ili oesteoartritisom, bol u leđima, generalni inflamatorni bol, posthepatična neuralgija, dijabetičarska neuropatija, inflamatorni neuropatski bol (trauma), trigeminalana neuralgija ili centralni bol.
22.Jedinjenje za upotrebu prema zahtevu 18, gde je poremećaj posredovan neodgovarajućom aktivnošću PI-3-kinaze astma.
23. Jedinjenje za upotrebu prema zahtevu 18, gde je poremećaj posredovan neodgovarajućom aktivnošću PI3-kinaze COPD.
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