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HRP20151386T1 - Fenil aminopirimidinski spojevi i njihova primjena - Google Patents

Fenil aminopirimidinski spojevi i njihova primjena Download PDF

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Publication number
HRP20151386T1
HRP20151386T1 HRP20151386TT HRP20151386T HRP20151386T1 HR P20151386 T1 HRP20151386 T1 HR P20151386T1 HR P20151386T T HRP20151386T T HR P20151386TT HR P20151386 T HRP20151386 T HR P20151386T HR P20151386 T1 HRP20151386 T1 HR P20151386T1
Authority
HR
Croatia
Prior art keywords
pyrimidin
cyanomethyl
benzamide
morpholinophenylamino
phenylamino
Prior art date
Application number
HRP20151386TT
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English (en)
Inventor
Christopher John Burns
Andrew Craig Donohue
John Thomas Feutrill
Thao Lien Thi Nguyen
Andrew Frederick Wilks
Jun Zeng
Original Assignee
Ym Biosciences Australia Pty 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 Ym Biosciences Australia Pty Ltd filed Critical Ym Biosciences Australia Pty Ltd
Publication of HRP20151386T1 publication Critical patent/HRP20151386T1/hr

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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Claims (18)

1. Spoj formule Ib [image] u kome je Z je nezavisno odabrano od N i CH; R1 je nezavisno odabran od H, halogena, OH, CONHR2, CON(R2)2, CF3, R2OR2, CN, morfolino, tiomorfolinila, tiomorfolino-1,1-dioksida, supstituiranog ili nesupstituiranog piperidinila, supstituiranog ili nesupstituiranog piperazinila, imidazolila, supstituiranog ili nesupstituiranog pirolidinila i C1-4alkilena u kome su atomi ugljika po izboru zamijenjeni sa NRY i/ili O supstituiranim sa morfolinom, tiomorfolinilom, tiomorfolino-1, 1-dioksidom, supstituiranim ili nesupstituiranim piperidinilom, supstituiranim ili nesupstituiranim piperazinilom, imidazolilom ili supstituiranim ili nesupstituiranim pirolidinilom; R2 je supstituiran ili nesupstituiran sa C1-4alkil; RY je H ili supstituiran ili nesupstituiran C1-4alkil; R8 je RXCN; RX je supstituiran ili nesupstituiran C1-4alkilen u kome do 2 atoma ugljika mogu biti po izboru zamijenjena sa CO, NS2R, NRY, CONRY, SOL, SO2 ili O; R11 je H ili C1-4alkil, U kome su supstituti odabrani iz grupe koja se sastoji od C1-4 alkil, C3-6 cikloalkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkilaril, aril, heterociklil, halo, haloaril, haloheterociklil, hidroksi, C1-4 alkoksi, ariloksi, karboksi, amino, C1-6alkilacil, arilacil, heterociklilacil, acilamino, aciloksi, C1-6alkilsulfenil, arilsulfonil i ciano; ili njegov enantiomer, njegov prolijek ili njegova farmaceutski prihvatljiva sol, gdje su prolijekovi odabrani od: • spojevi u kojima su aminokiselinski ostatak, ili polipeptidni lanac od dva ili više aminokiselinskih ostataka kovalentno vezani peptidnom vezom za slobodnu amino, hidroksi ili karboksilnu grupu spomenutog spojevi formule Ib; • spojevi u kojima su karbonat, karbamat, amid ili alkil estar kovalentno vezani za slobodnu amino, amido, hidroksi grupu ili grupu karboksilne kiseline spomenutog spojevi formule Ib preko karbonilnog ugljika bočnog lanca prolijeka; i • spojevi u kojima je slobodni hidroksil spomenutog spojevi formule Ib pridružen preko veze fosfor-kisik za fosfatni derivat spojevi (kao što je kiselina, sol ili kiselina, ili estar).
2. Spoj prema patentnom zahtjevu 1 gdje R1 je morfolino.
3. Spoj prema patentnom zahtjevu 1 ili patentnom zahtjevu 2 gdje Z je CH.
4. Spoj prema patentnom zahtjevu 1 odabrano od: N-(cianometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida; N-(2-cianopropan-2-il)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(3-morfolinofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-tiomorfblinofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-jodofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-N-(4-(2-(4-morfolinofenilamino)pirimidin-4-il)fenil)metansulfonamida; N-(cianometil)-4-(2-(4-(morfolinometil)fenilamino)pirimidin-4-il)benzamida; N-(2-(cianometilamino)-2-oksoetil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-(4-hidroksipiperidin-1-il)fenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-(4-metilpiperazin-1-il)fenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-(3-hidroksipiperidin-1-il)fenilamino)-5-metilpirimidin-4-il)benzamida; 4-(2-(4-(1-benzilpiperidin-4-iloksi)fenilamino)pirimidin-4-il)-N-(cianometil)benzamida; N-(cianometil)-4-(2-(6-morfolinopiridin-3-ilamino)pirimidin-4-il)benzamida; 4-(2-(4-(4-acetilpiperazin-1-il)fenilamino)pirimidin-4-il)-N-(cianometil)benzamida; N-(4-(2-(4-morfolinofenilamino)pirimidin-4-il)fenil)-N-(prop-2-inil)metansulfonamid tozilata; N-(cianometil)-4-(2-(4-(4-hidroksipiperidin-1-il)fenilamino)-5-metilpirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-(piperidin-4-iloksi)fenilamino)pirimidin-4-il)benzamida; 5-(4-(4-(cianometilkarbamoil)fenil)pirimidin-2-ilamino)-N,N-dimetil-2-morfolinobenzamida; N-terc-butil-5-(4-(4-(cianometilkarbamoil)fenil) pirimidin-2-ilamino)-2-morfolinobenzamida; 5-(4-(4-(cianometilkarbamoil)fenil)pirimidin-2-ilamino)-N-etil-2-morfolinobenzamida; N-(cianometil)-4-(2-(3-fluoro-4-morfolinofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-morfolino-3-(trifluorometil)fenilamino)pirimidin-4-il)benzamida; 5-(4-(4-(N-(cianometil)metilsulfonamido)fenil)pirimidin-2-ilamino)-N-(2-(dimetilamino)etil)-2-morfolinobenzamida; N-(cianometil)-N-(4-(2-(4-morfolino-3-(trifluorometil)fenilamino)pirimidin-4-il)fenil)metansulfonamida; N-(cianometil)-4-(2-(3-(propoksimetil)fenilamino)pirimidin-4-il)benzamida; 4-(2-(3-(aliloksimetil)-4-morfolinofenilamino)pirimidin-4-il)-N-(cianometil)benzamida; N-(cianometil)-4-(2-(4-(1-etilpiperidin-4-iloksi)fenilamino)pirimidin-4-il)benzamida; N-(cianometil)-N-(4-(2-(3-fluoro-4-morfolinofenilamino)pirimidin-4-il)fenil)metansulfonamida; N-(4-(2-(3-ciano-4-morfolinofenilamino)pirimidin-4-il)fenil)-N-(cianometil)metansulfonamida; 2-ciano-N-(4-(2-(4-morfolinofenilamino)pirimidin-4-il)fenil)acetamida; N-(cianometil)-4-(2-(4-(2-morfolinoetoksi)fenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-{[4-(1,1-diokso-1λ6,4-tiomorpholin-4-il)fenil]amino}pirimidin-4-il)benzamida; N-(cianometil)-4-[2-({4-[(1,1-diokso-1λ6,4-tiomorfolin-4-il)metil]fenil}amino)pirimidin-4-il]benzamida; N-(cianometil)-N-metil-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida; i N-(cianometil)-4-(5-metil-2-(4-morfolinofenilamino)pirimidin-4-il)benzamida. i njihove farmaceutsko prihvatljive soli.
5. Spoj prema patentnom zahtjevu 1 koje je [image] ili njegova farmaceutski prihvatljiva sol.
6. Spoj prema zahtjevu 5 koje je hidrohloridna sol slijedećeg spojevi [image]
7. Spoj prema patentnom zahtjevu 1 koje je [image] ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 7, gdje je spoj kinazni inhibitor.
9. Spoj prema patentnom zahtjevu 8, prema kome je kinazni inhibitor JAK2 inhibitor.
10. Proces za pripremu spojevi formule Ib prema patentnom zahtjevu 1, koji sadrži korak vezivanja spojevi formule II [image] gdje je R11 definiran u patentnom zahtjevu 1 i X je klor koji je zatim konvertiran u jod prije vezivanja sa spojevima koja su označena formulama III i IV. [image] pri čemu su Z, R1 i R8 definirani kao što je u patentnom zahtjevu 1; i M je B ili metal.
11. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 9, i farmaceutski prihvatljivi nosač.
12. Implant koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 9.
13. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9, ili farmaceutska kompozicija prema patentnom zahtjevu 11 za primjenu u metodi liječenja bolesti povezanih sa kinazom, gdje spomenuta metoda uključuje davanje efektivne količine spomenutog spoja ili farmaceutske kompozicije subjektu kod koga postoji takva potreba.
14. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 13, gdje je bolest povezana sa kinazom imunološka ili inflamatorna bolest, bolest hiperproliferacije, virusno oboljenje, bolest metabolizma, ili vaskularno oboljenje.
15. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 14, gdje su imunološko ili inflamatorno oboljenje presađeni organ.
16. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 14, gdje je hiperproliferativno oboljenje rak ili mijeloproliferativna bolest.
17. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 16 gdje je hiperproliferativna bolest mijeloproliferativna bolest odabrana iz grupe koja se sastoji od slijedećih bolesti: policitemija vera (PV), primarna mijelofibroza, trombocitemija, esencijalna trombocitemija (ET), agnoneična mijeloidna metaplazija (AMM), idiopatska mijelofibroza (IMF), hronična mijeloidna leukemija (CML), sistemska mastocistoza (SM), hronična neutrofilna leukemija (CNL), mijelodisplazni sindrom (MDS) i sistemska bolest masnih ćelija (SMCD).
18. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 17, gdje je mijeloproliferativna bolest odabrana iz grupe koju čine policitemija vera (PV), primarna mijelofibroza, trombocitemija, i esencijalna trombocitemija (ET).
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