HRP20121069T1 - Supstituirani derivati amida kao inhibitori protein kinaze - Google Patents

Supstituirani derivati amida kao inhibitori protein kinaze Download PDF

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Publication number
HRP20121069T1
HRP20121069T1 HRP20121069TT HRP20121069T HRP20121069T1 HR P20121069 T1 HRP20121069 T1 HR P20121069T1 HR P20121069T T HRP20121069T T HR P20121069TT HR P20121069 T HRP20121069 T HR P20121069T HR P20121069 T1 HRP20121069 T1 HR P20121069T1
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Croatia
Prior art keywords
phenyl
oxo
methyl
carboxamide
dihydro
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HRP20121069TT
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English (en)
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Tae-Seong Kim
David Bauer
Steven Bellon
Alessandro Boezio
Shon Booker
Deborah Choquette
Derin D'amico
Noel D'angelo
Celia Dominguez
Ingrid M. Fellows
Julie Germain
Russel Graceffa
Jean-Cristophe Harmange
Satoko Hirai
Daniel La
Matthew Lee
Longbin Liu
Mark H. Normal
Michele Pothashman
Philip Roveto
Ning Xi
Aaron C. Siegmund
Kevin Yang
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Amgen Inc.
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Publication of HRP20121069T1 publication Critical patent/HRP20121069T1/hr

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Claims (18)

1. Spoj formule I R-X-W-Y-R1 I njegovi enantiomeri, diastereomeri, farmaceutski prihvatljive soli i N-oksidi, gdje R je [image] gdje Z je izabran od N ili CR7; Z1 je izabran od N ili CR7; W je izabran iz grupe koju čine supstituirani ili nesupstituirani fenil, supstituirani ili nesupstituirani piridil, supstituirani ili nesupstituirani pirimidinil, supstituirani ili nesupstituirani piridazinil i supstituirani ili nesupstituirani pirazinil; X je O; Y je izabran od -NRaC(=O)-(CR3R4)p- i -NRaC(=S)-(CR3R4)p-; Ra je izabran iz grupe koju čine H, alkil, heterociklil, aril, alkenil i alkinil; R1 je izabran od: [image] i [image] gdje je Rb nezavisno izabran u svakom slučaju iz grupe koju čine H, arilalkil, 5-6-člani heterociklil-C1-3 alkil, C1-6-alkil, C6-10 aril, C6-10 heteroaril, C3-6 cikloalkil, benzil, C1-3 alkilaril, C1-3alkilheteroaril, metil, etil, izopropil, butil, sek-butil, izobutil, metoksimetil, -(C1-6)alkil, 2-hidroksi 2-metilbutil, 2-hidroksi-2-metilpropil, 2-hidroksipropil, 1-(1-hidroksiciklopropil) metil, etilaminometil, piperidin-1-ilmetil, pirolidin-1-ilmetil, piridil, tienil, fenil, 1-naftil, nitril, -C(=O)OR5a, -C(=O)NR5aRa i -C(=O)R5a; gdje je Rc jedan ili više supstituenata izabranih od H, metil, izopropil, terc-butil, bromo, fluoro i hidroksil; svako R3 i R4 nezavisno su izabrani iz grupe koju čine H, alkil, aril, heterociklil, arilalkil, cikloalkil i cikloalkilalkil; alternativno R3 i R4, zajedno sa atomom za koji su vezani, formiraju 3-6 –člani prsten; R5 je nezavisno izabran u svakom slučaju iz grupe koju čine H, alkil, haloalkil, heterociklilalkil, cikloalkilalkil, aril i heterociklil; R5a je nezavisno izabran u svakom sluičaju od H, alkil, haloalkil, arilalkil aminoalkil, heterociklilalkil, cikloalkilalkil, aril, heterociklil, alkenil, alkinil i cikloalkil; R7 je izabran iz grupe koju čine H, halo, cijano i alkil; R8* je jedan ili više supstituenata nezavisno izabranih u svakom slučaju od OC(=O)NRaR5, -NRaC(=O)OR5 i -NRaC(=O)-R5; p je 0, 1, 2 ili 3; i gdje je svaka alkil, aril, heteroaril, cikloalkil, alkenil, alkinil, heterociklil i alkoksi grupa od bilo kojeg R, R1, R3, R4, R5, R7, R8* i Ra izborno nezavisno supstituirana sa jednom ili više grupa nezavisno izabranih u svakom slučaju od halo, okso, -NRaR5, -OR5a, -CO2R5, -C(=O)R5, (C1-C6)alkilamino, -NH-N=NH, (C1-C6)alkil, (C1-C6)alkinil, (C3-C6)cikloalkil, (C1-C6)haloalkil, di(C1-C6)alkilamino, (C1-C6)alkilamino-(C1-C6)alkil, (C1-C6)hidroksialkilamino, (C1-C6)alkilamino-(C1-C6)alkilamino, fenil, heterociklik, heteroaril, -(CR3R4)palkil-S(=O)-alkil i -(CR3R4)palkil-S(O)2-alkil, pri čemu je svaki alkenil naveden ovdje u prethodnom tekstu – linearni ili razgranati radikal od dva do dvanaest atoma ugljika koji ima najmanje jednu ugljik-ugljik dvogubu vezu i pri čemu je svaki alkinil naveden ovdje u prethodnom tekstu linearni ili razgranati radikal od dva do dvanaest atoma ugljika koji ima najmanje jednu ugljik-ugljik trogubu vezu.
2. Spoj prema patentnom zahtjevu 1, naznačen time što, W je supstituiran ili nesupstituiran fenil; i njegove farmaceutski prihvatljive soli.
3. Spoj prema patentnom zahtjevu 1, naznačen time što, W je supstituiran ili nesupstituiran piridil; i njegove farmaceutski prihvatljive soli.
4. Spoj prema patentnom zahtjevu 1, naznačen time što, Y je izabran od -NHC(=O)- i -NHC(=O)-(CH2)p-; i gdje je p jednako 0 ili 1; i njegove farmaceutski prihvatljive soli.
5. Spoj prema patentnom zahtjevu 1, naznačen time što, Y je -NHC(=O)-; i njegove farmaceutski prihvatljive soli.
6. Spoj prema patentnom zahtjevu 1, naznačen time što, p je 0; i njegove farmaceutski prihvatljive soli.
7. Spoj i njegove farmaceutski prihvatljive soli i solvati izabrani od slijedećih N-(3-fluoro-4-(2-(3-metil-1,2,4-oksadiazol-5-il)tieno[3,2-b]piridin-7-iloksi)fenil)-1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(3-fluoro-4-((2-(1-metil-1H-imidazol-5-il)tieno[3,2-b]piridin-7-il)oksi)fenil)-1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(3-fluoro-4-((2-(1-metil-1H-imidazol-5-il)tieno[3,2-b]piridin-7-il)oksi)fenil)-1-((2R)-2-hidroksipropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(3-fluoro-4-(7H-pirolo[2,3-d]pirimidin-4-iloksi)fenil)-1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(3-fluoro-4-(1H-pirolo[2,3-b]piridin-4-iloksi)fenil)-1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; Metil(6-((4-(((1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-il)karbonil)amino)fenil)oksi)-1H-benzimidazol-2-il)karbamat; N-(4-(2-(azetidin-1-karbonil)tieno[3,2-b]piridin-7-iloksi)-3-fluorofenil)-5-metil-3-okso-2-fenil-1-propil-2,3-dihidro-1H-pirazol-4-karboksamid; 7-(2-fluoro-4-(1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)-N-metiltieno[3,2-b]piridin-2-karboksamid; N-(3-fluoro-4-(2-(1-metilpiperazin-4-karbonil)tieno[3,2-b]piridin-7-iloksi)fenil)-1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(2-(dimetilamino)etil)-7-(2-fluoro-4-(1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)tieno[3,2-b]piridin-2-karboksamid; N-(4-(2-(3-(dimetilamino)pirolidin-1-karbonil)tieno[3,2-b]piridin-7-iloksi)-3-fluorofenil)-1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; 7-(2-fluoro-4-(1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)-N,N-dimetiltieno[3,2-b]piridin-2-karboksamid; 7-(2-fluoro-4-(1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)tieno[3,2-b]piridin-2-karboksamid; N-(2-(dimetilamino)etil)-7-(2-fluoro-4-(1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)-N-metiltieno[3,2-b]piridin-2-karboksamid; 7-(2-fluoro-4-(1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)-N-(2-metoksietil)tieno[3,2-b]piridin-2-karboksamid; N-(4-(2-(azetidin-1-karbonil)tieno[3,2-b]piridin-7-iloksi)-3-fluorofenil)-1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-ciklopropil-7-(2-fluoro-4-(1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)tieno[3,2-b]piridin-2-karboksamid 7-(2-fluoro-4-(5-metil-3-okso-2-fenil-1-propil-2,3-dihidro-1H-pirazol-4-karboksamido) fenoksi)tieno[3,2-b]piridin-2-karboksamid; N-(3-fluoro-4-(6-(pirolidin-1-karboksamido)pirimidin-4-iloksi)fenil)-1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(3-fluoro-4-(6-(pirolidin-1-karboksamido)pirimidin-4-iloksi)fenil)-5-metil-3-okso-2-fenil-1-propil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(6-(4-(1,5-dimetil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)-2-fluorofenoksi)pirimidin-4-il)morfolin-4-karboksamid; N-(6-(2-fluoro-4-(5-metil-3-okso-2-fenil-1-propil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)pirimidin-4-il)morfolin-4-karboksamid; N-(6-(2-fluoro-4-(5-metil-3-okso-2-fenil-1-propil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)pirimidin-4-il)piperidin-1-karboksamid; N-(6-(2-fluoro-4-(5-metil-3-okso-2-fenil-1-propil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)pirimidin-4-il)-4-metilpiperazine-1-karboksamid; (R)-N-(4-(6-(3-(dimetilamino)pirolidin-1-karboksamido)pirimidin-4-iloksi)-3-fluorofenil)-5-metil-3-okso-2-fenil-1-propil-2,3-dihidro-1H-pirazol-4-karboksamid; (R)-N-(4-(6-aminopirimidin-4-iloksi)-3-fluorofenil)-1-(2-hidroksipropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(3-fluoro-4-(2-(pirolidin-1-karboksamido)piridin-4-iloksi)fenil)-1,5-dimetil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(4-(4-(1,5-dimetil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)-2-fluorofenoksi)piridin-2-il)piperidin-1-karboksamid; (R)-N-(4-(2-(3-(dimetilamino)pirolidin-1-karboksamido)piridin-4-iloksi)-3-fluorofenil)-1,5-dimetil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(3-fluoro-4-(2-(pirolidin-1-karboksamido)piridin-4-iloksi)fenil)-1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(3-fluoro-4-(2-(pirolidin-1-karboksamido)piridin-4-iloksi)fenil)-5-metil-3-okso-2-fenil-1-propil-2,3-dihidro-1H-pirazol-4-karboksamid; N-(4-(4-(1,5-dimetil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)-2-fluorofenoksi) piridin-2-il)morfolin-4-karboksamid; N-(4-(2-fluoro-4-(1-(2-hidroksi-2-metilpropil)-5-metil-3-okso-2-fenil-2,3-dihidro-1H-pirazol-4-karboksamido)fenoksi)piridin-2-il)piperidin-1-karboksamid; N-(3-fluoro-4-(2-(pirolidin-1-karboksamido)piridin-4-iloksi)fenil)-3-okso-2-fenil-2,3-dihidropiridazin-4-karboksamid; [image] [image] i [image]
8. Farmaceutska kompozicija koja sadrži farmaceutski prihvatljiv nosač i spoj prema bilo kojem od patentnih zahtjeva 1-7.
9. Spoj prema bilo kojem od patentnih zahtjeva 1-7 za uporabu u postupku za liječenje kancera kod subjekta.
10. Spoj za uporabu prema patentnom zahtjevu 9 koji sačinjava kombinaciju sa spojem koji je izabran od sredstava tipa antibiotika, alkilirajućih sredstava, antimetabolita, hormonalnih sredstava, imunoloških sredstava, sredstava tipa interferona i raznih sredstava.
11. Spoj prema bilo kojem od patentnih zahtjeva 1-7 za uporabu u smanjenju veličine tumora kod subjekta.
12. Spoj prema bilo kojem od patentnih zahtjeva 1-7 za uporabu u liječenju poremećaja posredovanih preko HGF kod subjekta.
13. Spoj prema bilo kojem od patentnih zahtjeva 1-7 za uporabu u smanjenju metastaze kod tumora kod subjekta.
14. Uporaba spoja prema bilo kojem od patentnih zahtjeva 1-7 za pripremu lijeka za liječenje kancera kod subjekta.
15. Uporaba prema patentnom zahtjevu 14, naznačena time što lijek dalje sadrži spoj koji je izabran od sredstava tipa antibiotika, alkilirajućih sredstava, antimetabolita, hormonalnih sredstava, imunoloških sredstava, sredstava tipa interferona i raznih sredstava.
16. Uporaba spoja prema bilo kojem od patentnih zahtjeva 1-7 za pripremu lijeka za smanjenje veličine tumora kod subjekta.
17. Uporaba spoja prema bilo kojem od patentnih zahtjeva 1-7 za pripremu lijeka za liječenje poremećaja posredovanih preko HGF kod subjekta.
18. Uporaba spoja prema bilo kojem od patentnih zahtjeva 1-7 za pripremu lijeka za smanjenje metastaze kod tumora kod subjekta.
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MY177111A (en) 2020-09-07
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