ME02372B - Imidazotriazini i imidazopiramidini kao inhibitori kinaze - Google Patents

Imidazotriazini i imidazopiramidini kao inhibitori kinaze

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Publication number
ME02372B
ME02372B MEP-2016-13A MEP1316A ME02372B ME 02372 B ME02372 B ME 02372B ME P1316 A MEP1316 A ME P1316A ME 02372 B ME02372 B ME 02372B
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Montenegro
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alkyl
nrc2rd2
cr7r8
haloalkyl
independently selected
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Brian Metcalf
Meizhong Xu
Colin Zhang
Ding-Quan Qian
David M Burns
Yunlong Li
Wenqing Yao
Jincong Zhuo
Chunhong He
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Incyte Holdings Corp
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Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of ME02372B publication Critical patent/ME02372B/me

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Claims (27)

1. Spoj formule l: ili njegovafarmaceutski prihvatljiva sol ili njegov prolijek, pri čemu: A je N; Cy1 je aril, heteroaril, cikloalkil, iliheterocikloalkil, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W-X-Y-Z; Cy2 jearil, heteroaril, cikloalkil, ili heterokicloalkil, svaki opcionalnozamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; L1 je (CR4R5)m; L2 je (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t, (CR7R8)s-(arilen)-(CR7R8)t, (CR7R8)s-(heterocikloalkilen)-(CR7R8)t, (CR7R8)s-(heteroarilen)-(CR7R8)t, (CR7R8)sO(CR7R8)t, (CR7R8)sS(CR7R8)t, (CR7R8)sC(O)(CR7R8)t, (CR7R8)sC(O)NR9(CR7R8)t, (CR7R8)sC(O)O(CR7R8)t, (CR7R8)sOC(O)(CR7R8)t, (CR7R8)sOC(O)NR9(CR7R8)t, (CR7R8)sNR9(CR7R8)t, (CR7R8)sNR9C(O)NR9(CR7R8)t, (CR7R8)sS(O)(CR7R8)t, (CR7R8)sS(O)NR7(CR8R9)t, (CR7R8)sS(O)2(CR7R8)t, ili (CR7R8)sS(O)2NR9(CR7R8)t, pri čemu navedeni cikloalkilen, arilen, heterocikloalkilen,ili heteroarilen je opcionalno zamijenjensa 1, 2, ili 3 supstituenta nezavisnoizabrani od Cy4, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1 Rd1P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRe1Rd1, S(O)2Rb1, NRc1S(O)2Rb1, i S(O)2NRc1Rd1; R1 je H ili -W"-X"-Y"-Z"; R2 jeH, halo, C1-6 alkil,C2-6 alkenil,C2-6 alkinil,C1-6 haloalkil,CN, NO2,ORA, SRA, C(O)RB, C(O)NRCRD, C(O)ORA, OC(O)RB, OC(O)NRCRD,NRCRD, NRCC(O)RB, NRCC(O)NRCRD, NRCC(O)ORA, S(O)RB, S(O)NRCRD, S(O)2RB, NRCS(O)2RB, ili S(O)2NRCRD; ili R2 i-L2-Cy2 su povezani zajedno da bi formiraligrupu formule: pri čemu je prsten B spojeni arilni ili spojeni heteroarilni prsten, svaki opcionalnozamijenjen sa 1, 2, ili 3 -W’-X’-Y’-Z’; R4 je H; R5 je izabran od H, halo, OH, C1-6 alkil, i cikloalkil; ili R4 i R5 zajednosa C atomom na koji su vezani formiraju 3, 4, 5, 6, ili 7-člani cikloalkil; R7 i R8 su nezavisno izabrani odH, halo, OH, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, C1-6 haloalkil, CN, i NO2; ili R7 iR8 zajednosa C atomom za koji su povezani od 3, 4, 5, 6, ili 7-člana cikloalkilnog ili heterocikloalkilnog prstena, svaki opcionalno zamijenjen sa 1, 2,ili 3 supstituenta nezavisno izabranih od halo, OH, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, C1-6 haloalkil,CN, i NO2; R9 jeH, C1-6 alkil,C2-6 alkenil,ili C2-6 alkinil; W, W’, i W" su nezavisno odsutni ili nezavisno odabrani od C1-6 alkilen, C2-6 alkenilen, C2-6 alkinilen, O, S, NRh, CO, COO,CONRh,SO, SO2,SONRh iNRhCONRi, pri čemusvaki od C1-6 alkilena,C2-6 alkenilena,i C2-6 alkinilenaje opcionalno zamijenjen sa 1, 2 ili 3 supstituentanezavisno izabranih od halo, C1-6 alkil, C1-6 haloalkil, OH, C1-6 alkoksi, C1-6 haloalkoksi,amino, C1-6 alkilamino, i C2-8 dialkilamino;X, X’, i X" su nezavisno odsutni ili nezavisno izabrani od C1-6 alkilena,C2-6 alkenilena, C2-6 alkinilena, arilena, cikloalkilena,heteroarilena, i heterocikloalkilena, pri čemu svaki od C1-6 alkilena, C2-6 alkenilena,C2-6 alkinilena,arilena, cikloalkilena, heteroarilena, iheterocikloalkilena je opcionalno zamijenjensa 1, 2 ili 3 supstituenta nezavisnoizabranih od halo, CN, NO2, OH, C1-6 alkil, C1-6 haloalkil, C2-8 alkoksialkil, C1-6 alkoksi, C1-6 haloalkoksi,C2-8 alkoksialkoksi,cikloalkil, heterocikloalkil, C(O)ORj, C(O)NRhRi, amino. C1-6 alkilamino, i C2-8dialkilamino; Y, Y’, i Y" su nezavisno odsutni ilinezavisno izabrani od C1-6 alkilena, C2-6 alkenilena,C2-6 alkinilena,O, S, NRh,CO, COO, CONRh,SO, SO2,SONRh, iNRhCONRi, pri čemusvaki od C1-6 alkilena,C2-6 alkenilena,i C2-6 alkinilenaje opcionalno zamijenjen sa 1, 2 ili 3 supstituentanezavisno izabranih od halo, C1-6 alkil, C1-6 haloalkil, OH, C1-6 alkoksi, C1-6 haloalkoksi,amino, C1-6 alkilamino, i C2-8 diaikilamino; Z, Z’, i Z" su nezavisno izabrani od H, halo,C1-6 alkil,C2-6 alkenil,C2-6 alkinil,C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2,NRc2S(O)2Rb2, SS(O)2NRc2Rd2, aril,cikloalkil, heteroaril, i heterocikloalkil, gdje navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil,aril, cikloalkil, heteroaril, i heterocikloalkil je opcionalno zamijenjen sa 1, 2, 3, 4 ili 5 supstituenta nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenil,C2-6 alkinil,C1-6 haloalkil,halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2 , C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, Nrc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2,S(O)NRc2Rd2, S(O)2Rb2 , NRc2S(O)2Rb2, i S(O)2NRc2Rd2; pri čemu dva susjedna -W-X-Y-Z, zajedno sa atomima sa kojima supovezani, opcionalno formiraju spojeni cikloalkilni prsten od 4-20 članova ilispojeni heterocikloalkilni prsten od 4-20 članova, svaki opcionalno zamijenjensa 1, 2, ili 3, supstituenta nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, Nrc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(=NRg)NRc3Rd3, NRc3C(=NR9)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3, S(O)2NRc3Rd3,aril, cikloalkil, heteroaril, i heterocikloalkil; pri čemu dva susjedna -W’-X’-Y’-Z’, zajedno sa atomima sa kojima supovezani, opcionalno formiraju spojeni cikloalkilni prsten od 4-20 članova ilispojeni heterocikloalkilni prsten od 4-20 članova, svaki opcionalno zamijenjensa 1, 2, ili 3, supstituenta nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil,halosulfanil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3,C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3 , NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3,C(=NRg)NRc3Rd3, NRc3C(=NRg)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3, S(O)2NRc3Rd3, aril,cikloalkil, heteroaril, i heterocikloalkil; Cy4 je nezavisno izabran od aril, cikloalkil, heteroaril,i heterocikloalkil, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 supstituentanezavisno izabranih od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, Nrc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(=NRg)NRc4Rd4, NRc4C(=NRg)NRc4Rd4, P(Rf4)2, P(OR4)2, P(O)Re4Rf4, P(O)ORe4ORf4, S(O)Rb4, S(O)NRc4Rd4, S(O)2Rb4, NRc4S(O)2Rb4, i S(O)2NRc4Rd4; RA je H, C1-4 alkil, C2-4 alkenil, C2-4 alkinil,cikloalkil, heterocikloalkil, aril, iliheteroaril gdje navedeni C1-4 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, heterocikloalkil, aril ili heteroaril je opcionalno zamijenjensa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, i C1-4 alkil ; RB jeH, C1-4 alkil,C2-4 alkenil,C2-4 alkinil,cikloalkil, heterocikloalkil, aril, iliheteroaril gdje navedeni C1-4 alkil, C2-4 alkenil,ili C2-4 alkinil,cikloalkil, heterocikloalkil, aril, ili heteroaril je opcionalno zamijenjen sa 1,2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, i C1-4 alkil; RC iRD sunezavisno izabrani od H, C1-4 alkil, C2-4 alkenil, ili C2-4 alkinil, gdje navedeni C1-4 alkil, C2-4 alkenil,ili C2-4 alkinil,je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH,CN, amino, halo, i C1-4 alkil; ili RC i RD zajedno sa N atomom za koji su povezani uheterocikloalkilnu grupu od 4-, 5-, 6-ili 7- članova ili heteroarilnu grupu,svaku opcionalno zamijenjenih sa 1, 2,ili 3 supstituenta nezavisno odabranihod OH, CN, amino, halo, i C1-4 alkil; Ra, Ra1, Ra2, Ra3, i Ra4 su nezavisnoizabrani od H, C1-6alkil, C1-6haloalkil, C2-6alkenil, C2-6 alkinil, aril,cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil,cikloalkilalkil, i heterocikloalkilalkil, gdje navedeni C1-6alkil, C1-6 haloalkil, C2-6alkenil, C2-6 alkinil,aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil jeopcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH,CN, amino, halo, C1-6 alkil, C1-6 alkoksi,C1-6 haloalkil, i C1-6haloalkoksi; Rb, Rb1, Rb2, Rb3, i Rb4 su nezavisno izabrani od H, C1-6 alkil, C1-6 haloalkil,C2-6 alkenil, C2-6 alkinil, aril, cikloalkil,heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, i heterocikloalkilalkil,pri čemu navedeni C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alknil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkilje opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi; Rc i Rd su nezavisno izabrani od H, C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil,arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil, pri čemunavedeni C1-10 alkil,C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil,heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkilje opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi; ili Rc i Rd zajedno sa N atomom za koji su prikvačeniformiraju heterocikloalkilnu grupu od 4-, 5-, 6- ili 7-člana ili heteroarilnu grupu, svaki opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisnoizabranih odOH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi; Rc1 iRd1 su nezavisno odabrani od H, C1-10 alkil, C1-6 haloalkil,C2-6 alkenil,C2-6 alkinil, aril, heteroaril, cikloalkil,heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil, pri čemu navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil,heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocicloalkilalkil je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabrani od OH, CN,amino, halo, C1-6alkil, C1-6 alkoksi, C1-6 haloalkil,i C1-6 haloalkoksi; ili Rc1 i Rd1 zajedno sa N atomom sakojim su spojeni formiraju heterocikloalkilnu grupu od 4-, 5-, 6- ili 7-članova ili heteroarilnu grupu, svaki opcionalno zamijenjen sa 1,2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi; Rc2 iRd2 su nezavisno odabrani od H, C1-10 alkil, C1-6 haloalkil,C2-6 alkenil,C2-6 alkinil, aril, heteroaril, cikloalkil,heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, heterocikloalkilalkil, arilcikloalkil, arilheterocikloalkil, arilheteroaril, biaril,heteroarilcikloalkil, heteroarilheterocikloalkil, heteroarilaril,i biheteroaril, pri čemu navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril,cikloalkil, heterocikloalkil, arilalkil,heteroarilalkil, cikloalkilalkil, heterocikloalkilalkil, arilcikloalkil, arilheterocikloalkil,arilheteroaril, biaril, heteroarilcikloalkil, heteroarilheterocikloalkil, heteroarilaril, i biheteroaril je svaki opcionalno zamijenjen sa 1, 2, ili 3supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, hidroksialkil;cijanoalkil, aril, heteroaril, C(O)ORa4, C(O)Rb4, S(O)2Rb3,alkoksialkil, i alkoksialkoksi; ili Rc2 i Rd2 zajedno sa N atomom za kojisu spojeni formiraju heterocikloalkilnu grupu od 4-, 5-, 6- ili 7-članova iliheteroarilnu grupu, svaki opcionalno zamijenjen sa 1, 2, ili 3 supstituentanezavisno izabrnim 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, hidrohialkil, cianoalkil, aril,aril, heteroalkil, C(O)ORa4, C(O)Rb4, S(O)2Rb3,alkoksialkil,i alkoksialkoksi; Rc3 i Rd3 su nezavisno izabrani od H, C1-10 alkil, C1-6 haloalkil,C2-6 alkenil,C2-6 alkinil, aril, heteroaril, cikloalkil,heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil, pri čemu navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil,heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabrani od OH, CN,amino, halo, C1-6alkil, C1-6 alkoksi, C1-6 haloalkil,i C1-6 haloalkoksi; ili Rc3 i Rd3 zajedno sa N atomom za kojisu spojeni formiraju heterocikloalkilnu grupu od 4-, 5-, 6- ili 7-članova iliheteroarilnu grupu, svaki opcionalno zamijenjen sa 1, 2, ili 3 supstituentanezavisno izabranih od OH, CN, amino, halo, C1-6alkil, C1-6 alkoksi, C1-6haloalkil, i C1-6 haloalkoksiOH, CN, amino,halo, C1-6alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi; Rc4 i Rd4 sunezavisno izabrani od H, C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil,arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil, pričemu navedeni C1-10alkil, C1-6haloalkil, C2-6 alkenil, C2-6 alkinil,aril, heteroaril, cikloalkil,heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil je opcionalno zamijenjensa 1, 2, ili 3 supstituenta nezavisnoizabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil,i C1-6 haloalkoksi; ili Rc4 i Rd4 zajedno sa N atomom za koji su spojeniformiraju heterocikloalkilnu grupu od4-, 5-, 6- ili 7-člana ili heteroarilnu grupu, svaki opcionalno zamijenjen sa 1,2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi; Re, Re1, Re2, i Re4 sunezavisno izabrani od H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, (C1-6 alkoksi)-C1-6 alkil, C2-6 alkinil,aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, cikloalkilalkil,heteroarilalkil, i heterocikloalkilalkil; Rf, Rf1, Rf2, i Rf4 sunezavisno izabrani od H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6alkinil,aril, cikloalkil, heteroaril, i heterocikloalkil; Rg je H, CN, i NO2; Rh i Ri su nezavisno izabrani od H i C1-6 alkil; Rj je H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril,cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil; m je 1,ili 2; r je 0, 1, 2, 3, 4, 5, ili 6; s je 0, 1, 2, 3, ili 4; i t je0, 1, 2, 3, ili 4.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu (a) Cy1 je aril ili heteroaril, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W-X-Y-Z; (b) Cy1 je aril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W-X-Y-Z; (c) Cy1 je heteroaril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W-X-Y-Z; ili (d) Cy1 je hinolinil opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W-X-Y-Z, naročito hinolinil.
3. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu (a) Cy2 je aril ili heteroaril, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; (b) Cy2 je aril ili heteroaril, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’ pri čemu bar jedan od navedenih -W’-X’-Y’-Z’ je C(O)NRc2Rd2; (b) Cy2 je aril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; ili (d) Cy2 je heteroaril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5-W’-X’-Y’-Z’.
4. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu L1 je CH2 ili CH2CH2 ili cikloalkilen; ili pri čemu L1 je CH2 ili ciklopropilen.
5. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu L2 je (CR7R8)r.
6. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu L2 je (CR7R8)r i r je 0.
7. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva so, pri čemu L2 je (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t, (CR7R8)s-(arilen)-(CR7R8)t,(CR7R8)s-(heterocikloalkilen)-(CR7R8)t, ili (CR7R8)s-(heteroarilen)-(CR7R8)t, gdje je navedeni cikloalkilen, arilen, heterocikloalkilen, ili heteroarilen opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od Cy4, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1, i S(O)2NRc1Rd1.
8. Spoj prema patentnom zahtjev u 1, ili njegova farmaceutski prihvatljiva sol, pri čemu L2 je (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t, ili (CR7R8)s-(arilen)-(CR7R8)t, gdje navedeni cikloalkilen ili arilen, je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od Cy4, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1, i S(O)2NRc1Rd1.
9. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva so, pri čemu L2 je (CR7R8)s-(cikloalkilen)-(CR7R8)t ili (CR7R8)s-(arilen)-(CR7R8)t, gdje navedeni cikloalkilen ili arilen, je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabrani od Cy4, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1,NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRc1Rd1, S(O)2 Rb1, NRc1S(O)2 Rb1, i S(O)2 NRc1Rd1.
10. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu L2 je cikloalkilen ili arilen; naročito gdje L2 je arilen.
11. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu (a) Cy2 je aril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; (b) pri čemu Cy2 je heteroaril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; (c) Cy2 je cikloalkil opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; ili (d) pri čemu Cy2 je heterocikloalkil opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’.
12. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu R1 je H; ili pri čemu R2 je H; ili pri čemu R5 je H; ili pri čemu R7 je H; ili pri čemu R8 je H; ili pri čemu R9 je H.
13. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu -W-X-Y-Z je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, S(O)2NRc2Rd2, aril, cikloalkil, heteroaril, i heterocikloalkil, pri čemu navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil su opcionalno zamijenjeni sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabrani od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, Nrc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg) Nrc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2OR12, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, i S(O)2NRc2Rd2 ; naročito pri čemu -W-X-Y-Z je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, Nrc2C(O)Rb2, Nrc2C(O)NRc2Rd2, Nrc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg) NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, ili S(O)2NRc2Rd2 ; naročito pri čemu -W-X-Y-Z je halo, C1-6alkil, C1-6 haloalkil, CN, NO2, N3, ili ORa2; naročito pri čemu -W-X-Y-Z je ORa2; naročito pri čemu -W-X-Y-Z je metoksi.
14. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu -W'-X'-Y'-Z' je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, S(O)2NRc2Rd2, aril, cikloalkil, heteroaril, i heterocikloalkil, pri čemu navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil su opcionalno zamijenjeni sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabrani od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg) Nrc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, i S(O)2NRc2Rd2 ; naročito pri čemu -W'-X'-Y'-Z' je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, Nrc2C(O)Rb2, Nrc2C(O)NRc2Rd2, Nrc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg), NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, ili S(O)2NRc2Rd2; naročito pri čemu -W'-X'-Y'-Z' je halo, C1-6alkil, C1-6haloalkil, CN, NO2, N3, ORa2 ili C(O)Rc2RNd2 ; naročito pri čemu -W’-X’-Y’-Z’ je halo, C1-6 alkil, C1-6 haloalkil, CN, NO2, N3, ili ORa2, naročito pri čemu-W'-X'-Y'-Z' je halo ili C(O)NRc2Rd2.
15. Spoj prema pri čemu zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, sa formulom IIa:
16. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, sa formulom formulu III:
17. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, sa formulom VIII:
18. Spoj prema patentnom zahtjevu 1, izabrano od: N-{(1R)-1-[(Dimetilamino)karbonyl]-2-metilpropil}-4-[7-(1-hinolin-6-iletil)imidazo[1,2-b] [1,2,4]triazin-2il]benzamid 2-Fluoro-N-(trans-4-hidroksicikloheksil)-4-[7-(1-hinolin-6-iletil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamid; 2-Fluoro-N-metil-4-[7-(1-hinolin-6-iletil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamid; N-Ciklopropil-2-fluoro-4-[7-(1-hinolin-6-iletil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamid; 2-Fluoro-N-[1-(metoksimetil)ciklopropil]-4-[7-(1-hiinolin-6-iletil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamid, ili njegove farmaceutski prihvatljive soli.
19. Spoj, koji je 6-(4-Fluorofenil)-3-(4-metoksibenzil)imidazo[1,2-a]pirimidin ili njegova farmaceutski prihvatljiva sol.
20. Pripravak koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 19, ili njegovu farmaceutski prihvatljivu sol, i najmanje jedan farmaceutski prihvatljiv nosač.
21. Spoj prema bilo kojem od patentnih zahtjeva 1 do 19, ili njegova farmaceutski prihvatljiva sol, za upotrebu u metodi inhibiranja aktivnosti receptora ili ne-receptorske tirozin kinaze uključujući kontakt navedene kinaze sa spojem.
22. Spoj prema patentnom zahtjevu 21, pri čemu kinaza pripada Met, PDGFR, HER, FLK, Src, Abl, ili JAK potfamilijama; naročito pri čemu je navedena kinaza c-Met, Ron, PDGFR beta, c-kit, EGFR, HER2, KDR, flt-3, Src, Abl, Jak1, Jak2, ili Jak3 kinaza; naročito pri čemu je navedena kinaza c-Met.
23. Spoj prema bilo kojem od patentnih zahtjeva od 1 do 19, ili njegova farmaceutski prihvatljiva sol, za upotrebu u metodi inhibiranja HGF/c-Met kinaze signalnog puta u ćeliji, uključujući kontakt navedene ćelije sa spojem.
24. Spoj prema bilo kojem od patentnih zahtjeva od 1 do 19, ili njegova farmaceutski prihvatljiva sol, za upotrebu u metodi inhibiranja proliferativne aktivnosti ćelije koja obuhvata kontaktiranje navedene ćelije sa spojem prema bilo kojem od patentnih zahtjeva 1 do 19, ili njegove farmaceutski prihvatljive soli.
25. Spoj prema bilo kojem od patentnih zahtjeva od 1 do 19, ili njegova farmaceutski prihvatljiva sol za upotrebu u metodi inhibiranja rasta tumora kod pacijenta, ili za upotrebu u metodi inhibicije metastaze tumora kod pacijenta, uključujući davanje, navedenim pacijentima, terapijski efektivne količine spoja prema bilo kojem od patentnih zahtjeva 1 do 19, ili njegove farmaceutski prihvatljive soli.
26. Spoj prema bilo kojem od patentnih zahtjeva od 1 do 19, ili njegova farmaceutski prihvatljiva sol za upotrebu u metodi liječenja bolesti kod pacijenta, naznačen time, da bolest povezana sa disregulacijom HGF/c-MET signalizirajućeg puta, uključujući administriranje, kod navedenog pacijenta, terapijski efektivne količine spoja; naročito pri čemu je navedena bolest karcinom, ateroskleroza, plućna fibroza, renalna fibroza, i regeneracija, bolest jetre, alergijski poremećaj, upalna bolest, autoimuni poremećaj, cerebrovaskularna bolest, kardiovaskularna bolest ili stanje povezano sa transplantacijom organa.
27. Spoj prema bilo kojem od patentnih zahtjeva 1 do 19, ili njegova farmaceutski prihvatljiva sol za upotrebu u metodi liječenja raka kod pacijenta koja obuhvaća primjenu kod navedenog pacijenta terapijski efektivne količine spoja; naročito pri čemu (a) navedeni rak je rak, muskuloskeletni sarkom, sarkom mekog tkiva, ili hematopoetski malignitet; (b) navedeni rak je rak mokraćnog mjehura, rak dojke, rak grlića materice, holangiokarcinom, kolorektalni rak, rak jednjaka, rak želuca, rak glave i vrata, rak bubrega, rak jetre, rak pluća, nazofaringealni rak, rak jajnika, rak gušterače, rak prostate, rak tiroidne žlezde, osteosarkom, sinovijalni sarkom, rabdomiosarkom, MFH/fibrosarkom, lejomiosarkom, Kapošijev sarkom, multipli mijelom, limfom, leukemija T ćelija odraslih, akutna mijelogena leukemija, kronična mijeloidna leukemija, glioblastom, astrocitom, melanom, mezoteliom ili Vilmov tumor ili; (c) navedeni rak je karcinom pluća, rak jetre, rak želuca, glioblastom, rak dojke ili rak bubrega.
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