ME01507B - Imidazotriazini i imidazopirimidini kao inhibitori kinaze - Google Patents

Imidazotriazini i imidazopirimidini kao inhibitori kinaze

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ME01507B
ME01507B MEP-2013-35A MEP3513A ME01507B ME 01507 B ME01507 B ME 01507B ME P3513 A MEP3513 A ME P3513A ME 01507 B ME01507 B ME 01507B
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imidazo
quinolin
ylcyclopropyl
pyrimidin
benzamide
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Jincong Zhuo
Brian Metcalf
Meizhong Xu
Chunhong He
Colin Zhang
Ding-Quan Qian
David M Burns
Yunlong Li
Wenqing Yao
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Incyte Holdings Corp
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Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of ME01507B publication Critical patent/ME01507B/me

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Claims (66)

1.Spoj formule 1: ili njegova farmaceutski prihvatljiva sol ili njegov predlijek, naznačeni time da: A je N ili CR3; i (a) pri čemu, kada A je N; Cy1 je aril, heteroaril, cykloalkil, ili heterocikloalkil, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 -W-X-Y-Z; Cy2 je aril, heteroaril, cikloalkil, ili heterokicloalkil, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’; L1 je CH2, CH2CH2, cikloalkilen, O ili S L2 je (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t, (CR7R8)s-(arilen)-(CR7R8)t, (CR7R8)s-(heteroci- kloalkilen)-(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, or (CR7R8)sS(O)2NR9(CR7R8)t, pri čemu je navedeni cikloalkilen, arilen, heterocikloalkilen, ili heteroarilen izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od Cy4, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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; R1 je H ili ⎯W"-X"-Y"-Z"; R2 je H, 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; R3 je H, cikloalkil, aril, heterocikloalkil, heteroaril, 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 i S(O)2NRCRD; gdje je navedeni cikloalkil, aril, heterocikloalkil, heteroaril ili C1-6 alkil izborno zamijenjen s 1,2 ili 3 supstituenta nezavisno odabrana od Cy5, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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; ili R2 i ⎯L2-Cy2 su povezani zajedno kako bi formirali skupinu formule: pri čemu je prsten B fuzionirani arilni ili fuzionirani heteroarilni prsten, svaki izborno zamijenjen s 1, 2 ili 3 -W’-X’-Y’-Z’; R4 je nezavisno odabran od H, halo, OH, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 alkoksija, alkoksialkila, cianoalkila, heterocikloalkila, cikloalkila, C1-6 haloalkila, CN, i NO2; R7 i R8 su nezavisno odabrani od H, halo, OH, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 alkoksija, C1-6 haloalkila, CN i NO2; ili R7 i R8 zajedno s C atomom za koji su povezani formiraju 3, 4, 5, 6 ili 7-člani cikloalkilni ili heterocikloalkilni prsten, svaki izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od halo, OH, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 alkoksija, C1-6 haloalkila, CN i NO2; R9 je H, C1-6 alkila, C2-6 alkenila ili C2-6 alkinila; W, W’ i W" su nezavisno odsutni ili nezavisno odabrani od C1-6 alkilena, C2-6 alkenilena, C2-6 alkinilena, O, S, NRh, CO, COO, CONRh, SO, SO2, SONRh i NRhCONRi, pri čemu je svaki od C1-6 alkilena, C2-6 alkenilena i C2-6 alkinilena izborno zamijenjen s 1, 2 ili 3 supstituenta odabrana od halo, C1-6 alkila, C1-6 haloalkila, OH, C1-6 alkoksija, C1-6 haloalkoksija, amina, C1-6 alkilamina i C2-8 dialkilamina; X, X’ i X" su nezavisno odsutni ili nezavisno odabrani 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 i heterocikloalkilena je izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od halo, CN, NO2, OH, C1-6 alkila, C1-6 haloalkila, C2-8 alkoksialkila, C1-6 alkoksija, C1-6 haloalkoksija, C2-8 alkoksialkoksija, cikloalkila, heterocikloalkila, C(O)ORj, C(O)NRhRi, amina, C1-6 alkilamina i C2-8 dialkilamina; Y, Y’ i Y" su nezavisno odsutni ili nezavisno odabrani od C1-6 alkilena, C2-6 alkenilena, C2-6 alkinilena, O, S, NRh, CO, COO, CONRh, SO, SO2, SONRh, i NRhCONRi, pri čemu je svaki od C1-6 alkilena, C2-6 alkenilena i C2-6 alkinilena izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od halo, C1-6 alkila, C1-6 haloalkila, OH, C1-6 alkoksija, C1-6 haloalkoksija, amina, C1-6 alkilamina i C2-8 dialkilamina; Z, Z’ i Z" su nezavisno odabrani od H, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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(=NR9)NRc2Rd2, NRc2C(=NR9)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, arila, cikloalkila, heteroarila i heterocikloalkila, gdje su navedeni C1-6 *alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril i heterocikloalkil izborno zamijenjeni s 1, 2, 3, 4 ili 5 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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 s atomima s kojima su povezani, izborno formiraju fuzionirani cikloalkilni prsten od 4-20 članova ili fuzionirani heterocikloalkilni prsten od 4-20 članova, svaki izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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, arila, cikloalkila, heteroarila i heterocikloalkila; pri čemu dva susjedna ⎯W’-X’-Y’-Z’, zajedno s atomima s kojima su povezani, izborno formiraju fuzionirani cikloalkilni prsten od 4-20 članova ili spojeni heterocikloalkilni prsten od 4-20 članova, svaki izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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, arila, cikloalkila, heteroarila i heterocikloalkila; Cy4 i Cy5 su nezavisno odabrani od arila, cikloalkila, heteroarila i heterocikloalkila, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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)b4, 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 ili heteroaril gdje je navedeni C1-4 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, heterocikloalkil, aril ili heteroaril izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo i C1-4 alkila; RB je H, C1-4 alkil, C2-4 alkenil, C2-4 alkinil, cicloalkil, heterocikloalkil, aril, ili heteroaril gdje je navedeni C1-4 alkil, C2-4 alkenil, ili C2-4 alkinil, cikloalkil, heterocikloalkil, aril, ili heteroaril izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo i C1-4 alkila; RC i RD su nezavisno odabrana od H, C1-4 alkila, C2-4 alkenila, ili C2-4 alkinila, gdje je navedeni C1-4 alkil, C2-4 alkenil, ili C2-4 alkinil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo i C1-4 alkila; ili RC i RD zajedno s N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjenu s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo i C1-4 alkila; Ra, Ra1, Ra2, Ra3, i Ra4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila i heterocikloalkilalkila, gdje je navedeni C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Rb, Rb1, Rb2, Rb3 i Rb4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila i heterocikloalkilalkila, pri čemu je navedeni C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alknil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Rc i Rd su nezavisno odabrani od H, C1-10 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, heteroarila, cikloalkila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila ili heterocikloalkilalkila, pri čemu je navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkila; ili Rc i Rd zajedno s N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjenu s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Rc1 i Rd1 su nezavisno odabrani od H, C1-10 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, heteroarila, cicloalkila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila ili heterocikloalkilalkila, pri čemu je navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cicloalkilalkil ili heterocicloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila, i C1-6 haloalkoksija; ili Rc1 i Rd1 zajedno s N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjenu s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Rc2 i Rd2 su nezavisno odabrani od H, C1-10 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, heteroarila, cikloalkila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila, heterocikloalkilalkila, arilcikloalkila, arilheterocikloalkila, arilheteroarila, biarila, heteroarilcikloalkila, heteroarilheterocikloalkila, heteroarilarila i biheteroarila, pri čemu je 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 svaki izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila, C1-6 haloalkoksija, hidroksialkila, cianoalkila, arila, heteroarila, C(O)ORa4, C(O)Rb4, S(O)2Rb3,alkoksialkila i alkoksialkoksija; ili Rc2 ili Rd2 zajedno sa N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjenu s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila, C1-6 haloalkoksija, hidroksialkila, cianoalkila, arila, heteroarila, C(O)ORa4, C(O) Rb4, S(O)2Rb3, alkoksialkila i alkoksialkoksija; Rc3 i Rd3 su nezavisno odabrani od H, C1-10 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, heteroarila, cikloalkila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila ili heterocikloalkilalkila, pri čemu je navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksi; ili Rc3 i Rd3 zajedno s N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjenu s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Rc4 i Rd4 su nezavisno odabrani od H, C1-10 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, heteroarila, cikloalkila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila ili heterocikloalkilalkila, pri čemu je navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila, i C1-6 haloalkoksija; ili Rc4 i Rd4 zajedno sa N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Re, Re1, Re2 i Re4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, (C1-6 alkoksi)-C1-6 alkila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, cikloalkilalkila, heteroarilalkila i heterocikloalkilalkila; Rf, Rf1, Rf2 i Rf4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila i heterocikloalkila; Rg je H, CN i NO2; Rh i Ri su nezavisno odabrani od H i C1-6 alkila; Rj je H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil; r je 0, 1, 2, 3, 4, 5 ili 6; s je 0, 1, 2, 3 ili 4; i t je 0, 1, 2, 3 ili 4; i (b) pri čemu, kada je A CR3: L’ je cikloalkilen, O ili S; a sve druge varijable su definirane kao pod (a)
2.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da A jest N.
3.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da A jest CR3.
4.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da A jest CH.
5.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy1 jest aril ili heteroaril, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 -W-X-Y-Z.
6.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy1 jest aril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W-X-Y-Z.
7.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da Cy1 jest heteroaril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W-X-Y-Z.
8.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy1 jest kinonlinil izborno zamijenjen s 1, 2, 3, 4 ili 5 -W-X-Y-Z.
9.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy1 jest kinolinil.
10.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest aril ili heteroaril, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
11.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest aril ili heteroaril, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’ pri čemu najmanje jedan od navedenih -W’-X’-Y’-Z’ je C(O)NRc2Rd2.
12.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest aril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
13.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest heteroaril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
14.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L1 jest O ili S.
15.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L1 jest CH2 ili CH2CH2 ili cikloalkilen.
16.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L1 jest CH2 ili ciklopropilen.
17.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L1 jest cikloalkilen.
18.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L1 jest ciklopropilen.
19.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest (CR7R8)r.
20.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest (CR7R8)r i r je 0.
21.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest (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 izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od Cy4, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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)ORelORfi, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1, i S(O)2NRc1Rd1.
22.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t ili (CR7R8)-(arilen)-(CR7R8)t, gdje je navedeni cikloalkilen ili arilen izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od Cy4, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRclRad1, 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.
23.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest (CR7R8)s-(cikloalkilen)-(CR7R8)t ili (CR7R8)s-(arilen)-(CR7R8)t, gdje je navedeni cikloalkilen ili arilen izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od Cy4, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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)2 Rb1 i S(O)2NRc1Rd1.
24.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest cikloalkilen ili arilen.
25.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest arilen.
26.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest aril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
27.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest heteroaril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
28.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest cikloalkil izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
29.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest heterocikloalkil izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
30.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R1 jest H.
31.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R2 jest H.
32.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R3 jest H.
33.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R4 jest H.
34.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R7 jest H.
35.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R8 jest H.
36.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R9 jest H.
37.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da -W-X-Y-Z jest 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)ORe2ORf12, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, S(O)2NRc2Rd2, aril, cikloalkil, heteroaril i heterocicloalkil, pri čemu je navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril i heterocikloalkil izborno zamijenjen s 1, 2, 3, 4 ili 5 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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.
38.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da -W-X-Y-Z jest 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.
39.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da -W-X-Y-Z jest halo, C1-6 alkil, C1-6 haloalkil, CN, NO2, N3 ili ORa2.
40.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da –W-X-Y-Z jest ORa2.
41.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da –W-X-Y-Z jest metoksi.
42.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da – W’-X’-Y’-Z’ jest 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 je navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril i heterocikloalkil izborno zamijenjen sa 1, 2, 3, 4 ili 5 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, 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.
43.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da –W’-X’-Y’-Z’ jest 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.
44. Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da –W’-X’-Y’-Z’jest halo, C1-6 alkil, C1-6 haloalkil, CN, NO2, N3, ORa2 ili C(O)NRc2Rd2
45.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da -W’-X’-Y’-Z’ jest halo, C1-6 alkil, C1-6 haloalkil, CN, NO2, N3 ili ORa2.
46.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da -W’-X’-Y’-Z’ jest halo ili C(O)NRc2Rd2.
47.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da imaju formulu IIa ili IIb:
48.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da imaju formulu III:
49.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da imaju formulu VIII:
50.Spoj prema zahtjevu 1, naznačen time da je odabran od: 2-(4-fluorofenil)-7-(4-metoksibenzil)imidazo[1,2-b] [1,2,4]triazina; 2-(4-fluorofenil)-7-[1-(4-metoksifenil)ciklopropil]imidazo[1,2-b]-[1,2,4]-triazina; 6-(1-(2-(4-fluorofenil)imidazo[1,2-b][1,2,4]triazin-7-il)ciklopropil)kinolina; 6-(4-fluorofenil)-3-(4-metoksibenzil)imidazo[1,2-a]pirimidina; 6-(4-fluorofenil)-3-(1-(4-metoksifenil)ciklopropil)imidazo[1,2-a]pirimidina; 6-(1-(6-(4-fluorofenil)imidazo[1,2-a]pirimidin-3-il)ciklopropil)kinolina; 2-fluoro-N-metil-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-(4-bromo-3-fluorofenil)-7-[(4-metoksifenil)tio]imidazo[1,2-b][1,2,4]triazina; 2-fluoro-4-(3-[(4-metoksifenil)tio]imidazo[1,2-a]pirimidin-6-il)-N-metilbenzamida; 2-kloro-4-3-[(4-metoksifenil)tio]imidazo[1,2-a]pirimidin-6-il-N-metilbenzamida; 2-fluoro-N-metil-4-[3-(kinolin-6-ltio)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-N-metil-4-[3-(kinolin-6-iltio)imidazo[1,2-a]pirimidin-6-il]benzamida; metil-2-fluoro-4-[7-(kinolin-6-iltio)imidazo[1,2-b][1,2,4]triazin-2-il]benzoata; 2-(4-bromo-3-fluorofenil)-7-(4-metoksifenoksi)imidazo[1,2-b][1,2,4]triazina; 3-(4-metoksifenoksi)-6-(4-metil-1H-pirazol-1-il)imidazo[1,2-a]pirimidina; 6-(4-bromofenil)-3-(4-metoksifenoksi)imidazo[1,2-a]pirimidina; 2-kloro-N-metil-4-[3-(kinolin-6-iloksi)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-(4-bromofenil)-3-[(4-metoksifenil)tio]imidazo[1,2-a]pirimidina; 2-(4-fluorofenil)-7-[(4-metoksifenil)tio]imidazo[1,2-b][1,2,4]triazina; 6-(1-{6-[3-fluoro-4-(1-metil-2-okso-2-pirolidin-1-iletoksi)fenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 6-{1-[6-(1H-pirazol-1-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; 6-1-[6-(4-metil-1H-pirazol-1-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; N,N-dimetil-1-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-4-karboksamida; N-[1-(4-metil-1,3-tiazol-2-il)etil]-1-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-4-karboksamida; N-cikloheksil-3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-karboksamida; 3-(1-kinolin-6-ilciklopropil)-N-(tetrahidrofuran-2-ilmetil)imidazo[1,2-a]pirimidin-6-karboksamida; N-ciklobutil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-(1-{16-[4-(azetidin-1-ilkarbonil)fenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; N,N-dimetil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-N-(tetrahidrofuran-2-ilmetil)benzamida; N-(1-benzilpirolidin-3-il)-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(1-piridin-2-ilpiperidin-4-il)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(1-piridin-2-iletil)-4-[3-(1-kinolin-6-ilcilopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-{1-[6-(4-[(3S)-3-fluoropirolidin-1-il]karbonilfenil)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; N-[1-(metoksimetil)ciklobutil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(1-piridin-2-ilpirolidin-3-il)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-[1-(6-{4-[(3-piridin-2-ilpirolidin-1-il)karbonil]fenil}imidazo[1,2-a]pirimidin-3-il)ciklopropil]kinolina; 6-{1-[6-(4-[(3S)-3-(piridin-2-iloksi)pirolidin-1-il]karbonilfenil)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; N-[2-(piridin-2-iloksi)etil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[1-metil-2-(piridin-2-iloksi)etil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(2-fenoksietil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamid; N-(1S)-2,2-dimetil-1-[(metilamino)karbonil]propil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(1S)-1-[(dimetilamino)karbonil]-2,2-dimetilpropil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[(1S)-1-(azetidin-1-ilkarbonil)-2,2-dimetilpropil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-ciklopropil-3-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(piridin-2-ilmetil)-3-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N,N-dimetil-3-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-metil-3-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[(1S)-1-metil-2-(metilamino)-2-oksoetil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[(1R)-1-metil-2-(metilamino)-2-oksoetil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; (3R)-1-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzoil}pirolidin-3-karbonitrila; metil-4-{5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-il}-piperazin-1-karboksilata; 6-[1-(6-{6-[4-(metilsulfonil)piperazin-1-il]piridin-3-il}imidazo[1,2-a]pirimidin-3-il)ciklopropil]kinolina; N,N-dimetil-4-{5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-il}piperazin-1-karboksamida; N-(1S)-1-[(dimetilamino)karbonil]-2-metilpropil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-1-[(dimetilamino)karbonil]ciklobutil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[(1S)-1-(azetidin-1-ilkarbonil)-2,2-dimetilpropil]-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-karboksamida; N-(1S)-2,2-dimetil-1-[(metilamino)karbonil]propil-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-karboksamida; N-(1S)-1-[(ciklopropilamino)karbonil]-2,2-dimetilpropil-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-karboksamida; N-[(1S)-2-(dimetilamino)-1-metil-2-oksoetil]-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-karboksamida; N-[(1R)-2-(dimetilamino)-1-metil-2-oksoetil]-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-karboksamida; 6-(1-{6-[4-(2-okso-2-pirolidin-1-iletoksi)fenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 1-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}ciklopropankarbonitrila; N,N-dimetil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzensulfonamida; metil-2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzilkarbamata; N’-2-fluoro-4[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzil-N,N-dimetiluree; (3R)-1-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzil}pirolidin-3-ola; 6-(1-{6-[3-fluoro-4-(1H-pirazol-1-ilmetil)fenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 3-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzil}-1,3-oksazolidin-2-ona; 2-fluoro-N-metil-4-[7-(kinoksalin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 6-{1-[6-(4-kloro-1H-pirazol-1-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; 6-{1-[6-(2-metil-1,3-tiazol-4-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil} kinolina; 6-{1-[6-(1,3-tiazol-4-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; 3-fluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; (3S)-1-{3-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzoil}pirolidin-3-ola; 2,5-difluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2,5-difluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-ciklopropil-2,5-difluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2,5-difluoro-N-(trans-4-hidroksicikloheksil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 1-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}pirolidin-2-ona; 3-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-1,3-oksazolidin-2-ona; etil-4-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-1-il}piperidin-1-karboksilata; 2-(4-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-1H-pirazol-1-il)-N,N-dimetilacetamida; 5-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-N-metilpiridin-2-karboksamida; 5-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-N,N-dimetilpiridin-2-karboksamida; 6-(1-{6-[3-fluoro-4-(1-metil-1H-pirazol-4-il)fenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 6-(1-{6-[1-(fetrahidrofuran-3-il)-1H-pirazol-4-il]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 6-(1-{6-[1-(1-benzilpirolidin-3-il)-1H-pirazol-4-il]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 6-{1-[6-(1-metil-1H-pirazol-4-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; N,N-dimetil-4-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-1-il}piperidin1-karboksamida; 4-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-1-il}cikloheksanola; {4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-1-il} acetonitrila; N-metil-5-{4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]fenil}piridin-2-karboksamida; 6-{1-[2-(4-pirimidin-5-il-fenil)imidazo[1,2-b][1,2,4]triazin-7-il]ciklopropil}kinolina; 6-(1-{2-[4-(1-acetil-1,2,3,6-tetrahidropiridin-4-il)fenil]imidazo[1,2-b][1,2,4]triazin-7-il}ciklopropil)kinolina; 6-[1-(2-(4-[1-(metilsulfonil)-1,2,3,6-tetrahidropiridin-4-il]fenil}imidazo[1,2-b][1,2,4]triazin-7-il)ciklopropil]kinolina; N,N-dimetil-5-{4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]fenil}piridin-2-karboksamida; 6-(1-{2-[4-(1H-imidazol-1-il)fenil]imidazo[1,2-b][1,2,4]triazin-7-il}ciklopropil)-kinolina; 2-fluoro-N-(trans-4-hidroksicikloheksil)-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-ciklopropil-2-fluoro-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-metil-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[1-(metoksimetil)ciklopropil]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-4-(7-(1-(kinolin-6-il)ciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il)benzamida; 4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]-N-(tetrahidrofuran-2-ilmetil)benzamida; N-(piridin-2-ilmetil)-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-ciklopropil-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-ciklobutil-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-(1-piridin-2-ilciklopropil)-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-(2-hidroksi-1,1-dimetiletil)-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[(1S)-1-benzil-2-hidroksietil]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; (3R)-1-{4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzoil}pirolidin-3-ola; 4-(7-(1-(kinolin-6-il)ciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il)-N-(tetrahidro-2H-piran-4-il)benzamida; N-ciklopropil-N-metil-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[1-(metoksimetil)ciklopropil]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[1-(metoksimetil)ciklobutil]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[(1S)-1-(metoksimetil)-2-metilpropil]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[4-(metoksimetil)tetrahidro-2H-piran-4-il]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]-N-1,3-tiazol-2-ilbenzamida; N-pirimidin-4-il-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[4-(metoksimetil)tetrahidro-2H-piran-4-il]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-ciklopropil-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[1-(metoksimetil)ciklopropil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-N-(tetrahidro-2H-piran-4-il)benzamida; (3R)-1-{2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzoil}pirolidin-3-ola; 2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(trans-4-hidroksicikloheksil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 6-{2-[3-fluoro-4-(1H-imidazol-1-il)fenil]imidazo[1,2-b][1,2,4]triazin-7-ilmetil}kinolina; 3-{2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]fenil}-1,3-oksazolidin-2-ona; N-(1S)-2,2-dimetil-1-[(metilamino)karbonil]propil-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-(1S)-1-[(dimetilamino)karbonil]-2,2-dimetilpropil-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b] [1,2,4]triazin-2-il]benzamida; N-[(1S)-1-(azetidin-1-ilkarbonil)-2,2-dimetilpropil]-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-{(1S)-1-[(dimetilamino)karbonil]-3-metilbutil-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-{(1R)-3-metil-1-[(metilamino)karbonil]butil}-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-{(1R)-1-[(dimetilamino)karbonil]-3-metilbutil}-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[(1R)-1-(azetidin-1-ilkarbonil)-3-metilbutil]-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4] triazin-2-il]benzamida; 3-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-il} propanenitrila; 4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-ilacetonitrila; 2-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-il}acetamida; metil-4-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-il}piperidin-1-karboksilata; 2-fluoro-N-[(1S,2S)-2-hidroksiciklopentil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(2-hidroksietil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[1-(metoksimetil)ciklobutil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[4-(metoksimetil)tetrahidro-2H-piran-4-il]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-(ciklopropilmetil)-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-N-(tetrahidro-2H-piran-4-ilmetil)benzamida; N-[2-(dimetilamino)etil]-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(2-piperidin-1-iletil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[2-(1-metilpirolidin-2-il)etil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(piridin-2-ilmetil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(piridin-3-ilmetil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(piridin-4-ilmetil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(2-piridin-2-iletil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b] [1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(1-piridin-3-iletil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(1-piridin-4-iletil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[(1S)-1-(hidroksimetil)-2,2-dimetilpropil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[1-(hidroksimetil)ciklopentil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(2-metoksi-1-metiletil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-{1-[6-(3-fluoro-4-[(3S)-3-fluoropirolidin-1-il]karbonilfenil)imidazo[1,2-a]pirimidin-3-il]ciklopropil} kinolina; 2-fluoro-N-(piridin-2-ilmetil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-(1-piridin-2-ilciklopropil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-(1-piridin-2-ilpirolidin-3-il)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-N-[(3R)-tetrahidrofuran-3-il]benzamida; 2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-N-(tetrahidrofuran-2-ilmetil)benzamida; N-ciklopropil-2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-[(1S)-1-(metoksimetil)-2-metilpropil]-4-[3-(1-kinolin-6-ilcklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-metil-N-2-[metil(piridin-2-il)amino]etil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-N-ciklopropil-4[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-N-(tetrahidrofuran-3-il)benzamida; 2-kloro-N-(1-piridin-2-iletil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-(1-{6-[4-(Azetidin-1-ilkarbonil)-3-klorofenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 2-kloro-N-(1-piridin-2-ilpirolidin-3-il)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-N-[1-metil-2-(piridin-2-iloksi)etil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-N-(1S)-1-[(dimetilamino)karbonil]-2-metilpropil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-ciklopropil-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]izoindolin-1-ona; 2-etil-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]izoindolin-1-ona; 2-(2-metoksi-1-metiletil)-S-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]izoindolin-1 -ona; 2-(piridin-2-ilmetil)-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]izoindolin-1-ona; 2-metil-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]izoindolin-1-ona; N-etil-1-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}ciklopropankarboksamida; N-(1-piridin-2-iletil)-1-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}ciklopropankarboksamida; N-[1-metil-2-(piridin-2-iloksi)etil]-1-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}ciklopropankarboksamida; 2-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-2-hidroksi-N-metilacetamida; 2-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-2-hidroksi-N,N-dimetilacetamida; N-(3-[2-(4-bromo-3-fluorofenil)imidazo[1,2-b][1,2,4]triazin-7-il]metilfenil)-N’-etiluree; 2-(2,3-dihlorofenil)-7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-3-amina; 2,3-difluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-difluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzensulfonamida; N,N-dimetil-2-{3-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-1-il}acetamida; N-[(1S)-1-(azetidin-1-ilkarbonil)-2,2-dimetilpropil]-2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[2-(dimetilamino)-1-metil-2-oksoetil]-2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(2-azetidin-1-il-1-metil-2-oksoetil)-2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-2-[(3R)-3-metoksipirolidin-1-il]-1-metil-2-oksoetil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-[(1-hidroksiciklopropil)metil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; metil-4-(cijanometil)-4-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-il}piperidin-1-karboksilata; etil-4-(cijanometil)-4-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-il}piperidin-1-karboksilata; (1-acetil-4-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b] [1,2,4]triazin-2-il]-1H-pirazol-1-il}piperidin-4-il)acetonitrila, ili njihovih farmaceutski prihvatljivih soli.
51.Spoj prema zahtjevu 1, naznačen time da je 2-fluoro-N-metil-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamid ili njegova farmaceutski prihvatljiva sol.
52.Sastav, naznačen time da sadrži spoj bilo kojeg zahtjeva od 1 do 51 ili njegovu farmaceutski prihvatljivu sol i najmanje jedan farmaceutski prihvatljivi nosač.
53.Sastav, naznačen time da sadrži spoj prema zahtjevu 51 ili njegovu farmaceutski prihvatljivu sol i najmanje jedan farmaceutski prihvatljivi nosač.
54.Metoda inhibiranja aktivnosti receptorske ili nereceptorske tirozin-kinaze ex vivo, naznačena time da uključuje dovođenje navedene kinaze u kontakt sa spojem iz bilo kojeg zahtjeva od 1 do 51 ili njegovom farmaceutski prihvatljivom soli.
55.Metoda prema zahtjevu 54, naznačena time da navedena kinaza pripada podfamiliji Met, PDGFR, HER, FLK, Src, Abl ili Jak.
56.Metoda prema zahtjevu 54, naznačena time da je navedena kinaza c-Met, Ron, PDGFR beta, c-kit, EGFR, HER2, KDR, flt-3, Src, Abl, Jak1, Jak2 ili Jak 3 kinaza.
57.Metoda prema zahtjevu 54, naznačena time da je navedena kinaza c-Met.
58.Metoda inhibiranja signalnog puta HGF/c-Met kinaze u stanici ex vivo, naznačena time da uključuje dovođenje navedene stanice u kontakt sa spojem iz bilo kojeg zahtjeva od 1 do 51 ili njegovom farmaceutski prihvatljivom soli.
59.Metoda inhibiranja proliferativne aktivnosti stanice ex vivo, naznačena time da uključuje dovođenje navedene stanice u kontakt sa spojem iz bilo kojeg zahtjeva od 1 do 51 ili njegovom farmaceutski prihvatljivom soli.
60.Spoj prema bilo kojem zahtjevu od 1 do 51 ili njegova farmaceutski prihvatljiva sol, naznačeni time da se upotrebljavaju u inhibiciji rasta tumora kod pacijenata.
61.Spoj prema bilo kojem zahtjevu od 1 do 51 ili njegova farmaceutski prihvatljiva sol, naznačeni time da se upotrebljavaju u inhibiciji metastaze tumora kod pacijenata.
62.Spoj prema bilo kojem zahtjevu od 1 do 51 ili njegova farmaceutski prihvatljiva sol, naznačeni time da se upotrebljavaju u liječenju bolesti kod pacijenta, gdje je navedena bolest povezana s nepravilnom regulacijom signalnog puta HGF/c-MET.
63.Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 62, naznačeni time da se upotrebljavaju u liječenju bolesti pri čemu je navedena bolest rak, 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.
64.Spoj prema bilo kojem zahtjevu od 1 do 51 ili njegova farmaceutski prihvatljiva sol, naznačeni time da se upotrebljavaju u liječenju raka kod pacijenta.
65.Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 64, naznačeni time da se upotrebljavaju u liječenju raka pri čemu je navedeni rak karcinom, mišićnokoštani sarkom, sarkom mekog tkiva ili hematopoetski malignitet.
66.Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 64, naznačeni time da se upotrebljavaju u liječenju raka pri čemu je navedeni rak rak mokraćnog mjehura, rak dojke, rak grlića materice, kolangiokarcinom, rak debelog crijeva, rak jednjaka, rak želuca, rak glave i vrata, rak bubrega, rak jetre, rak pluća, nazofaringealni rak, rak jajnika, rak pankreasa, rak prostate, rak štitne žlijezde, osteosarkom, sinovijalni sarkom, rabdomiosarkom, MFH/fibrosarkom, leiomiosarkom, Kaposijev sarkom, multipli mijelom, limfom, leukemija odraslih T stanica, akutna mijelogena leukemija, kronična mijeloična leukemija, glioblastom, astrocitom, melanom, mezoteliom ili Wilmsov tumor. 1
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HUS2200052I1 (hu) 2023-01-28
US20180282340A1 (en) 2018-10-04
EA201691862A3 (ru) 2017-12-29
CL2007003341A1 (es) 2008-04-18

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