HRP20192102T1 - Benzopirazini protiv raka putem inhibicije fgfr kinaza - Google Patents

Benzopirazini protiv raka putem inhibicije fgfr kinaza Download PDF

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HRP20192102T1
HRP20192102T1 HRP20192102TT HRP20192102T HRP20192102T1 HR P20192102 T1 HRP20192102 T1 HR P20192102T1 HR P20192102T T HRP20192102T T HR P20192102TT HR P20192102 T HRP20192102 T HR P20192102T HR P20192102 T1 HRP20192102 T1 HR P20192102T1
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6alkyl
substituted
alkyl
4alkyl
cancer
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HRP20192102TT
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Steven John Woodhead
Christopher William Murray
Valerio Berdini
Gordon Saxty
Gilbert Ebai Besong
Lieven Meerpoel
Oliver Alexis Georges Querolle
Virginie Sophie Poncelet
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Astex Therapeutics Ltd.
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Claims (16)

1. Spoj formule (I) uključujući njegov bilo koji tautomerski ili stereokemijski izomerski oblik, pri čemu W je -N(R3)- ili -C(R3aR3b)-; svaki R2 je neovisno odabran od hidroksila, halogena, cijano, C1-4alkila, C2-4alkenila, C2-4alkinila, C1-4alkoksi, hidroksiC1-4alkila, hidroksiC1-4alkoksi, haloC1-4alkila, haloC1-4alkoksi, hidroksihaloC1-4alkila, hidroksihaloC1-4aloksi, C1-4aloksiC1-4alkila, haloC1-4alkoksiC1-4alkila, C1-4alkoksiC1-4alkila pri čemu svaki C1-4alkil može izborno biti supstituiran s jednom ili dvije hidroksilne skupine, hidroksihaloC1-4alkoksiC1-4alkila, R13, C1-4alkila supstituiranog s R13, C1-4alkila supstituiranog s -C(=O)-R13, C1-4alkoksi supstituiranog s R13, C1-4alkoksi supstituiranog s -C(=O)-R13, -C(=O)-R13, C1-4alkila supstituiranog s -NR7R8, C1-4alkila supstituiranog s -C(=O)-NR7R8, C1-4alkoksi supstituiranog s -NR7R8, C1-4alkoksi supstituiranog s -C(=O)-NR7R8, -NR7R8 i -C(=O)-NR7R8; ili kada su dvije R2 skupine vezane na susjedni atom ugljika mogu biti uzete skupa kako bi tvorile radikal formule: - O-(C(R17)2)p-O-; - X-CH=CH-; ili - X-CH=N-; pri čemu R17 predstavlja vodik ili fluorin, p predstavlja 1 ili 2 i X predstavlja O ili S; Y predstavlja -CR18=N-OR19 ili-E-D; E predstavlja vezu, -(CR22R23)n-, C2-4alkendiil izborno supstituiran s R22, C2-4alkindiil izborno supstituiran s R22, -CO-(CR22R23)s-, -(CR22R23)s-CO-, -NR22-(CR22R23)s-, -(CR22R23)s-NR22-, -O-(CR22R23)s-, -(CR22R23)s-O-, -S(O)m-(CR22R23)s-,-(CR22R23)s-S(O)m-, -(CR22R23)s-CO-NR22-(CR22R23)s ili -(CR22R23)s-NR22-CO-(CR22R23)s-; D predstavlja 3 do 12-eročlani monociklični ili biciklični prsten karbociklila ili 3 do 12-eročlani monociklični ili biciklični prsten heterociklila koji sadrži barem jedan heteroatom odabran od N, O ili S, pri čemu spomenuti karbociklil i heterociklil mogu svaki biti izborno supstituirani s jednom ili više (npr. 1, 2 ili 3) R1 skupina; pod uvjetom da kada Y predstavlja -E-D, i E predstavlja vezu, tada D ne predstavlja pri čemu R1' predstavlja vodik, C1-6alkil, C2-4alkenil, hidroksiC1-6alkil, haloC1-6alkil, hidroksihaloC1-6alkil, cijanoC1-4alkil, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može biti izborno supstituiran s jednom ili dvije hidroksilne skupine, C1-6alkil supstituiran s -NR4R5, C1-6alkil supstituiran s -C(=O)-NR4R5, -S(=O)2-C1-6alkil, -S(=O)2haloC1-6alkil, -S(=O)2NR14R15, C1-6alkil supstituiran s -S(=O)2-C1-6alkil, C1-6alkil supstituiran s -S(=O)2haloC1-6alkil, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s –NH-S(=O)2-C1-6alkil, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkil, C1-6alkil supstituiran s –NR12-S(=O)2NR14R15, R6, C1-6alkil supstituiran s R6, C1-6alkil supstituiran s -C(=O)-R6, hidroksiC1-6alkil supstituiran s R6, C1-6alkil supstituiran s -Si(CH3)3, C1-6alkil supstituiran s -P(=O)(OH)2 ili C1-6alkil supstituiran s -P(=O)(OC1-6alkil)2; i svaki R1a je neovisno odabran od vodika, C1-4alkila, hidroksiC1-4alkila, C1-4alkila supstituiranog s amino ili mono- ili di(C1-4alkil)amino ili -NH(C3-8cikloalkil), cijanoC1-4alkila, C1-4alkoksiC1-4alkila, i C1-4alkila supstituiranog s jednim ili više fluoro atoma; R1 predstavlja vodik, halo, cijano, C1-6alkil, C1-6alkoksi, -C(=O)-O- C1-6alkil, C2-4alkenil, hidroksiC1-6alkil, haloC1-6alkil, hidroksihaloC1-6alkil, cijanoC1-4alkil, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može izborno biti supstituiran s jednom ili dvije hidroksilne skupine, -NR4R5, C1-6alkil supstituiran s -O-C(=O)- C1-6alkilom, C1-6alkil supstituiran s -NR4R5, -C(=O)-NR4R5, -C(=O)-C1-6alkil-NR4R5, C1-6alkil supstituiran s -C(=O)-NR4R5, -S(=O)2-C1-6alkil, -S(=O)2-haloC1-6alkil, -S(=O)2-NR14R15, C1-6alkil supstituiran s -S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -S(=O)2-haloC1-6alkilom, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s -NH-S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkilom, C1-6alkil supstituiran s -NR12-S(=O)2-NR14R15, R6, C1-6alkil supstituiran s R6, -C(=O)-R6, C1-6alkil supstituiran s - C(=O)-R6, hidroksiC1-6alkil supstituiran s R6, C1-6alkil supstituiran s -Si(CH3)3, C1-6alkil supstituiran s -P(=O)(OH)2 ili C1-6alkil supstituiran s -P(=O)(OC1-6alkil)2, R3a predstavlja -NR10R11, hidroksil, C1-6alkoksi, hidroksiC1-6alkoksi, C1-6alkoksi supstituiran s -NR10R11, C1-6alkilom, C2-6alkenil, C2-6alkinil, haloC1-6alkil izborno supstituiran s -O-C(=O)-C1-6alkilom, hidroksiC1-6alkil izborno supstituiran s -O-C(=O)-C1-6alkilom, hidroksiC2-6alkenil, hidroksiC2-6alkinil, hidroksihaloC1-6alkil, cijanoC1-6alkil, C1-6alkil supstituiran s karboksilom, C1-6alkil supstituiran s -C(=O)-C1-6alkilom, C1-6alkil supstituiran s -C(=O)-O-C1-6alkilom, C1-6alkil supstituiran s C1-6alkoksiC1-6alkil-O-C(=O)-, C1-6alkil supstituiran s C1-6alkoksiC1-6alkil-C(=O)-, C1-6alkil supstituiran s -O-C(=O)-C1-6alkilom, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može izborno biti supstituiran s jednom ili više hidroksilnih skupina ili s -O-C(=O)-C1-6alkilom, C2-6alkenil supstituiran s C1-6alkoksi, C2-6alkinil supstituiran s C1-6alkoksi, C1-6alkil supstituiran s R9 i izborno supstituiran s -O-C(=O)-C1-6alkilom, C1-6alkil supstituiran s -C(=O)-R9, C1-6alkil supstituiran s hidroksilom i R9, C2-6alkenil supstituiran s R9, C2-6alkinil supstituiran s R9, C1-6alkil supstituiran s -NR10R11, C2-6alkenil supstituiran s-NR10R11, C2-6alkinil supstituiran s -NR10R11, C1-6alkil supstituiran s hidroksilom i -NR10R11, C1-6alkil supstituiran s jednim ili dva halogena i -NR10R11, -C1-6alkil-C(R12)=NO-R12, C1-6alkil supstituiran s -C(=O)-NR10R11, C1-6alkil supstituiran s-O-C(=O)-NR10R11, -S(=O)2-C1-6alkil, -S(=O)2-haloC1-6alkil, -S(=O)2-NR14R15, C1-6alkil supstituiran s -S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -S(=O)2haloC1-6alkilom, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s -NR12-S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkilom, C1-6alkil supstituiran s NR12-S(=O)2-NR14R15, R13, C1-6alkil supstituiran s -P(=O)(OH)2 ili C1-6alkil supstituiran s -P(=O)(OC1-6alkil)2; R3b predstavlja vodik ili hidroksil; pod uvjetom da ako R3a predstavlja -NR10R11, tada R3b predstavlja vodik; ili R3a i R3b su uzeti skupa kako bi tvorili =O, kako bi tvorili =NR10, kako bi tvorili ciklopropil skupa s atomom ugljika na kojeg su vezani, kako bi tvorili=CH-C0-4alkil supstituiran s R3c, ili kako bi tvorili pri čemu je prsten A monociklični 5 do 7-eročlani zasićeni heterocikl koji sadrži jedan heteroatom odabran od N, O ili S, spomenuti heteroatom nije smješten u alfa poziciju duple veze, pri čemu je prsten A izborno supstituiran s cijano, C1-4alkilom, hidroksiC1-4alkilom, H2N-C1-4alkilom, (C1-4alkil)NH-C1-4alkilom, (C1-4alkil)2N-C1-4alkilom, haloC1-4alkil)NH-C1-4alkilom, C1-4alkoksiC1-4alkilom, -C(=O)-NH2, - C(=O)-NH(C1-4alkil), -C(=O)-N(C1-4alkil)2; R3c predstavlja vodik, hidroksil, C1-6alkoksi, R9, -NR10R11, cijano, -C(=O)-C1-6alkil ili -CH(OH)- C1-6alkil; R3 predstavlja hidroksil, C1-6alkoksi, hidroksiC1-6alkoksi, C1-6alkoksi supstituiran s - NR10R11, C1-6alkil, C2-6alkenil, C2-6alkinil, haloC1-6alkil izborno supstituiran s -O-C(=O)-C1-6alkilom, hidroksiC1-6alkil izborno supstituiran s -O-C(=O)-C1-6alkilom, hidroksiC2-6alkenil, hidroksiC2-6alkinil, hidroksihaloC1-6alkil, cijanoC1-6alkil, C1-6alkil supstituiran s karboksilom, C1-6alkil supstituiran s -C(=O)-C1-6alkilom, C1-6alkil supstituiran s -C(=O)-O-C1-6alkilom, C1-6alkil supstituiran s C1-6alkoksiC1-6alkil-O-C(=O)-, C1-6alkil supstituiran s C1-6alkoksiC1-6alkil-C(=O)-, C1-6alkil supstituiran s -O-C(=O)-C1-6alkilom, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može izborno biti supstituiran s jednom ili dvije hidroksilne skupine ili s -O-C(=O)-C1-6alkilom, C2-6alkenil supstituiran s C1-6alkoksi, C2-6alkinil supstituiran s C1-6alkoksi, C1-6alkil supstituiran s R9 i izborno supstituiran s -O-C(=O)-C1-6alkilom, C1-6alkil supstituiran s -C(=O)-R9, C1-6alkil supstituiran s hidroksilom i R9, C2-6alkenil supstituiran s R9, C2-6alkinil supstituiran s R9, C1-6alkil supstituiran s -NR10R11, C2-6alkenil supstituiran s -NR10R11, C2-6alkinil supstituiran s -NR10R11, C1-6alkil supstituiran s hidroksilom i -NR10R11, C1-6alkil supstituiran s jednim ili dva halogena i -NR10R11, -C1-6alkil-C(R12)=NO-R12, C1-6alkil supstituiran s -C(=O)-NR10R11, C1-6alkil supstituiran s -O-C(=O)-NR10R11, -S(=O)2-C1-6alkil, -S(=O)2-haloC1-6alkil, -S(=O)2-NR14R15, C1-6alkil supstituiran s -S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -S(=O)2-haloC1-6alkilom, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s -NR12-S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkilom, C1-6alkil supstituiran s -NR12-S(=O)2-NR14R15, R13, C1-6alkil supstituiran s -P(=O)(OH)2 ili C1-6alkil supstituiran s -P(=O)(OC1-6alkil)2; R4 i R5 svaki neovisno predstavljaju vodik, C1-6alkil, C1-6alkil supstituiran s -NR14R15, hidroksiC1-6alkil, haloC1-6alkil, hidroksihaloC1-6alkil, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može izborno biti supstituiran s jednom ili dvije hidroksilne skupine,-S(=O)2-C1-6alkil, -S(=O)2-haloC1-6alkil, -S(=O)2-NR14R15, -C(=O)-NR14R15, -C(=O)-O-C1-6alkil, -C(=O)-R13, C1-6alkil supstituiran s -S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -S(=O)2-haloC1-6alkilom, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s –NH-S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkilom, C1-6alkil supstituiran s –NH-S(=O)O2-NR14R15, R13 ili C1-6alkil supstituiran s R13; R6 predstavlja C3-8cikloalkil, C3-8cikloalkenil, fenil, 4 do 7-eročlani monociklični heterociklil koji sadrži barem jedan heteroatom odabran od N, O ili S; spomenuti C3-8cikloalkil, C3-8cikloalkenil, fenil, 4 do 7-eročlani monociklični heterociklil, izborno i svaki neovisno mogu biti supstituirani s 1, 2, 3, 4 ili 5 supstituenata, svaki supstituent neovisno je odabran od cijano, C1-6alkila, cijanoC1-6alkila, hidroksila, karboksila, hidroksiC1-6alkila, halogena, haloC1-6alkila, hidroksihaloC1-6alkila, C1-6alkoksi, C1-6alkoksiC1-6alkila, C1-6alkil-OC(=O)-, -NR14R15, -C(=O)-NR14R15, C1-6alkil supstituiran s -NR14R15, C1-6alkil supstituiran s -C(=O)-NR14R15, -S(=O)2-C1-6alkil, -S(=O)2-haloC1-6alkil, -S(=O)2-NR14R15, C1-6alkil supstituiran s -S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -S(=O)2-haloC1-6alkilom, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s -NH-S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkilom ili C1-6alkil supstituiran s -NH-S(=O)2-NR14R15; R7 i R8 svaki neovisno predstavljaju vodik, C1-6alkil, hidroksiC1-6alkil, haloC1-6alkil, hidroksihaloC1-6alkil ili C1-6alkoksiC1-6alkil; R9 predstavlja C3-8cikloalkil, C3-8cikloalkenil, fenil, naftil, ili 3 do 12-eročlani monociklični ili biciklični heterociklil koji sadrži barem jedan heteroatom odabran od N, O ili S, spomenuti C3-8cikloalkil, C3-8cikloalkenil, fenil, naftil, ili 3 do 12-eročlani monociklični ili biciklični heterociklil svaki izborno i svaki neovisno su supstituirani s 1, 2, 3, 4 ili 5 supstituenata, svaki supstituent izborno je odabran od =O, C1-4alkila, hidroksila, karboksila, hidroksiC1-4alkila, cijano, cijanoC1-4alkila, C1-4alkil-O-C(=O)-, C1-4alkil supstituiran s C1-4alkil-O-C(=O)-, C1-4alkil-C(=O)-, C1-4alkoksiC1-4alkil pri čemu svaki C1-4alkil može izborno biti supstituiran s jednom ili dvije hidroksilne skupine, halogen, haloC1-4alkil, hidroksihaloC1-4alkil, -NR14R15, -C(=O)-NR14R15, C1-4alkil supstituiran s -NR14R15, C1-4alkil supstituiran s -C(=O)-NR14R15, C1-4alkoksi, -S(=O)2-C1-4alkil, -S(=O)2-haloC1-4alkil, -S(=O)2-NR14R15, C1-4alkil supstituiran s - S(=O)2-NR14R15, C1-4alkil supstituiran s -NH-S(=O)2-C1-4alkilom, C1-4alkil supstituiran s -NH-S(=O)2-haloC1-4alkilom, C1-4alkil supstituiran s -NH-S(=O)2-NR14R15, R13, - C(=O)-R13, C1-4alkil supstituiran s R13, fenil izborno supstituiran s R16, fenilC1-6alkil pri čemu je fenil izborno supstituiran s R16, 5 do 6-eročlani aromatski monociklični heterociklil koji sadrži barem jedan heteroatom odabran od N, O ili S pri čemu je spomenuti heterociklil izborno supstituiran s R16; ili kada su dva od supstituenata R9 vezana na isti atom, mogu biti uzeti skupa kako bi tvorili 4 do 7-eročlani zasićeni monociklični heterociklil koji sadrži barem jedan heteroatom odabran od N, O ili S; R10 i R11 svaki neovisno predstavljaju vodik, karboksil, C1-6alkil, cijanoC1-6alkil, C1-6alkil supstituiran s -NR14R15, C1-6alkil supstituiran s -C(=O)-NR14R15, haloC1-6alkil, hidroksiC1-6alkil, hidroksihaloC1-6alkil, C1-6alkoksi, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može izborno biti supstituiran s jednom ili dvije hidroksilne skupine, R6, C1-6alkil supstituiran s R6 , -C(=O)-R6, -C(=O)-C1-6alkil, -C(=O)-hidroksiC1-6alkil, -C(=O)-haloC1-6alkil,-C(=O)-hidroksihaloC1-6alkil, C1-6alkil supstituiran s -Si(CH3)3, -S(=O)2-C1-6alkil, -S(=O)2-haloC1-6alkil, -S(=O)2-NR14R15, C1-6alkil supstituiran s -S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -S(=O)2-haloC1-6alkilom, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s -NH-S(=O)2-C1-6alkilom, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkilom, C1-6alkil supstituiran s karboksilom, ili C1-6alkil supstituiran s-NH-S(=O)2-NR14R15; R12 predstavlja vodik ili C1-4alkil izborno supstituiran s C1-4alkoksi; R13 predstavlja C3-8cikloalkil ili zasićeni 4 do 6-eročlani monociklični heterociklil koji sadrži barem jedan heteroatom odabran od N, O ili S, pri čemu spomenuti C3-8cikloalkil ili monociklični heterociklil su izborno supstituirani s 1, 2 ili 3 supstituenata svaki izborno odabran od vodika, hidroksila, C1-6alkila, haloC1-6alkila, =O, cijano, - C(=O)-C1-6alkila, C1-6alkoksi, ili -NR14R15; R14 i R15 svaki neovisno predstavljaju vodik, ili haloC1-4alkil, ili C1-4alkil izborno supstituiran sa supstituentom odabranim od hidroksila, C1-4alkoksi, amino ili mono-ili di(C1-4alkil)amino; R16 predstavlja hidroksil, halogen, cijano, C1-4alkil, C1-4alkoksi, -NR14R15 ili -C(=O)NR14R15; R18 predstavlja vodik, C1-6 alkil, C3-8 cikloalkil, C1-4alkil supstituiran s C3-8 cikloalkilom; R19 predstavlja vodik; C1-6 alkil; C3-8 cikloalkil; C1-6alkil supstituiran s -O-R20;-(CH2)r-CN; -(CH2)r CONR20R21; -(CH2)r1-NR20R21; -(CH2)r -NR20COR21 ; -(CH2)r1-NR20-(CH2)s-SO2-R21; -(CH2)r1-NHSO2-NR20R21 ; -(CH2)r1-NR20CO2R21 ; -(CH2)r-SO2NR20R21; fenil izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata svaki neovisno odabran od halogena, C1-4alkila, C1-4alkoksi, cijano ili amino; 5 ili 6-eročlani aromatski monociklični heterocikl koji sadrži barem jedan heteroatom odabran od N, O ili S; spomenuti heterocikl je izborno supstituiran s 1, 2, 3 ili 4 supstituenata svaki izborno odabran od halogena, C1-4alkila, C1-4alkoksi, cijano ili amino; pri čemu spomenuti C1-6alkil i C3-8cikloalkil, mogu izborno biti supstituirani s jednom ili više R20 skupina R20 i R21 neovisno predstavljaju vodik, C1-6alkil, hidroksiC1-6alkil, -(CH2)n-O-C1-6alkil, ili kada su povezani na atom dušika R20 i R21 mogu biti uzeti skupa kako bi tvorili s atomom dušika na koji su vezani monociklični zasićeni 4, 5 ili 6-eročlani prsten koji izborno sadrži daljnji heteroatom odabran od O, S ili N; R22 i R22 neovisno predstavljaju vodik, C1-6alkil, ili hidroksiC1-6alkil; m neovisno predstavlja cijeli broj jednak 0, 1 ili 2; n neovisno predstavlja cijeli broj jednak 0, 1, 2, 3 ili 4; s neovisno predstavlja cijeli broj jednak 0, 1, 2, 3 ili 4; r neovisno predstavlja cijeli broj jednak 1, 2, 3, ili 4; r1 neovisno predstavlja cijeli broj jednak 2, 3 ili 4; pod uvjetom da kada su R3a i R3b uzeti skupa kako bi formirali =O, n=0, Y predstavlja -E-D, i E predstavlja vezu, tada D ne predstavlja nesupstituirani fenil; njegov N-oksid, njegovu farmaceutski prihvatljivu sol ili njegov solvat.
2. Spoj prema zahtjevu 1, pri čemu Y predstavlja -CR18=N-OR19.
3. Spoj prema zahtjevu 1, pri čemu Y je -E-D.
4. Spoj prema zahtjevu 3, pri čemu E predstavlja: (i) vezu, C2-4alkendiil, -CO-(CR22R23)s-, -(CR22R23)s-CO-, -NR22-(CR22R23)s-, - (CR22R23)s-NR22-, -(CR22R23)s-CO-NR22-(CR22R23)s- ili -(CR22R23)s-NR22-CO-(CR22R23)s-; ili (ii) vezu; ili (iii) C2-4alkendiil, -CO-(CR22R23)s-, -(CR22R23)s-CO-, -NR22-(CR22R23)s-, -(CR22R23)s-NR22-, -(CR22R23)s-CO-NR22-(CR22R23)s- ili -(CR22R23)s-NR22-CO-(CR22R23)s-.
5. Spoj prema zahtjevu 3, pri čemu D je (i) izborno supstituirani pirazolil; ili (ii) piperidinil, piridinil, fenil, pirolil, imidazolil, triazolil, pirolopiridinil, 1,3-benzodioksolil, indolil, tiazolil, ciklopentil, azetidinil, morfolinil, tetrazolil, oksazolil, piperazinil, 1,2,3,6-tetrahidropiridinil, 2,5-dihidropirolil, pirimidinil, pirolidinil, tiadiazolil, oksadiazolil, spomenuti prsteni su izborno supstituirani; pri čemu su izborni supstituenti kao što su definirani u zahtjevu 1.
6. Spoj prema bilo kojem od prethodnih zahtjeva pri čemu W je -N(R3)-.
7. Spoj prema bilo kojem od zahtjeva 1 do 5, pri čemu W je -C(R38R3b)-.
8. Spoj prema bilo kojem od prethodnih zahtjeva, pri čemu R2 je neovisno odabran od hidroksila, halogena, cijano, C1-4alkila, C2-4alkenila, C1-4alkoksi, hidroksiC1-4alkila, hidroksiC1-4alkoksi, haloC1-4alkoksi, C1-4alkoksiC1-4alkila, R13, C1-4alkoksi supstituiranog s R13, -C(=O)-R13, C1-4alkila supstituiranog s NR7R8, C1-4alkoksi supstituiranog s NR7R8, -NR7R8 ili -C(=O)-NR7R8.
9. Spoj prema zahtjevu 8, pri čemu R2 predstavlja C1-4alkoksi.
10. Spoj prema bilo kojem od zahtjeva 1 do 6, 8 ili 9, pri čemu R3 predstavlja (i) C1-6alkil, hidroksiC1-6alkil, hidroksihaloC1-6alkil, haloC1-6alkil, C1-6alkil supstituiran s -C(=O)-C1-6alkilom, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može izborno biti supstituiran s jednom ili dvije hidroksilne skupine, C1-6alkil supstituiran s R9, C1-6alkil supstituiran s -NR10R11, C1-6alkil supstituiran s hidroksilom i -NR10R11, C1-6alkil supstituiran s jednim ili dva halogena i -NR10R11, C1-6alkil supstituiran s -C(=O)-OC1-6alkilom, C1-6alkil supstituiran s -O-C(=O)-NR10R11, C1-6alkil supstituiran s karboksilom, C1-6alkil supstituiran s -NR12-S(=O)2-C1-6alkilom, C1-6alkil supstituiran s-NR12-S(=O)2-NR14R15, C1-6alkil supstituiran s hidroksilom i R9, -C1-6alkil-C(R12)=N-O-R12, C1-6alkil supstituiran s -C(=O)-NR10R11, C1-6alkil supstituiran s -C(=O)-R9, C2-6alkinil supstituiran s R9, hidroksiC1-6alkoksi, C2-6alkenil, C2-6alkinil ili R13; ili (ii) C2-6alkinil, haloC1-6alkil izborno supstituiran s -O-C(=O)-C1-6alkilom, hidroksiC1-6alkil izborno supstituiran s -O-C(=O)-C1-6alkilom, hidroksihaloC1-6alkil, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može izborno biti supstituiran s jednom ili dvije hidroksilne skupine ili s -O-C(=O)-C1-6alkilom, C1-6alkil supstituiran s R9, C2-6alkinil supstituiran s R9,C1-6alkil supstituiran s -NR10R11, C1-6alkil supstituiran s -OC(=O)-NR10R11.
11. Spoj prema zahtjevu 1, pri čemu Y predstavlja -CR18=N-ILI19 ili -E-D; R18 i R19 predstavlja C1-6alkil; E predstavlja vezu, C2-4alkendiil, -CO-(CR22R23)s-, -NR22-(CR22R23)s-, -(CR22R23)s-NR22-, -(CR22R23)s-CONR22-(CR22R23)s- ili -(CR22R23)s-NR22-CO-(CR22R23)s-; D je piperidinil, piridinil, fenil, pirolil, imidazolil, triazolil, pirolopiridinil, 1,3-benzodioksolil, indolil, tiazolil, ciklopentil, azetidinil, morfolinil, tetrazolil, oksazolil, piperazinil, 1,2,3,6-tetrahidropiridinil, 2,5-dihidropirolil, pirimidinil, pirolidinil, tiadiazolil, oksadiazolil, pirazolil, spomenuti prsteni su izborno supstituirani s halo, cijano, C1-6alkilom, C1-6alkoksi, -C(=O)-O-C1-6alkilom, hidroksiC1-6alkilom, - NR4R5, C1-6alkil supstituiran s -O-C(=O)- C1-6alkilom, C1-6alkil supstituiran s -NR4R5,-C(=O)-NR4R5, -C(=O)-C1-6alkil-NR4R5, R6, C1-6alkil supstituiran s R6; W je -N(R3)-; R2 predstavlja C1-4alkoksi; n je jednak 2; R3 predstavlja C2-6alkinil, haloC1-6alkil izborno supstituiran s -O-C(=O)-C1-6alkilom, hidroksiC1-6alkil izborno supstituiran s -O-C(=O)-C1-6alkilom, hidroksihaloC1-6alkil, C1-6alkoksi C1-6alkil pri čemu svaki C1-6alkil može izborno biti supstituiran s jednom ili dvije hidroksilne skupine ili s -O-C(=O)-C1-6alkilom, C1-6alkil supstituiran s -O-C(=O)-NR10R11; R9 predstavlja C3-6cikloalkil, 3-člani zasićeni heterociklil, izborno supstituirani 5-eročlani zasićeni heterocikl, izborno supstituirani 6-eročlani aromatski ili zasićeni heterocikl, izborno supstituirani biciklični heterocikl; R10 i R11 predstavljaju vodik, C1-6alkil, haloC1-6alkil, hidroksiC1-6alkil, C1-6alkil supstituiran s -NR14R15, C1-6alkil supstituiran s karboksilom; R6 predstavlja 6-eročlani monociklični zasićeni ili aromatski heterociklil koji je izborno supstituiran; R14 i R15 svaki neovisno predstavljaju vodik ili C1-4alkil; R22 i R23 svaki neovisno predstavljaju vodik; pri čemu su izborni supstituenti kao što su definirani u zahtjevu 1.
12. Spoj prema bilo kojem zahtjevu 1 do 11 ili njegova farmaceutski prihvatljiva sol ili solvat.
13. Farmaceutski sastav koji sadrži spoj formule (I) prema bilo kojem od zahtjeva 1 do 12.
14. Spoj prema bilo kojem od zahtjeva 1 do 12 za (i) uporabu u liječenju; ili (ii) uporabu u profilaksi ili liječenju raka posredovanim FGFR kinazom; ili (iii) uporabu u profilaksi ili liječenju raka; ili (iv) uporabu u liječenju raka pri čemu je rak odabran od multiplog mijeloma, mijeloproliferativnih poremećaja, raka endometrija, raka prostate, raka mjehura, raka pluća, raka jajnika, raka dojke, raka želuca, kolorektalnog raka, i oralnog raka pločastih stanica; ili (v) uporabu u liječenju raka pri čemu je rak odabran od raka pluća, posebice raka pluća nemalih stanica, raka pločastih stanica, raka jetre, raka bubrega, raka dojke, raka debelog crijeva, kolorektalnog raka, raka prostate; ili (vi) uporabu u liječenju raka pri čemu je rak odabran od raka prostate, raka mjehura, raka pluća kao što je rak pluća nemalih stanica, raka dojke, raka želuca, te raka jetre; (vii) uporabu u liječenju raka pri čemu je rak multipli mijelom; ili (viii) uporabu u liječenju raka pri čemu je rak multipli mijelom pozitivne t(4;14) translokacije; ili (ix) uporabu u liječenju raka pri čemu je rak rak mjehura; ili (x) uporabu u liječenju raka pri čemu je rak rak mjehura s FGFR3 kromosomskom translokacijom; ili (xi) uporabu u liječenju raka pri čemu je rak rak mjehura s FGFR3 točkastom mutacijom; ili (xii) uporabu u liječenju raka pri čemu je rak tumor s mutantom FGFR1, FGFR2, FGFR3 ili FGFR4; ili (xiii) uporabu u liječenju raka pri čemu je rak tumor s mutantom pojačane funkcije FGFR2 ili FGFR3; ili (xiv) uporabu u liječenju raka pri čemu je rak tumor s pretjeranom ekspresijom FGFR1.
15. Spoj prema bilo kojem od zahtjeva 1 do 12 za uporabu u liječenju raka pri čemu je spomenuti spoj korišten u kombinaciji s jednim ili više agensa protiv raka.
16. Proizvod koji sadrži kao prvi aktivni sastojak spoj prema bilo kojem od zahtjeva 1 do 12 i kao daljnji aktivni sastojak jedan ili više agenasa protiv raka, kao kombinacijski pripravak za simultanu, odvojenu ili sekvencijalnu uporabu u liječenju pacijenata koji pate od raka.
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