SI2840080T1 - Dušik vsebujoča heterociklična spojina ali njena sol - Google Patents

Dušik vsebujoča heterociklična spojina ali njena sol Download PDF

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SI2840080T1
SI2840080T1 SI201330883T SI201330883T SI2840080T1 SI 2840080 T1 SI2840080 T1 SI 2840080T1 SI 201330883 T SI201330883 T SI 201330883T SI 201330883 T SI201330883 T SI 201330883T SI 2840080 T1 SI2840080 T1 SI 2840080T1
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amino
dimethylamino
methyl
group
substituted
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Masaru Takasaki
Toshiaki Tsujino
Shintarou TANABE
Megumi Ookubo
Kimihiko Sato
Atsushi Hirai
Daisuke Terada
Shinsuke INUKI
Shinsuke Mizumoto
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Fujifilm Corporation
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Claims (14)

  1. DUŠIK VSEBUJOČA HETEROCIKLIČNA SPOJINA ALI NJENA SOL EP 2 840 080 B1 PATENTNI ZAHTEVKI
    1. Spojina predstavljena s splošno formulo [1]-(1): [Formula 6]
    (v formuli, R2a predstavlja atom vodika ali C1-6 alkilno skupino, ki je lahko substituirana, R4a predstavlja atom vodika ali C1-6 alkilno skupino, ki je lahko substituirana, R17a predstavlja atom vodika ali C1-6 alkilno skupino, ki je lahko substituirana, pod pogojem da R17a lahko oblikuje divalentno dušik vsebujočo heterociklično skupino, ki je lahko substituirana skupaj z R4a, atom dušika k kateremu se R4a veže, in atom ogljika k kateremu se veže R17a, R17b in R18b sta enaka ali različna in predstavljata atom vodika ali C1-6 alkilno skupino, ki je lahko substituirana, pod pogojem da R17b in R18b lahko oblikujeta C(=0) skupaj z atomom ogljika, k kateremu sta vezana, ali R17b in R18b lahko oblikujeta heterociklično skupino, ki je lahko substituirana skupaj z atomom ogljika, k kateremu sta vezana, R9a predstavlja C1-6 alkilno skupino, ki je lahko substituirana, C1-6 alkoksi skupino, ki je lahko substituirana, heterociklično skupino, ki je lahko substituirana ali N(R15)(R16) (v formuli, R15 predstavlja atom vodika, C1-6 alkilno skupino, ki je lahko substituirana, C2-6 alkenilno skupino, ki je lahko substituirana, C2-6 alkinilno skupino, ki je lahko substituirana, ali C3-8 cikloalkilno skupino, ki je lahko substituirana, in R16 predstavlja C1-6 alkilno skupino, ki je lahko substituirana, C2-6 alkenilno skupino, ki je lahko substituirana, C2-e alkinilno skupino, ki je lahko substituirana, C3-8 cikloalkilno skupino, ki je lahko substituirana, arilno skupino, ki je lahko substituirana ali heterociklilno skupino, ki je lahko substituirana, ali R15 in R16 lahko oblikujeta ciklično amino skupino, ki je lahko substituirana skupaj z atomom dušika k kateremu je pripeta), R12a predstavlja C1-6 alkilno skupino, ki je lahko substituirana, arilno skupino, ki je lahko substituirana ali heterociklično skupino, ki je lahko substituirana , X2a predstavlja C1-6 alkilen skupino, ki je lahko substituirana, ali divalentno aliciklično ogljikovodikovo skupino, ki je lahko substituirana, kjer je divalentna aliciklična ogljikovodikova skupina izbrana izmed 1,2-ciklobutilena, 1,3-ciklobutilena, 1,2-ciklopentilena, 1,3-ciklopentilena, 1,2-cikloheksilena, 1,3-cikloheksilena, 1,4-cikloheksilena, biciklo(3.2.1)octilena, biciklo(2.2.0)heksilena, in biciklo(5.2.0)nonilena, ali divalentne aromatične ogljikovodikove skupine, ki je lahko substituirana, kjer je divalentna aromatična ogljikovodikova skupina izbrana izmed fenilena, indenilena, naftilena, fluorenilena, fenantrenilena, antrilena in pirenilena in X3a predstavlja C2-6 alkinilensko skupino, ki je lahko substituirana, ali N(R22)-C(=0) (v formuli, R22 predstavlja atom vodika, C1-6 alkilno skupino, ki je lahko substituirana, C2-6 alkenilno skupino, ki je lahko substituirana, C2-6 alkinilno skupino, ki je lahko substituirana, ali imino zaščitno skupino izbrano izmed aril(Ci-6 alkilne)skupine, (C1-6 alkoksi)(Ci-e alkilno) skupino, acilno skupino, C1-6 alkoksikarbonilno skupino, aril(Ci-6 alkoksi)karbonilno skupino, ariloksikarbonilno skupino, C1-6 alkilsulfonilno skupino, arilsulfonilno skupino, in sililno skupino) ali njeno sol.
  2. 2. Spojina ali njena sol po zahtevku 1, kjer R2a je C1-6 alkilna skupina , ki je lahko substituirana, substituent C1-6 alkilne skupine, ki je lahko substituiran kot R2a je atom halogena, hidroksilna skupina, C1-6 alkilamino skupina, ki je lahko substituirana z eno ali večimi skupinami, izbranimi izmed substituentne skupine A-3, di(Ci-6 alkil)amino skupine, ki je lahko substituirana z eno ali večimi skupinami izbranimi izmed substituentne skupine A-3 ali heterociklične skupine, ki je lahko substituirana z eno ali večimi skupinami, izbranimi izmed ene ali večih skupin izbranimi izmed substituentne skupine A-3, in substituentna skupina A-3 je sestavljena iz atoma halogena, hidroksilne skupine, ki je lahko zaščitena s hidroksilnmo zaščitno skupino izbrane izmed C1-6 alkilne skupine, C2-6 alkenilne skupine, aril(Ci-6 alkil) skupine, (C1-6 alkoksi)(Ci-6 alkil) skupine, aril(Ci-6 alkoksi)(Ci-e alkil) skupine, acil skupine, C1-6 alkoksikarbonilne skupine, aril(Ci-6alkoksi)karbonilne skupine, C1-6 alkilsulfonilne skupine, arilsulfonilne skupine, sililne skupine, tetrahidrofuranilne skupine, in tetrahidropiranilne skupine, in C1-6 alkilne skupine, ki je lahko substituirana s hidroksilno skupino.
  3. 3. Spojina ali njena sol po zahtevku 1 ali 2, kjer R4a je atom vodika ali C1-6 alkilna skupina.
  4. 4. Spojina ali njena sol po katerem koli zahtevku 1 do 3, kjer R17a je atom vodika ali Ci-6 alkilna skupina.
  5. 5. Spojina ali njena sol po katerem koli zahtevku 1 do 4, kjer R17b in R18b sta enaka ali različna, in predstavljata C1-6 alkilno skupino, ali R17b in R18b oblikujeta C(=0) skupaj z atomom ogljika, k kateremu sta pripeta.
  6. 6. Spojina ali njena sol po katerem koli zahtevku 1 do 5, kjer R9a je N(R15)(R16) (v formuli, R15 predstavlja atom vodika, C1-6 alkilno skupino, ki je lahko substituirana, C2-6 alkenilno skupino, ki je lahko substituirana, C2-6 alkinilno skupino, ki je lahko substituirana ali C3-8 cikloalkilno skupino, ki je lahko substituirana, in R16 predstavlja C1-6 alkilno skupino, ki je lahko substituirana, C2-6 alkenilno skupino, ki je lahko substituirana, C2-6 alkilno skupino, ki je lahko substituirana, C3-8 cikloalkilno skupino, ki je lahko substituirana, arilno skupino, ki je lahko substituirana ali heterociklično skupino, ki je lahko substituirana, ali R15 in R16 lahko oblikujeta ciklično amino skupno, ki je lahko substituirana skupaj z atomom dušika, k kateremu sta pripeta).
  7. 7. Spojina ali njena sol po katerem koli zahtevku 1 do 6, kjer R12a je arilna skupina, ki je lahko substituirana.
  8. 8. Spojina ali njena sol po katerem koli zahtevku 1 do 7, kjer X2a je C1-6 alkilenska skupina, ki je lahko substituirana ali divalentna aliciklična ogljikovodikova skupina, ki je lahko substituirana.
  9. 9. Spojina ali njena sol po katerem koli zahtevku 1 to 8, kjer X3a je C2-6 alkinilenska skupina, ki je lahko substituirana, prednostno etinilenska skupina.
  10. 10. Spojina ali njena sol po zahtevku 1, ki je spojina izbrana izmed (S,E)-N-(3-(2- (4-(dimetilamino)-N-metil-2-butenamid)propanamido)fenil)-4-(propilamin)-2-((2-(piridin-4-il)etil)amino)pirimidin-5-karboksamid, (S,E)-2-((4- karbamoilfenil)amino)-N-(3-(2-(4-(dimetilamino)-N-metil-2-butenamid) propanamido)fenil)-4-(propilamin)pirimidin-5-karboksamid, (E)-2-((4- karbamoilfenil)amino)-N-(3-(2-(4-(dimetilamino)-N-metil-2-butenamid) aktamido)cikloheksil)-4-(propilamin)pirimidin-5-karboksamid, (S,E)-2-((4-karbamoilfenil)amino)-N-(3-(2-(4-(dietilamino)-N-metil-2-butenamid) propanamido)fenil)-4-(propilamino)pirimidin-5-karboksamid, (S,E)-2-((4- karbamoilfenil)amino)-N-(3-(2-(4-(dimetilamino)-N-metil-2-butenamid) propaneamido)propil)-4-(propilamin)pirimidin-5-karboksamid, (S,E)-N-(3-(2-(4-(dimetilamino)-N-metil-2-butenamid)propanamido)fenil)-2-(izokuinolin-6-ilamino)-4-(propilamino)pirimidin-5-karboksamid, (S,E)-2-(cinolin-6-ilamino)-N-(3-(2-(4-(dimetilamino)-N-metil-2-butenamido)propanamido)fenil)-4-(propilamino)pirimidin-5-karboksamid, (S,E)-4-(dimetilamino)-N-(1-((5-(2-((3-fluorofenil)amino)-4-(propilamino)pirimidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (S,E)-N-(1-((5-(2-((3-cianofenil)amino)- 4-(propilamino)pirimidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (S,E)-4-((5-(5-(2-(4-(dimetilamino)-N- metil-2-butenamid)propaneamido)-1-pentin-1-il)-4-(propilamino)pirimidin-2-il)amino)benzamid, (S,E)-N-(1-((5-(2-((4-cianofenil)amino)-4- (propilamino)pirimidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (E)-4-(dimetilamino)-N-(2-((5-(2-((4- fluorofenil)amino)-4-(propilamino)pirimidin-5-il)-4-pentin-1-il)amino)-2-oksoetil)-N-metil-2-butenamid, (E)-N-(2-((5-(2-((4-cianofenil)amin)-4- (propilamino)primidin-5-il)-4-pentin-1-il)annin)-2-oksoetil)-4-(dimetilamino)-N-metil-2-butenamid, (S,E)-4-(dimetilamino)-N-(1-((5-(2-((3- fluorofenil)amino)-4-(propilamino)primidin-5-il)-4-pentin-1-il)amin)-1-oksobutan-2-il)-N-metil-2-butenamid, (S, E)-4-(dimetilamino)-N-(1-((5-(2-((3-fluoro-4-metoksifenil)amino)-4-(propilamino)primidin-5-il)-4-pentin-1-il)amino)- 1- oksopropan-2-il)-N-metil-2-butenamid, (S,E)-4-(dimetilamino)-N-(1-((5-(2-((6- fluoropiridin-3-il)amino)-4-(propilamino)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (S,E)-4-(dimetilamino)-N-(1-((5-(2-((6-fluoropiridin-3-il)amino)-4-((4-metoksifenil)amino)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (E)-4-(dimetilamino)-N-(2-((5-(2-((3-fluorofenil)amino)-4-(propilamino)primidin-5-il)-4-pentin-1-il)amino)-2-oksoetil)-N-metil-2-butenamid, (S,E)-N-(5-(2-((4-cianofenil)amino)-4- (propilamino)primidin-5-il)-4-pentin-1-il)-1-(4-(dimetilamino)-2-butenoil)pirolidin- 2- karboksamid, (S,E)-N-(1-((5-(4-(ciklopropilamino)-2-((3-fluoro-4- metoksifenil)amino)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (S,E)-4-(dimetilamino)-N-(1-((5-(2-((3-fluoro-4-metoksifenil)amino)-4-((3-fluoropropil)amino)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (S, E)-N-(1-((5-(2-((4- cianofenil)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)amino)-3-hidroksi-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (2S,4R)-1-((E)-4- (dimetilamino)-2-butenoil)-N-(5-(2-((3-fluorofenil)amino)-4-(propilamin)primidin- 5-il)-4-pentin-1 -il)-4-hidroksipirolidin-2-karboksamid, (2S,4S)-1 -((E)-4- (dimetilamino)-2-butenoil)-4-fluoro-N-(5-(2-((3-fluorofenil)amino)-4-(metilamino)primidin-5-il)-4-pentin-1-il)pirolidin-2-karboksamid, (2S,4S)-1-((E)-4-(dimetilamino)-2-butenoil)-N-(5-(2-((3-fluorofenil)amino)-4-(metilamino) primidin-5-il)-4-pentin-1-il)-4-metoksipirolidin-2-karboksamid, (2S,4S)-1-((E)-4-(dimetilamino)-2-butenoil)-4-fluoro-N-(5-(2-((4-fluorofenil)amino)-4-(metilamino)primidin-5-il)-4-pentin-1-il)pirolidin-2-karboksamid, (2S,4R)-1-((E)-4-(dimetilamino)-2-butenoil)-4-fluoro-N-(5-(2-((4-fluorofenil)amino)-4-(metilamino)primidin-5-il)-4-pentin-1-il)pirolidin-2-karboksamid, (2S,4S)-1-((E)-4-(dimetilamino)-2-butenoil)-N-(5-(2-((4-fluorofenil)amino)-4-(metilamino )primidin-5-il)-4-pentin-1-il)-4-metoksipirolidin-2-karboksamid, (2S,4R)-1-((E)-4-(dimetilamino)-2-butenoil)-N-(5-(2-((4-fluorofenil)amino)-4-(metilamino )primidin-5-il)-4-pentin-1-il)-4-metoksipirolidin-2-karboksamid, (S,E)-1-(4-(dimetilamino)-2-butenoil)-N-(5-(2-((4-fluorofenil)amino)-4-(metilamino) primidin-5-il)-4-pentin-1-il)azetidin-2-karboksamid, (2S,4S)-N-(5-(2-((4- cianofenil)amino)-4-(metilamino)primidin-5-il)-4-pentin-1-il)-1-((E)-4-(dimetilamino)-2-butenoil)-4-fluoropirolidin-2-karboksamid, (E)-N-(2-((5-(2-((4-cianofenil)amino)-4-(metilamino)primidin-5-il)-4-pentin-1-il)amino)-2-oksoetil)-4-(dimetilamino)-N-metil-2-butenamid, (S,E)-4-(dimetilamino)-N-(1-((3-((2-((3-fluorofenil)amino)-4-(propilamin)primidin-5-il)etinil)fenil)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (S,E)-4-((5-((3-(2-(4-(dimetilamino)-N-metil-2-butenamid)propanamido)fenil)etinil)-4-(propilamin)primidin-2-il)amino)benzamid, (S,E)-N-(1-((5-(2-((4-cianofenil)amino)-4-(pirolidin-1- il)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (S,E)-4-(dimetilamino)-N-(1-((5-(2-((2-fluoropiridin-4- il)amino)-4-(pirolidin-1 -il)primidin-5-il)-4-pentin-1-il)amino)-1 -oksopropan-2-il)-N-metil-2-butenamid, (S,E)-4-(dimetilamino)-N-(1-((5-(2-((2-fluoropiridin-4-il)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (S,E)-N-(1-((5-(4-(ciklopropilamin)-2-((2-fluoropiridin-4-il)amino)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (S, E)-4-(dimetilamino)-N-metil-N-(1 -((5-(2-((3- metilizotiazol-5-il)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-2-butenamid, (S,E)-4-(dimetilamino)-N-(1-((5-(4-((3- metoksipropil)amino)-2-((2-metoksipiridin-4-il)amino)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (S,E)-1-(4-(dimetilamino)-2-butenoil)-N-(5-(4-((3-metoksipropil)amino)-2-((metoksipiridin-4-il)amino) primidin-5-il)-4-pentin-1-il)pirolidin-2-karboksamid, (2S,4S)-1-((E)-4- (dimetilamino)-2-butenoil)-4-fluoro-N-(5-(4-((3-metoksipropil)amino)-2-((metoksipiridin-4-il)amino)primidin-5-il)-4-pentin-1-il)pirolidine-2-karboksamid, (SlE)-1-(4-(dimetilamino)-2-butenoil)-N-(5-(2-((2-metoksipiridin-4-il)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)pirrolidin-2-karboksamid, (2S,4S)-1-((E)-4-(dimetilamino)-2-butenoil)-4-fluoro-N-(5-(2-((2-metoksipiridin-4-il)amino)- 4- (propilamin)primidin-5-il)-4-pentin-1-il)pirolidin-2-karboksamid, (E)-4- (dimetilamino)-N-(2-((5-(2-((2-metoksipiridin-4-il)amino)-4-(propilamin)primidin- 5- il)-4-pentin-1-il)amino)-2-oksoetil)-N-metil-2-butenamid, (S,E)-4- (dimetilamino)-N-(1-((5-(2-((3-fluorofenil)amino)-4-((4-metoksifenil)amino) primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (S,E)-4-(dimetilamino)-N-(1-((5-(2-((3-fluorofenil)amino)-4-morfolinopirimidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (E)-4- (dimetilamino)-N-(2-((5-(2-((4-fluorofenil)amino)-4-((3-fluoropropil)amino) primidin-5-il)-4-pentin-1-il)amino)-2-oksoetil)-N-metil-2-butenamid, (S,E)-N- (1-((5-(2-((4-cianofenil)amino)-4-(ciklopropilamin)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-4-(dimetilamino))-N-metil-2-butenamid, (S,E)-N-(1-((5-(2-((4-cianofenil)amino)-4-((3-fluoropropil)amino)primidin-5-il)-4-pentin- 1- il)amino)-1-oksopropan-2-il)-4-(dimetilamino))-N-metil-2-butenamid, (S,E)- 4- (dimetilamino))-N-(1-((5-(4-(ethilamino)-2-((1-metil-1H-indazol-5-il)amino) primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (S,E)-N-(1-((5-(4-(ciklopropilamin)-2-((1-metil-1H-indazol-5-il)amino)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-4-(dimetilamino))-N-metil-2-butenamid, (S,E)-4-(dimetilamino))-N-metil-N-(1-((5-(2-((1-metil-1H-indazol- 5- il)amino)-4-(metilamino)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)- 2- butenamid, (S,E)-N-(5-(2-((1H-indazol-5-il)amino)-4-(metilamino)primidin- 5-il)-4-pentin-1-il)-1-(4-(dimetilamino)-2-butenoil)pirolidin-2-karboksamid, (S,E)-N-(5-(2-((1H-indazol-5-il)amino)-4-(ethilamino)primidin-5-il)-4-pentin-1-il)-1-(4-(dimetilamino)-2-butenoil)pirolidin-2-karboksamid, (S,E)-N-(5-(2-((1H-indazol-5-il)amino)-4-((3-metoksipropil)amino)primidin-5-il)-4-pentin-1-il)-1-(4-(dimetilamino)-2-butenoil)pirolidin-2-karboksamid, (E)-4-(dimetilamino)-N-((S)-1-(((1Sl3R)-3-((2-((3-fluorofenil)amino)-4-(propilamin)primidin-5-il)etinil) ciklloheksil)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (E)-4- (dimetilamino)-N-((S)-1-(((1S,3R)-3-((2-((3-fluorofenil)amino)-4-(propilamin) primidin-5-il)etinil)ciklobutil)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (E)-N-((S)-1-(((1S,3R)-3-((2-((4-cianofenil)amino)-4-(metilamino)primidin-5-il)etinil)ciklobutil)amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (E)-4-(dimetilamino)-N-((S)-1-(((1S,3R)-3-((2-((3- fluorofenil)amino)-4-(metilamino)primidin-5-il)etinil)ciklobutil)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (E)-N-((S)-1-(((1S,3R)-3-((2-((4- cianofenil)amino)-4-(metilamino)primidin-5-il)etinil)ciklobutil)amino)-1- oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (E)-N-((S)-1- (((1S,3R)-3-((2-((3-cianofenil)amino)-4-(metilamino)primidin-5-il)etinil)ciklobutil) amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (E)-4- (dimetilamino)-N-((S)-1-(((1S,3R)-3-((2-((3-fluoro-4-metoksifenil)amino)-4- (metilamino)primidin-5-il)etinil)ciklobutil)amino)-1-oksopropan-2-il)-N-metil-2- butenamid, (E)-4-(dimetilamino)-N-((S)-1-(((1S,3R)-3-((2-((4- fluorofenil)amino)-4-(metilamino)primidin-5-il)etinil)ciklobutil)amino)-1- oksopropan-2-il)-N-metil-2-butenamid, (E)-N-((S)-1-(((1S,3R)-3-((2-((3- cianofenil)amino)-4-(ciklopropilamin)primidin-5-il)etinil)ciklobutil)amino)-1- oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (E)-4-(dimetilamino)- N-((S)-1-(((1S*,3R*)-3-((2-((2-fluoropiridin-4-il)amino)-4-(propilamin)primidin-5- il)etinil)ciklobutil)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (E)-4- (dimetilamino)-N-((S)-1-(((1S,3R)-3-((2-((2-metoksipiridin-4-il)amino)-4- (propilamin)primidin-5-il)etinil)ciklobutil)amino)-1-oksopropan-2-il)-N-metil-2- butenamid, (E)-N-((S)-1-(((1S,3R)-3-((2-((4-cianofenil)amino)-4- (metilamino)primidin-5-il)etinil)cikloheksil)amino)-1-oksopropan-2-il)-4- (dimetilamino)-N-metil-2-butenamid, (E)-N-((S)-1-(((1S*,3R*)-3-((2-((4- cianofenil)amino)-4-(ciklopropilamin)primidin-5-il)etinil)ciklobutil)amino)-1- oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (E)-N-((S)-1- (((1S*,3R*)-3-((4-(ciklopropilamin)-2-((4-fIuorofenil)amino)primidin-5- ii)etinil)ciklobutil)amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2- butenamid, (E)-N-((S)-1-(((1S*,3R*)-3-((4-(ciklopropilamin)-2-((3-fluoro-4- metoksifenil)amino)primidin-5-il)etinil)ciklobutil)amino)-1-oksopropan-2-il)-4- (dimetilamino)-N-metil-2-butenamid, (E)-4-(dimetilamino)-N-((S)-1-(((1S,3R)-3- ((2-((3-fluorofenil)amino)-4-((3-fluoropropil)amino)primidin-5-il)etinil) ciklobutil)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (E)-N-((S)-1- (((1S,3R)-3-((2-((4-cianofenil)amino)-4-((3-fluoropropil)amino)primidin-5-il)etinil)ciklobutil)amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (E)-4-(dimetilamino)-N-((S)-1-(((1S,3R)-3-((2-((3- fluorofenil)amino)-4-((3-metoksipropil)amino)primidin-5-il)etinil)ciklobutil)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (E)-N-((S)-1-(((1 S, 3R)-3-((2-((4-cianofenil)amino)-4-((3-metoksipropil)amino)primidin-5-il)etinil)ciklobutil)amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamid, (E)-4-(dimetilamino)-N-((S)-1 -(((1 S,3R)-3-((2-((3-fluoro-4- metoksifenil)amino)-4-(metilamino)primidin-5-il)etinil)cikloheksil)amino)-1-oksopropan-2-il)-N-metil-2-butenamid, (S,E)-4-(dimetilamino)-N-metil-N-(1-((5-(2-((2-metilpiridin-4-il)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-2-butenamid, (S,E)-N-(1-((5-(2-(benzo[d]thiazol- 6-ilamino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-4-(dimetilamino)-N-metil-2-butenamidI (S,E)-1-(4-(dimetilamino)-2-butenoil)-N-(5-(2-((1-metil-1H-indazol-5-il)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)pirolidin-2-karboksamid, (S,E)-1-(4-(dimetilamino)-2-butenoil)-N-(5-(2-((1-metil-1H-pirazolo[3^4D]piridin-5-il)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)pirolidin-2-karboksamid, (S,E)-1-(4-(dimetilamino)-2-butenoil)-N-(5-(2-((1-(2-metoksietil)-1H-pirazolo[3,4-b]piridin-5-il)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)pirolidin-2-karboksamid, (S,E)-4-(dimetilamino)-N-metil-N-(1-((5-(2-((3-metil-1H-pirazolo[3,4-b]piridin-5-il)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)amino)-1-oksopropan-2-il)-2-butenamid, (S,E)-1-(4- (dimetilamino)-2-butenoil)-N-(5-(2-((3-metil-1H-pirazolo[3,4-b]piridin-5-il)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)pirolidin-2-karboksamid, in (S,E)-1-(4-(dimetilamino)-2-butenoil)-N-(5-(2-((3-metoksi-1H-pirazolo[3,4- b]piridin-5-il)amino)-4-(propilamin)primidin-5-il)-4-pentin-1-il)pirolidin-2- karboksamid.
  11. 11. Farmacevtski sestavek, ki vsebuje spojino ali njeno sol po katerem koli od zahtevkov 1 do 10.
  12. 12. Spojina ali njena sol po katerem koli od zahtevkov 1 do 10 ali farmacevtski sestavek po zahtevku 11 za uporabo pri zdravljenju bolezni ali stanja, ki se nanaša na FLT3.
  13. 13. Spojina ali njena sol po kateremkoli od zahtevkov 1 do 10 ali farmacevtski sestavek po zahtevku 11 za uporabo pri zdravljenju akutne mieloične levkemije.
  14. 14. Spojina ali njena sol po kateremkoli od zahtevkov 1 do 10 ali farmacevtski sestavek po zahtevku 11 za uporabo kot zaviralec FLT3.
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