HRP20230657T1 - Spojevi i pripravci za liječenje hematoloških poremećaja - Google Patents

Spojevi i pripravci za liječenje hematoloških poremećaja Download PDF

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HRP20230657T1
HRP20230657T1 HRP20230657TT HRP20230657T HRP20230657T1 HR P20230657 T1 HRP20230657 T1 HR P20230657T1 HR P20230657T T HRP20230657T T HR P20230657TT HR P20230657 T HRP20230657 T HR P20230657T HR P20230657 T1 HRP20230657 T1 HR P20230657T1
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pyridin
carboxamide
methylpyridin
oxazole
piperidin
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HRP20230657TT
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Venkateshwar Rao Gummadi
Susanta Samajdar
Kavitha Nellore
Girish DAGINAKATTE
Wesley Roy BALASUBRAMANIAN
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Aurigene Oncology Limited
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P35/02—Antineoplastic agents specific for leukemia

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (23)

1. Spoj formule II, ili njegova farmaceutski prihvatljiva sol, za uporabu u liječenju ili prevenciji akutne mijeloične leukemije (AML), pri čemu je AML otporan na liječenje inhibitorom tirozin kinaze 3 (FLT-3) sličnom FMS-u; [image] pri čemu X1 i X3 su nezavisno CH ili N; X2 je CR2 ili N; ukoliko jedan i ne više od jednog X1, X2 ili X3 je N; A je O ili S; Y je -CH2- ili O; Z je aril ili heterociklil; Ri, pri svakoj pojavnosti, je nezavisno halo ili opcionalno supstituirani heterociklil; pri čemu supstituent je alkil, alkoksi, aminoalkil, halo, hidroksil, hidroksi alkil ili -NRaRb; R2 je hidrogen, opcionalno supstituirani cikloalkil, opcionalno supstituirani aril, opcionalno supstituirani heterociklil ili -NRaRb; pri čemu supstituent je alkil, amino, halo ili hidroksil; R3, pri svakoj pojavnosti, je alkil ili hidroksil; Ra iRb su nezavisno hidrogen, alkil, acil ili heterociklil; 'm' i 'n' su nezavisno 0, 1 ili 2; i 'p' je 0 ili 1.
2. Spoj za uporabu prema zahtjevu 1, pri čemu A je O ili S; Y je -CH2- ili O; Z je aril ili heterociklil; Ri, pri svakoj pojavnosti, je nezavisno halo ili opcionalno supstituirani heterociklil; pri čemu supstituent je alkil, alkoksi, aminoalkil, halo, hidroksil ili -NRaRb; gdje Ra i Rb su nezavisno hidrogen, alkil, ili heterociklil; R2 je hidrogen, cikloalkil, opcionalno supstituirani heterociklil ili -NRaRb, gdje supstituent je odabran od amino, halo ili hidroksil; 'm' i 'n' su nezavisno 0, 1 ili 2; i 'p' je 0 ili 1.
3. Spoj za uporabu prema zahtjevu 1, pri čemu [image] Je [image] [image]
4. Spoj za uporabu prema bilo kojem od zahtjeva 1-3, pri čemu Z je (a) aril ili 5-ili 6-člani heterociklil, ili (b) odabran od fenil, furanil, tienil, pirrolil, pirazolil, imidazolil, oksazolil, isoksazolil, tiazolil, isotiazolil, 1H-tetrazolil, oksadiazolil, triazolil, piridil, pirimidinil, pirazinil, piridazinil, azetidinil, oxetanil, imidazolidinil, pirrolidinil, oksazolidinil, tiazolidinil, pirazolidinil, tetrahidrofuranil, piperidinil, piperazinil, tetrahidropiranil, morfolinil, tiomorfolinil, 1,4-dioksanil, dioksidotiomorfolinil, oksapiperazinil, oksapiperidinil, tetrahidrofuril, tetrahidropiranil, tetrahidrotiofenil, dihidropiranil i azabiciklo[3.2.1]oktanil; svaki od kojih je opcionalno supstituiran sa alkil, alkoksi, halo, hidroksil, hidroksi alkil ili -NRaRb; i Ra i Rb su nezavisno hidrogen, alkil ili acil.
5. Spoj za uporabu prema zahtjevu 1 predstavljen formulom (IIA): [image] ili njegova farmaceutski prihvatljiva sol.
6. Spoj za uporabu prema zahtjevu 5, pri čemu A je O ili S; Y je -CH2- ili O; Ri, pri svakoj pojavnosti, je nezavisno halo ili opcionalno supstituirani heterociklil; pri čemu supstituent je alkil, alkoksi, aminoalkil, halo, hidroksil ili -NRaRb; gdje Ra i Rb su nezavisno hidrogen, alkil, ili heterociklil; R2 je hidrogen, cikloalkil, opcionalno supstituirani heterociklil ili -NRaRb, gdje supstituent je odabran od amino, halo ili hidroksil; i 'm' i 'n' su nezavisno 0, 1 ili 2.
7. Spoj za uporabu prema zahtjevu 1, predstavljen (IIB): [image] ili njegova farmaceutski prihvatljiva sol.
8. Spoj za uporabu prema zahtjevu 7, pri čemu A je O ili S; Y je -CH2- ili O; Ri, pri svakoj pojavnosti, je nezavisno halo ili opcionalno supstituirani heterociklil; pri čemu supstituent je alkil, alkoksi, aminoalkil, halo, hidroksil ili -NRaRb; gdje Ra i Rb su nezavisno hidrogen, alkil, ili heterociklil; R2 je hidrogen, cikloalkil, opcionalno supstituirani heterociklil ili -NRaRb, gdje supstituent je odabran od amino, halo ili hidroksil; i 'm' i 'n' su nezavisno 0, 1 ili 2.
9. Spoj za uporabu prema zahtjevu 1, pri čemu spoj je spoj formule (IIC) [image] ili njegova farmaceutski prihvatljiva sol.
10. Spoj za uporabu prema bilo kojem od zahtjeva 1-9, pri čemu R1 je opcionalno supstituirani heterociklil; pri čemu supstituent je alkil, alkoksi, aminoalkil, halo, hidroksil, hidroksi alkil ili -NRaRb; iRa iRb su nezavisno hidrogen ili acil, ili pri čemu R1 je opcionalno supstituirani heterociklil; i supstituent je alkil, alkoksi, aminoalkil, halo, hidroksil ili -NRaRb; gdje Ra i Rb su nezavisno hidrogen, alkil, ili heterociklil; ili pri čemu R1 je halo.
11. Spoj za uporabu prema zahtjevu 10, pri čemu R1 je opcionalno supstituirani pirazolil, pri čemu opcionalni supstituent je alkil, hidroksil ili -NRaRb.
12. Spoj za uporabu prema bilo kojem od zahtjeva 1-11, pri čemu R2 je hidrogen, cikloalkil, poput ciklopropila; opcionalno supstituirani heterociklil, poput piperidinila, pirrolidinila, morfolinila, piperazinila, azetidinila, pirazolila, furanila ili azabiciklo[3.2.1]oktanila; pri čemu supstituent je hidroksil, halo, alkil ili amino; ili -NRaRb, gdje supstituent je odabran od amino, halo ili hidroksil.
13. Spoj za uporabu prema bilo kojem od zahtjeva 1-12, pri čemu R3 je alkil.
14. Spoj za uporabu prema bilo kojem od zahtjeva 1-13, pri čemu m je 0 ili 2, i p je 0 ili 1.
15. Spoj za uporabu prema zahtjevu 1, pri čemu je spoj formule (II) odabran od: 6'-amino-N-(2-morfolinooksazolo[4,5-b]piridin-6-il)-[2,3'-bipiridin]-6-karboksamid; 6'-amino-N-(5-ciklopropil-2-morfolinooksazolo[4,5-b]piridin-6-il)-[2,3'-bipiridin]-6-karboksamid hidroklorid; N-(5-ciklopropil-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid hidroklorid; N-(2,5-di(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-6-(1H-pirazol-4-il)pikolinamid hidroklorid; N-(2, 5-di(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-6-(1H-pirazol-4-il)pikolinamid; 2-(2-metilpiridin-4-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 6-kloro-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)pikolinamid; N-(2,5-di(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-6-(1-metil-1H-pirazol-4-il)pikolinamid; 2-(2-kloropiridin-4-il)-N-(2,5-di(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; (S)-2-(2-metilpiridin-4-il)-N-(2-morfolino-5-(pirrolidin-3-ilamino)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 6'-amino-N-(2-morfolinooksazolo[5,4-b]piridin-5-il)-[2,3'-bipiridin]-6-karboksamid; 6'-amino-N-(2-morfolinotiazolo[4,5-c]piridin-6-il)-[2,3'-bipiridin]-6-karboksamid; 6'-amino-N-(2-morfolinotiazolo[5,4-b]piridin-5-il)-[2,3'-bipiridin]-6-karboksamid; 2-(2-metilpiridin-4-il)-N-(2-morfolinotiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 6'-amino-N-(2-morfolinotiazolo[4,5-b]piridin-6-il)-[2,3'-bipiridin]-6-karboksamid; N-(2-morfolinotiazolo[4,5-b]piridin-6-il)-6-(1H-pirazol-4-il)pikolinamid; 3-(4-(aminometil)piperidin-1-il)-5-fluoro-N-(2-morfolinotiazolo[4,5-b]piridin-6-il)benzamid; 2-(4-(aminometil)piperidin-1-il)-5-fluoro-N-(2-morfolinotiazolo[4,5-b]piridin-6-il)benzamid; 2-(2-metilpiridin-4-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)-6-(1H-pirazol-4-il)pikolinamid; N-(2,5-di(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)-6-(1H-pirazol-4-il)pikolinamid; N-(2,5-di(piperidin-1-il)tiazolo[4, 5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(2,5-dimorfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(4-metilpiperazin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(2,5-di(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-2-(6-metoksipiridin-3-il)oksazol-4-karboksamid; N-(2,5-di(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-3-il)oksazol-4-karboksamid; N-(2, 5-di(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-2-(2-hidroksipiridin-3-il)oksazol-4-karboksamid; 2-(2-hidroksipiridin-3-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; N-(2, 5-di(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-2-(6-hidroksipiridin-3-il)oksazol-4-karboksamid; 2-(2-metoksipiridin-4-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 2-(2-metilpiridin-3-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 2-(3-metilpiridin-4-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; N-(2, 5-di(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-2-(3-metilpiridin-4-il)oksazol-4-karboksamid; 2-(6-metilpiridin-3-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 6-(1-metil-1H-pirazol-4-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)pikolinamid; N-(2,5-di(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-2-(6-metilpiridin-3-il)oksazol-4-karboksamid; (S)-N-(5-(3-aminopirrolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (S)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (R)-N-(5-(3-aminopirrolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (R)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (S)-2-(3-aminopirrolidin-1-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; (S)-6-(3-hidroksipirrolidin-1-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)pikolinamid; (S)-6-(3-aminopirrolidin-1-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)pikolinamid; (S)-2-(3-hidroksipirrolidin-1-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; (S)-N-(5-ciklopropil-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(3-hidroksipirrolidin-1-il)oksazol-4-karboksamid; (S)-2-(3-aminopirrolidin-1-il)-N-(5-ciklopropil-2-morfolinooksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 2-(2-metilpiridin-4-il)-N-(5-(piperidin-1-il)-2-(pirrolidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid hidroklorid; N-(2-(2,6-dimetilmorfolino)-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid hidroklorid; N-(2,5-di(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)-6-(1-metil-1H-pirazol-4-il)pikolinamid hidroklorid; 6-(1-metil-1H-pirazol-4-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)pikolinamid; N-(2,5-di(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-3-il)oksazol-4-karboksamid hidroklorid; N-(2-((2S,6R)-2,6-dimetilmorfolino)-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; 2-(2-metilpiridin-3-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 2-(2-hidroksipiridin-3-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; N-(2,5-di(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)-2-(2-metoksipiridin-4-il)oksazol-4-karboksamid; 2-(6-metoksipiridin-3-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 2-(2-metoksipiridin-4-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; (S)-N-(5-(3-fluoropiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; 2-(6-metilpiridin-3-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 2-(3-metilpiridin-4-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; (S)-6-(3-aminopirrolidin-1-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)pikolinamid; (S)-6-(3-hidroksipirrolidin-1-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)pikolinamid; (S)-6-(3-aminopirrolidin-1-il)-N-(2,5-di(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)pikolinamid; (S)-N-(2, 5-di(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)-6-(3-hidroksipirrolidin-1-il)pikolinamid; (S)-2-(3-aminopirrolidin-1-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; (S)-N-(5-(3-aminopirrolidin-1-il)-2-morfolinotiazolo[4, 5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (S)-2-(3-aminopirrolidin-1-il)-N-(5-ciklopropil-2-morfolinotiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; N-(5-ciklopropil-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (S)-2-(3-hidroksipirrolidin-1-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; (S)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (S)-N-(5-ciklopropil-2-morfolinotiazolo[4,5-b]piridin-6-il)-6-(3-hidroksipirrolidin-1-il)pikolinamid; (S)-N-(5-ciklopropil-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(3-hidroksipirrolidin-1-il)oksazol-4-karboksamid; (S)-N-(5-ciklopropil-2-morfolinotiazolo[4,5-b]piridin-6-il)-6-(1-(2-hidroksipropil)-1H-pirazol-4-il)pikolinamid; (S)-N-(5-ciklopropil-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(1-(2-hidroksipropil)-1H-pirazol-4-il)oksazol-4-karboksamid; N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(6-metoksipiridin-3-il)oksazol-4-karboksamid; (S)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(6-metoksipiridin-3-il)oksazol-4-karboksamid; (R)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(6-metoksipiridin-3-il)oksazol-4-karboksamid; (S)-N-(5-(azetidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-6-(3-hidroksipirrolidin-1-il)pikolinamid; N-(5-(3-hidroksiazetidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (S)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)tiofen-2-karboksamid; (S)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)furan-2-karboksamid; (S)-N-(5-(3-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(4-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid (R)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(4-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)furan-2-karboksamid; N-(5-(azetidin-1-il)-2-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; 2-(2-metilpiridin-4-il)-N-(2-(piperidin-1-il)-5-(pirrolidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 2-(2-metilpiridin-4-il)-N-(2-morfolino-5-(pirrolidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 5-(2-metilpiridin-4-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)furan-2-karboksamid; N-(5-(azepan-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; 2-(2-aminopiridin-4-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid hidroklorid; N-(5-(azetidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (R)-N-(5-(3-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (R)-N-(5-(3-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)furan-2-karboksamid; (S)-6-(1-(2-hidroksipropil)-1H-pirazol-4-il)-N-(2-morfolino-5-(piperidin-1-il)tiazolo[4, 5-b]piridin-6-il)pikolinamid N-(5-(4-fluoropiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)furan-2-karboksamid N-(5-(4-fluoropiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid hidroklorid N-(5-(1-metil-1H-pirazol-4-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(3-fluorofenil)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(4-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)furan-2-karboksamid; N-(5-(3-fluoropiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)furan-2-karboksamid; (S)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(6-metoksipiridin-3-il)oksazol-4-karboksamid; N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (R)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(6-metoksipiridin-3-il)oksazol-4-karboksamid; N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(6-metoksipiridin-3-il)oksazol-4-karboksamid; (S)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)furan-2-karboksamid; (S)-N-(5-(3-hidroksipirrolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)tiofen-2-karboksamid; N-(5-(azetidin-1-il)-2-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; 2-(2-metilpiridin-4-il)-N-(2-(piperidin-1-il)-5-(pirrolidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 5-(2-metilpiridin-4-il)-N-(2-morfolino-5-(piperidin-1-il)oksazolo[4,5-b]piridin-6-il)furan-2-karboksamid; N-(5-(azetidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; 2-(2-metilpiridin-4-il)-N-(2-morfolino-5-(pirrolidin-1-il)oksazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; N-(5-(4-hidroksipiperidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)furan-2-karboksamid; (R)-N-(5-(3 -hidroksipiperidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-5-(2-metilpiridin-4-il)furan-2-karboksamid; N-(5-(furan-3-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(3-fluoropiperidin-1-il)-2-morfolinooksazolo [4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(4-hidroksipiperidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(4-fluoropiperidin-1-il)-2-morfolinooksazolo [4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; (S)-N-(5-(3-aminopiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; 2-(2-metilpiridin-4-il)-N-(2-morfolino-5-(1H-pirazol-4-il)tiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; N-(5-(6-fluoropiridin-3-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(3-hidroksi-8-azabiciklo[3.2.1]octan-8-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(2-(3-hidroksipiperidin-1-il)-5-(piperidin-1-il)tiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; 2-(2-acetamidopiridin-4-il)-N-(5-(4-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; N-(2-(3-hidroksipiperidin-1-il)-5-(4-hidroksipiperidin-1-il)tiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; 2-(2-acetamidopiridin-4-il)-N-(5-(3-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid; 2-(2-aminopiridin-4-il)-N-(5-(3-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid hidroklorid; 5-(2-aminopiridin-4-il)-N-(5-(4-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)furan-3-karboksamid hidroklorid; 2-(2-aminopiridin-4-il)-N-(5-(4-hidroksipiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid hidroklorid; 2-(2-aminopiridin-4-il)-N-(5-(4-fluoropiperidin-1-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)oksazol-4-karboksamid hidroklorid; N-(5-(2-fluoropiridin-4-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(4-fluoropiperidin-1-il)-2-(3-hidroksipiperidin-1-il)tiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid; N-(5-(4-aminopiperidin-1-il)-2-(3-hidroksipiperidin-1-il)tiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid hidroklorid;i N-(5-(2-hidroksipiridin-4-il)-2-morfolinotiazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)oksazol-4-karboksamid hidroklorid; ili njegova farmaceutski prihvatljiva sol.
16. Spoj za uporabu prema zahtjevu 1, pri čemu je spoj [image] ili njegova farmaceutski prihvatljiva sol.
17. Spoj za uporabu prema zahtjevu 1, pri čemu je spoj [image]
18. Spoj za uporabu prema zahtjevu 1, pri čemu je spoj [image] ili njegova farmaceutski prihvatljiva sol.
19. Spoj za uporabu prema zahtjevu 1, pri čemu je spoj [image]
20. Spoj za uporabu prema bilo kojem od prethodnih zahtjeva, pri čemu je AML naznačen mutacijom u FLT3 genu.
21. Spoj za uporabu prema zahtjevu 20, pri čemu je mutacija interna tandem duplikacija (ITD).
22. Spoj za uporabu prema zahtjevu 20, pri čemu je mutacija D835H, D835V, D835Y, K663Q, N841L, ili F691L mutacija.
23. Spoj za uporabu prema zahtjevu 20, pri čemu mutacija je mutacija D835Y.
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