HRP20130220T1 - Modulatori indolamin 2,3-dioksigenaze i postupci upotrebe istih - Google Patents

Modulatori indolamin 2,3-dioksigenaze i postupci upotrebe istih Download PDF

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Publication number
HRP20130220T1
HRP20130220T1 HRP20130220TT HRP20130220T HRP20130220T1 HR P20130220 T1 HRP20130220 T1 HR P20130220T1 HR P20130220T T HRP20130220T T HR P20130220TT HR P20130220 T HRP20130220 T HR P20130220T HR P20130220 T1 HRP20130220 T1 HR P20130220T1
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HR
Croatia
Prior art keywords
amino
methyl
fluorophenyl
hydroxyimino
bromo
Prior art date
Application number
HRP20130220TT
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English (en)
Inventor
Andrew P. Combs
Eddy. W. Yue
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Incyte Corporation
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Family has litigation
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Application filed by Incyte Corporation filed Critical Incyte Corporation
Publication of HRP20130220T1 publication Critical patent/HRP20130220T1/hr

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/4245—Oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Claims (38)

1. Spoj formule: [image] ili njegova farmaceutski prihvatljiva sol, naznačena time da: W, X1 i X2 su nezavisno odabrani od (CRaRb)t, (CRaRb)uO(CRaRb)v, (CRaR0)uC(O)(CRaRb)v, (CRaRb)uC(O)NRc(CRaRb)v, (CRaRb)uC(O)O(CRaRb)v, (CRaRb)uC(S)(CRaRb)v, (CRaRb)uC(S)NRc(CRaRb)v, (CRaRb)uS(O)(CRaRb)v, (CRaRb)uS(O)NRc(CRaRb)v, (CRaRb)uS(O)2(CRaRb)v, (CRaRb)uS(O)2NRc(CRaRb)v, (CRaRb)uNRc(CRaRb)v i (CRaRb)uC(=NRd)NRc(CRaRb)v; R2 predstavlja H, C1-6 alkil ili C3-7 cikloalkil; R3a i R5a su nezavisno odabrani od C1-8 alkila, C2-8 alkenila, C2-8 alkinila, arila, cikloalkila, heteroarila i heterocikloalkila od kojih svaki može biti izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, Cy1, CN, NO2, ORel, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rh1, NRg1C(O)ORe1, C(=NR)NRg1Rh1, NRglC(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1; R3b predstavlja aril ili heteroaril od kojih svaki može biti izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy2, CN, NO2, ORel, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRglRh1, NRg1C(O)NRg1Rgl, NRg1Rh1, NRglC(O)Rh1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)OR ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1; R5b predstavlja H, C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil, gdje je svaki spomenuti C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rh1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)R11, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRglRh1; Cy1 i Cy2 su nezavisno odabrani od arila, heteroarila, cikloalkila i heterocikloalkila od kojih svaki može biti izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-4 alkila, C2-4 alkenila, C2-4 alkinila, C1-4 haloalkila, CN, NO2, ORe3, SRc3, C(O)Rf3, C(O)NRg3Rh3, C(O)ORe3, OC(O)Rf3, OC(O)NRg3Rh3 NRg3Rh3, NRg3C(O)Rh3, NRg3C(O)ORg3, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRglRh1, P(Rf3)2, P(ORe3)2, P(O)Re3Rf3, P(O)ORe3ORf3, S(O)Rf3, S(O)NRg3Rh3, S(O)2Rf3 i S(O)2NRg3Rh3; Ra i Rb su nezavisno odabrani od H, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, cikloalkilalkila, heteroarilalkila, heterocikloalkilalkila, CN, NO2, ORe4, SRe4, C(O)Rf4, C(O)NRg4R, C(O)ORe4, OC(O)Rf4, OC(O)NRg4Rh4, NRg4Rh4, NR94C(O)Rh4, NRg4C(O)ORe4, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf4)2, P(ORe4)2, P(O)Re4Rf4, P(O)ORe4ORf4, S(O)Rf4, S(O)NRg4Rh4, S(O)2R i S(O)2NRg4Rh4; Rc predstavlja H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, arilalkil ili cikloalkilalkil; Rd predstavlja H, ORd1, CN ili NO2; Rd1 predstavlja H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, arilalkil ili cikloalkilalkil; Re1, Re3 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; Rf1, Rf3 i Rf4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila i heterocikloalkila; Rg1, Rg3 i Rg4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila; Rh1, Rh3 i Rh4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila; ili Rgl i Rhl zajedno s atomom dušika za koji su vezani formiraju heterocikloalkilnu skupinu s 4, 5, 6 ili 7 članova; ili Rg3 i Rh3 zajedno s atomom dušika za koji su vezani formiraju heterocikloalkilnu skupinu s 4, 5, 6 ili 7 članova; ili Rg4 i Rh4 zajedno s atomom dušika za koji su vezani formiraju heterocikloalkilnu skupinu s 4, 5, 6 ili 7 članova; Ri predstavlja H, CN ili NO2; a predstavlja 0 ili 1; b predstavlja 0 ili 1; n predstavlja 0 ili 1; p predstavlja 0 ili 1; t predstavlja 1, 2, 3, 4, 5 ili 6; u predstavlja 0, 1, 2, 3, 4, 5 ili 6; i v predstavlja 0, 1, 2, 3, 4, 5 ili 6.
2. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da n predstavlja 0.
3. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da p predstavlja 1.
4. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da R50 predstavlja H.
5. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da R3b predstavlja fenil izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, Cy2, CN, NO2, ORe1, SRel, C(O)Rh1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rh1, NRg1C(O)ORe1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rh1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1.
6. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da i a i b predstavljaju 0.
7. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da a predstavlja 0.
8. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da b predstavlja 1.
9. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da R3b predstavlja heteroaril izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halogo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, Cy2, CN, NO2, ORe1, SRel, C(O)Rf1, C(O)NRglRh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rhl, NRg1C(O)NRglRh1, NRg1Rhl NRg1C(O)Rh1, NRglC(O)ORe1, P(Rf1)2, P(ORe1)2, P(O)RelRf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRglRh1, S(O)2Rf1 i S(O)2NRg1Rh1.
10. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da W predstavlja (CRaRb)t ili (CRaRb)uO(CRaRb)v.
11. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da R2 predstavlja H.
12. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, naznačen time da n predstavlja 0.
13. Spoj prema patentnom zahtjevu 12 ili njegova farmaceutski prihvatljiva sol, naznačen time da p predstavlja 1.
14. Spoj prema patentnom zahtjevu 13 ili njegova farmaceutski prihvatljiva sol, naznačen time da R5b predstavlja H.
15. Spoj prema patentnom zahtjevu 14 ili njegova farmaceutski prihvatljiva sol, naznačen time da W predstavlja (CRaRb)t ili (CRaRb)uO(CRaRb)v.
16. Spoj prema patentnom zahtjevu 15 ili njegova farmaceutski prihvatljiva sol, naznačen time da a predstavlja 0.
17. Spoj prema patentnom zahtjevu 16 ili njegova farmaceutski prihvatljiva sol, naznačen time da b predstavlja 0.
18. Spoj prema patentnom zahtjevu 17 ili njegova farmaceutski prihvatljiva sol, naznačen time da R3b predstavlja fenil izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRglRh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRglC(O)Rf1, NRglC(O)ORe1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rhl, S(O)2Rf1 i S(O)2NRglRh1.
19. Spoj prema patentnom zahtjevu 15 ili njegova farmaceutski prihvatljiva sol, naznačen time da b predstavlja 1.
20. Spoj prema patentnom zahtjevu 19 ili njegova farmaceutski prihvatljiva sol, naznačen time da R3b predstavlja heteroaril izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRglRh1, NRg1Rh1 NRglC(O)Rh1, NRg1C(O)ORf1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1.
21. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da i n i p predstavljaju 0.
22. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da X1 predstavlja (CRaRb)t, (CRaRb)uC(O)(CRaRb)v, (CRaRb)uC(O)NRc(CRaRb)v ili (CRaRb)uC(O)O(CRaRb)v.
23. Spoj prema patentnom zahtjevu 1 formule: [image] ili njegova farmaceutski prihvatljiva sol, naznačen time da: X1 predstavlja (CRaRb)t ili (CRaRb)uC(O)(CRaRb)v; R3b predstavlja C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil od kojih svaki može biti izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy1, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1; R3b predstavlja aril ili heteroaril od kojih svaka može biti izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-6alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1; R5b predstavlja H, C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil, gdje je svaki spomenuti C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil , heteroaril ili heterocikloalkil izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rf1, NRhg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2ORf1 i S(O)2NRg1Rh1; Cy1 i Cy2 su nezavisno odabrani od arila, heteroarila, cikloalkila i heterocikloalkila od kojih svaki može biti izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-4 alkila, C2-4 alkenila, C2-4aikinila, C1-4 haloalkila, CN, NO2, ORe, SRe3, C(O)Re3, C(O)NRg3Rh3, C(O)ORe3, OC(O)Rf3, OC(O)NRg3Rh3, NRg3Rh3, NRg3C(O)Rh3, NRg3C(O)ORe3, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf3)2, P(ORe3)2, P(O)Re3Rf3, P(O)ORe3ORf3, S(O)Rf3, S(O)NRg3Rh3, S(O)2ORf3 i S(O)2NRg3Rh3; Ra i Rb su nezavisno odabrani od H, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, cikloalkilalkila, heteroarilalkila, heterocikloalkilalkila, CN, NO2, ORe4, SRe4, C(O)Rf4, C(O)NRg4Rh4, C(O)ORe4, OC(O)Rf4, OC(O)NRg4Rh4, NRg4Rh4, NRg4C(O)Rh4, NRg4C(O)ORe4, C(=NRi)NRg4Rh4, NRg1C(=NRi)NRg1Rh1, P(Rf4)2, P(ORe4)2, P(O)R4Rf4, P(O)ORe4ORf4, S(O)Rf4, S(O)NRg4Rh4, S(O)2Rf4 i S(O)2NRg4Rh4; Re1, Re3 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, helerocikloalkila, arilalkila, cikloalkilalkila, heteroarilalkila i heterocikloalkilatkila; Rf1, Rf3 i Rf4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila i heterocikloalkila; Rg1, Rg3 i Rg4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila; Rh1, Rh3 i Rh4 su nezavisno odabrani od H, C1-6alkila, C1-6haloalkila, C2-6alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila; ili Rg1 i Rh1 zajedno sa atomom dušika za koji su vezani formiraju heterocikloalkilnu skupinu s 4, S, 6 ili 7 članova; ili Rg3 i Rh3 zajedno sa atomom dušika za koji su vezani formiraju heterocikloalkilnu skupinu s 4, 5, 6 ili 7 članova ; ili Rg4 i Rh4 zajedno sa atomom dušika za koji su vezani formiraju heterocikloalkilnu skupinu s 4, 5, 6 ili 7 članova; Ri predstavlja H, CN ili NO2; a predstavlja 0 ili 1; t predstavlja 1, 2, 3, 4, 5 ili 6; u predstavlja 0, 1, 2, 3, 4, 5 ili 6; i v predstavlja 0, 1, 2, 3, 4, 5 ili 6.
24. Spoj prema patentnom zahtjevu 23 ili njegova farmaceutski prihvatljiva sol, naznačen time da R3a predstavlja C1-8 alkil.
25. Spoj prema patentnom zahtjevu 23 ili njegova farmaceutski prihvatljiva sol, naznačen time da R5b predstavlja H, aril ili heteroaril, gdje svaki spomenuti aril i heteroaril može biti izborno supstituiran s 1, 2, 3, 4 ili 5 supstituenata nezavisno odabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRglRh1, NRg1C(O)NRglRh1, NRglRh1, NRg1C(O)Rh1, NRglC(O)ORe1, C(=NRi)NRglRh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rfl, P(O)ORe1ORf1, S(O)Rf1, S(O)NRglRh1, S(O)2Rf1 i S(O)2NRglRh1.
26. Spoj prema patentnom zahtjevu 1, naznačen time da je odabran od: N-benzil-4-(benzilamino)-N-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; 4-[(anilinokarbonil)amino]-N-(3-klorofenil)-N-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; tert-butil {4-[({4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino)karbonil]benzil}karbamata; 4-(aminometil)-N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamida; 4-{[(benzilamino)karbonil]amino}-N-(3-bromo-4-fluorofenil)-N-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}morfolin-4-karboksamida; N-(3-bromo-4-fluorofenil)-N-hidroksi-4-(metilamino)-1,2,5-oksadiazol-3-karboksimidamida; N/-{4-[(E,Z)-[(3-bromo4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-4-karboksamida; tert-butil 4-{4-[({4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino)karbonil]benzil}piperazin-1-karboksilata; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazo1-3-il}-4-(piperazin-1-ilmetil)benzamida; 1-benzoil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-4-karboksamida; N(4)-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-N(1)-fenilpiperidin-1,4-dikarboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-etilpiperidin-4-karboksamida; 4-[(benzoilamino)metil]-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-cijanofenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-fenilpiperidin-4-karboksamida; N-(3-bromo-4-fluorofenil)-4-({4-[(1,1-dioksidotiomorfolin-4-il)metil]benzil}amino)-N-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; N-(3-bromo-4-fluorofenil)-N-hidroksi-4-{[4-(morfolin-4-ilmetil)benzil]amino}-1,2,5-oksadiazol-3-karboksimidamida; N-(3-cijano-4-fluorofenil)-4-({4-[(1,1-dioksidotiomorfolin-4-il)metil]benzil}amino)-N-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; N-(3-bromo-4-fluorofenil)-N-hidroksi-4-[(piridin-3-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamida; N-(3-cijano-4-fluorofenil)-N-hidroksi-4-[(piridin-4-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamida; 4-[(3-cijanobenzil)amino]-N-(3-cijano-4-fluorofenil)-N-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; N-(3-Bromo-4-fluorofenil)-N-hidroksi-4-[(1H-tetrazol-5-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamida; N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}ciklopentankarboksamida; N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metilj-1,2,5-oksadiazol-3-il}nikotinamida; N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metilj-1,2,5-oksadiazol-3-il}izonikotinamida; N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metoksibenzamida; N-{4-[(E,Z)-[(3-klorofenil)arnino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il)-3-metoksibenzamida; N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metoksibenzamida; 2-kloro-N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamida; 3-kloro-N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamida; 4-kloro-N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamida; N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,3-dimetilbutanamida; N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-jodobenzamida; N-{4-[(E,Z)-[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-cijanobenzamida; N-{4-[(E,Z)-{[4-fluoro-3-(trifluorometil)fenil]amino}(hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamida; N-{4-[(E,Z)-{[4-fluoro-3-(trifluorometil)fenil]amino}(hidroksiimino)metil]-1,2,5-oksadiazol-3-il}izonikotinamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}izonikotinamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-cijanobenzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-cijanobenzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-naftamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-naftamida; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-iI}piperidin-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-furamida; N-{4-[(E,Z)-(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}tiofen-2-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-fenil-5-(trifluorometil)-1H-pirazol-4-karboksamida; 4-(acetilamino)-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid tert-butil {4-[({4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino)karbonil]benzil}karbamat N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-benzotiofen-2-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,3-tiazol-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-benzotiofen-3-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}tiofen-3-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1H-imidazol-2-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-1,2,3-tiadiazol-5-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,2,3-tiadiazol-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,1-benzizoksazol-3-karboksamida; 4-(aminometil)-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; N-(3-bromo-4-fluorofenil)-N'-hidroksi-4-({[(2-feniletil)amino]karbonil}amino)-1,2,5-oksadiazol-3-karboksimidamida; N-(3-bromo-4-fluorofenil)-4-{[(ciklopentilamino)karbonil]amino}-N'-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; N-(3-bromo-4-fluorofenil)-4-({[(3-cijanofenil)amino]karbonil}amino)-N'-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-tert-butil-1-metil-1H-pirazol-5-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metoksiacetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}ciklopentankarboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}butanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metilpropanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}propanamida; N-{4-[(E,Z)-(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}cikloheksankarboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1H-benzimidazol-5-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino]{hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-fenoksiacetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}ciklobutankarboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-metilbutanamida; /V-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazo1-3-il}-3-piridin-3-ilpropanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}kinolin-6-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-klorofenoksi)acetamida; N-{4-[(E,Z)-(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-bromofenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3il}-2-(4-fluorofenoksi}acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-tert-butilfenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-klorofenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3,4-diklorofenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-naftiloksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2,3-diklorofenoksi)acetamida; N-{4-[(E,Z)-(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-klorofenoksi)-2-metilpropanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-klorofenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-metoksifenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-metoksifenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-metoksifenoksi)acetamida; benzil {4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazo!-3-ii}karbamata; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-1-karboksamida; N-(3-bromo-4-fluorofenil)-4-({[(3-cijanofenil)(metil)amino]karbonil}amino)-N'-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; 4-({[benzil(metil)amino]karbonil}amino)-N-(3-bromo-4-fluorofenil)-N-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-feniiacetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-metoksifenil)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-metoksifenil)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-metoksifenil)acetamida; N-{4-[(E,Z)-[(3-bromo4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-cijanobenzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-bromofenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-bromofenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-klorofenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-klorofenil) propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]1,2,5-oksadiazol-3-il)-3-(2-fiuorofenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-fluorofenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(2-klorofenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-metilfenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-(trifluorometil)fenil)propanamida; N-{4-[(E,Z)-[(3-bromo4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-fluorofenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(2-metoksifenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-metoksifenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-metoksifenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino]hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-metilfenil)propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofeniI)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-[4- (trifluorometil)fenil]propanamida; 3-[2,5-bis(trifluorometil)fenil)-N-{4-[(£>Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}propanamida; 3-[3,5-bis(trifluorometil)fenil]-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}propanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metil-3-fenilpropanamida; 2-benzil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,3-dimetilbutanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-[4-(trifluorometil)pirimidin-2-il]piperidin-4-karboksamida; 1-benzil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-tert-butil-1H-pirazol-5-karboksamida; 2-(benziloksi)-N-{4-[(E,Z)-[{3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-(4-klorofenil)ciklopentankarboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-fenoksibenzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,4,6-triklorobenzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metoksibenzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-metoksibenzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,2-difenilacetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-(trifluorometoksi)benzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metoksibenzamida; N-{4-[(E,Z)-(3-bromo-4-fiuorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,4-dimetoksibenzamida; N-(4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-nitrofenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}bifenil-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2,6-diklorobenzil)-1,3-tiazol-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,6-dimetoksibenzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-nitrobenzamida; 5-bromo-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,3-dimetilbutanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino]{hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-tienil)acetamida: N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino]{hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-fenilbutanamida; N-{4-[{E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,2-dimetilpropanamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-(morfolin-4-ilmetil)benzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-[(1,1-dioksidotiomorfolin-4-il)metil]benzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-(fenilacetil)piperidin-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-(metilsulfonil)piperidin-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-piridin-4-il-1,3-tiazol-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-nitrobenzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-ii}-3-nitrobenzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-izopropilpiperidin-4-karboksamida; tert-butil 4-{4-[({4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil)]-1,2,5-oksadiazol-3-il}amino)karbonil]-1,3-tiazol-2-il}piperidin-1-karboksilata; N-{4-[(E,Z)-[(3-bromo-4-fiuorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-ii}-2-fenil-1,3-tiazol-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metil-1,3-tiazol-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-piperidin-4-il-1,3-tiazol-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-cijanofenoksi)acetamida; tert-butil 3-[({4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino)karbonil]piperidin-1-karboksilata; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino]hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-nitrofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-nitrofenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-nitrofenoksi)acetamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-3-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-2-piridin-3-il-1,3-tiazol-5-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-1,3-tiazol-5-karboksamida; 2-amino-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,3-tiazol-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-2-pirazin-2-il-1,3-tiazol-5-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazo!-3-il}-4-metil-2-[4-(trifluorometil)fenil]-1,3-tiazol-5-karboksamida; N-{4-[(E,Z)-[(3-bromo4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,4-dimetil-1,3-tiazol-5-karboksamida; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}pirolidin-2-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fiuorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1.5-dimetil-1H-pirazoi-3-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-5-kloro-1-metil-1H-pirazol-4-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,3-dimetil-1H-pirazol-5-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-metil-1H-imidazol-2-karboksamida; 4-[(acetilamino)metil]-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metilpiperidin-4-karboksamida; 1-acetil-N-{4-[(E,Z)-(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-3-karboksamida; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazoi-3-il}-4-metilpiperidin-4-karboksamida; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino)(hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-fenilpiperidin-4-karboksamida; 4-(benzilamino)-N-(3-bromo-4-fluorofenil)-N'-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-etilpiperidin-3-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-etilpiperazin-1-karboksamida; 4-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperazin-1-karboksamida; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(1-etilpiperidin-4-il)-1,3-tiazol-4-karboksamida; N-(3-bromo-4-fluorofenil)-N-hidroksi-4-[(1,3-tiazol-4-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamida; N-(3-bromo-4-fluorofenil)-4-[(4-cijanobenzil)amino]-N-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; N-(3-bromo-4-fluorofenil)-N'-hidroksi-4-{[(1-metilpiperidin-4-il)metil]amino}-1,2,5-oksadiazol-3-karboksimidamida; N-(3-bromo-4-fluorofenil)-N-hidroksi-4-{[4-(piperazin-1-ilmetil)benzil]amino}-1,2,5-oksadiazol-3-karboksimidamida; N-(3-bromo-4-fluorofenil)-4-({4-[(4-etilpiperazin-1-il)metil]benzil}amino)-N'-hidroksi-1,2,5-oksadiazol-3-karboksimidamida; N-(3-bromo-4-fluorofenil)-N'-hidroksi-4-[(piridin-4-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamida; i N-(3-bromo-4-fluorofenil)-4-[(3-cijanobenzil)amino]-N-hidroksi-1,2,5-oksadiazol-3-karboksimidamida ili njihove farmaceutski prihvatljive soli.
27. Spoj prema patentnom zahtjevu 1, naznačen time da je odabran od: N-{4-[[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-fenilacetamida; N-{4-[[(3-klorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamida; i N-{4-[(benzilamino)(hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamida; ili njihove farmaceutski prihvatljive soli.
28. Farmaceutski sastav, naznačen time da sadrži spoj prema bilo kojem patentnom zahtjevu od 1 do 27 ili njegovu farmaceutski prihvatljivu sol i farmaceutski prihvatljivi nosač.
29. Metoda za modulaciju aktivnosti indolamin 2,3-dioksigenaze, naznačena time da obuhvaća kontakt spomenute indolamin 2,3-dioksigenaze ex vivo sa spojem prema bilo kojem patentnom zahtjevu od 1 do 27 ili s njegovom farmaceutski prihvatljivom soli ili farmaceutskim sastavom prema patentnom zahtjevu 28.
30. Metoda prema patentnom zahtjevu 29, naznačena time da navedena modulacija predstavlja inhibiciju.
31. Spoj prema bilo kojem patentnom zahtjevu od 1 do 27 ili njegova farmaceutski prihvatljiva sol ili farmaceutski sastav prema patentnom zahtjevu 28, naznačen time da se koristi u inhibiciji imunosupresije kod pacijenta.
32. Spoj prema bilo kojem patentnom zahtjevu od 1 do 27 ili njegova farmaceutski prihvatljiva sol ili farmaceutski sastav prema patentnom zahtjevu 28, naznačen time da se koristi u liječenju raka, virusne infekcije, depresije, neurodegenerativnog poremećaja, traume, staračke katarakte, odbacivanja transplantiranog organa ili autoimune bolesti pacijenta.
33. Spoj, sol ili sastav prema patentnom zahtjevu 32, naznačen time da se koristi za liječenje raka kod pacijenta.
34. Spoj, sol ili sastav prema patentnom zahtjevu 32, naznačen time da je spomenuti rak odabran od raka kolona, raka gušterače, raka dojke, raka prostate, raka pluća, raka mozga, raka jajnika, raka vrata materice, raka testisa, raka bubrega, raka glave i vrata, limfoma, leukemije i melanoma.
35. Spoj, sol ili sastav prema patentnom zahtjevu 32, naznačen time da se koristi u kombinaciji s cjepivom protiv raka, protuvirusnim sredstvom, kemoterapeutikom, imunosupresantom, zračenjem, cjepivom protiv tumora, cjepivom protiv virusa, terapijom citokinima ili inhibitorom tirozin kinaze.
36. Spoj, sol ili sastav prema patentnom zahtjevu 35, naznačen time da spomenuta terapija citokinima predstavlja terapiju s IL-2.
37. Spoj, sol ili sastav prema patentnom zahtjevu 35, naznačen time da spomenuti kemoterapeutik predstavlja citotoksični agens.
38. Spoj, sol ili sastav prema patentnom zahtjevu 32, naznačen time da se koristi u kombinaciji s anti-CTLA-4 antitijelom.
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