ME02461B - Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih - Google Patents

Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih

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Publication number
ME02461B
ME02461B MEP-2016-96A MEP9616A ME02461B ME 02461 B ME02461 B ME 02461B ME P9616 A MEP9616 A ME P9616A ME 02461 B ME02461 B ME 02461B
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ME
Montenegro
Prior art keywords
amino
methyl
fluorophenyl
oxadiazol
bromo
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MEP-2016-96A
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English (en)
Inventor
Andrew P Combs
Eddy W Yue
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Incyte Holdings Corp
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Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of ME02461B publication Critical patent/ME02461B/me

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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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    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
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Claims (14)

1. Jedinjenje formuleili njegova farmaceutski prihvatljiva so, za upotrebu u tretmanu kancera u kombinaciji sa anti-PD-1 antitelom gde su: W, X1, i X2 nezavisno izabrani od (CRaRb)t, (CRaRb)uO(CRaRb)v, (CRaRb)uC(O)(CRaRb)v, (CRaRb)uC(O)NRc(CRaRb)v, (CRaRb)uC(O)O(CRaRb)v, (CRaRb)uC(S)(CRaRb)u, (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 je H, C1-6 alkil ili C3-7 cikloalkil;R3a i R5a su nezavisno izabrani od C1-8 alkila, C2-8 alkenila, C2-8 alkinila, arila, cikloalkila, heteroarila i heterocikloalkila, svaki opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, 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 je aril ili heteroaril svaki opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih 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, 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;R5b je H, C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil gde su spomenuti C1-8 alkil, C2-8 alkenil, C2-5 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil opciono supstituisani sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenilaC2-6 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, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRh1R, 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;Cy1 i Cy2 su opciono izabrani od arila, heteroarila, cikloalkila i heterocikloalkila, svaki supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-4 alkila, C2-4 alkenila, C2-4 alkinila, C1-4 haloalkila, CN, NO2, ORe3, SRe3, C(O)Rf3, 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)2Rf3 i S(O)2NRg3Rh3;Ra i Rb su nezavisno izabrani 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)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf4)2, P(ORe4)2, P(O)Re4Rf4, P(O)ORe4ORf4, S(O)Rf4, S(O)NRg4Rh4, S(O)2Rf4 i S(O)2NRg4Rh4;Rc je H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila ili cikloalkilalkila;Rd je H, ORd1, CN ili NO2;Rd1 je H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, arilalkil ili cikloalkilalkil;Rel, Re3 i R64 su nezavisno izabrani 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 izabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila i heterocikloalkila;Rg1, Rg3 i Rg4 nezavisno su izabrani od H, C1-6 alkil, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila;Rh1, Rh3 i Rh4 su nezavisno izabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila;ili Rg1 i Rh1 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu;ili Rg3 i Rh3 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu;ili Rg4 i Rh4 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu;Ri je H, CN ili NO2;a je 0 ili 1;b je 0 ili 1;n je 0 ili 1;p je 0 ili 1;t je 1, 2, 3, 4, 5 ili 6;u je 0, 1, 2, 3, 4, 5 ili 6; iv je 0, 1, 2, 3, 4, 5 ili 6.
2. Jedinjenje ili so za upotrebu prema zahtevu 1, pri čemu R2 jeste H.
3. Jedinjenje ili so za upotrebu prema zahtevu 2, pri čemu n jeste 0.
4. Jedinjenje ili so za upotrebu prema zahtevu 3, pri čemu p jeste 1.
5. Jedinjenje ili so za upotrebu prema zahtevu 4, pri čemu R5b jeste H.
6. Jedinjenje ili so za upotrebu prema zahtevu 5, pri čemu a jeste 0.
7. Jedinjenje ili so za upotrebu prema zahtevu 6, pri čemu b jeste 0.
8. Jedinjenje ili so za upotrebu prema zahtevu 7, pri čemu R3b jeste fenil opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C1-6 alkinila, C1-4 haloalkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1, P(Rf1)2, P(ORe1)2, P(O)Re1Rt1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)1Rf1 i S(O)2NRg1Rh1.
9. Jedinjenja ili so za upotrebu prema zahtevu 6, pri čemu b jeste 1.
10. Jedinjenja ili so za upotrebu prema zahtevu 9, pri čemu W jeste (CRaRb)t ili (CRaRb)uO(CRaRb)v.
11. Jedinjenje ili so za upotrebu prema zahtevu 10, pri čemu R3b je heteroaril, opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih 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)NRg1Rh1, Ng1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1 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.
12. Jedinjenje ili so za upotrebu prema zahtevu 1, pri čemu jedinjenje ima formulu: gde je: X1 (CRaRb)t ili (CRaRb)uC(O)(CRaRb)v; R3a je C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil, svaki opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih 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)ORe1Rf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1; R3b je aril ili heteroaril, svaki opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih 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, 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; R5b je H, C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil; gde su spomenuti C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil svaki opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih 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, NRg1R , NRg1C(O)Rf1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe10Rf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1; Cy1 i Cy2 su nezavisno izabrani kao aril, heteroaril, cikloalkil i heterocikloalkil, svaki opciono supstituisan sa 1, 2, 3,4 ili 5 supstituenata nezavisno izabranih od halo, C1-4 alkila, C2-4 alkenila, C2-4 alkinila, C1-4 haloalkila, CN, NO2, ORe3, SRe3, C(O)Rf3, 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)zRf3 i S(O)2NRg3Rh3; Ra i Rb su nezavisno izabrani 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)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf4)2, P(ORe4)2 P(O)Re4Rf4, P(O)ORe4ORf4, S(O)Rf4, S(O)NRg4Rh4, S(O)2Rf4 i S(O)2NRg4Rh4; Re1, Re3 i Re4 su nezavisno izabrani 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 izabrani 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 izabrani 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 izabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila; ili Rg1 i Rh1 zajedno sa N atomom za koji su vezani, formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu; ili Rg3 i Rh3 zajedno sa N atomom za koji su vezani, formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu; ili Rg4 i Rh4 zajedno sa N atomom za koji su vezani, formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu; Ri je H, CN ili NO2; a je 0 ili 1; t je 1, 2, 3, 4, 5 ili 6; u je 0, 1, 2, 3, 4, 5 ili 6; i v je 0, 1, 2, 3, 4, 5 ili 6.
13. Jedinjenje ili so za upotrebu prema zahtevu 1, pri čemu je jedinjenje izabrano od: N-benzil-4-(benzilamino)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; 4-[(anilinokarbonil)amino]-N-(3-hlorofenil)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; Terc-butil{4-[({4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino)karbonil]benzil} karbamat; 4-(aminometil)-N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; 4-{[(benzilamino)karbonil]amino}-N-(3-bromo-4-fluorofenil)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}morfolin-4-karboksamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-(metilamino)-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-4-karboksamid; Terc-butil4-{4-[({4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino) karbonil]benzil}piperazin-1-karboksilat; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-(piperazin-1-ilmetil) benzamid; 1-benzoil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin- 4-karboksamid; N(4)-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-N(1)-fenilpiperidin- 1,4-dikarboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-etilpiperidin-4- karboksamid; 4-[(benzoilamino)metil]-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol- 3-il}benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-cijanofenoksi) acetamid; N-{4-[(E,Z-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-fenilpiperidin-4-karboksamid; N-(3-bromo-4-fluorofenil)-4-({4-[(1,1-dioksidotiomorfolin-4-il)metil]benzil}amino)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-{[4-(morfolin-4-ilmetil)benzil]amino}-1,2,5-oksadiazol-3-karboksimidamid; N-(3-cijano-4-fluorofenil)-4-({4-[(1,1-dioksidotiomorfolin-4-il)metil]benzil}amino)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-[(piridin-3-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamid; N-(3-cijano-4-fluorofenil)-N’-hidroksi-4-[(piridin-4-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamid; 4-[(3-cijanobenzil)amino]-N-(3-cijano-4-fluorofenil)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-[(1H-tetrazol-5-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}ciklopentankarboksamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il} izonikotinamid; N-{4-[(E,Z-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metoksibenzamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-metoksibenzamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metoksibenzamid; 2-hloro-N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; 3-hloro-N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; 4-hloro-N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,3-dimetilbutanamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-jodobenzamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-cijanobenzamid; N-{4-[(E,Z)-{[4-fluoro-3-(trifluorometil)fenil]amino}(hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamid; N-{4-[(E,Z-{[4-fluoro-3-(trifluorometil)fenil]amino}(hidroksiimino)metil]-1,2,5-oksadiazol-3-il}izonikotinamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il} izonikotinamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-cijanobenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-cijanobenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-naftamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-naftamid; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-furamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}tiofen-2-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-fenil-5-(trifluorometil)- 1H-pirazol-4-karboksamid; 4-(acetilamino)-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid Terc-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-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,3-tiazol-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-benzotiofen-3-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}tiofen-3-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1H-imidazol-2-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-1,2,3-tiadiazol-5-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,2,3-tiadiazol-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,1-benzizoksazol-3-karboksamid; 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-karboksimidamid; N-(3-bromo-4-fluorofenil)-4-{[(ciklopentilamino)karbonil]amino}-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-4-({[(3-cijanofenil)amino]karbonil}amino)-N’-hidroksi-1,2,5-oksadiazol-3 -karboksimidamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-terc-butil-1-metil-1H-pirazol-5 -karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metoksiacetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}ciklopentankarboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}butanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metilpropanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}cikloheksankarboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1H-benzimidazol-5-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-fenoksiacetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}ciklobutankarboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-metilbutanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-piridin-3-ilpropanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}kinolin-6-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-hlorofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-bromofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-fluorofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-terc-butilfenoksi) acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-hlorofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3,4-dihlorofenoksi) acetamid; 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-dihlorofenoksi) acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-hlorofenoksi)-2-metilpropanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-hlorofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-metoksifenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-metoksifenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-metoksifenoksi)acetamid; Benzil {4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}karbamat; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-1-karboksamid; N-(3-bromo-4-fluorofenil)-4-({[(3-cijanofenil)(metil)amino]karbonil}amino)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; 4-({[benzil(metil)amino]karbonil}amino)-N-(3-bromo-4-fluorofenil)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-fenilacetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-metoksifenil)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-metoksifenil)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-metoksifenil)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-cijanobenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-bromofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-bromofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-hlorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-hlorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(2-fluorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-fluorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(2-hlorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-metilfenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-(trifluorometil)fenil) propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-fluorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(2-metoksifenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-metoksifenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-metoksifenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-metilfenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-[4-(trifluorometil)fenil] propanamid; 3-[2,5-bis(trifluorometil)fenil]-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}propanamid; 3-[3,5-bis(trifluorometil)fenil]-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metil-3-fenilpropanamid; 2-benzil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,3-dimetilbutanamid; 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-karboksamid; 1-benzil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-terc-butil-1H-pirazol-5-karboksamid; 2-(benziloksi)-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-(4-hlorofenil)ciklopentan karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-fenoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,4,6-trihlorobenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-metoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,2-difenilacetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-(trifluorometoksi)benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,4-dimetoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-nitrofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}bifenil-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2,6-dihlorobenzil)-1,3-tiazol-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,6-dimetoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-nitrobenzamid; 5-bromo-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,3-dimetilbutanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-tienil)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-fenilbutanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,2-dimetilpropanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-(morfolin-4-ilmetil)benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-[(1,1-dioksidotiomorfolin- 4-il)metil]benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-(fenilacetil)piperidin-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-(metilsulfonil)piperidin-4-karboksamid; 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-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-nitrobenzamid; N-(4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-nitrobenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-izopropilpiperidin-4-karboks amid; Terc-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-karboksilat; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-fenil-1,3-tiazol-4-karboks amid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metil-1,3-tiazol-4-karboks amid; 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-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-cijanofenoksi)acetamid; Terc-butil 3-[({4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino)karbonil] piperidin-1-karboksilat; 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)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-nitrofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-3-karboksamid; 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-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-1,3-tiazol-5-karboks amid; 2-amino-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,3-tiazol-4-karboks amid; 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-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-2-[4-(trifluorometil) fenil]-1,3-tiazol-5-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,4-dimetil-1,3-tiazol-5-karboksamid; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}pirolidin-2-karboks amid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,5-dimetil-1H-pirazol-3-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-5-hloro-1-metil-1H-pirazol-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,3-dimetil-1H-pirazol-5-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-metil-1H-imidazol-2-karboksamid; 4-[(acetilamino)metil]-N-{4-[(E,Z-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3- il}benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metilpiperidin-4-karboks amid; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-3-karboks amid; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metilpiperidin- 4-karboksamid; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-fenilpiperidin- 4-karboksamid; 4-(benzilamino)-N-(3-bromo-4-fluorofenil)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-etilpiperidin-3-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-etilpiperazin-1-karboksamid; 4-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperazin-1-karboks amid; 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-karboksamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-[(1,3-tiazol-4-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-4-[(4-cijanobenzil)amino]-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-{[(1-metilpiperidin-4-il)metil]amino}-1,2,5-oksadiazol-3 -karboksimidamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-{[4-(piperazin-1-ilmetil)benzil]amino}-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-4-({4-[(4-etilpiperazin-1-il)metil]benzil}amino)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimid amid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-[(piridin-4-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamid; i N-(3-bromo-4-fluorofenil)-4-[(3-cijanobenzil)amino]-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-fenilacetamid; N-{4-[[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; i N-{4-[(benzilamino)(hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; ili njihove farmaceutski prihvatljive soli.
14. Jedinjenje ili so za upotrebu prema zahtevu 1, pri čemu je spomenuti kancer izabran od kancera debelog creva, pankreasa, kancera dojke, kancera prostate, kancera pluća, kancera mozga, kancera jajnika, cervikalnog kancera, kancera testisa, kancera bubrega, kancera glave i vrata, limfoma, leukemije i melanoma.
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Families Citing this family (261)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2473521C (en) * 2002-01-22 2014-04-15 Biomatera Inc. Method of drying biodegradable polymers
ATE398616T1 (de) * 2005-02-04 2008-07-15 Ctg Pharma S R L Neue 4-aminochinolinderivate als antimalariamittel
WO2006088833A2 (en) 2005-02-14 2006-08-24 Wyeth Interleukin-17f antibodies and other il-17f signaling antagonists and uses therefor
ME02461B (me) 2005-05-10 2017-02-20 Incyte Holdings Corp Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih
GB0512091D0 (en) * 2005-06-14 2005-07-20 Novartis Ag Organic compounds
DE102005053947A1 (de) * 2005-11-11 2007-05-16 Univ Ernst Moritz Arndt Neue Arzneimittel
EP1971583B1 (en) 2005-12-20 2015-03-25 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
WO2007095050A2 (en) * 2006-02-09 2007-08-23 Incyte Corporation N-hydroxyguanidines as modulators of indoleamine 2,3-dioxygenase
MX2009002019A (es) 2006-08-24 2009-03-09 Novartis Ag Derivados de 2-(pirazin-2-il)-tiazol y 2-(1h-pirazol-3-il)-tiazol asi como compuestos relacionados como inhibidores de la estearoil-coa-desaturasa (scd) para el tratamiento de trastornos metabolicos, cardiovasculares, y otros.
US20080125470A1 (en) * 2006-09-19 2008-05-29 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
US20080146624A1 (en) * 2006-09-19 2008-06-19 Incyte Corporation Amidines as modulators of indoleamine 2,3-dioxygenase
CL2007002650A1 (es) * 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
CA2662574A1 (en) 2006-09-22 2008-03-27 Novartis Ag Heterocyclic organic compounds
US20080182882A1 (en) * 2006-11-08 2008-07-31 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
MX2009006728A (es) 2006-12-20 2009-09-09 Novartis Ag Heterociclos de 5 miembros 2-sustituidos como inhibidores de scd.
WO2008115804A1 (en) * 2007-03-16 2008-09-25 Lankenau Institute For Medical Research Novel ido inhibitors and methods of use thereof
US20090170842A1 (en) 2007-11-14 2009-07-02 University Of Kansas Brca1-based breast or ovarian cancer prevention agents and methods of use
EP2227233B1 (en) * 2007-11-30 2013-02-13 Newlink Genetics Ido inhibitors
US20090253706A1 (en) * 2008-04-03 2009-10-08 Muller Alexander J Methods and Compositions for the Treatment of Rheumatoid Arthritis and Other Inflammatory Diseases
HRP20180282T1 (hr) 2008-04-17 2018-03-23 Io Biotech Aps Imunoterapija na bazi indoleamin 2, 3-dioksigenaze
SG10201805844QA (en) * 2008-07-08 2018-08-30 Incyte Holdings Corp 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
MX2012003377A (es) 2009-09-25 2012-05-08 Bayer Cropscience Ag N-(1,2,5-oxadiazol-3-il)benzamidas y su utilizacion como herbicidas.
JP2012041325A (ja) * 2010-08-23 2012-03-01 Bayer Cropscience Ag オキサジアゾリノン誘導体およびその有害生物の防除用途
DK2654758T3 (en) 2010-12-22 2017-07-10 Idogen Ab A composition comprising at least two compounds which induce indolamine 2,3-dioxygenase (IDO) for the treatment of an autoimmune disorder or immune rejection of organs.
NO2694640T3 (me) 2011-04-15 2018-03-17
US9096583B2 (en) 2011-11-16 2015-08-04 Basf Se Substituted 1,2,5-oxadiazole compounds and their use as herbicides II
AU2012338748A1 (en) * 2011-11-18 2014-06-05 Basf Se Substituted 1,2,5-oxadiazole compounds and their use as herbicides III
KR101229365B1 (ko) * 2012-07-02 2013-02-18 대한민국 〔ｚ〕­ｎ­〔３­〔２，４­디플루오로페닐아미노〕­１­〔４­나이트로페닐〕­３­옥소프로프­１­엔­２­일〕­２­메톡시벤즈아마이드를 유효성분으로 함유하는 신경퇴행성 질환 예방 및 치료용 약학적 조성물
WO2014066834A1 (en) 2012-10-26 2014-05-01 The University Of Chicago Synergistic combination of immunologic inhibitors for the treatment of cancer
CN105377812B (zh) 2013-06-21 2018-09-18 组合化学工业株式会社 2-氨基-2-肟基-n-烷氧基亚氨代乙酰基氰化物的制备方法及其制备中间体
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
RU2536041C1 (ru) * 2013-10-11 2014-12-20 ФЕДЕРАЛЬНОЕ ГОСУДАРСТВЕННОЕ БЮДЖЕТНОЕ УЧРЕЖДЕНИЕ НАУКИ ИНСТИТУТ ОРГАНИЧЕСКОЙ ХИМИИ им. Н.Д. ЗЕЛИНСКОГО РОССИЙСКОЙ АКАДЕМИИ НАУК (ИОХ РАН) 3,3'-бис(фтординитрометил-onn-азокси)-4,4'-дифуразаниловый эфир и способ его получения
CA2929552C (en) * 2013-11-08 2022-05-17 Incyte Holdings Corporation Process for the synthesis of an indoleamine 2,3-dioxygenase inhibitor
CN103570727B (zh) 2013-11-12 2015-08-19 复旦大学 一种n-苄基色胺酮衍生物及其制备方法和应用
SMT201800643T1 (it) 2013-12-24 2019-01-11 Bristol Myers Squibb Co Composti triciclici come agenti anticancro
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
CN106535884A (zh) * 2014-06-06 2017-03-22 弗雷克萨斯生物科学公司 免疫调节剂
AU2015271709B2 (en) 2014-06-06 2020-11-26 Bristol-Myers Squibb Company Antibodies against glucocorticoid-induced tumor necrosis factor receptor (GITR) and uses thereof
GB201414730D0 (en) 2014-08-19 2014-10-01 Tpp Global Dev Ltd Pharmaceutical compound
US10183082B2 (en) * 2014-09-09 2019-01-22 H. Lee Moffitt Cancer Center And Research Institute, Inc. PET probes of radiofluorinated carboximidamides for IDO-targeted imaging
CN105481789B (zh) * 2014-09-15 2020-05-19 中国科学院上海有机化学研究所 一种吲哚胺-2,3-双加氧酶抑制剂及其制备方法
BR112017008809A2 (pt) 2014-11-05 2017-12-19 Flexus Biosciences Inc agentes imunorreguladores
UY36390A (es) 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen
UY36391A (es) 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido1), sus métodos de síntesis y composiciones farmacèuticas que las contienen
TWI711630B (zh) 2014-11-21 2020-12-01 美商必治妥美雅史谷比公司 抗ｃｄ７３抗體及其用途
WO2016100851A1 (en) 2014-12-18 2016-06-23 Lankenau Institute For Medical Research Methods and compositions for the treatment of retinopathy and other ocular diseases
TW201630907A (zh) 2014-12-22 2016-09-01 必治妥美雅史谷比公司 ＴＧＦβＲ拮抗劑
JP6180663B2 (ja) 2014-12-23 2017-08-16 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｔｉｇｉｔに対する抗体
WO2016127052A1 (en) 2015-02-05 2016-08-11 Bristol-Myers Squibb Company Cxcl11 and smica as predictive biomarkers for efficacy of anti-ctla4 immunotherapy
BR112017017135A2 (pt) 2015-03-02 2018-04-03 Rigel Pharmaceuticals, Inc. inibidores de tgf-beta
AU2016242978A1 (en) 2015-04-03 2017-11-23 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase for the treatment of cancer
TW201642897A (zh) 2015-04-08 2016-12-16 Ｆ 星生物科技有限公司 Ｈｅｒ２結合劑治療
BR112017020952A2 (pt) 2015-04-13 2018-07-10 Five Prime Therapeutics Inc método de tratamento de câncer, composição e uso da composição
WO2016169421A1 (zh) 2015-04-21 2016-10-27 江苏恒瑞医药股份有限公司 咪唑并异吲哚类衍生物、其制备方法及其在医药上的应用
EP3294736B1 (en) 2015-05-11 2020-07-22 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
US9725449B2 (en) 2015-05-12 2017-08-08 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
US10174024B2 (en) 2015-05-12 2019-01-08 Bristol-Myers Squibb Company 5H-pyrido[3,2-B]indole compounds as anticancer agents
EP3294324A1 (en) 2015-05-13 2018-03-21 Agenus Inc. Vaccines for treatment and prevention of cancer
MX2017015041A (es) 2015-05-29 2018-02-26 Squibb Bristol Myers Co Anticuerpos contra el miembro 4 de la superfamilia del receptor del factor de necrosis tumoral (ox40) y sus usos.
MX2017016502A (es) 2015-06-29 2018-03-12 Univ Rockefeller Anticuerpos contra cd40 con actividad agonista mejorada.
CN107709338A (zh) * 2015-07-02 2018-02-16 葛兰素史克知识产权开发有限公司 吲哚胺2,3‑双加氧酶的抑制剂
GB201511790D0 (en) 2015-07-06 2015-08-19 Iomet Pharma Ltd Pharmaceutical compound
AU2016293667A1 (en) 2015-07-14 2018-01-04 Kyowa Kirin Co., Ltd. A therapeutic agent for a tumor comprising an IDO inhibitor administered in combination with an antibody
WO2017009842A2 (en) 2015-07-16 2017-01-19 Biokine Therapeutics Ltd. Compositions and methods for treating cancer
WO2017019175A1 (en) 2015-07-24 2017-02-02 Newlink Genetics Corporation Salts and prodrugs of 1-methyl-d-tryptophan
EP3328861A1 (en) 2015-07-28 2018-06-06 Bristol-Myers Squibb Company Tgf beta receptor antagonists
US20180250303A1 (en) 2015-08-25 2018-09-06 Bristol-Myers Squibb Company Tgf beta receptor antagonists
CN106565696B (zh) * 2015-10-09 2020-07-28 江苏恒瑞医药股份有限公司 噁二唑类衍生物、其制备方法及其在医药上的应用
EP3371208B8 (en) 2015-11-02 2024-10-23 Five Prime Therapeutics, Inc. Cd80 extracellular domain polypeptides and their use in cancer treatment
MY198562A (en) 2015-11-03 2023-09-05 Janssen Biotech Inc Antibodies specifically binding pd-1 and their uses
CN108472245A (zh) 2015-11-04 2018-08-31 因赛特公司 用于吲哚胺2,3-双加氧酶抑制及其适应症的药物组合物和方法
JP6983776B2 (ja) 2015-11-19 2021-12-17 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company グルココルチコイド誘発腫瘍壊死因子受容体（ｇｉｔｒ）に対する抗体およびその使用
CN108368174B (zh) 2015-11-23 2023-04-14 戊瑞治疗有限公司 用于癌症治疗的单独fgfr2抑制剂或与免疫刺激剂的组合
CR20180286A (es) 2015-12-03 2018-07-16 Glaxosmithkline Ip Dev Ltd Dinucleotidos de purina cíclicos como moduladores de sting
WO2017106062A1 (en) 2015-12-15 2017-06-22 Merck Sharp & Dohme Corp. Novel compounds as indoleamine 2,3-dioxygenase inhibitors
CN106883193B (zh) * 2015-12-15 2021-10-15 上海翰森生物医药科技有限公司 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
WO2017106291A1 (en) 2015-12-15 2017-06-22 Bristol-Myers Squibb Company Cxcr4 receptor antagonists
CN106883194A (zh) * 2015-12-16 2017-06-23 江苏恒瑞医药股份有限公司 噁二唑类衍生物、其制备方法及其在医药上的应用
US9624185B1 (en) * 2016-01-20 2017-04-18 Yong Xu Method for preparing IDO inhibitor epacadostat
CN105646389B (zh) * 2016-01-28 2019-06-28 中国科学院上海有机化学研究所 一种作为吲哚胺-2,3-双加氧酶抑制剂的氨基磺酸脂及其制备方法和用途
EP3400226A1 (en) 2016-02-02 2018-11-14 Emcure Pharmaceuticals Limited Derivatives of pyrroloimidazole or analogues thereof which are useful for the treatment of inter alia cancer
CN107033097B (zh) * 2016-02-04 2022-02-08 江苏恒瑞医药股份有限公司 噁二唑类衍生物、其制备方法及其在医药上的应用
EP3416725A1 (en) * 2016-02-19 2018-12-26 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of obesity
TW201736373A (zh) * 2016-02-19 2017-10-16 Chia Tai Tianqing Pharmaceutical Group Co Ltd 作為免疫調節劑的三並環化合物
WO2017149469A1 (en) 2016-03-03 2017-09-08 Emcure Pharmaceuticals Limited Heterocyclic compounds useful as ido and/or tdo modulators
CA3016187A1 (en) 2016-03-04 2017-09-08 Bristol-Myers Squibb Company Combination therapy with anti-cd73 antibodies
CN107176933B (zh) * 2016-03-09 2020-10-09 中国科学院上海有机化学研究所 一种含氮烷基化和芳基化亚砜亚胺的吲哚胺-2,3-双加氧酶抑制剂
BR112018070602A2 (pt) 2016-04-07 2019-02-05 Glaxosmithkline Ip Dev Ltd composto, composição farmacêutica, uso do composto, e, método para tratar uma doença ou distúrbio
SI3440076T1 (sl) 2016-04-07 2022-09-30 Glaxosmithkline Intellectual Property Development Limited Heterociklični amidi uporabni kot proteinski modulatorji
CN109071665B (zh) 2016-04-18 2022-11-01 塞德斯医疗公司 结合人cd40的激动性抗体及其用途
WO2017181849A1 (zh) * 2016-04-20 2017-10-26 江苏豪森药业集团有限公司 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
CN107304191B (zh) * 2016-04-20 2023-09-29 上海翰森生物医药科技有限公司 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
KR20190003686A (ko) 2016-05-04 2019-01-09 브리스톨-마이어스 스큅 컴퍼니 인돌아민 2,3-디옥시게나제의 억제제 및 그의 사용 방법
US10323004B2 (en) 2016-05-04 2019-06-18 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
CN109414421A (zh) 2016-05-04 2019-03-01 百时美施贵宝公司 吲哚胺2,3-双加氧酶的抑制剂及其使用方法
EP3452451A4 (en) 2016-05-04 2019-11-13 Bristol-Myers Squibb Company INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS AND METHODS OF USE
EP3452450A1 (en) * 2016-05-04 2019-03-13 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
AR108586A1 (es) * 2016-06-10 2018-09-05 Lilly Co Eli Compuestos de 2,3-dihidro-1h-indol
EP4512829A3 (en) 2016-07-14 2025-06-11 Bristol-Myers Squibb Company Antibodies against tim3 and uses thereof
AU2017300123A1 (en) 2016-07-20 2019-01-31 Glaxosmithkline Intellectual Property Development Limited Isoquinoline derivatives as PERK inhibitors
US20190292179A1 (en) 2016-07-21 2019-09-26 Bristol-Myers Squibb Company TGF Beta RECEPTOR ANTAGONISTS
BR112019001980A2 (pt) * 2016-08-02 2019-05-07 Shandong Luye Pharmaceutical Co., Ltd. inibidor de ido1 e método de preparação e aplicação do mesmo
WO2018039430A1 (en) * 2016-08-24 2018-03-01 H. Lee Moffitt Cancer Center & Research Institute, Inc. Radiofluorinated carboximidamides as ido targeting pet tracer for cancer imaging
CN109843322A (zh) 2016-08-26 2019-06-04 百时美施贵宝公司 吲哚胺2,3-双加氧酶的抑制剂及其使用方法
WO2018044663A1 (en) * 2016-08-29 2018-03-08 Merck Sharp & Dohme Corp. Novel substituted n'-hydroxycarbamimidoyl-1,2,5-oxadiazole compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
CA3037333A1 (en) 2016-09-19 2018-03-22 University Of South Florida Method of targeting oncolytic viruses to tumors
WO2018054365A1 (en) 2016-09-24 2018-03-29 Beigene, Ltd. NOVEL 5 or 8-SUBSTITUTED IMIDAZO [1, 5-a] PYRIDINES AS SELECTIVE INHIBITORS OF INDOLEAMINE AND/OR TRYPTOPHANE 2, 3-DIOXYGENASES
WO2018072697A1 (zh) * 2016-10-17 2018-04-26 上海医药集团股份有限公司 含噁二唑环化合物、制备方法、中间体、组合物及应用
UY37466A (es) 2016-11-03 2018-01-31 Phenex Discovery Verwaltungs Gmbh N-hidroxiamidinheterociclos sustituidos como moduladores de la indolamina 2,3-dioxigenasa
EP3544965A4 (en) 2016-11-28 2020-05-20 Shanghai Fochon Pharmaceutical Co., Ltd. Sulfoximine, sulfonimidamide, sulfondiimine and diimidosulfonamide compounds as inhibitors of indoleamine 2, 3-dioxygenase
CN106883224B (zh) * 2017-01-03 2019-10-22 中国药科大学 苯并含氮杂环类吲哚胺-2,3-双加氧酶1抑制剂及其用途
CN106866648B (zh) * 2017-01-03 2019-10-22 中国药科大学 邻苯二甲酰亚胺类吲哚胺-2,3-双加氧酶1抑制剂及其用途
WO2018132279A1 (en) 2017-01-05 2018-07-19 Bristol-Myers Squibb Company Tgf beta receptor antagonists
JP2020506895A (ja) 2017-01-17 2020-03-05 ボード オブ レジェンツ, ザ ユニバーシティ オブ テキサス システムBoard Of Regents, The University Of Texas System インドールアミン２，３−ジオキシゲナーゼおよび／またはトリプトファンジオキシゲナーゼの阻害剤として有用な化合物
CN106866571B (zh) * 2017-01-20 2018-06-29 中国药科大学 杂环脲类化合物及其药物组合物和应用
US10927086B2 (en) * 2017-02-24 2021-02-23 Merck Sharp & Dohme Corp. Substituted sulfoximine compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
EP3600299B1 (en) * 2017-03-29 2022-11-30 Merck Sharp & Dohme LLC Novel substituted n'-hydroxycarbamimidoyl-1,2,5-oxadiazole compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
CN106967004B (zh) * 2017-03-29 2019-09-17 中国药科大学 含脲基的ido1和ido2双重抑制剂、其制法及其医药用途
CN110709420A (zh) 2017-03-31 2020-01-17 戊瑞治疗有限公司 使用抗gitr抗体的癌症组合疗法
CN108689958B (zh) * 2017-04-05 2021-09-17 南京华威医药科技集团有限公司 一种含有肼基的吲哚胺2,3-双加氧化酶抑制剂
TWI788340B (zh) 2017-04-07 2023-01-01 美商必治妥美雅史谷比公司 抗icos促效劑抗體及其用途
CA3059939A1 (en) 2017-04-21 2018-10-25 Kyn Therapeutics Indole ahr inhibitors and uses thereof
US11046679B2 (en) 2017-04-24 2021-06-29 Nanjing Transthera Biosciences Co. Ltd. Indoleamine 2,3-dioxygenase inhibitor and application
CN108794423B (zh) * 2017-04-27 2022-07-19 鲁南制药集团股份有限公司 亚氨脲衍生物
EA201992586A1 (ru) 2017-04-28 2020-03-03 Файв Прайм Терапьютикс, Инк. Способы лечения с помощью полипептидов внеклеточного домена cd80
WO2018209049A1 (en) 2017-05-12 2018-11-15 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
CN109081818B (zh) * 2017-06-14 2022-04-22 南京华威医药科技集团有限公司 新型吲哚胺2,3-双加氧化酶抑制剂
CN109111438B (zh) * 2017-06-26 2021-11-02 正大天晴药业集团股份有限公司 用于ido抑制剂的脒类化合物
IL271601B2 (en) 2017-06-30 2024-05-01 Bristol Myers Squibb Co Amorphous and crystalline forms of ido inhibitors
CN110891942B (zh) * 2017-07-14 2022-06-07 四川科伦博泰生物医药股份有限公司 噁二唑类衍生物、其制备方法及其在医药上的应用
WO2019021208A1 (en) 2017-07-27 2019-01-31 Glaxosmithkline Intellectual Property Development Limited USEFUL INDAZOLE DERIVATIVES AS PERK INHIBITORS
JP7186764B2 (ja) 2017-07-28 2022-12-09 ブリストル－マイヤーズ スクイブ カンパニー 抗癌剤としての環状ジヌクレオチド
KR20200051646A (ko) 2017-08-17 2020-05-13 이케나 온콜로지, 인코포레이티드 Ahr 억제제 및 이의 용도
US10953032B2 (en) 2017-08-31 2021-03-23 Bristol-Myers Squibb Company Cyclic dinucleotides as anticancer agents
CN111051327B (zh) 2017-08-31 2023-11-03 百时美施贵宝公司 作为抗癌剂的环二核苷酸
JP7316263B2 (ja) 2017-08-31 2023-07-27 ブリストル－マイヤーズ スクイブ カンパニー 抗癌剤としての環状ジヌクレオチド
CA3071217A1 (en) 2017-08-31 2019-03-07 Multimmune Gmbh Hsp70 based combination therapy
CN109422739B (zh) * 2017-09-01 2022-07-12 药捷安康(南京)科技股份有限公司 氘代的吲哚胺2，3-双加氧酶抑制剂及其应用
CN108863976B (zh) * 2017-09-11 2022-09-16 郑州泰基鸿诺医药股份有限公司 用作ido调节剂的化合物及其应用
EP4176876A1 (en) 2017-09-14 2023-05-10 Lankenau Institute for Medical Research Methods and compositions for the treatment of cancer
TW201927771A (zh) 2017-10-05 2019-07-16 英商葛蘭素史密斯克藍智慧財產發展有限公司 可作為蛋白質調節劑之雜環醯胺及其使用方法
JP7291130B2 (ja) 2017-10-05 2023-06-14 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド インターフェロン遺伝子の刺激物質（ｓｔｉｎｇ）の調節物質
WO2019074822A1 (en) 2017-10-09 2019-04-18 Bristol-Myers Squibb Company INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS AND METHODS OF USE
WO2019074749A1 (en) * 2017-10-09 2019-04-18 Merck Sharp & Dohme Corp. NOVEL SUBSTITUTED CYCLOBUTYLPYRIMIDINE AND CYCLOBUTYLPYRIMIDINE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE (IDO)
EP3694502B1 (en) * 2017-10-09 2023-08-02 Merck Sharp & Dohme LLC Novel substituted cyclobutylbenzene compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
US11203592B2 (en) 2017-10-09 2021-12-21 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
WO2019075090A1 (en) 2017-10-10 2019-04-18 Tilos Therapeutics, Inc. ANTI-LAP ANTIBODIES AND USES THEREOF
EP3694867B1 (en) 2017-10-10 2025-12-24 Bristol-Myers Squibb Company Cyclic dinucleotides as anticancer agents
EP3697801B1 (en) 2017-10-16 2024-11-20 Bristol-Myers Squibb Company Cyclic dinucleotides as anticancer agents
CN109678813A (zh) * 2017-10-18 2019-04-26 中国科学院上海有机化学研究所 吲哚胺-2,3-双加氧酶抑制剂盐及其制备方法
KR20200074214A (ko) 2017-11-01 2020-06-24 브리스톨-마이어스 스큅 컴퍼니 암을 치료하는데 사용하기 위한 면역자극 효능작용 항체
CN109748911B (zh) * 2017-11-06 2022-03-11 中国药科大学 一种含三氮唑的ido抑制剂、其制备方法及其医药用途
JP7167146B2 (ja) 2017-11-06 2022-11-08 ブリストル－マイヤーズ スクイブ カンパニー Ｈｐｋ１阻害剤として有用なイソフラノン化合物
CN107987031A (zh) * 2017-12-01 2018-05-04 华东理工大学 一种靶向吲哚胺-2,3-双加氧酶1氮芥类抑制剂及其制备方法和应用
EP3724177A1 (en) 2017-12-12 2020-10-21 Phenex Discovery Verwaltungs-GmbH Oxalamides as modulators of indoleamine 2,3-dioxygenase
CN108003111A (zh) * 2017-12-14 2018-05-08 华东理工大学 一种hdac1和ido1双靶点抑制剂及其制备方法和应用
CN109942565B (zh) * 2017-12-20 2021-03-26 海创药业股份有限公司 一种吲哚胺-2,3-双加氧酶抑制剂及其制备方法和用途
JP7284759B2 (ja) 2017-12-27 2023-05-31 ブリストル－マイヤーズ スクイブ カンパニー 抗ｃｄ４０抗体およびその使用
WO2019136112A1 (en) 2018-01-05 2019-07-11 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
US11813280B2 (en) 2018-01-05 2023-11-14 Dicerna Pharmaceuticals, Inc. Reducing beta-catenin and IDO expression to potentiate immunotherapy
CN120192415A (zh) 2018-01-12 2025-06-24 百时美施贵宝公司 抗tim3抗体及其用途
CN110054622B (zh) * 2018-01-18 2021-02-23 四川科伦博泰生物医药股份有限公司 噁二唑类衍生物、其制备方法及其在医药上的应用
CN108586378B (zh) 2018-01-22 2020-06-19 南京华威医药科技集团有限公司 吲哚胺2,3-双加氧化酶抑制剂及其制备方法和用途
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
CN110092750B (zh) 2018-01-29 2023-07-21 北京诺诚健华医药科技有限公司 五氟硫烷基取代的酰胺类化合物、其制备方法及其在医药学上的应用
US10519187B2 (en) 2018-02-13 2019-12-31 Bristol-Myers Squibb Company Cyclic dinucleotides as anticancer agents
CN110156674A (zh) * 2018-02-13 2019-08-23 中国科学院上海有机化学研究所 一种作为吲哚胺-2,3-双加氧酶抑制剂的螺环化合物
WO2019173587A1 (en) 2018-03-08 2019-09-12 Bristol-Myers Squibb Company Cyclic dinucleotides as anticancer agents
KR20250154550A (ko) 2018-03-21 2025-10-28 파이브 프라임 테라퓨틱스, 인크. 산성 pH에서 VISTA에 결합하는 항체
PE20210665A1 (es) 2018-03-23 2021-03-31 Bristol Myers Squibb Co Anticuerpos contra mica y/o micb y sus usos
WO2019185870A1 (en) 2018-03-29 2019-10-03 Phenex Discovery Verwaltungs-GmbH Spirocyclic compounds as modulators of indoleamine 2,3-dioxygenase
CN112218657A (zh) 2018-04-12 2021-01-12 百时美施贵宝公司 Cd73拮抗剂抗体和pd-1/pd-l1轴拮抗剂抗体的抗癌组合疗法
US20190314324A1 (en) 2018-04-13 2019-10-17 The University Of Chicago Combination of micheliolide derivatives or nanoparticles with ionizing radiation and checkpoint inhibitors for cancer therapy
WO2019204257A1 (en) 2018-04-16 2019-10-24 Arrys Therapeutics, Inc. Ep4 inhibitors and use thereof
WO2019206800A1 (en) 2018-04-24 2019-10-31 Phenex Discovery Verwaltungs-GmbH Spirocyclic compounds as modulators of indoleamine 2,3-dioxygenase
US12037323B2 (en) 2018-05-03 2024-07-16 Bristol-Myers Squibb Company Uracil derivatives as Mer-AXL inhibitors
GB201807924D0 (en) 2018-05-16 2018-06-27 Ctxt Pty Ltd Compounds
CN110526898A (zh) 2018-05-25 2019-12-03 北京诺诚健华医药科技有限公司 3-吲唑啉酮类化合物、其制备方法及其在医药学上的应用
GB201809050D0 (en) 2018-06-01 2018-07-18 E Therapeutics Plc Modulators of tryptophan catabolism
WO2020006018A1 (en) 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Substituted naphthyridinone compounds useful as t cell activators
PL3814347T3 (pl) 2018-06-27 2023-07-24 Bristol-Myers Squibb Company Związki naftyrydynonu użyteczne jako aktywatory komórek t
MY201995A (en) 2018-07-09 2024-03-28 Five Prime Therapeutics Inc Antibodies binding to ilt4
JP7700036B2 (ja) 2018-07-11 2025-06-30 ファイヴ プライム セラピューティクス インク 酸性ｐＨでＶＩＳＴＡと結合する抗体
EP3823604A4 (en) 2018-07-17 2022-03-16 Board of Regents, The University of Texas System Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase
US12145927B2 (en) 2018-07-23 2024-11-19 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
WO2020023355A1 (en) 2018-07-23 2020-01-30 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
US11253525B2 (en) 2018-08-29 2022-02-22 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
US10959986B2 (en) 2018-08-29 2021-03-30 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
JP2022504839A (ja) 2018-10-10 2022-01-13 ティロス・セラピューティクス・インコーポレイテッド 抗ｌａｐ抗体変異体及びその使用
US11274150B2 (en) 2018-11-16 2022-03-15 Bristol-Myers Squibb Company Anti-human natural killer cell inhibitory receptor group 2A protein (NKG2A) antibodies
AR117200A1 (es) * 2018-11-30 2021-07-21 Syngenta Participations Ag Derivados de tiazol microbiocidas
CN111689952A (zh) * 2019-03-14 2020-09-22 复旦大学 含硫代四元环结构的2,3-双加氧酶抑制剂及其制备方法和用途
CN111909107B (zh) * 2019-05-10 2023-02-03 药康众拓(江苏)医药科技有限公司 Ido/hdac双重抑制剂及其药物组合物和应用
WO2020231713A1 (en) 2019-05-13 2020-11-19 Bristol-Myers Squibb Company AGONISTS OF ROR GAMMAt
US20230295087A1 (en) 2019-05-13 2023-09-21 Bristol-Myers Squibb Company AGONISTS OF ROR GAMMAt
CN111943906B (zh) * 2019-05-14 2023-12-15 中国医学科学院药物研究所 脒类衍生物、及其制法和药物组合物与用途
EP3969438A1 (en) 2019-05-16 2022-03-23 Stingthera, Inc. Oxoacridinyl acetic acid derivatives and methods of use
JP2022533194A (ja) 2019-05-16 2022-07-21 スティングセラ インコーポレイテッド ベンゾ［ｂ］［１，８］ナフチリジン酢酸誘導体および使用方法
CN112062732B (zh) * 2019-06-10 2023-10-24 鲁南制药集团股份有限公司 一种ido抑制剂及其组合物、制备方法和用途
GB201910304D0 (en) 2019-07-18 2019-09-04 Ctxt Pty Ltd Compounds
GB201910305D0 (en) 2019-07-18 2019-09-04 Ctxt Pty Ltd Compounds
WO2021026179A1 (en) 2019-08-06 2021-02-11 Bristol-Myers Squibb Company AGONISTS OF ROR GAMMAt
AR119821A1 (es) 2019-08-28 2022-01-12 Bristol Myers Squibb Co Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t
MX2022003204A (es) 2019-09-19 2022-04-18 Bristol Myers Squibb Co Anticuerpos de union al supresor de activacion de linfocitos t que contiene inmunoglobulina con dominio v (vista) a ph acido.
JP7629459B2 (ja) 2019-11-19 2025-02-13 ブリストル－マイヤーズ スクイブ カンパニー Ｈｅｌｉｏｓタンパク質の阻害剤として有用な化合物
AU2020394424A1 (en) 2019-11-26 2022-06-16 Ikena Oncology, Inc. Polymorphic carbazole derivatives and uses thereof
CA3159071A1 (en) 2019-11-26 2021-06-03 Tamar I. ROSENBAUM Salts/cocrystals of (r)-n-(4-chlorophenyl)-2-((1s,4s)-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide
AU2020409429A1 (en) 2019-12-18 2022-06-16 Ctxt Pty Ltd Compounds
KR20220120624A (ko) 2019-12-23 2022-08-30 브리스톨-마이어스 스큅 컴퍼니 T 세포 활성화제로서 유용한 치환된 피페라진 유도체
CN115103841B (zh) 2019-12-23 2024-12-27 百时美施贵宝公司 可用作t细胞激活剂的经取代的喹啉酮基哌嗪化合物
WO2021133752A1 (en) 2019-12-23 2021-07-01 Bristol-Myers Squibb Company Substituted heteroaryl compounds useful as t cell activators
BR112022012179A2 (pt) 2019-12-23 2022-09-06 Bristol Myers Squibb Co Compostos de quinazolina substituída úteis como ativadores de célula t
AR120823A1 (es) 2019-12-23 2022-03-23 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos útiles como activadores de células t
CN111138425A (zh) * 2020-01-06 2020-05-12 中国药科大学 三氮唑类衍生物及其制备方法与用途
CA3166898A1 (en) 2020-01-06 2021-07-15 Hifibio (Hk) Limited Anti-tnfr2 antibody and uses thereof
CN115210261B (zh) 2020-01-07 2025-07-18 高诚生物医药公司 抗半乳糖凝集素-9抗体及其用途
JP2023510918A (ja) 2020-01-15 2023-03-15 ブループリント メディシンズ コーポレイション Ｍａｐ４ｋ１阻害剤
JP2023516459A (ja) 2020-03-09 2023-04-19 ブリストル－マイヤーズ スクイブ カンパニー 増強されたアゴニスト活性を有するｃｄ４０に対する抗体
TW202140441A (zh) 2020-03-23 2021-11-01 美商必治妥美雅史谷比公司 經取代之側氧基異吲哚啉化合物
EP4132971A1 (en) 2020-04-09 2023-02-15 Merck Sharp & Dohme LLC Affinity matured anti-lap antibodies and uses thereof
US20230192867A1 (en) 2020-05-15 2023-06-22 Bristol-Myers Squibb Company Antibodies to garp
WO2021258010A1 (en) 2020-06-19 2021-12-23 Gossamer Bio Services, Inc. Oxime compounds useful as t cell activators
IL300537A (en) 2020-08-10 2023-04-01 Gv20 Therapeutics Llc Compositions and methods for treating autoimmune diseases and cancer by targeting IGSF8
CA3198456A1 (en) 2020-10-14 2022-04-21 Five Prime Therapeutics, Inc. Anti-c-c chemokine receptor 8 (ccr8) antibodies and methods of use thereof
JP2024501207A (ja) 2020-12-16 2024-01-11 ゴッサマー バイオ サービシズ、インコーポレイテッド Ｔ細胞活性化剤として有用な化合物
WO2022169921A1 (en) 2021-02-04 2022-08-11 Bristol-Myers Squibb Company Benzofuran compounds as sting agonists
US20240368150A1 (en) 2021-02-12 2024-11-07 Hoffmann-La Roche Inc. Bicyclic tetrahydroazepine derivatives for the treatment of cancer
CN113105366B (zh) * 2021-03-04 2022-05-24 中国药科大学 一类含苯基羟肟结构衍生物及其制法与用途
JP2024510176A (ja) 2021-03-08 2024-03-06 ブループリント メディシンズ コーポレイション Ｍａｐ４ｋ１阻害剤
US11918582B2 (en) 2021-03-15 2024-03-05 Rapt Therapeutics, Inc. Pyrazole pyrimidine compounds and uses thereof
EP4314068A1 (en) 2021-04-02 2024-02-07 The Regents Of The University Of California Antibodies against cleaved cdcp1 and uses thereof
EP4320125A1 (en) 2021-04-05 2024-02-14 Bristol-Myers Squibb Company Pyridinyl substituted oxoisoindoline compounds for the treatment of cancer
IL307343A (en) 2021-04-06 2023-11-01 Bristol Myers Squibb Co Pyridinyl substituted oxisoisoindoline compounds
JP2024527608A (ja) 2021-07-14 2024-07-25 ブループリント メディシンズ コーポレイション Ｍａｐ４ｋ１阻害剤としての複素環化合物
TW202321238A (zh) 2021-07-15 2023-06-01 美商纜圖藥品公司 Ｍａｐ４ｋ１抑制劑
WO2023122778A1 (en) 2021-12-22 2023-06-29 Gossamer Bio Services, Inc. Pyridazinone derivatives useful as t cell activators
WO2023122777A1 (en) 2021-12-22 2023-06-29 Gossamer Bio Services, Inc. Oxime derivatives useful as t cell activators
WO2023122772A1 (en) 2021-12-22 2023-06-29 Gossamer Bio Services, Inc. Oxime derivatives useful as t cell activators
JP2025503312A (ja) 2022-02-01 2025-01-30 アルビナス・オペレーションズ・インコーポレイテッド Ｄｇｋ標的化化合物およびその使用
CN119654312A (zh) 2022-08-08 2025-03-18 百时美施贵宝公司 用作t细胞活化剂的取代的四唑基化合物
WO2024036101A1 (en) 2022-08-09 2024-02-15 Bristol-Myers Squibb Company Tertiary amine substituted bicyclic compounds useful as t cell activators
CR20250042A (es) 2022-08-11 2025-03-25 Hoffmann La Roche Derivados de tetrahidrotiazepina bicíclicos
CN119677732A (zh) 2022-08-11 2025-03-21 豪夫迈·罗氏有限公司 双环四氢氮杂䓬衍生物
CA3262845A1 (en) 2022-08-11 2024-02-15 F. Hoffmann-La Roche Ag BICYCLIC TETRAHYDROTHIAZEPINE DERIVATIVES
EP4568746A1 (en) 2022-08-11 2025-06-18 F. Hoffmann-La Roche AG Bicyclic tetrahydrothiazepine derivatives
WO2024137865A1 (en) 2022-12-22 2024-06-27 Gossamer Bio Services, Inc. Compounds useful as t cell activators
TW202509014A (zh) 2023-05-10 2025-03-01 美商纜圖藥品公司 ＧＳＫ３α抑制劑及其使用方法
WO2024254227A1 (en) 2023-06-07 2024-12-12 Bristol-Myers Squibb Company Spirocyclic substituted oxoisoindolinyl piperidine-2,6-dione compound
WO2024263853A1 (en) 2023-06-23 2024-12-26 Bristol-Myers Squibb Company Substituted oxoisoindolinyl piperidine-2,6-dione compound as anticancer agent
WO2025030002A2 (en) 2023-08-02 2025-02-06 Arvinas Operations, Inc. Dgk targeting compounds and uses thereof
WO2025064197A1 (en) 2023-09-02 2025-03-27 Bristol-Myers Squibb Company Substituted azetidinyl oxoisoindolinyl piperidine-2,6-dione compounds
WO2025096487A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096505A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096539A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096490A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096489A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096494A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096488A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025226767A1 (en) 2024-04-24 2025-10-30 Bristol-Myers Squibb Company Substituted 3-(5-(6-aminopyridin-2-yl)-4-fluoro-1-oxoisoindolin-2-yl)piperidine-2,6-dione compounds for use in the treatment of cancer
CN118908989B (zh) * 2024-10-10 2024-12-17 江苏长泰药业股份有限公司 一种用于预防肺结节恶性转化的丙酮酸盐衍生物纳米雾化剂及其制备方法

Family Cites Families (129)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3236855A (en) 1964-01-17 1966-02-22 Merck & Co Inc Certain n-phenyl(thiazole-hydroxamidine) compounds and their preparation
US3354174A (en) 1964-02-19 1967-11-21 Sterling Drug Inc 1-and 2-benzimidazolyl-lower-alkylamidoximes, amidines-, and guanidines
DE1453353A1 (de) 1964-02-20 1970-01-15 Nottmeyer Maschf Heinrich Maschine zum Einpressen von Duebeln in eine vorgebohrte Platte oder dergleichen Werkstueck
US3286855A (en) 1965-06-01 1966-11-22 Standard Trailer Company Crane extension and resulting crane assembly
US3553228A (en) 1967-09-26 1971-01-05 Colgate Palmolive Co 3-substituted-4h(1)benzopyrano(3,4-d) isoxazoles
DE2040628A1 (de) 1970-08-17 1972-02-24 Fahlberg List Veb Neue herbizide Mittel
US3948928A (en) 1972-03-17 1976-04-06 Dainippon Pharmaceutical Co., Ltd. 3-Substituted-1,2-benzisoxazoles and pharmaceutically acceptable acid addition salts thereof
JPS5621033B2 (me) 1973-09-05 1981-05-16
CA1080234A (en) 1975-09-11 1980-06-24 Daniel Farge Derivatives of amidoximes
FR2323683A1 (fr) 1975-09-11 1977-04-08 Philagro Sa Nouveaux derives d'amidoximes, leur preparation et les compositions qui les contiennent
US4634665A (en) 1980-02-25 1987-01-06 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4399216A (en) 1980-02-25 1983-08-16 The Trustees Of Columbia University Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US5179017A (en) 1980-02-25 1993-01-12 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4323681A (en) * 1980-09-29 1982-04-06 American Home Products Corporation 4-Amino-2-substituted-5-pyrimidinecarboxamidoximes and carbothioamides
US5156840A (en) 1982-03-09 1992-10-20 Cytogen Corporation Amine-containing porphyrin derivatives
JPS58208275A (ja) * 1982-05-20 1983-12-03 Lion Corp ５−アミノ−ピラゾ−ル誘導体及び該化合物を含有する抗腫瘍剤
DE3462259D1 (de) 1983-07-22 1987-03-05 Bayer Ag Substituted furazans
US4507485A (en) 1984-01-23 1985-03-26 Bristol-Myers Company 3,4-Disubstituted-1,2,5-oxadiazoles having histamine H2 -receptor antagonist activity
JPS60193968A (ja) * 1984-03-13 1985-10-02 Toyo Jozo Co Ltd シクロペンテン環を有するイミダゾ−ルアミドオキシムおよびその製造法
JPS6259283A (ja) 1985-09-10 1987-03-14 Kaken Pharmaceut Co Ltd セフアロスポリン化合物
US5057313A (en) 1986-02-25 1991-10-15 The Center For Molecular Medicine And Immunology Diagnostic and therapeutic antibody conjugates
DE3883899T3 (de) 1987-03-18 1999-04-22 Sb2, Inc., Danville, Calif. Geänderte antikörper.
JP2696342B2 (ja) * 1988-06-27 1998-01-14 日本曹達株式会社 アミジン誘導体、その製造方法及び殺ダニ剤・農園芸用殺菌剤
ES2051986T3 (es) 1988-07-05 1994-07-01 Akzo Nv Compuestos con actividad broncodilatadora.
IL162181A (en) 1988-12-28 2006-04-10 Pdl Biopharma Inc A method of producing humanized immunoglubulin, and polynucleotides encoding the same
US5530101A (en) 1988-12-28 1996-06-25 Protein Design Labs, Inc. Humanized immunoglobulins
DE3920358A1 (de) 1989-06-22 1991-01-17 Behringwerke Ag Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung
US5859205A (en) 1989-12-21 1999-01-12 Celltech Limited Humanised antibodies
JPH0420710A (ja) 1990-05-12 1992-01-24 Hitachi Home Tec Ltd ポットバーナの運転制御装置
JPH04297449A (ja) 1991-03-27 1992-10-21 Hokko Chem Ind Co Ltd Ｎ−ヒドロキシベンジルグアニジン誘導体および農園芸用殺菌剤
JPH05186458A (ja) 1991-04-26 1993-07-27 Japan Tobacco Inc 新規なベンゾピラン誘導体
FR2677019B1 (fr) 1991-05-27 1994-11-25 Pf Medicament Nouvelles piperidines disubstituees-1,4, leur preparation et leur application en therapeutique.
EP0940468A1 (en) 1991-06-14 1999-09-08 Genentech, Inc. Humanized antibody variable domain
EP0617706B1 (en) 1991-11-25 2001-10-17 Enzon, Inc. Multivalent antigen-binding proteins
US5714350A (en) 1992-03-09 1998-02-03 Protein Design Labs, Inc. Increasing antibody affinity by altering glycosylation in the immunoglobulin variable region
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
JP2709677B2 (ja) * 1992-06-19 1998-02-04 株式会社大塚製薬工場 ホスホン酸ジエステル誘導体
US5827690A (en) 1993-12-20 1998-10-27 Genzyme Transgenics Corporatiion Transgenic production of antibodies in milk
FR2720396B1 (fr) 1994-05-27 1996-06-28 Adir Nouveaux N-pyridyl carboxamides et dérivés leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
US5731168A (en) 1995-03-01 1998-03-24 Genentech, Inc. Method for making heteromultimeric polypeptides
US5869046A (en) 1995-04-14 1999-02-09 Genentech, Inc. Altered polypeptides with increased half-life
US5731315A (en) 1995-06-07 1998-03-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Substituted sulfonic acid n- (aminoiminomethyl)phenylalkyl!-azaheterocyclamide compounds
ES2176484T3 (es) 1995-08-18 2002-12-01 Morphosys Ag Bancos de proteinas/(poli)peptidos.
BR9610988A (pt) * 1995-10-17 1999-04-06 Astra Pharma Prod Composto uso do mesmo fomulação farmacêutica e processo para produção do composto
AU1730497A (en) * 1996-02-17 1997-09-02 Agrevo Uk Limited Fungicidal 1,2,4-oxadiazoles and analogues
US5955495A (en) 1996-05-03 1999-09-21 Hoffmann-La Roche Inc. Method of treating diseases of the CNS
JPH11171702A (ja) 1997-09-24 1999-06-29 Takeda Chem Ind Ltd 害虫防除方法
AU1628599A (en) * 1997-12-05 1999-06-28 Medical College Of Georgia Research Institute, Inc. Regulation of t cell-mediated immunity by tryptophan
BR9813536A (pt) 1997-12-10 2000-10-10 Dainippon Ink & Chemicals "derivados oxima e produtos quìmicos agrìcolas incluindo os mesmos"
ES2177275T3 (es) 1998-06-02 2002-12-01 Takeda Chemical Industries Ltd Derivados de oxadiazolina y su uso como insecticidas.
ATE459616T1 (de) 1998-08-11 2010-03-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
FR2784678B1 (fr) 1998-09-23 2002-11-29 Sod Conseils Rech Applic Nouveaux derives de n-(iminomethyl)amines, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
JP3422486B2 (ja) 1999-03-03 2003-06-30 サムジン ファーマシューティカル カンパニー リミテッド ピペラジン誘導体及びその製造方法
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
AU765244B2 (en) 1999-04-09 2003-09-11 Abbott Gmbh & Co. Kg Prodrugs of thrombin inhibitors
IL146564A0 (en) 1999-05-24 2002-07-25 Mitsubishi Pharma Corp Phenoxypropylamine derivatives and pharmaceutical compositions containing the same
JP2001158785A (ja) 1999-11-30 2001-06-12 Takeda Chem Ind Ltd 農薬組成物
JP2001158786A (ja) 1999-11-30 2001-06-12 Takeda Chem Ind Ltd 哺乳動物の外部寄生虫防除剤
US6780858B2 (en) 2000-01-13 2004-08-24 Tularik Inc. Antibacterial agents
JP2001233861A (ja) 2000-02-22 2001-08-28 Ube Ind Ltd ピラゾールオキシム化合物、その製法及び用途
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
JP4188078B2 (ja) 2000-06-28 2008-11-26 スミスクライン ビーチャム ピー エル シー 湿式粉砕法
GB0108102D0 (en) 2001-03-30 2001-05-23 Pfizer Ltd Compounds
US7115639B2 (en) 2001-06-18 2006-10-03 Applied Research Systems Ars Holding N.V. Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists
AU2002337142B2 (en) 2001-09-19 2007-10-11 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
WO2003035092A1 (en) * 2001-10-26 2003-05-01 Angiolab Inc. Composition containing horse chestnut extract for anti-angiogenic and matrix metalloproteinase inhibitory activity
EP1441737B1 (en) 2001-10-30 2006-08-09 Novartis AG Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
GEP20063909B (en) 2002-01-22 2006-08-25 Warner Lambert Co 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d] PYRIMIDIN-7-ONES
MXPA04008680A (es) 2002-02-19 2004-12-06 Pharmacia Italia Spa Derivados de pirazol triciclicos, procedimientos para su preparacion y su uso como agentes anti-tumorales.
GB0208224D0 (en) 2002-04-10 2002-05-22 Celltech R&D Ltd Chemical compounds
EP2177601A1 (en) 2002-04-12 2010-04-21 Medical College of Georgia Research Institute, Inc Antigen-presenting cell populations and their use as reagents for enhancing or reducing immune tolerance
US7109354B2 (en) 2002-05-28 2006-09-19 3-Dimensional Pharmaceuticals, Inc. Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
JP4020710B2 (ja) 2002-06-25 2007-12-12 株式会社ミツバ ドアミラーセットプレート
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
US7157462B2 (en) 2002-09-24 2007-01-02 Euro-Celtique S.A. Therapeutic agents useful for treating pain
US7015321B2 (en) 2002-10-12 2006-03-21 The Scripps Research Institute Synthesis of non-symmetrical sulfamides using burgess-type reagents
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
CA2512729C (en) 2003-01-09 2014-09-16 Macrogenics, Inc. Identification and engineering of antibodies with variant fc regions and methods of using same
US20050079574A1 (en) 2003-01-16 2005-04-14 Genentech, Inc. Synthetic antibody phage libraries
US20050008625A1 (en) 2003-02-13 2005-01-13 Kalobios, Inc. Antibody affinity engineering by serial epitope-guided complementarity replacement
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
EP2260846B1 (en) * 2003-03-27 2018-11-28 Lankenau Institute for Medical Research Novel methods for the treatment of cancer
US7598287B2 (en) 2003-04-01 2009-10-06 Medical College Of Georgia Research Institute, Inc. Use of inhibitors of indoleamine-2,3-dioxygenase in combination with other therapeutic modalities
NZ544486A (en) 2003-06-13 2009-04-30 Biogen Idec Inc Aglycosyl anti-cd154 (cd40 ligand) antibodies and uses thereof
WO2005019190A2 (en) 2003-08-20 2005-03-03 Vertex Pharmaceuticals Incorporated (4 -amino -1,2, 5-oxadiazol-4-yl) -hetξroaromatic compounds useful as protein kinase inhibitors
WO2005018572A2 (en) 2003-08-22 2005-03-03 Biogen Idec Ma Inc. Improved antibodies having altered effector function and methods for making the same
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
DE10348023A1 (de) 2003-10-15 2005-05-19 Imtm Gmbh Neue Alanyl-Aminopeptidasen-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
DE10348022A1 (de) 2003-10-15 2005-05-25 Imtm Gmbh Neue Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
TW200610762A (en) 2004-06-10 2006-04-01 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2006028284A1 (ja) 2004-09-08 2006-03-16 Mitsubishi Pharma Corporation モルホリン化合物
WO2006056399A2 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of jak inhibitors and at least one of bcr-abl, flt-3, fak or raf kinase inhibitors
EP1838706A1 (en) 2004-12-24 2007-10-03 Prosidion Limited G-protein coupled receptor agonists
US7429667B2 (en) 2005-01-20 2008-09-30 Ardea Biosciences, Inc. Phenylamino isothiazole carboxamidines as MEK inhibitors
EP2418278A3 (en) 2005-05-09 2012-07-04 Ono Pharmaceutical Co., Ltd. Human monoclonal antibodies to programmed death 1(PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapeutics
ME02461B (me) 2005-05-10 2017-02-20 Incyte Holdings Corp Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih
WO2006133417A1 (en) 2005-06-07 2006-12-14 Valeant Pharmaceuticals International Phenylamino isothiazole carboxamidines as mek inhibitors
AU2006265601A1 (en) 2005-06-30 2007-01-11 Anthrogenesis Corporation Repair of tympanic membrane using placenta derived collagen biofabric
DE102005060466A1 (de) 2005-12-17 2007-06-28 Bayer Cropscience Ag Carboxamide
EP1971583B1 (en) 2005-12-20 2015-03-25 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
WO2007095050A2 (en) 2006-02-09 2007-08-23 Incyte Corporation N-hydroxyguanidines as modulators of indoleamine 2,3-dioxygenase
JP4297449B2 (ja) 2006-05-12 2009-07-15 株式会社サクラクレパス 墨汁
US20080125470A1 (en) 2006-09-19 2008-05-29 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
CL2007002650A1 (es) 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
WO2008036643A2 (en) 2006-09-19 2008-03-27 Incyte Corporation Amidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
US20080146624A1 (en) 2006-09-19 2008-06-19 Incyte Corporation Amidines as modulators of indoleamine 2,3-dioxygenase
US20080182882A1 (en) 2006-11-08 2008-07-31 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
AU2007333194A1 (en) 2006-12-08 2008-06-19 Exelixis, Inc. LXR and FXR modulators
TW200845991A (en) 2007-01-12 2008-12-01 Smithkline Beecham Corp N-substituted glycine derivatives: hydroxylase inhibitors
MX2010006457A (es) 2007-12-19 2010-07-05 Amgen Inc Compuestos fusionados de piridina, pirimidina y triazina como inhibidores de ciclo celular.
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
SG10201805844QA (en) 2008-07-08 2018-08-30 Incyte Holdings Corp 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
JO2885B1 (en) 2008-12-22 2015-03-15 ايلي ليلي اند كومباني Protein kinase inhibitors
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
SG10201508715YA (en) 2010-10-25 2015-11-27 G1 Therapeutics Inc Cdk inhibitors
DK2688887T3 (en) 2011-03-23 2015-06-29 Amgen Inc DEHYDRATED tricyclic DUALINHIBITORER OF CDK 4/6 AND FLT3
WO2014066834A1 (en) 2012-10-26 2014-05-01 The University Of Chicago Synergistic combination of immunologic inhibitors for the treatment of cancer
US9873683B2 (en) 2013-07-12 2018-01-23 Nippon Chemiphar Co., Ltd P2X4 receptor antagonist
CA2929552C (en) 2013-11-08 2022-05-17 Incyte Holdings Corporation Process for the synthesis of an indoleamine 2,3-dioxygenase inhibitor
JP2017508785A (ja) 2014-02-04 2017-03-30 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ 癌を治療するためのｐｄ−１アンタゴニストおよびｉｄｏ１阻害剤の組み合わせ
US20170209574A1 (en) 2014-10-03 2017-07-27 Novartis Ag Combination therapies
SG10202010506TA (en) 2015-07-30 2020-11-27 Macrogenics Inc Pd-1-binding molecules and methods of use thereof
BR112018004069A2 (pt) 2015-09-01 2021-07-13 First Wave Bio, Inc. composição farmacêutica sólida, preparação de enema compreendendo niclosamida, formulação de enema, uso de niclosamida e kit
CN108472245A (zh) 2015-11-04 2018-08-31 因赛特公司 用于吲哚胺2,3-双加氧酶抑制及其适应症的药物组合物和方法
JP2022543062A (ja) 2019-08-01 2022-10-07 インサイト・コーポレイション Ｉｄｏ阻害剤の投与レジメン
CA3179361A1 (en) 2020-04-27 2021-11-04 Armata Pharmaceuticals, Inc. Bacteriophage compositions for treating pseudomonas infection

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NO20170633A1 (no) 2008-02-07
KR20080005954A (ko) 2008-01-15
SI1879573T1 (sl) 2013-04-30
ES2401482T3 (es) 2013-04-22
CA2606783C (en) 2014-03-25
EP1879573A4 (en) 2009-07-08
IL186957A0 (en) 2008-02-09
NZ562919A (en) 2011-04-29
EP1879573B1 (en) 2012-12-19
US8034953B2 (en) 2011-10-11
PT2559690T (pt) 2016-07-07
HK1182381A1 (en) 2013-11-29

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