HRP20151143T1 - Novi antimalarijski agensi - Google Patents

Novi antimalarijski agensi Download PDF

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HRP20151143T1
HRP20151143T1 HRP20151143TT HRP20151143T HRP20151143T1 HR P20151143 T1 HRP20151143 T1 HR P20151143T1 HR P20151143T T HRP20151143T T HR P20151143TT HR P20151143 T HRP20151143 T HR P20151143T HR P20151143 T1 HRP20151143 T1 HR P20151143T1
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pyridin
phenyl
amine
methylsulfonyl
amino
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HRP20151143TT
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Michael John Witty
David Hardick
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Mmv Medicines For Malaria Venture
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    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/73Unsubstituted amino or imino radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D417/00Heterocyclic 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
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    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Claims (16)

1. Aminopiridin prema formuli (I), [image] naznačen time, da su X i Y neovisno odabrani između opcionalno supstituiranog arila i opcionalno supstituiranog heteroarila, kao i njihovih tautomera, geometrijskih izomera, optički aktivnih oblika, farmaceutski prihvatljivih soli, kompleksa i farmaceutski aktivnih derivata za upotrebu u liječenju ili profilaksi malarije.
2. Aminopiridin za upotrebu prema patentnom zahtjevu 1, naznačen time da je X opcionalno supstituiran aril.
3. Aminopiridin za upotrebu prema patentnom zahtjevu 2, naznačen time da je X opcionalno supstituiran fenil.
4. Aminopiridin za upotrebu prema patentnom zahtjevu 1, naznačen time da je X opcionalno supstituiran heteroaril.
5. Aminopiridin za upotrebu prema bilo kojem od patentnih zahtjeva od 1 do 4, naznačen time da je Y opcionalno supstituiran aril.
6. Aminopiridin za upotrebu prema bilo kojem od patentnih zahtjeva od 1 do 4, naznačen time da je Y opcionalno supstituiran heteroaril.
7. Aminopiridin za upotrebu prema patentnom zahtjevu 6, naznačen time da je Y opcionalno supstituiran piridin.
8. Aminopiridin za upotrebu prema bilo kojem od patentnih zahtjeva od 1 do 3, naznačen time da je X opcionalno supstituiran fenil odabran iz grupe koju čine opcionalno supstituirana C1-C6 alkil sulfonil fenil, opcionalno supstituirana sulfonamid fenil, opcionalno supstituirana fenil amid i opcionalno supstituirana karbonil fenil grupa.
9. Aminopiridin za upotrebu prema patentnom zahtjevu 1, naznačen time da je X opcionalno supstituiran fenil odabran iz grupe koju čine opcionalno supstituirana sulfonil fenil, opcionalno supstituirana fenil amid i opcionalno supstituirana amid karbonil fenil grupa i da je Y opcionalno supstituiran piridin.
10. Aminopiridin za upotrebu prema bilo kojem od patentnih zahtjeva od 1 do 9, naznačen time da je aminopiridin odabran iz grupe koja slijedi: 3-(6-metoksipiridin-3-il)-5-(4-metilsulfonilfenil)piridin-2-amin; 5-(4-metilsulfonilfenil)-3-[3-(trifluorometil)fenil]piridin-2-amin; 3-[2-amino-5-(4-metilsulfonilfenil)piridin-3-il]fenol; 4-[2-amino-5-(4-metilsulfonilfenil)piridin-3-il]-2-metoksifenol; 4-[2-amino-5-(4-metilsulfonilfenil)piridin-3-il]fenol; 4-[2-amino-5-(6-metoksipiridin-3-il)piridin-3-il]-2-metoksifenol; 4-[6-amino-5-[4-(4-metilpiperazin-1-il)fenil]piridin-3-il]-2,6-dimetilfenol; [4-[6-amino-5-(6-metoksipiridin-3-il)piridin-3-il]fenil]metanol; 4-[6-amino-5-[4-(4-metilpiperazin-1-il)fenil]piridin-3-il]fenol; (N,N-dimetil){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N,N-dimetil benzamid; 5-(2-metoksipiridin-5-il)-3-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(pirimidin-5-il)piridin-2-amin; (morfolino){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 3,5-di(2-metoksipiridin-5-il)piridin-2-amin; (N-metil piperazin){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 3,5-di-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-[3-(metilsulfonil)fenil]piridin-2-amin; (N-metil){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-metilbenzamid; {4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]fenil}(morfolino)metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzamid; 4-[6-amino-5-(2-metoksipiridin-5-il)piridin-3-il]benzojeva kiselina; N{4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}metil sulfonamid; 4-[6-amino-5-(6-metoksipiridin-3-il)piridin-3-il]-N-(3-hidroksipropil)-benzamid; 5-(benzo[c][[1,2,5]oksadiazol-6-il)-3-(2-metoksipiridin-5-il)piridin-2-amin; N-ciklopropil-{4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 5-(H-imidazo[1,2-a]piridin-6-il)-3-(2-metoksipiridin-5-il)piridin-2-amin; 3-(2-metoksipiridin-3-il)-5-(1-metil-1H-indazol-6-il)piridin-2-amin; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-ciklopropilbenzamid; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-(2-morfolino etil) benzamid; 3-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzamid; 3-(2-metoksipiridin-5-il)-5-[4-(5-metil-1,3,4-oksadiazol-2-il)fenil]piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-(6-morfolinopiridin-3-il)piridin-2-amin; 5-[4-(1H-pirazol-1-il)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-(kinolin-6-il)piridin-2-amin; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-[2-(pirolidin-1-il)etil]benzamid; 5-[2-(trifluoro metil)-4-(metilsulfonil)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin; {4-[2-amino-3-(4-karbamoilfenil)piridin-5-il]fenil}(morfolino)metanon; 4-[2-amino-3-(2-metilpiridin-5-il)piridin-5-il]benzamid; [4-(2-amino-5-metilpiridin-3-il)-N-(2-hidroksietil) benzamido](morfolino) metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzensulfonamid; 4-[2-amin-3-(4-benzamido)piridin-5-il]benzamid; {4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]fenil}(4-metilpiperazin-1-il) metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-[4-(aminometil)tiazol-2-il]benzamid; {4-[2-amino-3-(4-(trifluorometil)fenil)piridin-5-il]fenil}(morfolino)metanon; 3-(2-metoksipiridin-3-il)-5-[4-(metilsulfonilfenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(piridin-3-il)piridin-2-amin; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzonitril; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzonitril; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzamid; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}-N-metilbenzamid; 3-(H-imidazo[1,2-a]piridin-6-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metoksipirimidin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(kinoksalin-7-il)piridin-2-amin; 3-(furan-3-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-[4-(5-metil-1,3,4-oksadiazol-2-il)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-kloro-2-metoksipiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[3-(trifluorometoksi)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[4-(trifluorometoksi)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[2-(pirolidin-1-il)piridin-5-il]piridin-2-amin; 3-[2-kloro-4-(trifluorometil)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-metoksipiridin-4-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(2-morfolino piridin-5-il)piridin-2-amin; 3-[2-(trifluorometil)piridin-4-il]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metilpiridin-5-il)-5-[4-(metil sulfonil)fenil]piridin-2-amin; 3-[2-(trifluoro-metil)piridin-5-il]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-{4-[2-(pirolidin-1-il) etoksi]fenil}-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(4-morfolinofenil)piridin-2-amin; 3-[4-(1H-pirazol-1-il)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}pirimidin-2-amin; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzamid; 3-(6-metoksi-2-metilpiridin-3-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(izokinolin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(kinolin-6-il)piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-p-tolilpiridin-2-amin; {5-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]piridin-2-il}metanol; 3-(2-metilbenzo[d]tiazol-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; N{4-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]fenil}-2-(dimetilamino) acetamid; 3-(2-fluorpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[2-(metilsulfonil)piridin-5-il]piridin-2-amin; N{5-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]piridin-2-il}acetamid; 3-(benzo[c][1,2,5]oksadiazol-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il]-N-(2-hidroksietil) benzamid; 3-[4-(trifluorometil)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-metilpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; i 5-[3-fluoro-4-(metilsulfonil)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin.
11. Aminopiridin odabran iz grupe koju čine: 3-(6-metoksipiridin-3-il)-5-(4-metilsulfonilfenil)piridin-2-amin; 5-(4-metilsulfonilfenil)-3-[3-(trifluorometil)fenil]piridin-2-amin; 3-[2-amino-5-(4-metilsulfonilfenil)piridin-3-il]fenol; 4-[2-amino-5-(4-metilsulfonilfenil)piridin-3-il]-2-metoksifenol; 4-[2-amino-5-(6-metoksipiridin-3-il)piridin-3-il]-2-metoksifenol; 4-[6-amino-5-[4-(4-metilpiperazin-1-il)fenil]piridin-3-il]-2,6-dimetilfenol; [4-[6-amino-5-(6-metoksipiridin-3-il)piridin-3-il]fenil]metanol; 4-[6-amino-5-[4-(4-metilpiperazin-1-il)fenil]piridin-3-il]fenol; (N,N-dimetil){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N,N-dimetil benzamid; 5-(2-metoksipiridin-5-il)-3-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(pirimidin-5-il)piridin-2-amin; (morfolino){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; (N-metil piperazin){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 3,5-di-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-[3-(metil sulfonil)fenil]piridin-2-amin; (N-metil){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-metilbenzamid; {4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]fenil}(morfolino)metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzamid; 4-[6-amino-5-(2-metoksipiridin-5-il)piridin-3-il]benzojeva kiselina; N{4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}metil sulfonamid; 4-[6-amino-5-(6-metoksipiridin-3-il)piridin-3-il]-N-(3-hidroksipropil)-benzamid; 5-(benzo[c][1,2,5]oksadiazol-6-il)-3-(2-metoksipiridin-5-il)piridin-2-amin; N-ciklopropil-{4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 5-(H-imidazo[1,2-a]piridin-6-il)-3-(2-metoksipiridin-5-il)piridin-2-amin; 3-(2-metoksipiridin-3-il)-5-(1-metil-1H-indazol-6-il)piridin-2-amin; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N(2-morfolino etil) benzamid; 3-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzamid; 3-(2-metoksipiridin-5-il)-5-[4-(5-metil-1,3,4-oksadiazol-2-il)fenil]piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-(6-morfolinopiridin-3-il)piridin-2-amin; 5-[4-(1H-pirazol-1-il)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-(kinolin-6-il)piridin-2-amin; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-[2-(pirolidin-1-il) etil]benzamid; 5-[2-(trifluoro metil)-4-(metilsulfonil)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin; {4-[2-amino-3-(4-karbamoil fenil)piridin-5-il]fenil}(morfolino)metanon; 4-[2-amino-3-(2-metilpiridin-5-il)piridin-5-il]benzamid; [4-(2-amino-5-metilpiridin-3-il)-N-(2-hidroksietil)benzamido](morfolino) metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5 il]benzen sulfonamid; 4-[2-amino-3-(4-benzamido)piridin-5-il]benzamid; {4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]fenil}(4-metilpiperazin-1-il) metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N[4-(aminometil) tiazol-2-il]benzamid; {4-[2-amino-3-(4-(trifluorometil)fenil)piridin-5-il]fenil}(morfolino)metanon; 3-(2-metoksipiridin-3-il)-5-[4-(metil sulfonil fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(piridin-3-il)piridin-2-amin; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzonitril; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzonitril; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzamid; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}-N-metilbenzamid; 3-(H-imidazo[1,2-a]piridin-6-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metoksi pirimidin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(kinoksalin-7-il)piridin-2-amin; 3-(furan-3-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-[4-(5-metil-1,3,4-oksadiazol-2-il)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-kloro-2-metoksipiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[3-(trifluorometoksi)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[4-(trifluorometoksi)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[2-(pirolidin-1-il)piridin-5-il]piridin-2-amin; 3-[2-kloro-4-(trifluorometil)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-metoksipiridin-4-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(2-morfolino piridin-5-il)piridin-2-amin; 3-[2-(trifluorometil)piridin-4-il]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metilpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-[2-(trifluoro-metil)piridin-5-il]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-{4-[2-(pirolidin-1-il) etoksi]fenil}-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(4-morfolinofenil)piridin-2-amin; 3-[4-(1H-pirazol-1-il)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}pirimidin-2-amin; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzamid; 3-(6-metoksi-2-metilpiridin-3-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(izokinolin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(kinolin-6-il)piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-p-tolilpiridin-2-amin; {5-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]piridin-2-il}metanol; 3-(2-metilbenzo[d]tiazol-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; N-{4-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]fenil}-2-(dimetilamino)acetamid; 3-(2-fluorpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[2-(metilsulfonil)piridin-5-il]piridin-2-amin; N-{5-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]piridin-2-il}acetamid; 3-(benzo[c][1,2,5]oksadiazol-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il]-N-(2-hidroksietil) benzamid; 3-[4-(trifluorometil)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-metilpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; i 5-[3-fluoro-4-(metilsulfonil)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin.
12. Aminopiridin opisan u patentnom zahtjevu 10 za upotrebu u vidu medikamenta, odabran iz grupe koju čine: 3-(6-metoksipiridin-3-il)-5-(4-metilsulfonilfenil)piridin-2-amin; 5-(4-metilsulfonilfenil)-3-[3-(trifluorometil)fenil]piridin-2-amin; 3-[2-amino-5-(4-metilsulfonilfenil)piridin-3-il]fenol; 4-[2-amino-5-(4-metilsulfonilfenil)piridin-3-il]-2-metoksifenol; 4-[2-amino-5-(6-metoksipiridin-3-il)piridin-3-il]-2-metoksifenol; 4-[6-amino-5-[4-(4-metilpiperazin-1-il)fenil]piridin-3-il]-2,6-dimetilfenol; [4-[6-amino-5-(6-metoksipiridin-3-il)piridin-3-il]fenil]metanol; 4-[6-amino-5-[4-(4-metilpiperazin-1-il)fenil]piridin-3-il]fenol; (N,N-dimetil){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N,N-dimetil benzamid; 5-(2-metoksipiridin-5-il)-3-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(pirimidin-5-il)piridin-2-amin; (morfolino){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 3,5-di(2-metoksipiridin-5-il)piridin-2-amin; (N-metil piperazin){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 3,5-di-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-[3-(metil sulfonil)fenil]piridin-2-amin; (N-metil){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-metilbenzamid; {4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]fenil}(morfolino)metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzamid; 4-[6-amino-5-(2-metoksipiridin-5-il)piridin-3-il]benzojeva kiselina; N-{4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}metil sulfonamid; 4-[6-amino-5-(6-metoksipiridin-3-il)piridin-3-il]-N-(3-hidroksipropil)-benzamid; 5-(benzo[c][1,2,5]oksadiazol-6-il)-3-(2-metoksipiridin-5-il)piridin-2-amin; N-ciklopropil-{4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 5-(H-imidazo[1,2-a]piridin-6-il)-3-(2-metoksipiridin-5-il)piridin-2-amin; 3-(2-metoksipiridin-3-il)-5-(1-metil-1H-indazol-6-il)piridin-2-amin; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-(2-morfolinoetil)benzamid; 3-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-benzamid; 3-(2-metoksipiridin-5-il)-5-[4-(5-metil-1,3,4-oksadiazol-2-il)fenil]piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-(6-morfolinopiridin-3-il)piridin-2-amin; 5-[4-(1H-pirazol-1-il)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-(kinolin-6-il)piridin-2-amin; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N[2-(pirolidin-1-il)etil]benzamid; 5-[2-(trifluoro metil)-4-(metilsulfonil)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin; {4-[2-amino-3-(4-karbamoilfenil)piridin-5-il]fenil}(morfolino)metanon; 4-[2-amino-3-(2-metilpiridin-5-il)piridin-5-il]benzamid; [4-(2-amino-5-metilpiridin-3-il)-N-(2-hidroksietil)benzamido](morfolino) metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen sulfonamid; 4-[2-amino-3-(4-benzamido)piridin-5-il]benzamid; {4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]fenil}(4-metilpiperazin-1-il) metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N[4-(aminometil)tiazol-2-il]benzamid; {4-[2-amino-3-(4-(trifluorometil)fenil)piridin-5-il]fenil}(morfolino)metanon; 3-(2-metoksipiridin-3-il)-5-[4-(metil sulfonil fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(piridin-3-il)piridin-2-amin; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzonitril; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzonitril; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzamid; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}-N-metilbenzamid; 3-(H-imidazo[1,2-a]piridin-6-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metoksi pirimidin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(kinoksalin-7-il)piridin-2-amin; 3-(furan-3-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-[4-(5-metil-1,3,4-oksadiazol-2-il)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-kloro-2-metoksipiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[3-(trifluorometoksi)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[4-(trifluorometoksi)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[2-(pirolidin-1-il)piridin-5-il]piridin-2-amin; 3-[2-kloro-4-(trifluorometil)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-metoksipiridin-4-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(2-morfolinopiridin-5-il)piridin-2-amin; 3-[2-(trifluorometil)piridin-4-il]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metilpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-[2-(trifluoro-metil)piridin-5-il]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-{4-[2-(pirolidin-1-il)etoksi]fenil}-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(4-morfolinofenil)piridin-2-amin; 3-[4-(1H-pirazol-1-il)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}pirimidin-2-amin; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzamid; 3-(6-metoksi-2-metilpiridin-3-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(izokinolin-5-il)-5-[4-(metil sulfonil)fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(kinolin-6-il)piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-p-tolilpiridin-2-amin; {5-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]piridin-2-il}metanol; 3-(2-metilbenzo[d]tiazol-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; N-{4-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]fenil}-2-(dimetilamino)acetamid; 3-(2-fluorpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[2-(metilsulfonil)piridin-5-il]piridin-2-amin; N-{5-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]piridin-2-il}acetamid; 3-(benzo[c][1,2,5]oksadiazol-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il]-N-(2-hidroksietil) benzamid; 3-[4-(trifluorometil)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-metilpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; i 5-[3-fluoro-4-(metilsulfonil)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin.
13. Farmaceutska formulacija koja sadrži najmanje jedan od derivata odabran iz grupe koju čine: 3-(6-metoksipiridin-3-il)-5-(4-metilsulfonilfenil)piridin-2-amin; 5-(4-metilsulfonilfenil)-3-[3-(trifluorometil)fenil]piridin-2-amin; 3-[2-amino-5-(4-metilsulfonilfenil)piridin-3-il]fenol; 4-[2-amino-5-(4-metilsulfonilfenil)piridin-3-il)]-2-metoksifenol; 4-[2-amino-5-(6-metoksipiridin-3-il)piridin-3-il]-2-metoksifenol; 4-[6-amino-5-[4-(4-metilpiperazin-1-il)fenil]piridin-3-il]-2,6-dimetilfenol; [4-[6-amino-5-(6-metoksipiridin-3-il)piridin-3-il]fenil]metanol; 4-[6-amino-5-[4-(4-metilpiperazin-1-il)fenil]piridin-3-il]fenol; (N,N-dimetil){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N,N-dimetil benzamid; 5-(2-metoksipiridin-5-il)-3-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metil sulfonil)fenil]-3-(pirimidin-5-il)piridin-2-amin; (morfolino){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 3,5-di(2-metoksipiridin-5-il)piridin-2-amin; (N-metil piperazin){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 3,5-di-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-[3-(metil sulfonil)fenil]piridin-2-amin; (N-metil){4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-metilbenzamid; {4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]fenil}(morfolino)metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzamid; 4-[6-amino-5-(2-metoksipiridin-5-il)piridin-3-il]benzojeva kiselina; N-{4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}metil sulfonamid; 4-[6-amino-5-(6-metoksipiridin-3-il)piridin-3-il]-N-(3-hidroksipropil) benzamid; 5-(benzo[c][1,2,5]oksadiazol-6-il)-3-(2-metoksipiridin-5-il)piridin-2-amin; N-ciklopropil-{4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen}sulfonamid; 5-(H-imidazo[1,2-a]piridin-6-il)-3-(2-metoksipiridin-5-il)piridin-2-amin; 3-(2-metoksipiridin-3-il)-5-(1-metil-1H-indazol-6-il)piridin-2-amin; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N-(2-morfolinoetil)benzamid; 3-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzamid; 3-(2-metoksipiridin-5-il)-5-[4-(5-metil-1,3,4-oksadiazol-2-il)fenil]piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-(6-morfolinopiridin-3-il)piridin-2-amin; 5-[4-(1H-pirazol-1-il)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin; 3-(2-metoksipiridin-5-il)-5-(kinolin-6-il)piridin-2-amin; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N[2-(pirolidin-1-il)etil]benzamid; 5-[2-(trifluorometil)-4-(metilsulfonil)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin; {4-[2-amino-3-(4-karbamoilfenil)piridin-5-il]fenil}(morfolino)metanon; 4-[2-amino-3-(2-metilpiridin-5-il)piridin-5-il]benzamid; [4-(2-amino-5-metilpiridin-3-il)-N-(2-hidroksietil) benzamido](morfolino) metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]benzen sulfonamid 4-[2-amin-3-(4-benzamido)piridin-5-il]benzamid; {4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]fenil}(4-metilpiperazin-1-il) metanon; 4-[2-amino-3-(2-metoksipiridin-5-il)piridin-5-il]-N[4-(aminometil)tiazol-2-il]benzamid; {4-[2-amino-3-(4-(trifluorometil)fenil)piridin-5-il]fenil}(morfolino)metanon; 3-(2-metoksipiridin-3-il)-5-[4-(metilsulfonilfenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(piridin-3-il)piridin-2-amin; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzonitril; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzonitril; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzamid; 4-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}-N-metilbenzamid; 3-(H-imidazo[1,2-a]piridin-6-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metoksipirimidin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(kinoksalin-7-il)piridin-2-amin; 3-(furan-3-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-[4-(5-metil-1,3,4-oksadiazol-2-il)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-kloro-2-metoksipiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[3-(trifluorometoksi)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[4-(trifluorometoksi)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[2-(pirolidin-1-il)piridin-5-il]piridin-2-amin; 3-[2-kloro-4-(trifluorometil)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-metoksipiridin-4-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(2-morfolino piridin-5-il)piridin-2-amin; 3-[2-(trifluorometil)piridin-4-il]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(2-metilpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-[2-(trifluoro-metil)piridin-5-il]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-{4-[2-(pirolidin-1-il)etoksi]fenil}-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(4-morfolinofenil)piridin-2-amin; 3-[4-(1H-pirazol-1-il)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}pirimidin-2-amin; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il}benzamid; 3-(6-metoksi-2-metilpiridin-3-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(izokinolin-5-il)-5-[4-(metil sulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-(kinolin-6-il)piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-p-tolilpiridin-2-amin; {5-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]piridin-2-il}metanol; 3-(2-metilbenzo[d]tiazol-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; N-{4-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]fenil}-2-(dimetilamino) acetamid; 3-(2-fluorpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 5-[4-(metilsulfonil)fenil]-3-[2-(metilsulfonil)piridin-5-il]piridin-2-amin; N-{5-[2-amino-5-(4-(metilsulfonil)fenil)piridin-3-il]piridin-2-il}acetamid; 3-(benzo[c][1,2,5]oksadiazol-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-{2-amino-5-[4-(metilsulfonil)fenil]piridin-3-il]-N-(2-hidroksietil) benzamid; 3-[4-(trifluorometil)fenil]-5-[4-(metilsulfonil)fenil]piridin-2-amin; 3-(3-metilpiridin-5-il)-5-[4-(metilsulfonil)fenil]piridin-2-amin; i 5-[3-fluoro-4-(metilsulfonil)fenil]-3-(2-metoksipiridin-5-il)piridin-2-amin i njihovi farmaceutski prihvatljivi nosači, razrjeđivači ili ekscipijensi.
14. Farmaceutska formulacija koji sadrži aminopiridin prema formuli (I) i antimalarijski agens, naznačen time da su X i Y definirani u bilo kojem od prethodnih patentnih zahtjeva.
15. Aminopiridin za upotrebu prema bilo kom od patentnih zahtjeva od 1 do 10, naznačen time da se aminopiridin ili njegova farmaceutska formulacija primjenjuju u kombinaciji sa ko-agensom koji je od koristi u liječenju malarije.
16. Aminopiridin za upotrebu prema patentnom zahtjevu 15, naznačen time da je ko-agens odabran iz grupe koju čine artemeter, klorokin, meflokin, kinin, atovakvon/progvanil, doksiciklin, artesunat, hidroksiklorokin, halofantrin, pirimetamin-sulfadoksin, primakin i piperakin.
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