HRP20150185T1 - Inhibitori kinaza koji reguliraju signalne puteve u apoptozi - Google Patents

Inhibitori kinaza koji reguliraju signalne puteve u apoptozi Download PDF

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HRP20150185T1
HRP20150185T1 HRP20150185AT HRP20150185T HRP20150185T1 HR P20150185 T1 HRP20150185 T1 HR P20150185T1 HR P20150185A T HRP20150185A T HR P20150185AT HR P20150185 T HRP20150185 T HR P20150185T HR P20150185 T1 HRP20150185 T1 HR P20150185T1
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cyclopropyl
triazol
phenyl
carboxamide
picolinamide
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HRP20150185AT
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Britton Corkey
Michael Graupe
Keith Koch
Lawrence S. Melvin
Gregory Notte
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Gilead Sciences, Inc.
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Publication of HRP20150185T1 publication Critical patent/HRP20150185T1/hr

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Claims (17)

1. Spoj formule (I) [image] gdje: R1 je alkil od 1-10 atoma ugljika, cikloalkil od 3-8 atoma ugljika, alkenil koji sadrži do 10 atoma ugljika, alkinil koji sadrži do 10 atoma ugljika, aril, heteroaril ili heterociklil, od kojih su svi opcionalno supstituirani sa 1, 2, ili 3 supstituenta izabrana od halo, okso, alkila od 1-6 atoma ugljika, cikloalkila od 3-8 atoma ugljika, heterociklila, fenila, fenoksija, halo, -CN, -O-R6, -C(O)-R6, -OC(O)-R6 -C(O)-O-R6, - N(R6)-C(O)-O-R7, -N(R6)-C(O)-R7, -N(R6)-C(O)-N(R6)(R7), i -C(O)-N(R6)(R7), gdje su alkil, cikloalkil, heterociklil, fenil, i fenoksi opcionalno supstituirani sa 1, 2, ili 3 supstituenta izabrana od alkila od 1-6 atoma ugljika, cikloalkila od 3-8 atoma ugljika, alkoksija od 1-6 atoma ugljika, hidroksila, i halo; pod uvjetom da R1 nije metil kada je R3 morfolinil ili furil; gdje su R6 i R7 nezavisno izabrani iz grupe koja se sastoji od vodika, alkila od 1-6 atoma ugljika, ili cikloalkila od 3-8 atoma ugljika; ili R6 i R7 kada uzeti zajedno sa dušikom za koji su vezani formiraju heterocikl; R2 je vodik, halo, cijano, alkoksi, ili alkil opcionalno supstituiran sa halo; R3 je aril, heteroaril, ili heterociklil, od kojih su svi opcionalno supstituirani sa 1, 2 ili 3 supstituenta izabrana od alkila od 1-6 atoma ugljika, alkoksija od 1-6 atoma ugljika, cikloalkila od 3-8 atoma ugljika, cikloalkilalkila, arila, arilalkila, heteroarila, heteroarilalkila, heterociklila, heterociklilalkila, halo, haloalkoksija, okso, -CN, -O-R6, -O-C(O)-R6, -O-C(O)-N(R6)(R7), -S-R6, -N(R6)(R7), -S(=O)-R6, -S(=O)2R6, -S(=O)2-N(R6)(R7), -S(=O)2-O-R6, -N(R6)-C(O)-R7, -N(R6)-C(O)-O-R7, -N(R6)-C(O)-N(R6)(R7), -C(O)-R6, -C(O)-O-R6, -C(O)-N(R6)(R7), i -N(R6)-S(=O)2-R7, gdje je alkil, alkoksi, cikloalkil, aril, heteroaril ili heterociklil dalje opcionalno supstituiran sa jednim ili više supstituenata izabranih od halo, hidroksila, okso, -CN, i -O-R6; uz uvjet da heteroaril ili heterociklil grupa uključuje bar jedan prsten atoma dušika; X1, X2, X3, X4, X5, X6, X7 i X8 su nezavisno C(R4) ili N, u kojoj svaki R4 je nezavisno vodik, hidroksil, halo, alkil od 1-6 ugljikovih atoma, alkoksi od 1-6 ugljikovih atoma, ili cikloalkil od 3-8 ugljikovih atoma, gdje je alkil ili cikloalkil dalje opcionalno supstituiran sa jednim ili više supstituenata izabranih od halo, hidroksila, okso, -CF3, -O-CF3, -N(R6)(R7), -C(O)-R6, -C(O)-O-R7, -C(O)-N(R6)(R7), -CN, -O-R6; ili X5 i X6 ili X6 i X7 su vezani da formiraju fuzionirani cikloalkil, fuzionirani aril, ili fuzionirani heteroaril, od kojih su svi opcionalno supstituirani sa alkilom od 1-6 atoma ugljika, hidroksilom, ili halo; i uz uvjet da najmanje jedan od X2, X3, i X4 je C(R4); najmanje dva od X5, X6, X7, i X8 su C(R4); i najmanje jedan od X2, X3, X4, X5, X6, X7 i X8 je N.
2. Spoj patentnog zahtjeva 1, gdje X1 je N.
3. Spoj patentnog zahtjeva 2, gdje (i) X2 i X5 su N, (ii) X2 je C(R4) i X5 je N, ili (iii) X2 je N i X5 je C(R4).
4. Spoj patentnog zahtjeva 3, gdje X3, X4, X6, X7, i X8 su C(R4).
5. Spoj patentnog zahtjeva 4, gdje je R1 opcionalno supstituiran alkilom, opcionalno supstituiran cikloalkilom, ili opcionalno supstituiran heterociklilom.
6. Spoj patentnog zahtjeva 5, gdje su alkil, cikloalkil, i heterociklil opcionalno supstituirani sa 1, 2, ili 3 supstituenata izabrana od hidroksila, halo, ili cikloalkila.
7. Spoj patentnog zahtjeva 6, gdje je R3 opcionalno supstituirani aril, opcionalno supstituirani heteroaril ili opcionalno supstituirani heterociklil, gdje heteroaril ili heterociklil grupe sadrže 1, 2 ili 3 prstena dušikovog atoma.
8. Spoj patentnog zahtjeva 7, gdje je R3 izabrano od [image] [image] [image] [image] [image] [image] [image] gdje: R11 je vodik, alkil, ili cikloalkil, gdje su alkil i cikloalkil opcionalno supstituirani hidroksilom ili halo; R12 je vodik, alkil, cikloalkil, -S(=O)-R6 ili -S(=O)2R6, gdje su alkil i cikloalkil opcionalno supstituirani hidroksilom ili halo; i gdje su R3 aril, heteroaril, i heterociklil grupe opcionalno supstituirani alkilom, cikloalkilom, halo, cijanom, -OR6, u kojima su alkil i cikloalkil opcionalno supstituirani hidroksilom ili halo.
9. Spoj patentnog zahtjeva 8, gdje je R2 vodik ili halo.
10. Spoj patentnog zahtjeva 9, izabrano od: 6-ciklopropil-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3,4'-bipiridin-2'-karboksamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4,5-dimetil-1H-imidazol-1-il)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-6-(2-hidroksipropan-2-il)-3,4'-bipiridin-2'-karboksamid. 6'-ciklopropil-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-2,3'-bipiridin-6-karboksamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(5-metil-4-(trifluorometil)-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-1-il)pikolinamid; 6-ciklopropil-N-(6-(4-((2R)-3-hidroksibutan-2-il)-4H-1,2,4-triazol-3-il)piridin-2-il)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(6-(4-((2S,3R)-3-hidroksibutan-2-il)-4H-1,2,4-triazol-3-il)piridin-2-il)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(6-(4-((2S,3S)-3-hidroksibutan-2-il)-4H-1,2,4-triazol-3-il)piridin-2-il)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(6-(4-(1-(pirolidin-1-il)propan-2-il)-4H-1,2,4-triazol-3-il)piridin-2-il)-3,4'-bipiridin-2'-karboksamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(6-ciklopropilpiridin-3-il)-7,8-dimetilhinolin-2-karboksamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)hinolin-2-karboksamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(6-ciklopropilpiridin-3-il)hinolin-2-karboksamid; 4-((4-ciklopropil-2-metil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4,5,6,7-tetrahidro-1H-benzo[d]imidazol-1-il)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4-(trifluorometil)-1H-imidazol-1-il)pikolinamid; N-(6-(4-ciklopropil4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4-(trifluorometil)-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-1-il)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4-(perfluoroetil)-1H-imidazol-1-il)pikolinamid; 4-((3-ciklopropil-1H-1,2,4-triazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4-(2,2,2-trifluoro-1-hidroksietil)-1H-imidazol-1-il)pikolinamid; 6-ciklopropil-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-5'-metil-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(2-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-4-il)-3,4'-bipiridin-2'-karboksamid; N-(2-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-4-il)-4-(hinolin-3-il)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4-metil-1H-imidazol-1-il)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4-izopropil-1H-imidazol-1-il)pikolinamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(3-hidroksipiperidin-1-il)pikolinamid; 6-ciklopropil-N-(6-(4-izopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3,4'-bipiridin-2'-karboksamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4-etil-3-oksopiperazin-1-il)pikolinamid; (R)-6-ciklopropil-N-(6-(4-(1,1,1-trifluoropropan-2-il)-4H-1,2,4-triazol-3-il)piridin-2-il)-3,4'-bipiridin-2'-karboksamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4-(N-metilsulfamoil)fenil)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(hinolin-3-il)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4-fenil-1H-imidazol-1-il)pikolinamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-(4-(metilsulfonil)fenil)pikolinamid N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-fenil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-(piridin-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4,-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-(piridin-3-il)-4H-1,2,4-triazo]-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-(piridin-4-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-(pirimidin-5-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-(but-2-inil)-4H-1,2,4-triazol-3-il)fenil)-6-ciklopropil-3,41-bipiridin-21-karboksamid; 6-ciklopropil-N-(3-(4-(1-(piridin-3-iloksi)propan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-(1-(2,2,2-trifluoroetoksi)propan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-fenil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-(piridin-2-il)-4H-1,2,4-triazol-3-il)fenil)pikolinamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-(piridin-3-il)-4H-1,2,4-triazol-3-il)fenil)pikolinamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-(piridin-4-il)-4H-1,2,4-triazol-3-il)fenil)pikolinamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-(pirimidin-5-il)-4H-1,2,4-triazol-3-il)fenil)pikolinamid; N-(3-(4-(but-2-inil)-4H-1,2,4-triazol-3-il)fenil)-4-(4-ciklopropil-1H-imidazol-1-il)pikolinamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-(1-(piridin-3-iloksi)propan-2-il)-4H-1,2,4-triazol-3-il)fenil)pikolinamid i 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-(l-(2,2,2-trifluoroetoksi)propan-2-il)-4H-1,2,4-triazol-3-il)fenil)pikolinamid.
11. Spoj patentnog zahtjeva 9, izabrano od: 6-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(2-ciklopropilpirimidin-5-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(2,2,2-trifluoroetil)-3,4'-bipiridin-2'-karboksamid; 4-((imidazo[1,2-a]piridin-3-il)-N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-pikolinamid; 4-((2-aminopirolidin-5-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-fenilpikolinamid; N-(3-(4-(tetrahidro-2H-piran-4-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1H-imidazol-1-il)pikolinamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-4-fenilpikolinamid; N-(3-(4-(3-amino-3-oksopropil)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1H-1,2,4-triazol-1-il)pikolinamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-6-fenilpikolinamid; N-(3-(4-(2-acetamidoetil)-4H-I,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-4-(4-metilpiperazin-1-il)pikolinamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-2,3'-bipiridin-6-karboksamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-4-morfolinpikolinamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-6-(hinolin-6-il)pikolinamid; (R)-N-(3-(4-(1-hidroksipropan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,41-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-hidroksi-3,4'-bipiridin-2'-karboksamid; (S)-N-(3-(4-(1-hidroksipropan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)4-(3-oksopiperazin-1-il)pikolinamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-metoksi-3,4'-bipiridin-2'-karboksamid; 4-((3-aminopirolidin-1-il)-N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)pikolinaimid; 6-amino-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; (R)-N-(3-(4-(2-hidroksipropil)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 5-metoksi-N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; Metil 2'-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenilkarbamoil)-3,4'-bipiridin-6-ilkarbamat; (S)-N-(3-(4-(2-hidroksipropil)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 4-((1-metil-1H-imidazol-5-il)-N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1-metil-1H-imidazol-5-il)pikolinamid; 4-((1H-benzo[d]imidazol-1-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(2,4-dimetoksipirimidin-5-il)pikolinamid; N-(3-(4-((1-hidroksiciklopropil)metil)=4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-fenil-1H-imidazol-1-il)pikolinamid; N-(3-(4-ciklobutil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N2'-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2',6-dikarboksamid; (S)-N-(3-(4-(1,1,1-trifluoropropan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopentil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(trifluorometil)-3,4'-bipiridin-2'-karboksamid; N2'-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2',5-dikarboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(2-metil-1H-imidazol-1-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-metil-3,4'-bipiridin-2'-karboksamid; 5-cijano-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-metil-1H-imidazol-1-il)pikolinamid; 2-amino-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4,5-dimetil-1H-imidazol-1-il)pikolinamid; N-(3-(4-((1S,2S)-2-metilciklopropil)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-2-metoksi-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(trifluorometil)-1H-imidazol-1-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(2,2,2-trifluoroetoksi)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2.4-triazol-3-il)fenil)-4-(1-metil-1H-pirazol-4-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(2-metoksipirimidin-5-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-metil-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(imidazo[1,2-a]piridin-3-il)pikolinamid; 6'-metil-N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-(2,2,2-trifluoroetil)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 6-hloro-[3,2',5',4"]terpiridin-2"-karboksilna kiselina [3-(4-ciklopropil-4H-[1,2,4]triazol-3-il)-fenil]amid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(pirolidin-1-il)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-5-(trifluorometil)-3,4'-bipiridin-2'-karboksamid; N-3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1,2-dimetil-1H-imidazol-5-il)pikolinamid; 4-((1H-benzo[d][1,2,3]triazol-1-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-sulfamoilfenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-5-metoksi-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-fluoro-5-metil-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-5-fluoro-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-2-metil-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4,5,6,7-tetrahidro-1H-benzo[d]imidazol-1-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(N-metilsulfamoil)fenil)pikolinamid; N5-tert-butil-N2'-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2',5-dikarboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(pirazin-2-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(N-izopropilsulfamoil)fenil)pikolinamid; 5-hloro-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(3-(metilsulfonil)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(izohinolin-4-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(2-(metilsulfonil)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1,5-dimetil-1H-pirazol-4-il)pikolinamid; 6-ciklobutil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-izopropil-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(metilsulfonil)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(dimetilamino)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1H-pirolo[2,3-b]piridin-5-il)pikolinamid; 6-ciklopropoksi-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1H-imidazo[4,5-b]piridin-1-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-fluoro-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(2-oksoimidazolidin-1-il)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(3H-imidazo[4,5-b]piridin-3-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-izopropoksi-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1H-imidazo[4,5-c]piridin-1-il)pikolinamid; 6-ciklobutoksi-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4,-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(hinolin-3-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(N-ciklopropilsulfamoil)fenil)pikolinamid; 6-ciklopentil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(imidazo[2,1-b][1,3,4]tiadiazol-5-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(5-ciklopropilpirazin-2-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(1-metil-2-oksopirolidin-3-il)-3,4'-bipiridin-2'-karboksamid; 4-((4-hloro-1H-imidazol-1-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; 6-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-5-fluoro-3,4'-bipiridin-2'-karboksamid; (S)-4-(4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-(3-metilbutan-2-il)-4H-1,2,4-triazol-3-il)fenil)pikolinamid; 6'-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-2,3'-bipiridin-6-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(5-metil-4-(trifluorometil)-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-1-il)pikolinamid; 4-((5-ciklopropil-4-metil-4H-1,2,4-triazol-3-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; 4-((3-ciklopropil-1,2,4-oksadiazol-5-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(3-metil-1,2,4-oksadiazol-5-il)pikolinamid; 6-ciklopropil-N-(3-(4-(3-hidroksibutan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(5-(1-hidroksietil)-1,3,4-oksadiazol-2-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(6-metoksihinolin-3-il)pikolinamid; 6-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-5'-metil-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6'-metil-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1-(2,2,2-trifluoroetil)-1H-pirolo[3,2-b]piridin-6-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1-izopropil-1H-pirolo[3,2-b]piridin-6-il)pikolinamid; (S)-6-ciklopropil-N-(3-(4-(3,3-dimetilbutan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-sec-butil-4H-1,2,4-triazol-3-il)fenil)-6-ciklopropil-3,4'-bipiridin-2'-karboksamid; (S)-6-ciklopropil-N-(3-(4-(1-ciklopropiletil)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-(pentan-3-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; (S)-6-ciklopropil-N-(3-(4-(1-metoksipropan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; (S)-N-(3-(4-sec-butil-4H-1,2,4-triazol-3-il)fenil)-6-ciklopropil-3,4'-bipiridin-2'-karboksamid; (S)-6-ciklopropil-N-(3-(4-(3-metilbutan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; (R)-6-ciklopropil-N-(3-(4-(1-(2,6-dimetilfenoksi)propan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; (S)-6-ciklopropil-N-(3-(4-(1,1,1-trifluoropropan-2-il)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklobutil-4H-1,2,4-triazol-3-il)fenil)-6-ciklopropil-3,4'-bipiridin-2'-karboksamid; (S)-6-ciklopropil-N-(3-(4-(1-feniletil)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-izopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-(ciklopropilmetil)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; 4-((4-ciklopropil-2-metil-1H-imidazol-1-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-izopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-(ciklopropilmetil)-4H-l,2,4-triazol-3-il)fenil)pikolinamid; 4-((4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-(1-feniletil)-4H-1,2,4-triazol-3-il)fenil)pikolinamid; (R)-4-(4-ciklopropil-11H-imidazol-1-il)-N-(3-(4-(1,1,1-trifluoropropan-2-il)-4H-1,2,4-triazol-3-il)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1,5-naftiridin-3-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(trifluorometil)-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-1-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(perfluoroetil)-1H-imidazol-1-il)pikolinamid; 4-((3-cydopropil-1H-1,2,4-triazol-1-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; 4-((5-ciklopropil-1H-1,2,4-triazol-1-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(2,2,2-trifluoro-1-hidroksietil)-1H-imidazol-1-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(2-etilpirimidin-5-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-5-etil-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)-4-fluorofenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)-4-fluorofenil)-6-etil-3,4'-bipiridin-2'-karboksamid; 6-tert-butil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(5,6,7,8-tetrahidro-1,6-naftiridin-3-il)pikolinamid; 6-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)-2-fluorofenil)-3,4'-bipiridin-2'-karboksamid; 5-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)-2-fluorofenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-etil-1H-imidazol-1-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(6-(2,2,2-trifluoroetil)-5,6,7,8-tetrahidro-1,6-naftiridin-3-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-izopropil-1H-imidazol-1-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(2-hidroksipropan-2-il)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)-5-fluorofenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)-5-fluorofenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(6-izopropil-5,6,7,8-tetrahidro-1,6-naftiridin-3-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(6-metil-5,6,7,8-tetrahidro-1,6-naftiridin-3-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(3-hidroksipiperidin-1-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-etil-3-oksopiperazin-1-il)pikolinamid; N-(3-(4-izopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-propil-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-neopentil-3,4'-bipiridin-2'-karboksamid;; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1-metil-2-fenil-1H-imidazol-5-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(etilsulfonil)fenil)-pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(izopropilsulfonil)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(etilamino)-3;4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(ciklopropilamino)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6'-(trifluorometil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(hinolin-3-il)-6-(trifluorometil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(1H-pirolo[3,2-b]piridin-6-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-ciklopropilfenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(metiltio)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(izobutiltio)-3,4'-bipiridin-2'-karboksamid; 5-hloro-6-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(2-metoksietilamino)-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(4-(metilsulfonil)piperazin-1-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-etil-5-fluoro-3,4'-bipiridin-2'-karboksamid; 5-hloro-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-etil-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-5,6-dietil-3,4'-bipiridin-2'-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(furo[3,2-b]piridin-6-il)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(3-metil-3H-imidazo[4,5-b]piridin-6-il)pikolinamid; 6-ciklopropil-N-(3-(4-(2-fenilciklopropil)-4H-1,2,4-triazol-3-il)fenil)-3,4'-bipiridin-2'-karboksamid; (S)-4-(4-ciklopropil-1H-imidazol-1-il)-N-(3-(4-(1,1,-trifluoropropan-2-il)-4H-1,2,4-triazol-3-il)fenil)pikolinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(ciklopropilmetil)-3,4'-bipiridin-2'-karboksamid; i 4-((5-ciklopropil-1,3,4-tiadiazol-2-il)-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)pikolinamid.
12. Spoj patentnog zahtjeva 9, izabrano od: N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3-(hinolin-3-il)benzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-5-(6-ciklopropilpiridin-3-il)-2,4-difluorobenzamid; 4-hloro-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-5-(6-ciklopropilpiridin-3-il)-2-fluorobenzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3-(4-(2,2,2-trifluoro-1-metoksietil)-1H-imidazol-1-il)benzamid; 3-((4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-4-metoksibenzamid; 4-hloro-3-(4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)benzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-5-(6-ciklopropilpiridin-3-il)-2-fluorobenzamid; 3-((4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-izopropil-4H-1,2,4-triazol-3-il)piridin-2-il)benzamid; (S)-3-(4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-(1-feniletil)-4H-1,2,4-triazol-3-il)piridin-2-il)benzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3-(1,5-naftiridin-3-il)benzamid; 3-((4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)benzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3-(4-izopropil-1H-imidazol-1-il)benzamid; 3-((4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-2-metilbenzamid; 5-((4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-2-metilbenzamid; 3-((4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4- triazol-3-il)piridin-2-il)-4-metilbenzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3-(6-(2-hidroksipropan-2-il)piridin-3-il)benzamid; 3-((4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-yi)piridin-2-il)-5-fluorobenzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3-(4-(2,2,2-trifluoro-1-hidroksietil)-1H-imidazol-1-il)benzamid; 3-((4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-5-metilbenzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3-(4,5-dimetil-1H-imidazol-1-il)benzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3-(4,5,6,7-tetrahidro-1H-benzo[d]imidazol-1-il)benzamid; 1-((3-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-ilkarbamoil)fenil)-5-metil-1H-imidazol-4-karboksilna kiselina; (S)-3-(4-ciklopropil-1H-imidazol-1-il)-N-(6-(4-(1-feniletil)-4H-1,2,4-triazol-3-il)piridin-2-il)benzamid; (S)-3-(4,5-dimetil-1H-imidazol-1-il)-N-(6-(4-(1,1,1-trifluoropropan-2-il)-4H-1,2,4-triazol-3-il)piridin-2-il)benzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3-(6-ciklopropilpiridin-3-il)benzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-3-(piridin-3-il)benzamid; N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-5-(6-ciklopropilpiridin-3-il)-2,4-difluorobenzamid; 4-hloro-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-5-(6-ciklopropilpiridin-3-il)-2-fluorobenzamid; i 3-((4-ciklopropil-1H-1,2,3-triazol-1-il)-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)benzamid.
13. Spoj patentnog zahtjeva 1, izabrano od: N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(6-ciklopropilpiridin-3-il)-7,8-dimetilhinolin-2-karboksamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-4-(piridin-3-il)hinolin-2-karboksamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-3,3'-bipiridin-5-karboksamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-5-fenilnikotinamid; N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-2-fenil izonikotinamid; 6'-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-2,3'-bipiridin-6-karboksamid; 6'-ciklopropil-N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-2,3'-bipiridin-4-karboksamid; 5-((2,5-difluorofenil)-N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)nikotinamid; N-(3-(4-ciklopropil-4H-1,2,4-triazol-3-il)fenil)-6-(6-ciklopropilpiridin-3-il)pirimidin-4-karboksamid; 6'-ciklopropil-N-(6-(4-ciklopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-2,3'-bipiridin-4-karboksamid; i 2-hidroksi-N-(3-(4-metil-4H-1,2,4-triazol-3-il)fenil)-6-fenilpirimidin-4-karboksamid.
14. Spoj patentnog zahtjeva 1, gdje X1 je C.
15. Spoj patentnog zahtjeva 14, izabrano od: N-(6-(1-ciklopropil-1H-imidazol-5-il)piridin-2-il)-4-(4,5-dimetil-1H-imidazol-1-il)pikolinamid; N-(6-(1-ciklopropil-1H-imidazol-5-il)piridin-2-il)-6-(2-hidroksipropan-2-il)-3,4'-bipiridin-2'-karboksamid; N-(6-(1-ciklopropil-1H-imidazol-5-il)piridin-2-il)-4-(hinolin-3-il)pikolinamid; 6-ciklopropil-N-(6-(1-ciklopropil-1H-imidazol-5-il)piridin-2-il)-3,4'-bipiridin-2'-karboksamid; 6-ciklopropil-N-(3-(1-ciklopropil-1H-imidazol-5-il)fenil)-3,4'-bipiridin-2'-karboksamid; N-(3-(1-ciklopropil-1H-imidazol-5-il)fenil)-3,4'-bipiridin-2'-karboksamid; 4-((1H-benzo[d]imidazol-1-il)-N-(3-(1-ciklopropil-1H-imidazol-5-il)fenil)pikolinamid; i N-(3-(1-ciklopropil-1H-imidazol-5-il)fenil)-4-(hinolin-3-il)pikolinamid.
16. Farmaceutski sastav koji sadrži efektivnu količinu jednog ili više spojeva prema bilo kojem od zahtjeva 1 do 15 i farmaceutski prihvatljiv nositelj.
17. Spoj prema bilo kojem od patentnih zahtjeva od 1 do 15 za primjenu u liječenju bolesti iz grupe autoimunih poremećaja, inflamatornih oboljenja, kardiovaskularnih oboljenja i neurodegenerativnih oboljenja.
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Families Citing this family (195)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ590887A (en) 2008-08-04 2012-09-28 Chdi Foundation Inc Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
TWI625121B (zh) * 2009-07-13 2018-06-01 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
SG182534A1 (en) 2010-01-25 2012-08-30 Chdi Foundation Inc Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
AU2011272782B2 (en) * 2010-07-02 2014-11-27 Gilead Sciences, Inc. Apoptosis signal-regulating kinase inhibitors
US9376709B2 (en) 2010-07-26 2016-06-28 Biomatrica, Inc. Compositions for stabilizing DNA and RNA in blood and other biological samples during shipping and storage at ambient temperatures
EP2598661B1 (en) 2010-07-26 2017-09-27 Biomatrica, INC. Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures
US9045485B2 (en) 2010-12-16 2015-06-02 Convergence Pharmaceuticals Limited ASK 1 inhibiting pyrrolopyrimidine derivatives
MX2014002459A (es) 2011-08-30 2014-04-10 Chdi Foundation Inc Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodos de uso de los mismos.
SI2750677T1 (sl) * 2011-08-30 2017-10-30 Chdi Foundation, Inc. Inhibitorji kinurenin-3-monooksigenaze, farmacevtski sestavki in postopki njihove uporabe
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
AU2015201188B2 (en) * 2012-01-27 2016-12-15 Gilead Sciences, Inc. Apoptosis signal-regulating kinase inhibitor
EP3249054A1 (en) 2012-12-20 2017-11-29 Biomatrica, INC. Formulations and methods for stabilizing pcr reagents
UY35212A (es) * 2012-12-21 2014-06-30 Gilead Sciences Inc Inhibidores de la quinasa que regula la señal de la apoptosis
CN105142624A (zh) 2013-01-10 2015-12-09 普尔莫凯恩股份有限公司 非选择性激酶抑制剂
JP2016519684A (ja) 2013-04-08 2016-07-07 デニス エム ブラウン 準最適に投与された薬物療法の有効性を改善するための及び／又は副作用を低減するための方法および組成物
US20160135446A1 (en) 2013-06-13 2016-05-19 Biomatrica, Inc. Cell stabilization
US9249151B2 (en) * 2013-08-23 2016-02-02 Boehringer Ingelheim International Gmbh Bis-amido pyridines
CN106132403B (zh) 2013-10-11 2020-04-28 普尔莫凯恩股份有限公司 喷雾干燥制剂
WO2015070366A1 (en) * 2013-11-12 2015-05-21 Merck Sharp & Dohme Corp. Aryl linked imidazole and triazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug
JP2016537433A (ja) 2013-11-26 2016-12-01 ギリアード サイエンシーズ， インコーポレイテッド 骨髄増殖性障害を処置するための治療
GB201321748D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
CA2937320A1 (en) 2014-01-20 2015-07-23 Gilead Sciences, Inc. Therapies for treating cancers
WO2015187499A1 (en) 2014-06-03 2015-12-10 Gilead Sciences, Inc. Use of an ask1 inhibitor for the treatment of liver disease, optionally in combination with a loxl2 inhibitor
JP6661554B2 (ja) 2014-06-10 2020-03-11 バイオマトリカ，インク． 周囲温度における血小板の安定化
AP2017009724A0 (en) 2014-07-17 2017-01-31 Chdi Foundation Inc Methods and compositions for treating hiv-related disorders
TW201618781A (zh) 2014-08-13 2016-06-01 吉李德科學股份有限公司 治療肺高血壓之方法
JP2017528471A (ja) 2014-09-24 2017-09-28 ギリアード サイエンシーズ， インコーポレイテッド 肝疾患を処置する方法
MA41252A (fr) 2014-12-23 2017-10-31 Gilead Sciences Inc Formes solides d'un inhibiteur d'ask 1
BR112017013382A2 (pt) 2014-12-23 2018-02-14 Gilead Sciences Inc método para preparar um composto, composto, e, ácido.
TW201639573A (zh) 2015-02-03 2016-11-16 吉李德科學股份有限公司 有關治療癌症之合併治療
SI3321265T1 (sl) 2015-03-04 2020-07-31 Gilead Sciences, Inc. Spojine 4,6-diamino-pirido(3,2-d)pirimidina in njihova uporaba kot modulatorji toličnih receptorjev
HUE043310T2 (hu) 2015-07-06 2019-08-28 Gilead Sciences Inc COT modulátorok és eljárások alkalmazásukra
EP3319963B1 (en) * 2015-07-09 2020-01-08 Janssen Pharmaceutica NV Substituted 4-azaindoles and their use as glun2b receptor modulators
KR200483190Y1 (ko) 2015-09-11 2017-04-13 주식회사 엔젤악기 바로크식 운지법과 독일식 운지법의 선택 적용이 가능한 리코더 링
TW201725044A (zh) 2015-10-01 2017-07-16 基利科學股份有限公司 用於治療癌症之btk抑制劑及查核點抑制劑之組合
ES2928164T3 (es) 2015-10-19 2022-11-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
LT3377488T (lt) 2015-11-19 2023-01-10 Incyte Corporation Heterocikliniai junginiai, kaip imunomoduliatoriai
WO2017100212A1 (en) 2015-12-08 2017-06-15 Biomatrica, Inc. Reduction of erythrocyte sedimentation rate
BR112017002594A2 (pt) 2015-12-17 2017-12-19 Gilead Sciences Inc compostos inibidores de cinase de ligação de tank
US20170174671A1 (en) * 2015-12-17 2017-06-22 Incyte Corporation Heterocyclic compounds as immunomodulators
BR112018012756A2 (pt) 2015-12-22 2018-12-04 Incyte Corp compostos heterocíclicos como imunomoduladores
AU2017228371A1 (en) 2016-03-04 2018-09-13 Gilead Sciences, Inc. Compositions and combinations of autotaxin inhibitors
EP3429997A1 (de) 2016-03-16 2019-01-23 Bayer CropScience Aktiengesellschaft N-(cyanbenzyl)-6-(cyclopropylcarbonylamino)-4-(phenyl)-pyridin-2-carboxamid-derivate und verwandte verbindungen als pestizide pflanzenschutzmittel
CA3019003A1 (en) 2016-04-08 2017-10-12 Gilead Sciences, Inc. Compositions and methods for treating cancer, inflammatory diseases and autoimmune diseases
MA44860A (fr) 2016-05-06 2019-03-13 Incyte Holdings Corp Composés hétérocycliques utilisés comme immunomodulateurs
WO2017205464A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
BR112018075737A2 (pt) 2016-06-13 2019-03-26 I-Mab anticorpo, composição, célula isolada, e, métodos para tratar câncer ou infecção em um paciente e para detectar expressão de pd-l1 em uma amostra.
SI3472167T1 (sl) 2016-06-20 2022-11-30 Incyte Corporation Heterociklične spojine kot imunomodulatorji
US20180016260A1 (en) 2016-07-14 2018-01-18 Incyte Corporation Heterocyclic compounds as immunomodulators
AU2017305303B2 (en) 2016-08-04 2020-05-28 Gilead Sciences, Inc. Cobicistat for use in cancer treatments
US20180057486A1 (en) 2016-08-29 2018-03-01 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018045150A1 (en) 2016-09-02 2018-03-08 Gilead Sciences, Inc. 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators
KR102268448B1 (ko) 2016-09-02 2021-06-22 길리애드 사이언시즈, 인코포레이티드 톨 유사 수용체 조정제 화합물
JP2020500183A (ja) 2016-10-27 2020-01-09 プルモキネ、インコーポレイテッド 肺高血圧症の治療のための併用療法
WO2018085069A1 (en) 2016-11-03 2018-05-11 Gilead Sciences, Inc. Combination of a bcl-2 inhibitor and a bromodomain inhibitor for treating cancer
CA3042398A1 (en) * 2016-11-11 2018-05-17 Gilead Sciences, Inc. Methods of treating liver disease
CN110036005B (zh) * 2016-11-16 2022-09-27 广东东阳光药业有限公司 酰胺衍生物及其在药物中的应用
WO2018097977A1 (en) 2016-11-22 2018-05-31 Gilead Sciences, Inc. Crystalline forms of a phosphate complex of a bet inhibitor
CA3042731A1 (en) * 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Inhibitors of interleukin-1 receptor-associated kinases and uses thereof
EP3558973B1 (en) 2016-12-22 2021-09-15 Incyte Corporation Pyridine derivatives as immunomodulators
AU2017382870B2 (en) 2016-12-22 2022-03-24 Incyte Corporation Benzooxazole derivatives as immunomodulators
CN110267953B (zh) 2016-12-22 2022-12-20 因赛特公司 四氢咪唑并[4,5-c]吡啶衍生物作为pd-l1内在化诱导剂
US20180179201A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
PL3572412T3 (pl) * 2017-01-22 2021-09-27 Fujian Cosunter Pharmaceutical Co., Ltd. Pochodna pirydyny jako inhibitor ask1 oraz sposób jej wytwarzania oraz zastosowanie
EP3572401B1 (en) * 2017-01-22 2021-09-29 Fujian Cosunter Pharmaceutical Co., Ltd. Ask1 inhibitor and preparation method and use thereof
US10584169B2 (en) 2017-01-24 2020-03-10 I-Mab Biopharma Us Limited Anti-CD73 antibodies and uses thereof
EP3580224B1 (en) 2017-02-07 2022-07-13 Biogen MA Inc. Ask1 inhibiting agents
US10314844B2 (en) 2017-02-24 2019-06-11 Gilead Sciences, Inc. Inhibitors of Bruton's tyrosine kinase
AR110998A1 (es) 2017-02-24 2019-05-22 Gilead Sciences Inc Inhibidores de la tirosina cinasa de bruton
WO2018157277A1 (en) * 2017-02-28 2018-09-07 Eli Lilly And Company Isoquinolin and naphthydrin compounds
CN111094250B (zh) * 2017-03-03 2022-11-04 江苏豪森药业集团有限公司 凋亡信号调节激酶抑制剂及其制备方法和应用
JOP20180017A1 (ar) 2017-03-14 2019-01-30 Gilead Sciences Inc مثبط كيناز منظم لإشارة تلاشي خلايا
JP2020512976A (ja) 2017-03-27 2020-04-30 ファーマケア，インク． アポトーシスシグナル調節キナーゼ１（ａｓｋ１）阻害剤化合物
KR20190126921A (ko) 2017-03-28 2019-11-12 길리애드 사이언시즈, 인코포레이티드 간 질환을 치료하는 방법
JOP20190221A1 (ar) 2017-04-05 2019-09-23 Seal Rock Therapeutics Inc مركبات مثبطات كيناز منظم لإشارات الاستماتة 1 (ask1) واستخداماتها
TW201902478A (zh) 2017-04-12 2019-01-16 美商基利科學股份有限公司 治療肝臟疾病之方法
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
PL3621615T3 (pl) 2017-05-12 2024-03-25 Enanta Pharmaceuticals, Inc. Inhibitory regulujące sygnał apoptozy kinazy 1 i sposoby ich stosowania
WO2018218042A1 (en) * 2017-05-25 2018-11-29 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2018218051A1 (en) * 2017-05-25 2018-11-29 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10246439B2 (en) 2017-05-25 2019-04-02 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
CN110770233B (zh) * 2017-06-19 2022-07-26 广东东阳光药业有限公司 稠合双环类化合物及其在药物中的应用
GB201711234D0 (en) * 2017-07-12 2017-08-23 Galapagos Nv Pyrrolopyrimidine and pyrrolopyridine derivatives
WO2019015559A1 (zh) * 2017-07-18 2019-01-24 南京圣和药业股份有限公司 作为ask抑制剂的杂环化合物及其应用
EP3284739A1 (de) 2017-07-19 2018-02-21 Bayer CropScience Aktiengesellschaft Substituierte (het)arylverbindungen als schädlingsbekämpfungsmittel
CN109400625B (zh) * 2017-08-17 2021-11-12 广东东阳光药业有限公司 稠合双环类化合物及其在药物中的应用
US10597382B2 (en) 2017-08-28 2020-03-24 Enanta Pharmaceuticals, Inc. Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
CN109456308B (zh) * 2017-09-06 2022-11-29 南京圣和药业股份有限公司 作为ask抑制剂的杂环化合物及其应用
US11034671B2 (en) 2017-09-08 2021-06-15 Sichuan Haisco Pharmaceutical Co., Ltd. Apoptosis signal-regulating kinase inhibitors and uses thereof
CN111518080A (zh) * 2017-10-12 2020-08-11 深圳市塔吉瑞生物医药有限公司 一种1,2,4-三氮唑类化合物
CN107793400B (zh) * 2017-10-31 2020-01-31 武汉九州钰民医药科技有限公司 吡啶类化合物及其在制备治疗肝脏疾病的药物中的应用
EP3710441A1 (en) * 2017-11-17 2020-09-23 Hepagene Therapeutics, Inc. Urea derivatives as inhibitors of ask1
CN109956928B (zh) * 2017-12-14 2021-07-09 四川科伦博泰生物医药股份有限公司 吡啶类化合物、其制备方法及用途
EP3728283B1 (en) 2017-12-20 2023-11-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
AU2018392212B9 (en) 2017-12-20 2021-03-18 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein
CN111801314B (zh) * 2018-01-02 2023-10-31 西尔洛克治疗公司 Ask1抑制剂化合物及其用途
CN111655678B (zh) * 2018-01-05 2023-08-22 广州市恒诺康医药科技有限公司 细胞凋亡信号调节激酶-1抑制剂及其应用
SI3752501T1 (sl) 2018-02-13 2023-08-31 Gilead Sciences, Inc. Inhibitorji pd-1/pd-l1
CN110294746B (zh) * 2018-03-21 2023-01-31 山东轩竹医药科技有限公司 一种新的ask1抑制剂及其应用
CN110294742B (zh) * 2018-03-21 2023-01-31 山东轩竹医药科技有限公司 并环类ask1抑制剂及其应用
HRP20230090T1 (hr) 2018-03-30 2023-03-17 Incyte Corporation Heterociklički spojevi kao imunomodulatori
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 ２，２，─環二核苷酸
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
WO2019200267A1 (en) 2018-04-12 2019-10-17 Terns, Inc. Tricyclic ask1 inhibitors
US10899735B2 (en) 2018-04-19 2021-01-26 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
CN110407806B (zh) * 2018-04-28 2021-08-17 深圳微芯生物科技股份有限公司 甲酰胺类化合物、其制备方法及其应用
KR20210005195A (ko) * 2018-05-02 2021-01-13 이난타 파마슈티칼스, 인코포레이티드 아폽토시스 신호 조절 키나제 1 억제제를 포함하는 테트라졸 및 이의 사용 방법
WO2019213239A1 (en) 2018-05-02 2019-11-07 Enanta Pharmaceuticals Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
TW202014193A (zh) 2018-05-03 2020-04-16 捷克科學院有機化學與生物化學研究所 包含碳環核苷酸之2’3’－環二核苷酸
CN112752756B (zh) 2018-05-11 2024-06-25 因赛特公司 作为PD-L1免疫调节剂的四氢-咪唑并[4,5-c]吡啶衍生物
CA3098873A1 (en) 2018-05-11 2019-11-14 Phosphorex, Inc. Microparticles and nanoparticles having negative surface charges
PL3793565T3 (pl) 2018-05-14 2022-05-02 Gilead Sciences, Inc. Inhibitory MCL-1
CA3104662A1 (en) * 2018-06-27 2020-01-02 Biogen Ma Inc. Ask1 inhibiting agents
WO2020006429A1 (en) * 2018-06-28 2020-01-02 Hepatikos Therapeutics, Llc Ask1 isoindolin-1-one inhibitors and methods of use thereof
TWI809427B (zh) 2018-07-13 2023-07-21 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
WO2020015721A1 (zh) * 2018-07-20 2020-01-23 福建广生堂药业股份有限公司 作为ask1抑制剂的晶型及其制备方法和应用
CN110818683B (zh) * 2018-08-10 2023-04-14 中国科学院上海药物研究所 2-吡啶取代脲结构小分子化合物及其合成和应用
WO2020030107A1 (zh) * 2018-08-10 2020-02-13 江苏豪森药业集团有限公司 一种含有酰胺类衍生物的药物组合物及其制备方法和应用
US11897898B2 (en) 2018-08-14 2024-02-13 Biogen Ma Inc. Pyridine macrocycle compounds as ASK1 inhibiting agents
JP2021534152A (ja) * 2018-08-14 2021-12-09 バイオジェン・エムエイ・インコーポレイテッドBiogen MA Inc. Ａｓｋ１阻害剤
TW202021967A (zh) * 2018-08-14 2020-06-16 大陸商江蘇豪森藥業集團有限公司 凋亡信號調節激酶１抑制劑的鹽及其晶型
US10968199B2 (en) 2018-08-22 2021-04-06 Enanta Pharmaceuticals, Inc. Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US20210213006A1 (en) * 2018-08-29 2021-07-15 Seal Rock Therapeutics, Inc. Methods of treating neurodegenerative diseases
WO2020063727A1 (zh) * 2018-09-30 2020-04-02 山东轩竹医药科技有限公司 三并环类ask1抑制剂及其应用
WO2020072656A1 (en) 2018-10-03 2020-04-09 Gilead Sciences, Inc. Imidozopyrimidine derivatives
WO2020086556A1 (en) 2018-10-24 2020-04-30 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
US11071730B2 (en) 2018-10-31 2021-07-27 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds
WO2020092621A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds as hpk1 inhibitors
US11345699B2 (en) 2018-11-19 2022-05-31 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
CN109608441A (zh) * 2018-12-26 2019-04-12 都创(上海)医药科技有限公司 一种ask1抑制剂的合成工艺
HUE065889T2 (hu) 2019-01-15 2024-06-28 Gilead Sciences Inc Izoxazol vegyület mint FXR agonista és az azt tartalmazó gyógyszerészeti készítmények
CN118388473A (zh) 2019-02-19 2024-07-26 吉利德科学公司 Fxr激动剂的固体形式
DK3934757T3 (da) 2019-03-07 2023-04-17 Inst Of Organic Chemistry And Biochemistry Ascr V V I 2'3'-cykliske dinukleotider og prodrugs deraf
US11766447B2 (en) 2019-03-07 2023-09-26 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3′3′-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
US20220143061A1 (en) 2019-03-07 2022-05-12 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
KR20210136081A (ko) 2019-03-11 2021-11-16 길리애드 사이언시즈, 인코포레이티드 화합물의 제제 및 그의 용도
US11466033B2 (en) 2019-03-25 2022-10-11 Enanta Pharmaceuticals, Inc. Substituted pyridines as apoptosis signal-regulating kinase 1 inhibitors
TW202212339A (zh) 2019-04-17 2022-04-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TWI751516B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
TWI770527B (zh) 2019-06-14 2022-07-11 美商基利科學股份有限公司 Cot 調節劑及其使用方法
WO2020255038A1 (en) 2019-06-18 2020-12-24 Janssen Sciences Ireland Unlimited Company Combination of hepatitis b virus (hbv) vaccines and pyridopyrimidine derivatives
US20210009718A1 (en) 2019-06-25 2021-01-14 Gilead Sciences, Inc. FLT3L-Fc FUSION PROTEINS AND METHODS OF USE
AR119594A1 (es) 2019-08-09 2021-12-29 Gilead Sciences Inc Derivados de tienopirimidina como inhibidores acc y usos de los mismos
AR119624A1 (es) 2019-08-09 2021-12-29 Incyte Corp Sales de un inhibidor de pd-1 / pd-l1
MX2022003578A (es) 2019-09-30 2022-05-30 Incyte Corp Compuestos de pirido[3,2-d]pirimidina como inmunomoduladores.
TW202124450A (zh) 2019-10-18 2021-07-01 美商四十七股份有限公司 用於治療骨髓發育不良症候群及急性骨髓白血病之組合療法
EP4052040A1 (en) 2019-10-31 2022-09-07 Forty Seven, Inc. Anti-cd47 and anti-cd20 based treatment of blood cancer
BR112022009031A2 (pt) 2019-11-11 2022-10-11 Incyte Corp Sais e formas cristalinas de um inibidor de pd-1/pd-l1
TWI778443B (zh) 2019-11-12 2022-09-21 美商基利科學股份有限公司 Mcl1抑制劑
EP4058144A1 (en) 2019-11-15 2022-09-21 Gilead Sciences, Inc. Triazole carbamate pyridyl sulfonamides as lpa receptor antagonists and uses thereof
CN111018831B (zh) * 2019-11-21 2022-05-31 中国药科大学 细胞凋亡信号调节激酶抑制剂及其应用
US20230105984A1 (en) 2019-12-23 2023-04-06 Svetlana Marukian Compositions and methods for the treatment of liver diseases and disorders
WO2021130638A1 (en) 2019-12-24 2021-07-01 Carna Biosciences, Inc. Diacylglycerol kinase modulating compounds
WO2021163064A2 (en) 2020-02-14 2021-08-19 Jounce Therapeutics, Inc. Antibodies and fusion proteins that bind to ccr8 and uses thereof
CA3175541A1 (en) 2020-03-30 2021-10-07 Gilead Sciences, Inc. Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound
CN115397824A (zh) 2020-04-02 2022-11-25 吉利德科学公司 用于制备cot抑制剂化合物的方法
CA3181922A1 (en) 2020-05-01 2021-11-04 Gilead Sciences, Inc. Cd73 inhibiting 2,4-dioxopyrimidine compounds
EP4161936A1 (en) 2020-06-03 2023-04-12 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
TWI838626B (zh) 2020-06-03 2024-04-11 美商基利科學股份有限公司 Lpa受體拮抗劑及其用途
CN113831323A (zh) * 2020-06-24 2021-12-24 武汉人福创新药物研发中心有限公司 芳杂环酰胺类化合物及其用途
CN111808079A (zh) * 2020-08-05 2020-10-23 中国药科大学 吲哚类ask1小分子抑制剂及其制备方法和应用
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
PE20231438A1 (es) 2020-11-06 2023-09-14 Incyte Corp Proceso para hacer un inhibidor de pd-1/pd-l1 y sales y formas cristalinas del mismo
US12091404B2 (en) 2021-03-11 2024-09-17 Gilead Sciences, Inc. GLP-1R modulating compounds
CN117120429A (zh) 2021-03-29 2023-11-24 吉利德科学公司 Khk抑制剂
TW202302145A (zh) 2021-04-14 2023-01-16 美商基利科學股份有限公司 ＣＤ４７／ＳＩＲＰα結合及ＮＥＤＤ８活化酶Ｅ１調節次單元之共抑制以用於治療癌症
TWI818538B (zh) 2021-05-11 2023-10-11 美商基利科學股份有限公司 Ｌｐａ受體拮抗劑及其用途
EP4337654A1 (en) 2021-05-13 2024-03-20 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
WO2022245671A1 (en) 2021-05-18 2022-11-24 Gilead Sciences, Inc. Methods of using flt3l-fc fusion proteins
TW202345826A (zh) 2021-06-04 2023-12-01 美商基利科學股份有限公司 治療nash之方法
TW202311256A (zh) 2021-06-18 2023-03-16 美商基利科學股份有限公司 用於治療ｆｘｒ誘發之搔癢之ｉｌ－３１調節劑
KR20240023629A (ko) 2021-06-23 2024-02-22 길리애드 사이언시즈, 인코포레이티드 디아실글리세롤 키나제 조절 화합물
MX2023014762A (es) 2021-06-23 2024-01-15 Gilead Sciences Inc Compuestos moduladores de diacilglicerol quinasa.
CN117396478A (zh) 2021-06-23 2024-01-12 吉利德科学公司 二酰基甘油激酶调节化合物
CN117377671A (zh) 2021-06-23 2024-01-09 吉利德科学公司 二酰基甘油激酶调节化合物
EP4423078A1 (en) 2021-10-28 2024-09-04 Gilead Sciences, Inc. Pyridizin-3(2h)-one derivatives
EP4422756A1 (en) 2021-10-29 2024-09-04 Gilead Sciences, Inc. Cd73 compounds
CA3238094A1 (en) 2021-12-08 2023-06-15 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
WO2023107954A1 (en) 2021-12-08 2023-06-15 Dragonfly Therapeutics, Inc. Antibodies targeting 5t4 and uses thereof
US20230203202A1 (en) 2021-12-08 2023-06-29 Dragonfly Therapeutics, Inc. Proteins binding nkg2d, cd16 and 5t4
KR20240125012A (ko) 2021-12-22 2024-08-19 길리애드 사이언시즈, 인코포레이티드 이카로스 아연 핑거 패밀리 분해제 및 이의 용도
WO2023122581A2 (en) 2021-12-22 2023-06-29 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
TW202340168A (zh) 2022-01-28 2023-10-16 美商基利科學股份有限公司 Ｐａｒｐ７抑制劑
TW202346277A (zh) 2022-03-17 2023-12-01 美商基利科學股份有限公司 Ｉｋａｒｏｓ鋅指家族降解劑及其用途
WO2023183817A1 (en) 2022-03-24 2023-09-28 Gilead Sciences, Inc. Combination therapy for treating trop-2 expressing cancers
TW202345901A (zh) 2022-04-05 2023-12-01 美商基利科學股份有限公司 用於治療結腸直腸癌之組合療法
TW202400138A (zh) 2022-04-21 2024-01-01 美商基利科學股份有限公司 Ｋｒａｓ ｇ１２ｄ調節化合物
US20240116928A1 (en) 2022-07-01 2024-04-11 Gilead Sciences, Inc. Cd73 compounds
WO2024059212A2 (en) * 2022-09-15 2024-03-21 Vanderbilt University 6,6 western core compounds as mglu5 negative allosteric modulators and methods of making and using the same
WO2024059216A2 (en) * 2022-09-15 2024-03-21 Vanderbilt University 6,6 southwestern core compounds as mglu5 negative allosteric modulators and methods of making and using the same
WO2024064668A1 (en) 2022-09-21 2024-03-28 Gilead Sciences, Inc. FOCAL IONIZING RADIATION AND CD47/SIRPα DISRUPTION ANTICANCER COMBINATION THERAPY
US20240254118A1 (en) 2022-12-22 2024-08-01 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof

Family Cites Families (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
CA1121825A (en) 1978-04-11 1982-04-13 Franco Bolasco 2-(2-thenoylthio)-propionylglycine: method for its preparation and pharmaceutical formulations containing said compound
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
US6159731A (en) 1997-02-12 2000-12-12 Massachusetts Institute Of Technology Daxx, a Fas-binding protein that activates JNK and apoptosis
AUPP285898A0 (en) * 1998-04-07 1998-04-30 Fujisawa Pharmaceutical Co., Ltd. Amido derivatives
DE60039677D1 (de) 1999-03-19 2008-09-11 Aventis Pharma Inc Akt-3 nukleinsäure, polypeptide und deren verwendung
US6881555B2 (en) 1999-03-19 2005-04-19 Aventis Pharmaceuticals Inc. AKT nucleic acids, polypeptides, and uses thereof
WO2001068585A1 (fr) * 2000-03-14 2001-09-20 Fujisawa Pharmaceutical Co., Ltd. Nouveaux composes amides
WO2002038179A1 (fr) * 2000-11-10 2002-05-16 Kissei Pharmaceutical Co., Ltd. Preventifs ou remedes de maladies du reticulum endoblastique liees au stress
US20040110785A1 (en) 2001-02-02 2004-06-10 Tao Wang Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
US20070237770A1 (en) 2001-11-30 2007-10-11 Albert Lai Novel compositions and methods in cancer
TW200400963A (en) 2002-05-21 2004-01-16 Wyeth Corp R-enantiomers of pyranoindole derivatives and the use thereof for the treatment of hepatitis C virus infection or disease
TW200400818A (en) 2002-05-21 2004-01-16 Wyeth Corp Method for the use of pyranoindole derivatives to treat infection with hepatitis C virus
EP1661581A1 (en) 2003-07-28 2006-05-31 Osaka Industrial Promotion Organization Remedy for cardiac failure comprising ask1 inhibitor as the active ingredient and method of screening the same
TW200526626A (en) 2003-09-13 2005-08-16 Astrazeneca Ab Chemical compounds
GB0324551D0 (en) 2003-10-21 2003-11-26 Karobio Ab Novel compounds
US7078064B2 (en) 2003-12-03 2006-07-18 George Zabrecky Compositions and methods useful for treating and preventing chronic liver disease, chronic HCV infection and non-alcoholic steatohepatitis
EP1794137A4 (en) 2004-09-27 2009-12-02 Kosan Biosciences Inc SPECIFIC KINASE INHIBITORS
WO2006053227A2 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Il-12 modulatory compounds
WO2006065946A1 (en) 2004-12-16 2006-06-22 Vertex Pharmaceuticals Incorporated Pyrid-2-ones useful as inhibitors of tec family protein kinases for the treatment of inflammatory, proliferative and immunologically-mediated diseases
EP1677113A1 (en) 2004-12-29 2006-07-05 Max-Delbrück-Centrum für Molekulare Medizin (MDC) Method for the identification of protein-protein interactions in disease related protein networks
US20070276050A1 (en) 2006-02-27 2007-11-29 Gilead Sciences, Inc. Methods for identifying ASK1 inhibitors useful for preventing and/or treating cardiovascular diseases
JP2009544625A (ja) 2006-07-20 2009-12-17 メーメット・カーラマン Ｒｈｏキナーゼのベンゾチオフェン阻害剤
WO2008016131A1 (fr) 2006-08-04 2008-02-07 Takeda Pharmaceutical Company Limited Composé hétérocyclique à cycles fusionnés
WO2008042867A2 (en) 2006-09-29 2008-04-10 Emiliem Inc. Modulators of multiple kinases
EP2104734A2 (en) 2006-12-08 2009-09-30 Asuragen, INC. Mir-20 regulated genes and pathways as targets for therapeutic intervention
WO2009011850A2 (en) 2007-07-16 2009-01-22 Abbott Laboratories Novel therapeutic compounds
WO2009027283A1 (en) 2007-08-31 2009-03-05 Merck Serono S.A. Triazolopyridine compounds and their use as ask inhibitors
US8426595B2 (en) 2007-12-11 2013-04-23 Xianhai Huang Gamma secretase modulators
JP5432982B2 (ja) 2008-03-31 2014-03-05 武田薬品工業株式会社 アポトーシスシグナル調節キナーゼ１阻害剤
US8178555B2 (en) 2008-06-24 2012-05-15 Takeda Pharmaceutical Company Limited Apoptosis signal-regulating kinase 1 inhibitors
US20110263441A1 (en) 2008-10-15 2011-10-27 Golub Todd R Compositions, kits, and methods for identification, assessment, prevention, and therapy of hepatic disorders
US20110294693A1 (en) 2008-11-17 2011-12-01 The George Washington University Compositions and Methods for Identifying Autism Spectrum Disorders
PA8854101A1 (es) 2008-12-18 2010-07-27 Ortho Mcneil Janssen Pharm Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa
US20120010272A1 (en) 2009-03-27 2012-01-12 Merck Sharp & Dohme Corp. RNA Interference Mediated Inhibition of Apoptosis Signal-Regulating Kinase 1 (ASK1) Gene Expression Using Short Interfering Nucleic Acid (siNA)
TWI625121B (zh) 2009-07-13 2018-06-01 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
WO2011041293A1 (en) 2009-09-30 2011-04-07 Takeda Pharmaceutical Company Limited Pyrazolo [1, 5-a] pyrimidine derivatives as apoptosis signal-regulating kinase 1 inhibitors
ES2445917T3 (es) 2010-02-03 2014-03-06 Takeda Pharmaceutical Company Limited Inhibidores de quinasa 1 reguladora de la señal de apoptosis
EP2534145A4 (en) 2010-02-08 2013-09-11 Kinagen Inc THERAPEUTIC METHODS AND COMPOSITIONS INVOLVING THE INHIBITION OF ALLOSTERIC KINASE
JP6065183B2 (ja) 2010-03-24 2017-01-25 アミテック セラピューティック ソリューションズ，インク． キナーゼ阻害に役立つ複素環式化合物
AU2011272782B2 (en) 2010-07-02 2014-11-27 Gilead Sciences, Inc. Apoptosis signal-regulating kinase inhibitors
WO2012054510A1 (en) 2010-10-19 2012-04-26 Comentis, Inc. Oxadiazole compounds which inhibit beta-secretase activity and methods of use thereof
WO2012068464A2 (en) 2010-11-18 2012-05-24 University Of Delaware Methods of treating and preventing thrombotic diseases using ask1 inhibitors
US9045485B2 (en) 2010-12-16 2015-06-02 Convergence Pharmaceuticals Limited ASK 1 inhibiting pyrrolopyrimidine derivatives
JP2014507160A (ja) 2011-02-22 2014-03-27 カリス ライフ サイエンシズ ルクセンブルク ホールディングス エス．アー．エール．エル． 循環バイオマーカー
EP2718721A4 (en) 2011-06-07 2014-10-01 Caris Life Sciences Luxembourg Holdings S A R L CIRCULATING BIOMARKERS FOR CANCER
UY34171A (es) 2011-07-01 2013-01-31 Gilead Sciences Inc Compuestos heterocíclicos fusionados como moduladores del canal iónico
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
AU2012335088B2 (en) 2011-11-11 2017-08-24 Gilead Apollo, Llc ACC inhibitors and uses thereof
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
UY35212A (es) 2012-12-21 2014-06-30 Gilead Sciences Inc Inhibidores de la quinasa que regula la señal de la apoptosis
AP2016009248A0 (en) 2013-12-20 2016-05-31 Gilead Sciences Inc Apoptosis signal-regulating kinase inhibitors
CN103896990B (zh) 2014-03-12 2017-02-08 石家庄诚志永华显示材料有限公司 有机电致发光材料及其应用
WO2015187499A1 (en) 2014-06-03 2015-12-10 Gilead Sciences, Inc. Use of an ask1 inhibitor for the treatment of liver disease, optionally in combination with a loxl2 inhibitor
JP2017528471A (ja) 2014-09-24 2017-09-28 ギリアード サイエンシーズ， インコーポレイテッド 肝疾患を処置する方法
EP3034499A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
BR112017013382A2 (pt) 2014-12-23 2018-02-14 Gilead Sciences Inc método para preparar um composto, composto, e, ácido.
MA41252A (fr) 2014-12-23 2017-10-31 Gilead Sciences Inc Formes solides d'un inhibiteur d'ask 1
CN107106873A (zh) 2015-01-09 2017-08-29 吉利德阿波罗公司 用于治疗非酒精性脂肪肝病的acc抑制剂组合治疗
SG11201807077RA (en) 2016-03-02 2018-09-27 Gilead Apollo Llc Solid forms of a thienopyrimidinedione acc inhibitor and methods for production thereof
JP6678779B2 (ja) 2016-06-13 2020-04-08 ギリアード サイエンシーズ， インコーポレイテッド Ｆｘｒ（ｎｒ１ｈ４）調節化合物
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
CA3042398A1 (en) 2016-11-11 2018-05-17 Gilead Sciences, Inc. Methods of treating liver disease
JOP20180017A1 (ar) 2017-03-14 2019-01-30 Gilead Sciences Inc مثبط كيناز منظم لإشارة تلاشي خلايا
KR20190126921A (ko) 2017-03-28 2019-11-12 길리애드 사이언시즈, 인코포레이티드 간 질환을 치료하는 방법
PT4122464T (pt) 2017-03-28 2024-06-27 Gilead Sciences Inc Combinações terapêuticas para o tratamento de doenças do fígado
TW201902478A (zh) 2017-04-12 2019-01-16 美商基利科學股份有限公司 治療肝臟疾病之方法
WO2019071216A1 (en) 2017-10-06 2019-04-11 Gilead Sciences, Inc. POLYTHERAPY COMPRISING AN ACC INHIBITOR

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