HRP20200690T1 - Agonisti triazola apj receptora - Google Patents

Agonisti triazola apj receptora Download PDF

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Publication number
HRP20200690T1
HRP20200690T1 HRP20200690TT HRP20200690T HRP20200690T1 HR P20200690 T1 HRP20200690 T1 HR P20200690T1 HR P20200690T T HRP20200690T T HR P20200690TT HR P20200690 T HRP20200690 T HR P20200690T HR P20200690 T1 HRP20200690 T1 HR P20200690T1
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HR
Croatia
Prior art keywords
image
alkyl
methyl
pyridinyl
dimethoxyphenyl
Prior art date
Application number
HRP20200690TT
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English (en)
Inventor
Ning Chen
Xiaoqi Chen
Yinhong CHEN
Alan C. Cheng
Richard V. Connors
Jeffrey Deignan
Paul John Dransfield
Xiaohui Du
Zice Fu
Julie Anne Heath
Daniel B. Horne
Jonathan Houze
Matthew R. Kaller
Aarif Yusuf KHAKOO
David John Kopecky
Su-Jen Lai
Zhihua Ma
Lawrence R. Mcgee
Julio C. Medina
Jeffrey T Mihalic
Nobuko Nishimura
Steven H. Olson
Vatee Pattaropong
Gayathri Swaminath
Xiaodong Wang
Kevin Yang
Wen-Chen Yeh
Mikkel V. DEBENEDETTO
Robert P. Farrell
Simon J. HedleyEDLEY
Ted C Judd
Frank Kayser
Original Assignee
Amgen Inc.
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Publication date
Application filed by Amgen Inc. filed Critical Amgen Inc.
Publication of HRP20200690T1 publication Critical patent/HRP20200690T1/hr

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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Claims (30)

1. Spoj s Formulom I ili Formulom II: [image] [image] ili njegova farmaceutski prihvatljiva sol, njegov tautomer, farmaceutski prihvatljiva sol tautomera, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što: R1 je nesupstituirani piridil, piridonil, ili piridin N-oksid, ili je piridil, piridonil, ili piridin N-oksid supstituiran s 1, 2, 3, ili 4 supstituenata R1a; R1a u svakom slučaju je neovisno odabran od -F, -CI, -Br, -I, -CN, -C1-C6 alkil, -C1-C6 haloalkil, -C1-C6 perhaloalkil, -OH, -O-(C1-C6 alkil), -O-(C1-C6 haloalkil), -O-(C1-C6 perhaloalkil), -C2-C6 alkenil, -O-(C1-C6 alkil)-OH, -O-(C1-C6 alkil)-O-(C1-C6 alkil), -O-(C1-C6 haloalkil)-OH, -O-(C1-C6 haloalkil)-O-(C1-C6 alkil), -O-(C1-C6 perhaloalkil)-OH, -O-(C1-C6 perhaloalkil)-O-(C1-C6 alkil), -NH2, -NH(C1-C6 alkil), -N(C1-C6 alkil)2, -C(=O)-(C1-C6 alkil), -C(=O)OH, -C(=O)-O-(C1-C6 alkil), -C(=O)NH2, -C(=O)NH(C1-C6 alkil), -C(=O)N(C1-C6 alkil)2, fenil, -C(=O)-(heterociklil), ili heterociklil skupine, pri čemu heterociklil skupina od -C(=O)-(heterociklil) ili heterociklil skupina je 3 do 7 člani prsten koji sadrži 1, 2, ili 3 heteroatoma odabrana od N, O, ili S; R2 je odabran od -H, ili C1-C4 alkila ili je odsutan u spojevima s Formulom II; R3 je odabran od nesupstituiranog C1-C10 alkila, C1-C10 alkila supstituiranog s 1, 2, ili 3 supstituenta R3a, skupine s formulom -(CR3bR3c)-Q, skupine s formulom -NH-(CR3bR3c)-Q, skupine s formulom -(CR3bR3c)-C(=O)-Q, skupine s formulom -(CR3dR3e)-(CR3fR3g)-Q, skupine s formulom -(CR3b=CR3c)-Q, ili skupine s formulom -(heterociklil)-Q, pri čemu heterociklil od -(heterociklil)-Q ima 5 do 6 članova prstena od kojih 1, 2, ili 3 su heteroatomi odabrani od N, O, ili S i nesupstituiran je ili je supstituiran s 1, 2, ili 3 supstituenata R3h; R3a u svakom slučaju je neovisno odabran od -F, -CI, -CN, -OH, -O-(C1-C6 alkil),-O-(C1-C6 haloalkil), -O-(C1-C6 perhaloalkil), -O-(C1-C6 alkil)-OH, -O-(C1-C6 alkil)-O-(C1-C6 alkil), C2-C6 alkenil, C2-C6 alkinil, -NH2, -NH(C1-C6 alkil), ili -N(C1-C6 alkil)2; R3b i R3c su neovisno odabrani od -H, -F, -CI, -CN, -C1-C6 alkil, -C1-C6 haloalkil, -C1-C6 perhaloalkil, -OH, -O-(C1-C6 alkil), -O-(C1-C6 haloalkil), -O-(C1-C6 perhaloalkil), -O-(C1-C6 alkil)-OH, -O-(C1-C6 alkil)-O-(C1-C6 alkil), -NH2, -NH(C1-C6 alkil), ili -N(C1-C6 alkil)2; R3d i R3e su neovisno odabrani od -H, -F, -CI, -CN, -C1-C6 alkil, -C1-C6 haloalkil, -C1-C6 perhaloalkil, -OH, -O-(C1-C6 alkil), -O-(C1-C6 haloalkil), -O-(C1-C6 perhaloalkil), -O-(C1-C6 alkil)-OH, -O-(C1-C6 alkil)-O-(C1-C6 alkil), -NH2, -NH(C1-C6 alkil), ili -N(C1-C6 alkil)2; R3f i R3g su neovisno odabrani od -H, -F, -CI, -CN, -C1-C6 alkil, -C1-C6 haloalkil, -C1-C6 perhaloalkil, -OH, -O-(C1-C6 alkil), -O-(C1-C6 haloalkil), -O-(C1-C6 perhaloalkil), -O-(C1-C6 alkil)-OH, -O-(C1-C6 alkil)-O-(C1-C6 alkil), -NH2, -NH(C1-C6 alkil), ili -N(C1-C6 alkil)2; R3h u svakom slučaju je neovisno odabran od -F, -CI, -CN, -C1-C6 alkil, -C1-C6 haloalkil, -C1-C6 perhaloalkil, -OH, -O-(C1-C6 alkil), -O-(C1-C6 haloalkil), -O-(C1-C6 perhaloalkil), -O-(C1-C6 alkil)-OH, -O-(C1-C6 alkil)-O-(C1-C6 alkil), -NH2, -NH(C1-C6 alkil), -N(C1-C6 alkil)2, ili okso; Q je monociklička ili biciklička skupina C3-C10 aril, monociklička ili biciklička heteroarilna skupina s 5 do 10 članova prstena koji sadrže 1, 2, ili 3 heteroatoma odabrana od N, O, ili S, skupina C3-C8 cikloalkil, ili 3 do 7 člana heterociklil skupina koja sadrži 1, 2, ili 3 heteroatoma odabrana od N, O, ili S, pri čemu su skupina C6-C10 aril, skupina heteroaril, skupina cikloalkil, i skupina heterociklil nesupstituirane ili su supstituirane s 1, 2, 3, ili 4 supstituenata RQ; RQ u svakom slučaju je neovisno odabran od -F, -CI, -Br, -I, -CN, -C1-C6 alkil, -C1-C6 haloalkil, -C1-C6 perhaloalkil, -C2-C6 alkenil, -C2-C6 alkinil, -OH, -O-(C1-C6 alkil), -O-(C1-C6 haloalkil), -O-(C1-C6 perhaloalkil), -NH2, -NH(C1-C6 alkil), -N(C1-C6 alkil)2, -C(=O)-(C1-C6 alkil), -C(=O)OH, -C(=O)-O-(C1-C6 alkil), -C(=O)NH2, -C(=O)NH(C1-C6 alkil), -C(=O)N(C1-C6 alkil)2, -S(=O)2-(C1-C6 alkil), fenil, ili heteroarilne skupine, i Q heterociklil skupina može biti supstituirana s 1 okso RQ supstituentom; R4 je odabran od monocikličke ili bicikličke skupine C6-C10 aril, monocikličke ili bicikličke heteroarilne skupine s 5 do 10 članova prstena koji sadrže 1, 2, ili 3 heteroatoma neovisno odabranih od N, O, ili S, ili monocikličke ili bicikličke heterociklil skupine s 5 do 10 članova prstena koji sadrže 1, 2, 3, ili 4 heteroatoma neovisno odabranih od N, O, ili S, pri čemu su skupina C6-C10 aril, heteroarilna skupina, ili heterociklil skupina nesupstituirane ili su supstituirane s 1, 2, ili 3 supstituenta R4a; R4a u svakom slučaju je neovisno odabran od -F, -CI, -Br, -I, -CN, -C1-C6 alkil, -C1-C6 haloalkil, -C1-C6 perhaloalkil, -OH, -O-(C1-C6 alkil), -O-(C1-C6 haloalkil), -O-(C1-C6 perhaloalkil), -NH2, -NH(C1-C6 alkil), -N(C1-C6 alkil)2, -C(=O)-(C1-C6 alkil), -C(=O)OH, -C(=O)-O-(C1-C6 alkil), -C(=O)NH2, -C(=O)NH(C1-C6 alkil), ili -C(=O)N(C1-C6 alkil)2, i heterociklil R4 skupina može biti dalje supstituirana s 1 okso supstituentom; i dodatno pri čemu: ako je R4 nesupstituirani ili supstituirani fenilni prsten i R3 je skupina s formulom -(CR3b=CR3c)-Q, tada je najmanje jedno od sljedećih istinito: a) R4 je supstituiran s najmanje jednom skupinom -O-(C1-C6 alkil); b) Q nije oksadiazol; c) R3b nije -H; d) R3c nije -H; e) R1 nije skupina 2-piridil; ili f) R4 je supstituiran s dvije ili više skupina -O-(C1-C6 alkil).
2. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što R1 je nesupstituirani piridil ili je piridil supstituiran s 1 ili 2 R1a supstituenata.
3. Spoj prema patentnom zahtjevu 2 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što R1a u svakom slučaju je neovisno odabran od -CH3, -CH2CH3, -F, -Cl, -Br, -CN,-CF3, -CH=CH2, -C(=O)NH2, -C(=O)NH(CH3), -C(=O)N(CH3)2, -C(=O)NH(CH2CH3), -OH, -OCH3,-OCHF2, -OCH2CH3, -OCH2CF3, -OCH2CH2OH, -OCH2C(CH3)2OH,-OCH2C(CF3)2OH, -OCH2CH2OCH3, -NH2, -NHCH3, -N(CH3)2, fenil, ili skupine s formulom [image] pri čemu simbol [image] , kada se povuče preko veze, označava točku vezanja na ostatak molekule.
4. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što je R1 odabran od [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] pri čemu simbol [image] , kada se povuče preko veze, označava točku vezanja na ostatak molekule.
5. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što je R1 odabran od [image] [image] [image] pri čemu simbol [image] , kada se povuče preko veze, označava točku vezanja na ostatak molekule.
6. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što R2 je -H.
7. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što R4 je fenil, piridil, pirimidinil, izoksazolil, indolil, ili naftil bilo koji od njih može biti nesupstituiran ili supstituiran s 1, 2, ili 3 supstituenta R4a.
8. Spoj prema patentnom zahtjevu 7 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što je R4a u svakom slučaju neovisno odabran od -CH3, -F, -CI, -Br, -CN, -CF3, -OCH3, -OCHF2, -OCH2CH3, -C(=O)OCH3, -C(=O)CH3, ili -N(CH3)2.
9. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što je R4 odabran od [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] ili [image] pri čemu simbol [image] , kada se povuče preko veze, označava točku vezanja na ostatak molekule.
10. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što R4 je fenil supstituiran s 1 ili 2 supstituenta R4a, pri čemu su R4a supstituenti skupine -O-(C1-C2 alkil).
11. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što Q je monociklička heteroarilna skupina s 5 ili 6 članova prstena koji sadrže 1 ili 2 heteroatoma odabrana od N, O, ili S i Q je nesupstituiran ili je supstituiran s 1 ili 2 supstituenta RQ.
12. Spoj prema patentnom zahtjevu 11 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što Q je pirimidinil ili piridil skupina i Q je nesupstituiran ili je supstituiran s 1 ili 2 supstituenta RQ.
13. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što Q je odabran od [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] ili pri čemu simbol [image] , kada se povuče preko veze, označava točku vezanja na ostatak molekule.
14. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što je R3 skupina s formulom -(CR3dR3e)-(CR3fR3g)-Q.
15. Spoj prema patentnom zahtjevu 14 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što R3 ima formulu [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] pri čemu simbol [image] , kada se povuče preko veze, označava točku vezanja na ostatak molekule.
16. Spoj prema patentnom zahtjevu 15 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što R3 ima formulu [image] [image] [image] [image] pri čemu simbol [image] , kada se povuče preko veze, označava točku vezanja na ostatak molekule.
17. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što je spoj (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(6-metoksi-2-piridinil)-4H-1,2,4-triazol-3-il)-1-metoksi-1-(5-metil-2-pirimidinil)-2-propansulfonamid; (2S,3R)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-3-(5-metil-2-pirimidinil)-2-butansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-metoksi-1-(5-metil-2-pirimidinil)-2-propansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-hidroksi-1-(5-metil-2-pirimidinil)-2-propansulfonamid; (1S,2R)-1-(5-kloro-2-pirimidinil)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-metoksi-2-propansulfonamid; (1S,2R)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-metoksi-1-(5-metil-2-pirazinil)-2-propansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-hidroksi-1-(5-metil-2-pirazinil)-2-propansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(3-piridinil)-4H-1,2,4-triazol-3-il)-1-metoksi-1-(5-metil-2-pirimidinil)-2-propansulfonamid; (2S,3R)-N-(4-(2,6-dimetoksifenil)-5-(3-piridinil)-4H-1,2,4-triazol-3-il)-3-(5-metil-2-pirimidinil)-2-butansulfonamid; (1R,2S)-1-(5-kloro-2-pirimidinil)-N-(4-(2,6-dimetoksifenil)-5-(3-piridinil)-4H-1,2,4-triazol-3-il)-1-etoksi-2-propansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-etoksi-1-(5-metil-2-pirimidinil)-2-propansulfonamid; (1S,2R)-N-(4-(2,6-dimetoksifenil)-5-(3-piridinil)-4H-1,2,4-triazol-3-il)-1-metoksi-1-(5-metil-2-pirazinil)-2-propansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(6-metil-2-piridinil)-4H-1,2,4-triazol-3-il)-1-hidroksi-1-(5-metil-2-pirimidinil)-2-propansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(3-piridinil)-4H-1,2,4-triazol-3-il)-1-etoksi-1-(5-metil-2-pirimidinil)-2-propansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-(5-fluoro-2-pirimidinil)-1-metoksi-2-propansulfonamid; (2S,3R)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-3-(5-metil-2-pirazinil)-2-butansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(3-piridinil)-4H-1,2,4-triazol-3-il)-1-etoksi-1-(5-fluoro-2-pirimidinil)-2-propansulfonamid; (1S,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-(1-metiletoksi)-1-(5-metil-2-pirimidinil)-2-propansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-(1-metiletoksi)-1-(5-metil-2-pirimidinil)-2-propansulfonamid; (1S,2R)-1-(5-kloro-2-pirimidinil)-N-(4-(2,6-dimetoksifenil)-5-(3-piridinil)-4H-1 ,2,4-triazol-3-il)-1-metoksi-2-propansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-metoksi-1-(5-metoksi-2-pirazinil)-2-propansulfonamid; (2S,3R)-N-(4-(2,6-dimetoksifenil)-5-(3-piridinil)-4H-1,2,4-triazol-3-il)-3-(5-metil-2-pirazinil)-2-butansulfonamid; (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-etoksi-1-(5-fluoro-2-pirimidinil)-2-propansulfonamid; (1R,2S)-N-(4-(4,6-dimetoksi-5-pirimidinil)-5-(6-metoksi-2-piridinil)-4H-1,2,4-triazol-3-il)-1-metoksi-1-(5-metil-2-pirimidinil)-2-propansulfonamid; (1R,2R)-1-(5-kloro-2-pirimidinil)-N-(4-(2,6-dimetoksifenil)-5-(3-piridinil)-4H-1 ,2,4-triazol-3-il)-1-etoksi-2-propansulfonamid; ili (1S,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-etoksi-1-(5-metil-2-pirimidinil)-2-propansulfonamid.
18. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što je spoj (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(6-metoksi-2-piridinil)-4H-1 ,2,4-triazol-3-il)-1-metoksi-1-(5-metil-2-pirimidinil)-2-propansulfonamid.
19. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što je spoj (2S,3R)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-3-(5-metil-2-pirimidinil)-2-butansulfonamid.
20. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što je spoj (1R,2S)-N-(4-(2,6-dimetoksifenil)-5-(3-piridinil)-4H-1,2,4-triazol-3-il)-1-etoksi-1-(5-fluoro-2-pirimidinil)-2-propansulfonamid.
21. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, naznačen time što je spoj (1S,2S)-N-(4-(2,6-dimetoksifenil)-5-(5-metil-3-piridinil)-4H-1,2,4-triazol-3-il)-1-(1-metiletoksi)-1-(5-metil-2-pirimidinil)-2-propansulfonamid.
22. Farmaceutski pripravak, naznačen time što sadrži spoj prema bilo kojem od patentnih zahtjeva 1-21 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, i najmanje jedno farmaceutski prihvatljivo pomoćno sredstvo, nosač ili razrjeđivač.
23. Farmaceutski pripravak prema patentnom zahtjevu 22, naznačen time što nadalje sadrži terapeutsko sredstvo odabrano od α-blokatora, β-blokatora, inhibitora angiotenzin konvertirajućeg enzima (ACE), blokatora angiotenzin-receptora (ARB, blokatora kalcijevih kanala, diuretika, inhibitora hiperpolarizacijske struje, aktivatora miozina, ili inhibitora neutralne endopeptidaze (NEP).
24. Spoj prema bilo kojem od patentnih zahtjeva 1-21 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, ili farmaceutski pripravak prema patentnom zahtjevu 22 naznačen time što je za uporabu za liječenje kardiovaskularnog stanja.
25. Spoj za uporabu prema patentnom zahtjevu 24, naznačen time što je kardiovaskularno stanje zatajenje srca.
26. Spoj za uporabu prema patentnom zahtjevu 24, naznačen time što je kardiovaskularno stanje zatajenje srca sa smanjenom ejekcijskom frakcijom.
27. Spoj za uporabu prema patentnom zahtjevu 24, naznačen time što je kardiovaskularno stanje zatajenje srca s očuvanom ejekcijskom frakcijom.
28. Spoj za uporabu prema patentnom zahtjevu 24, naznačen time što je kardiovaskularno stanje akutno zatajenje srca.
29. Spoj za uporabu prema patentnom zahtjevu 24, naznačen time što je kardiovaskularno stanje hipertenzija.
30. Spoj prema bilo kojem od patentnih zahtjeva 1-21 ili njegova farmaceutski prihvatljiva sol, stereoizomer bilo kojeg od prethodnih, ili njihova smjesa, ili farmaceutski pripravak prema patentnom zahtjevu 22 naznačen time što je za upotrebu u liječenju stanja gdje je poželjno aktivirati APJ receptor, pri čemu je stanje pretilost, dijabetes, dijabetička nefropatija ili kronična bolest bubrega.
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