HRP20201748T1 - Inhibitori diacilglicerol-aciltransferaze - Google Patents

Inhibitori diacilglicerol-aciltransferaze Download PDF

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HRP20201748T1
HRP20201748T1 HRP20201748TT HRP20201748T HRP20201748T1 HR P20201748 T1 HRP20201748 T1 HR P20201748T1 HR P20201748T T HRP20201748T T HR P20201748TT HR P20201748 T HRP20201748 T HR P20201748T HR P20201748 T1 HRP20201748 T1 HR P20201748T1
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Croatia
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pharmaceutically acceptable
inhibitors
pyridin
carboxamide
oxy
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HRP20201748TT
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Markus Boehm
Shawn Cabral
Matthew S. Dowling
Kentaro Futatsugi
Kim HUARD
Esther Cheng Yin LEE
Qifang Li
Allyn T. Londregan
Jana Polivkova
David A. Price
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Pfizer Inc.
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Publication of HRP20201748T1 publication Critical patent/HRP20201748T1/hr

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Claims (28)

1. Spoj Formule (I) [image] , naznačen time što svaki od D1 i D2 je neovisno N ili CH; R1 je H, ili (C1-C2)alkil, koji može biti supstituiran s jednim ili dva supstituenta, od kojih se svakog neovisno bira između fluora i (C3-C6)cikloalkila; R2 je H ili fluor; R3 je [image] , [image] ili [image] ; R4 je H, cijano ili (C1-C4)alkil, koji može biti supstituiran s jednim ili dva supstituenta, od kojih se svakog neovisno bira između -OH i -S(O)2R6; R5 je H ili -OH; i R6 je (C1-C4)alkil; ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima Formulu (Ia) [image] , ili njegova farmaceutski prihvatljiva sol.
3. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što je R3 [image] .
4. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što je R3 [image] .
5. Spoj u skladu s patentnim zahtjevom 3, ili njegova farmaceutski prihvatljiva sol, naznačen time što je R1 metil.
6. Spoj u skladu s patentnim zahtjevom 4, ili njegova farmaceutski prihvatljiva sol, naznačen time što je R1 metil.
7. Spoj u skladu s patentnim zahtjevom 6, ili njegova farmaceutski prihvatljiva sol, naznačen time što je R4 H, -CH2OH ili cijano.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je: (S)-2-(5-((3-etoksi-5-fluorpiridin-2-il)oksi)piridin-3-il)-N-(tetrahidrofuran-3-il)pirimidin-5-karboksamid; N-(2-cijanopropan-2-il)-2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)pirimidin-5-karboksamid; 2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(3-metil-1,1-dioksidotetrahidrotiofen-3-il)pirimidin-5-karboksamid; 2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(1-hidroksi-2-metilpropan-2-il)pirimidin-5-karboksamid; (S)-2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(tetrahidrofuran-3-il)pirimidin-5-karboksamid; (S)-2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(3-(hidroksimetil)tetrahidrofuran-3-il)pirimidin-5-karboksamid; (R)-2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(3-(hidroksimetil)tetrahidrofuran-3-il)pirimidin-5-karboksamid; 2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(2-metil-1-(metilsulfonil)propan-2-il)pirimidin-5-karboksamid; (S)-2-(5-((3-(2-fluoretoksi)piridin-2-il)oksi)piridin-3-il)-N-(tetrahidrofuran-3-il)pirimidin-5-karboksamid; 3-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(1-hidroksi-2-metilpropan-2-il)-1,2,4-triazine-6-karboksamid; N-(1,3-dihidroksi-2-metilpropan-2-il)-2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)pirimidin-5-karboksamid; (S)-3-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(tetrahidrofuran-3-il)-1,2,4-triazine-6-karboksamid; N-(1,1-dioksidotetrahidrotiofen-3-il)-2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)pirimidin-5-karboksamid; (R)-2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(tetrahidrofuran-3-il)pirimidin-5-karboksamid; ili 2-(5-((3-etoksipirazin-2-il)oksi)piridin-3-il)-N-(1-hidroksi-2-metilpropan-2-il)pirimidin-5-karboksamid; ili njihove farmaceutski prihvatljive soli.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je: (R)-2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(3-(hidroksimetil)tetrahidrofuran-3-il)pirimidin-5-karboksamid; (S)-2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(tetrahidrofuran-3-il)pirimidin-5-karboksamid; ili (S)-2-(5-((3-etoksipiridin-2-il)oksi)piridin-3-il)-N-(3-(hidroksimetil)tetrahidrofuran-3-il)pirimidin-5-karboksamid; ili njihove farmaceutski prihvatljive soli.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima strukturu: [image] , ili njegova farmaceutski prihvatljiva sol.
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima strukturu: [image] .
12. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s patentnim zahtjevom 1, ili farmaceutski prihvatljivu sol navedenog spoja, prisutan u terapijski djelotvornoj količini, u smjesi s najmanje jednim farmaceutski prihvatljivim pomoćnim sredstvom.
13. Pripravak u skladu s patentnim zahtjevom 12, naznačen time što dodatno sadrži najmanje jedno dodatno farmaceutsko sredstvo, kojeg se bira iz skupine koju čine protuupalno sredstvo, antidijabetičko sredstvo, te sredstvo za moduliranje kolesterola/lipida.
14. Pripravak u skladu s patentnim zahtjevom 13, naznačen time što se navedeno dodatno farmaceutsko sredstvo bira iz skupine koju čine inhibitor acetil-CoA karboksilaze (ACC), inhibitor diacilglicerol-O-aciltransferaze 1 (DGAT-1), inhibitori monoacilglicerol-O-aciltransferaze, inhibitor fosfodiesteraze (PDE)-10, aktivator AMPK, sulfonilurea, meglitinid, inhibitor α-amilaze, inhibitor α-glukozid-hidrolaze, inhibitor α-glukozidaze, agonist PPARγ, agonist PPARα/γ, bigvanid, modulator glukagonu sličnog peptida 1 (GLP-1), liraglutid, albiglutid, eksenatid, albiglutid, liksisenatid, dulaglutid, semaglutid, inhibitor tirozinske proteinske fosfataze-1B (PTP-1B), aktivator SIRT-1, inhibitor dipeptidil-peptidaze IV (DPP-IV), sekretagog inzulina, inhibitor oksidacije masnih kiselina, antagonist A2, inhibitor c-jun amino-terminalne kinaze (JNK), aktivatori glukokinaze (GKa), inzulin, mimetik inzulina, inhibitor glikogen-fosforilaze, agonist receptora VPAC2, inhibitori SGLT2, modulator receptora glukagona, modulatori GPR119, derivati ili analozi FGF21, modulatori receptora TGR5, modulatori receptora GPBAR1, agonisti GPR40, modulatori GPR120, aktivatori visokoafinitetnog receptora nikotinske kiseline (HM74A), inhibitori SGLT1, inhibitori ili modulatori karnitin palmitoil-transferaznih enzima, inhibitori fruktoza-1,6-difosfataze, inhibitori aldoza-reduktaze, inhibitori mineralokortikoidnog receptora, inhibitori TORC2, inhibitori CCR2 i/ili CCR5, inhibitori izoformi PKC (primjerice PKCα, PKCβ, PKCγ), inhibitori sintetaze masnih kiselina, inhibitori serin-palmitoil-transferaze, modulatori GPR81, GPR39, GPR43, GPR41, GPR105, Kv1.3, protein 4 koji se veže na retinol, glukokortikoidni receptor, receptori somatostaina, inhibitori ili modulatori PDHK2 ili PDHK4, inhibitori MAP4K4, modulatori porodice IL1, uklučujući IL1β, inhibitori HMG-CoA-reduktaze, inhibitori skvalen-sintetaze, fibrati, sekvestransi žučnih kiselina, inhibitori ACAT, inhibitori MTP, inhibitori lipooksigenaze, inhibitori apsorpcije kolesterola, modulatori PCSK9, inhibitori proteina za transport kolesterilnih estera i modulatori RXRα.
15. Pripravak u skladu s patentnim zahtjevom 13, naznačen time što je navedeno dodatno farmaceutsko sredstvo inhibitor acetil-CoA karboksilaze (ACC).
16. Pripravak u skladu s patentnim zahtjevom 12, naznačen time što dodatno sadrži najmanje jedno dodatno farmaceutsko sredstvo, kojeg se bira iz skupine koju čine cisteamin, ili njegova farmaceutski prihvatljiva sol, cistamin, ili njegova farmaceutski prihvatljiva sol, antioksidantni spoj, lecitin, kompleks vitamina B, pripravci žučnih soli, antagonisti kanabinoidnog receptora 1 (CB1), inverzni agonisti kanabinoidnog receptora 1 (CB1), regulatori aktivnosti receptora kojeg aktivira proliferator peroksisoma, benzotiazepinski ili benzotiepinski spoj, RNA protusmisleni konstrukt namijenjen inhibiranju tirozinske proteinske fosfataze PTPRU, supstituirani piperidin vezan preko heteroatoma i njegovi derivati, azaciklopentan derivat koji može inhibirati stearoil-koenzim alfa delta-9-desaturazu, acilamidni spoj s aktivnošću sekretagoga ili induktora adiponektina, kvaternarni amonijev spoj, glatiramer-acetat, pentraksinski proteini, inhibitor HMG-CoA-reduktaze, n-acetilcistein, izoflavonski spoj, makrolidni antibiotik, inhibitor galektina, protutijelo ili bilo koja njihova kombinacija.
17. Spoj u skladu s patentnim zahtjevom 1, ili farmaceutski prihvatljiva sol navedenog spoja, naznačen time što je namijenjen upotrebi kao medikament.
18. Spoj u skladu s patentnim zahtjevom 1, ili farmaceutski prihvatljiva sol navedenog spoja, naznačen time što je namijenjen upotrebi u postupku smanjivanja najmanje jednog stupnja težine u sustavima bodovanja težine nealkoholne bolesti masne jetre ili nealkoholnog steatohepatitisa, smanjivanja razine serumskih biljega aktivnosti nealkoholnog steatohepatitisa, smanjivanja aktivnosti bolesti nealkoholnog steatohepatitisa ili smanjivanja medicinskih posljedica nealkoholnog steatohepatitisa kod ljudi.
19. Spoj u skladu s patentnim zahtjevom 1, ili farmaceutski prihvatljiva sol navedenog spoja, naznačen time što je namijenjen upotrebi u postupku liječenja masne jetre, nealkoholne bolesti masne jetre, nealkoholnog steatohepatitisa, nealkoholnog steatohepatitisa uz fibrozu jetre, nealkoholnog steatohepotitisa uz cirozu ili nealkoholnog steatohepatitisa uz cirozu i hepatocelularnog karcinoma kod ljudi.
20. Spoj u skladu s patentnim zahtjevom 1, ili farmaceutski prihvatljiva sol navedenog spoja, naznačen time što je namijenjen upotrebi u postupku liječenja nealkoholnog steatohepatitisa uz fibrozu jetre kod ljudi.
21. Spoj u skladu s patentnim zahtjevom 1, ili farmaceutski prihvatljiva sol navedenog spoja, naznačen time što je namijenjen upotrebi u postupku liječenja hiperlipidemije, dijabetesa tip I, dijabetesa melitusa tip II, idiopatskog dijabetesa tip I (tip Ib), latentnog autoimunog dijabetesa kod odraslih (LADA), dijabetesa tip s ranim početkom 2 (EOD), atipičnog dijabetesa s početkom u mladenačkoj dobi (YOAD), dijabetesa kod mladih osoba s kasnijim početkom (MODY), dijabetesa povezanog s pothranjenošću, gestacijskog dijabetesa, koronarne bolesti srca, ishemičnog inzulta, restenoze nakon angioplastike, bolesti perifernih krvnih žila, povremenog šepanja, infarkta miokarda, dislipidemije, lipemije nakon obroka, stanja poremećene tolerancije glukoze (IGT), stanja poremećene razine glukoze u plazmi prilikom gladovanja, metaboličke acidoze, ketoze, artritisa, pretilosti, osteoporoze, hipertenzije, kongestivnog zatajenja srca, hipertrofije lijeve klijetke, bolesti perifernih arterija, dijabetične retinopatije, degeneracije makule, sive mrene, dijabetične nefropatije, glomeruloskleroze, kroničnog zatajenja bubrega, dijabetične neuropatije, metaboličkog sindroma, sindroma X, predmenstrualnog sindroma, angine pektoris, tromboze, ateroskleroze, prolaznih napadaja ishemije, inzulta, restenoze krvnih žila, hiperglikemije, hiperinzulinemije, hipertrigliceridemije, otpornosti na inzulin, poremećenog metabolizma glukoze, poremećaja erekcije, poremećaja kože i vezivnog tkiva, čireva na stopalima i ulceroznog kolitisa, poremećaja endotela i poremećene elastičnosti krvnih žila, hiper apo B lipoproteinemije, Alzheimerove bolesti, shizofrenije, poremećenih kognitivnih funkcija, upalne bolesti crijeva, ulceroznog kolitisa, Crohnove bolesti, te sindroma iritabilnih crijeva, nealkoholnog steatohepatitisa (NASH) ili nealkoholne bolest masne jetre (NAFLD), kod ljudi.
22. Dva odvojena farmaceutska pripravka koji sadrže (i) prvi pripravak u skladu s patentnim zahtjevom 12; i (ii) drugi pripravak koji sadrži najmanje jedno dodatno farmaceutsko sredstvo, kojeg se bira iz skupine koju čine protuupalno sredstvo, antidijabetičko sredstvo, te sredstvo za moduliranje kolesterola/lipida i najmanje jedno farmaceutski prihvatljivo pomoćno sredstvo; naznačeni time što su namijenjen upotrebi u postupku liječenja masne jetre, nealkoholne bolesti masne jetre, nealkoholnog steatohepatitisa, nealkoholnog steatohepatitisa uz fibrozu jetre, nealkoholnog steatohepotitisa uz cirozu ili nealkoholnog steatohepatitisa uz cirozu, te hepatocelularnog karcinoma kod ljudi.
23. Dva odvojena farmaceutska pripravka namijenjena upotrebi u postupku u skladu s patentnim zahtjevom 22, naznačeni time što se navedeni prvi pripravak i navedeni drugi pripravak primjenjuje istodobno.
24. Dva odvojena farmaceutska pripravka namijenjena upotrebi u postupku u skladu s patentnim zahtjevom 22, naznačeni time što se navedeni prvi pripravak i navedeni drugi pripravak primjenjuje uzastopno i bilo kojim redoslijedom.
25. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 18, naznačen time što postupak smanjuje portalnu hipertenziju, sposobnost sinteze proteina u jetri, te ublažava hiperbilirubinemiju ili encefalopatiju.
26. Kristal, naznačen time što sadrži spoj u skladu s patentnim zahtjevom 1 koji ima strukturu: [image] , ili njegovu farmaceutski prihvatljivu sol.
27. Kristal u skladu s patentnim zahtjevom 26, naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu kojeg čine vrijednosti 2θ od (za zračenje CuKα, valne duljine od 1,54056 Å) 5,3 ± 0,2, 7,7 ± 0,2, te 15,4 ± 0,2.
28. Kristal u skladu s patentnim zahtjevom 26, naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu kojeg čine vrijednosti 2θ od (za zračenje CuKα, valne duljine od 1,54056 Å) 6,5 ± 0,2, 9,3 ± 0,2, te 13,6 ± 0,2.
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EP3500564B1 (en) 2020-10-07
PT3500564T (pt) 2020-11-25
AR109179A1 (es) 2018-11-07
MD3500564T2 (ro) 2020-12-31
GEP20207159B (en) 2020-10-12
MY196330A (en) 2023-03-24
AU2017313420A1 (en) 2019-02-07

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