HRP20210783T1 - Derivati karboksamida - Google Patents

Derivati karboksamida Download PDF

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HRP20210783T1
HRP20210783T1 HRP20210783TT HRP20210783T HRP20210783T1 HR P20210783 T1 HRP20210783 T1 HR P20210783T1 HR P20210783T T HRP20210783T T HR P20210783TT HR P20210783 T HRP20210783 T HR P20210783T HR P20210783 T1 HRP20210783 T1 HR P20210783T1
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Croatia
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dihydro
dimethyl
cyclohexyl
carboxamide
oxo
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HRP20210783TT
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Anne-Marie D'souza
Mahbub AHMED
Robert Alexander Pulz
Lisa Ann ROONEY
Nichola Smith
Thomas Josef TROXLER
Kamlesh Jagdis Bala
Andrew BREARLEY
James Dale
David Porter
David Andrew Sandham
Duncan Shaw
Jessica Louise TAYLOR
Roger John Taylor
Joe WRIGGLESWORTH
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Novartis Ag
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Publication of HRP20210783T1 publication Critical patent/HRP20210783T1/hr

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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Claims (15)

1. Spoj formule (I): [image] ili njegova farmaceutski prihvatljiva sol, naznačen time, što R1 je (C3-C6)alkil ili (C3-C6)cikloalkil; R2 je metil; R3 se bira od (C6-C10)razgranatog alkila, (C6-C10)razgranatog alkenila, (C5-C8)cikloalkenila, (C5-C8)cikloalkila, ili Het; pri čemu je (C5-C8)cikloalkenil ili (C5-C8)cikloalkil nesupstituiran ili je supstituiran s jednim, dva, tri ili četiri supstituenta R4; i pri čemu je Het supstituiran s jednim, dva, tri ili četiri supstituenta R4; svaki R4 je neovisno odabran od halogena, (C1-C4)alkila, halo(C1-C4)alkila, (C1-C4)alkoksi, ili halo(C1-C4)alkoksi; ili dvije R4 skupine, kada su vezane na isti atom ugljika, mogu se uzeti zajedno s atomom ugljika na koji su vezane, tako da tvore ciklopentilni, tetrahidrofuranski ili dioksolanski prsten; pri čemu Het je 5-člani ili 6-člani potpuno zasićeni ili djelomično zasićeni heterociklički prsten koji sadrži a) jedan atom kisika na položaju 2- ili 3-, ili b) dva atoma kisika na položajima 2- i 5-, ili 2- i 6-, pri čemu je numeriranje relativno prema mjestu vezanja; i (C5-C8)cikloalkil može biti monociklički prsten ili premošteni prstenasti sustav koji sadrži 5, 6, 7 ili 8 ugljikovih atoma.
2. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time, što R1 je izo-propil, ciklobutil ili cikloheksil.
3. Spoj prema patentnom zahtjevu 1 ili zahtjevu 2, ili njegova farmaceutski prihvatljiva sol, naznačen time, što R3 je odabran iz niza koji čine 2,2-dimetilpentil, 2,2-dimetilpent-2-enil, ciklopentil, cikloheksil, cikloheksenil, tetrahidropiranil, dihidropiranil, dioksanil, tetrahidrofuranil, dioksolanil i biciklo[2.2.2]oktanil; pri čemu je ciklopentil, cikloheksil, cikloheksenil, ili biciklo[2.2.2]oktanil prsten nesupstituiran ili je supstituiran s jednim, dva, tri ili četiri supstituenta R4; i pri čemu je tetrahidropiranil, dihidropiranil, dioksanil, tetrahidrofuranil, ili dioksolanil prsten supstituiran s jednim, dva, tri ili četiri supstituenta R4; i svaki R4 je neovisno odabran od halogena, (C1-C4)alkila, halo(C1-C4)alkila, (C1-C4)alkoksi, ili halo(C1-C4)alkoksi; ili dvije R4 skupine, kada su vezane na isti atom ugljika, mogu se uzeti zajedno s atomom ugljika na koji su vezane, tako da tvore tetrahidrofuranski ili dioksolanski prsten.
4. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, ili njegova farmaceutski prihvatljiva sol, naznačen time, što R3 je [image] i m je 1, 2, 3 ili 4.
5. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, ili njegova farmaceutski prihvatljiva sol, naznačen time, što je svaki R4 neovisno odabran od metila, izopropila, terc-butila i metoksi.
6. Spoj prema patentnom zahtjevu 1, naznačen time, što je odabran iz skupine koju čine: [N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(4-izopropilcikloheks-1-en-1-il)-4-metilizoksazol-3-karboksamid]; N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(6-etil-4-metilcikloheks-1-en-1-il)-4-metilizoksazol-3-karboksamid; N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(6,6-dimetilcikloheks-1-en-1-il)-4-metilizoksazol-3-karboksamid; [N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(4-etilcikloheks-1-en-1-il)-4-metilizoksazol-3-karboksamid]; [5-(4-(terc-Butil)cikloheks-1-en-1-il)-N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid]; [N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-(4-metilcikloheks-1-en-1-il)izoksazol-3-karboksamid]; 5-(Ciklohept-1-en-1-il)-N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid; [N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-(4-(trifluorometil)cikloheks-1-en-1-il)izoksazol-3-karboksamid]; N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-(spiro[4.5]dek-7-en-8-il)izoksazol-3-karboksamid; [N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-(1-oksaspiro [4.5]dek-7-en-8-il)izoksazol-3-karboksamid]; N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(4,4-dimetilcikloheks-1-en-1-il)-4-metilizoksazol-3-karboksamid; N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(4,4-dimetilciklopent-1-en-1-il)-4-metilizoksazol-3-karboksamid; [N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-(2-oksaspiro [4.5]dek-7-en-8-il)izoksazol-3-karboksamid]; [N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(4-izopropoksicikloheks-1-en-1-il)-4-metilizoksazol-3-karboksamid]; N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(4,4-dimetilcikloheksil)-4-metilizoksazol-3-karboksamid; [N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(3,3-dimetilciklopentil)-4-metilizoksazol-3-karboksamid]; N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(3,3-dimetilbutil)-4-metilizoksazol-3-karboksamid; (Z)-N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(3,3-dimetilbut-1-en-1-il)-4-metilizoksazol-3-karboksamid; (E)-N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(3,3-dimetilbut-1-en-1-il)-4-metilizoksazol-3-karboksamid; 5-Cikloheksil-N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid; N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-(1,4-dioksaspiro[4.5]dekan-8-il)izoksazol-3-karboksamid; 5-(6-(terc-butil)-4-metoksitetrahidro-2H-piran-2-il)-N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid; 5-(6-(terc-butil)-4-metoksitetrahidro-2H-piran-2-il)-N-(2-ciklobutil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid; 5-(6-(terc-butil)tetrahidro-2H-piran-2-il)-N-(2-ciklobutil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid; 5-(6-(terc-butil)tetrahidro-2H-piran-2-il)-N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid; 5-(6-(terc-butil)tetrahidro-2H-piran-2-il)-N-(2-izopropil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid; N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(6-izopropil-3,6-dihidro-2H-piran-2-il)-4-metilizoksazol-3-karboksamid; N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-(6-metil-3,6-dihidro-2H-piran-2-il)izoksazol-3-karboksamid; N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-((2R,3S)-3,5,5-trimetil-1,4-dioksan-2-il)izoksazol-3-karboksamid; [5-(4-Bromo-5-metiltetrahidro-2H-piran-2-il)-N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid]; N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-(5-metil-3,6-dihidro-2H-piran-2-il)izoksazol-3-karboksamid; N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-(5-metiltetrahidro-2H-piran-2-il)izoksazol-3-karboksamid; 5-(4-(2-bromopropan-2-il)tetrahidrofuran-2-il)-N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid; N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(4-izopropiltetrahidrofuran-2-il)-4-metilizoksazol-3-karboksamid; 5-(4-(terc-butil)-1,3-dioksolan-2-il)-N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metilizoksazol-3-karboksamid; N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(5,5-dimetil-1,3-dioksan-2-il)-4-metilizoksazol-3-karboksamid; ili njihova farmaceutski prihvatljiva sol.
7. Spoj prema patentnom zahtjevu 1, naznačen time, što je N-(2-cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-((2R,3S)-3,5,5-trimetil-1,4-dioksan-2-il)izoksazol-3-karboksamid koji ima slijedeću formulu: [image] ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema patentnom zahtjevu 1, naznačen time, što je N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-5-(5,5-dimetil-1,3-dioksan-2-il)-4-metilizoksazol-3-karboksamid koji ima slijedeću formulu: [image] ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema patentnom zahtjevu 1, naznačen time, što je N-(2-Cikloheksil-1,5-dimetil-3-okso-2,3-dihidro-1H-pirazol-4-il)-4-metil-5-(1,4-dioksaspiro[4.5]dekan-8-il)izoksazol-3-karboksamid koji ima slijedeću formulu: [image] ili njegova farmaceutski prihvatljiva sol.
10. Farmaceutski pripravak, naznačen time, što sadrži terapijski učinkovitu količinu spoja prema bilo kojem od patentnih zahtjeva 1 do 5 ili 7 do 9 ili njegove farmaceutski prihvatljive soli i jedan ili više farmaceutski prihvatljivih nosača.
11. Kombinacija, naznačena time, što sadrži terapijski učinkovitu količinu spoja prema bilo kojem od patentnih zahtjeva 1 do 5 ili 7 do 9 ili njegove farmaceutski prihvatljive soli i jedno ili više terapijski aktivnih sredstava.
12. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5 ili 7 do 9 ili njegova farmaceutski prihvatljiva sol, naznačen time, što je za uporabu kao lijek.
13. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5 ili 7 do 9 ili njegova farmaceutski prihvatljiva sol, naznačen time, što je za uporabu u liječenju poremećaja ili bolesti odabranih od plućne hipertenzije uključujući plućnu arterijsku hipertenziju (PAH), fibroze, reumatoidnog artritisa, te zacjeljivanja prijeloma.
14. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5 ili 7 do 9 ili njegova farmaceutski prihvatljiva sol, naznačen time, što je za uporabu u liječenju poremećaja ili bolesti odabranih od glaukoma, nasljedne hemoragijske telangiektazije (HHT), proteinurije, zacjeljivanja rana, KOPB i astme.
15. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5 ili 7 do 9 ili njegova farmaceutski prihvatljiva sol, za uporabu prema zahtjevu 13, naznačen time, što je fibroza idiopatska plućna fibroza.
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