HRP20191001T1 - Spojevi 3-aminocikloalkila kao inhibitori ror-gama-t i njihove upotrebe - Google Patents

Spojevi 3-aminocikloalkila kao inhibitori ror-gama-t i njihove upotrebe Download PDF

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HRP20191001T1
HRP20191001T1 HRP20191001TT HRP20191001T HRP20191001T1 HR P20191001 T1 HRP20191001 T1 HR P20191001T1 HR P20191001T T HRP20191001T T HR P20191001TT HR P20191001 T HRP20191001 T HR P20191001T HR P20191001 T1 HRP20191001 T1 HR P20191001T1
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Croatia
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chloro
trifluoromethyl
carboxylic acid
indazol
fluoro
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HRP20191001TT
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Kenneth Jay BARR
John Maclean
Hongjun Zhang
Richard Thomas Beresis
Neville Anthony
Matthew H DANIELS
Blair LAPOINTE
Nunzio Sciammetta
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Merck Sharp & Dohme Corp.
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Publication of HRP20191001T1 publication Critical patent/HRP20191001T1/hr

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Claims (16)

1. Spoj prema formuli I ili njegova farmaceutski prihvatljiva sol ili solvat, pri čemu: je a bez veze ili veza; je z 3, 2 ili 1; je X C(O), CH2 ili CHRb; je Y N; n = 0, 1, 2, 3 ili 4; je A4 CR4 ili N, je A5 CR5 ili N, je A6 CR6 ili N, je A7 CR7 ili N, uz uvjet da ne više od dva od A4-A7 mogu biti N; je Rb (C1-4)alkil; je R1 (i) (C3-12)karbociklil; ili (ii) 4-člani do 12-člani heterociklil, oboje (i) i (ii) mogu izborno biti supstituirani jednim, dva, tri, četiri ili pet R8; je R2 hidroksikarbonil, hidroksikarbonil(C1-10)alkil, (C1-10)alkilsulfoksiaminokarbonil ili karbamoil; je R3 vodik, halogen, cijano, nitro, hidroksi, (C1-3)alkilC(O)O-, fenil, (C1-4)alkil, okso ili (C1-4)alkoksi, pri čemu su (C1-4)alkil i (C1-4)alkoksi izborno supstituirani jednim ili više halogena; izborno kad je z 3, a predstavlja odsutnost veze te su dvije R3 skupine vezane na dva ugljika smještena pored N atoma piperidinil prstena formiranog kada je z 3, na način da se dvije R3 skupine spajaju kako bi formirale most s 2- ili 3- ugljika s piperidinil prstenom kako bi se formirao azabiciklo [3.2.1]oktanil ili azabiciklo [3.3.1]nonanil prsten; su R4, R5, R6 i R7 nezavisno H, halogen, amino, cijano, hidroksi, (C1-3)alkoksi, (C1-4)alkil, (C0-10)alkil)aminokarbonil, (di)(C1-6)alkilaminokarbonil ili amino(C1-4)alkil, pri čemu su (C1-3)alkoksi, (C1-4)alkil, (C0-10)alkil)aminokarbonil, (di)(C1-6)alkilaminokarbonil i amino(C1-4)alkil izborno supstituirani jednim ili više halogena, hidroksilom ili (C1-3)alkoksi; ili skupina koja ima formulu izborno supstituirana jednim ili više od sljedećih supstituenata: (C1-10)alkil, halogen, amino, cijano, hidroksi, (C1-3)alkoksi, te pri čemu je m 1, 2, 3 ili 4; je R8 halogen, cijano, amino, nitro, hidroksi, okso, H2NC(O)-, (C1-3)alkoksikarbonil, (di)(C1-6)alkilaminokarbonil, (C1-4)alkil, (C3-7)cikloalkil, (C3-5)heterocikloalkil ili (C1-3)alkoksi, pri čemu su (C1-3)alkoksikarbonil, (di)(C1-6)alkilaminokarbonil, (C1-4)alkil i (C1-3)alkoksi izborno supstituirani jednim, dva ili tri halogena.
2. Spoj prema zahtjevu 1 koji ima formulu Ia ili njegova farmaceutski prihvatljiva sol ili solvat.
3. Spoj prema zahtjevu 1 koji ima formulu Ib ili njegova farmaceutski prihvatljiva sol ili solvat.
4. Spoj prema zahtjevu 1 koji ima formulu Ic ili njegova farmaceutski prihvatljiva sol ili solvat.
5. Spoj prema zahtjevu 2 koji ima formulu Id pri čemu je x 1, 2, 3, 4 ili 5, ili njegova farmaceutski prihvatljiva sol ili solvat.
6. Spoj prema zahtjevu 5 koji ima formulu Ie ili njegova farmaceutski prihvatljiva sol ili solvat.
7. Spoj prema zahtjevu 6 koji ima formulu If ili njegova farmaceutski prihvatljiva sol ili solvat.
8. Spoj prema zahtjevu 7 koji ima formulu Ig ili njegova farmaceutski prihvatljiva sol ili solvat.
9. Spoj prema zahtjevu 1, pri čemu su A4, A5, A6, A7 (i) CR4, CR5, CR6, CR7; ili (ii) N, CR5, CR6, CR7.
10. Spoj prema zahtjevu 9, pri čemu je R1 (C6-14)aril, izborno supstituiran jednim, dva, tri, četiri ili pet R8, izborno pri čemu je R1 fenil, izborno supstituiran jednim, dva ili tri R8.
11. Spoj prema zahtjevu 10, pri čemu je R1 fenil, izborno supstituiran jednim, dva ili tri R8; i R2 je C(O)OH.
12. Spoj prema zahtjevu 1 odabran od: (3R,4R i 3S, 4S)-1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-1H-pirazolo[4,3-b]piridin-3-il)-3-metilpiperidin-4-karboksilna kiselina; 8-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-1H-pirazolo[4,3-b]piridin-3-il)-8-azabiciklo[3.2.1]oktan-3-karboksilna kiselina; 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-4-fluoro-1H-indazol-3-il)pirolidin-3-karboksilna kiselina; (3R,4R i 3S,4S)-1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-4-fluoro-1H-indazol-3-il)-3-metilpiperidin-4-karboksilna kiselina; 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-4-fluoro-1H-indazol-3-il)-4-metilpiperidin-4-karboksilna kiselina; 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-4-fluoro-1H-indazol-3-il)-4-fenilpiperidin-4-karboksilna kiselina; 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-4-fluoro-1H-indazol-3-il)piperidin-4-karboksilna kiselina; [1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-4-fluoro-1H-indazol-3-il)piperidin-4-il] octena kiselina; 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-1H-pirazolo[4,3-b]piridin-3-il)-3-hidroksipiperidin-4-karboksilna kiselina; 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-1H-pirazolo[4,3-b]piridin-3-il)-1,2,3,6-tetrahidropiridin-4-karboksilna kiselina; 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-1H-pirazolo[4,3-b]piridin-3-il)piperidin-4-karboksilna kiselina; 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-1H-pirazolo[4,3-b]piridin-3-il)-4-fluoropiperidin-4-karboksilna kiselina; 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-1H-pirazolo[4,3-b]piridin-3-il)-3-fluoropiperidin-4-karboksilna kiselina; [1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-1H-pirazolo[4,3-b]piridin-3-il)azetidin-3-il] octena kiselina; 1-[1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-6-(dimetilkarbamoil)-1H-indazol-3-il]piperidin-4-karboksilna kiselina; 1-[1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-6-(hidroksimetil)-1H-indazol-3-il]piperidin-4-karboksilna kiselina; 1-(4-kloro-1-(2-kloro-6-(trifluorometil)benzoil)-1H-indazol-3-il)piperidin-4-karboksilna kiselina; 1-(1-(2-kloro-6-(trifluorometil)benzoil)-4-metil-1H-indazol-3-il)piperidin-4-karboksilna kiselina; 1-(1-(2-kloro-6-ciklopropilbenzoil)-4-fluoro-1H-indazol-3-il)piperidin-4-karboksilna kiselina; 1-(1-(2-kloro-6-ciklobutilbenzoil)-4-fluoro-1H-indazol-3-il)piperidin-4-karboksilna kiselina; (3R,4S i 3S,4R)-1-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-3-metilpiperidin-4-karboksilna kiselina; (3R,4R i 3S,4S)-1-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-3-metilpiperidin-4-karboksilna kiselina; 8-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-8-azabiciklo[3.2.1]oktan-3-karboksilna kiselina; 1R,5S)-9-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-9-azabiciklo[3.3.1]nonan-3-karboksilna kiselina; 1-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-2-etilpiperidin-4-karboksilna kiselina; 1-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-4-hidroksipiperidin-4-karboksilna kiselina; (3S,4R ili 3R,4S)-1-(1-(2-kloro-6-ciklopropilbenzoil)-4-fluoro-1H-indazol-3-il)-3-hidroksipiperidin-4-karboksilna kiselina; (3R,4S ili 3S,4R)-1-(1-(2-kloro-6-ciklopropilbenzoil)-4-fluoro-1H-indazol-3-il)-3-hidroksipiperidin-4-karboksilna kiselina; (3S,4R ili 3R,4S)-1-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-3-hidroksipiperidin-4-karboksilna kiselina; (3R,4S ili 3S,4R)-1-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-3-hidroksipiperidin-4-karboksilna kiselina; (3R,4R i 3S,4S)-1-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-3-hidroksipiperidin-4-karboksilna kiselina; (3R,4R)-1-(1-(2-kloro-6-ciklopropilbenzoil)-4-fluoro-1H-indazol-3-il)-3-hidroksi-4-metilpiperidin-4-karboksilna kiselina; (3S,4R ili 3R,4S)-1-(1-(2-kloro-6-ciklopropil benzoil)-4-fluoro-1H-indazol-3-il)-3-hidroksi-4-metilpiperidin-4-karboksilna kiselina; (3R,4S ili 3S,4R)-1-(1-(2-kloro-6-ciklopropilbenzoil)-4-fluoro-1H-indazol-3-il)-3-hidroksi-4-metilpiperidin-4-karboksilna kiselina; 1-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-2-oksopiperidin-4-karboksilna kiselina; 1-(1-(2-kloro-6-(trifluorometil)benzoil)-4-fluoro-1H-indazol-3-il)-2-metilpiperidin-4-karboksilna kiselina; 1-(1-(2-kloro-6-(trifluorometil)benzoil)-6-(3-metoksi azetidin-1-karbonil)-1H-indazol-3-il)piperidin-4-karboksilna kiselina; (S)-1-(1-(2-kloro-6-(trifluorometil)benzoil)-6-(2-metilpirolidin-1-karbonil)-1H-indazol-3-il)piperidin-4-karboksilna kiselina; (S)-1-(1-(2-kloro-6-(trifluorometil)benzoil)-6-(3-metoksipirolidin-1-karbonil)-1H-indazol-3-il)piperidin-4-karboksilna kiselina; i (R)-1-(1-(2-kloro-6-(trifluorometil)benzoil)-6-(3-metoksipirolidin-1-karbonil)-1H-indazol-3-il)piperidin-4-karboksilna kiselina.
13. Spoj odabran od: 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-4-fluoro-1H-indazol-3-il)-4-(trifluorometil)piperidin-4-ol; cis-4-[(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-4-fluoro-1H-indazol-3-il)amino]cikloheksankarboksilna kiselina; i 1-(1-{[2-kloro-6-(trifluorometil)fenil]karbonil}-1H-pirazolo[4,3-b]piridin-3-il)-4-(trifluorometil)piperidin-4-ol.
14. Farmaceutski sastav koji sadrži spoj prema bilo kojem od prethodnih zahtjeva ili njihovu farmaceutski prihvatljivu sol ili solvat i jednu ili više farmaceutski prihvatljivih pomoćnih tvari, izborno pri čemu farmaceutski sastav nadalje sadrži barem jedan dodatni terapeutski aktivni agens.
15. Spoj prema bilo kojem od zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol ili solvat, za uporabu u liječenju bolesti ili stanja posredovanog gamom t Orfan receptora povezanog s receptorom retinoične kiseline (ROR-gamaT), pri čemu je bolest ili stanje autoimuna bolest ili upalna bolest.
16. Spoj za uporabu prema zahtjevu 15, pri čemu je bolest ili stanje multipla skleroza, upalna bolest crijeva, Kronova bolest, ankilozantni spondilitis, psorijaza, reumatoidni artritis, astma, osteoartritis, Kawasakijeva bolest, Hashimotov tiroiditis ili lišmanijaza sluznice.
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