HRP20220127T1 - Supstituirani spoj piperidina i njegova uporaba - Google Patents

Supstituirani spoj piperidina i njegova uporaba Download PDF

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HRP20220127T1
HRP20220127T1 HRP20220127TT HRP20220127T HRP20220127T1 HR P20220127 T1 HRP20220127 T1 HR P20220127T1 HR P20220127T T HRP20220127T T HR P20220127TT HR P20220127 T HRP20220127 T HR P20220127T HR P20220127 T1 HRP20220127 T1 HR P20220127T1
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optionally substituted
alkyl
substituents selected
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HRP20220127TT
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Tatsuhiko Fujimoto
Kentaro Rikimaru
Koichiro Fukuda
Hiromichi Sugimoto
Takahiro Matsumoto
Norihito Tokunaga
Mariko Hirozane
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Takeda Pharmaceutical Company Limited
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Publication of HRP20220127T1 publication Critical patent/HRP20220127T1/hr

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Claims (9)

1. Spoj, naznačen time, da je predstavljen formulom: [image] u kojoj R1 je (1) atom vodika, (2) C1-6 alkil-karbonil skupina koja je opcionalno supstituirana s 1 do 7 supstituenata koji se biraju od sljedećih: (i) atom halogena, (ii) cijano skupina, (iii) hidroksi skupina, (iv) C3-10 cikloalkil skupina, (v) C1-6 alkoksi skupina, (vi) C6-14 aril skupina, (vii) C6-14 ariloksi skupina, (viii) pirazolil skupina, tiazolil skupina, pirimidinil skupina ili piridazinil skupina, od kojih je svaka opcionalno supstituirana s okso skupinom, (ix) pirazoliloksi skupina koja je opcionalno supstituirana s 1 do 3 C1-6 alkil skupine, (x) C1-6 alkil-karbonil skupina, (xi) C1-6 alkoksi-karbonil skupina, (xii) C1-6 alkil-karboniloksi skupina, (xiii) C1-6 alkilsulfonil skupina, (xiv) mono- ili di-C1-6 alkilamino skupina, (xv) C1-6 alkil-karbonilamino skupina i (xvi) (C1-6 alkil)(C1-6 alkil-karbonil) amino skupina, (3) C3-10 cikloalkil-karbonil skupina koja je opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od atoma halogena, cijano skupine, hidroksi skupine, okso skupine i C1-6 alkil skupine, (4) C1-6 alkoksi-karbonil skupina koja je opcionalno supstituirana s 1 do 6 supstituenata koji se biraju od deuterija, atoma halogena i C6-14 aril skupine, (5) C3-10 cikloalkiloksi-karbonil skupina koja je opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od C1-6 alkil skupine, (6) C6-14 aril-karbonil skupina koja je opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od atoma halogena i C6-14 aril skupine, (7) C6-14 ariloksi-karbonil skupina, (8) furilkarbonil skupina, tienilkarbonil skupina, pirazolilkarbonil skupina, izoksazolilkarbonil skupina ili piridilkarbonil skupina, od kojih je svaka opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od C1-6 alkil skupine, (9) azetidinilkarbonil skupina, oksetanilkarbonil skupina, pirolidinilkarbonil skupina, tetrahidrofuranilkarbonil skupina, tetrahidropiranilkarbonil skupina ili morfolinilkarbonil skupina, od kojih je svaka opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od okso skupine, C1-6 alkil-karbonil skupine, C1-6 alkoksi-karbonil skupine i C1-6 alkilsulfonil skupine, (10) mono- ili di-C1-6 alkil-karbamoil skupina koja je opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od atoma halogena, cijano skupine, hidroksi skupine i C1-6 alkoksi skupine, (11) mono- ili di-C3-10 cikloalkil-karbamoil skupina, (12) mono- ili di-C6-14 aril-karbamoil skupina, (13) C1-6 alkilsulfonil skupina, (14) C3-10 cikloalkilsulfonil skupina, (15) C6-14 arilsulfonil skupina koja je opcionalno supstituirana s 1 do 3 atoma halogena, (16) tienilsulfonil skupina, pirazolilsulfonil skupina, imidazolilsulfonil skupina, piridilsulfonil skupina ili dihidrokromenilsulfonil skupina, od kojih je svaka opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od C1-6 alkil skupine, (17) mono- ili di-C1-6 alkil-sulfamoil skupina, ili (18) C1-6 alkil-karbonil-karbonil skupina; R2 je C3-6 cikloalkil skupina, pirolidinil skupina, piperidinil skupina ili dioksanil skupina, od kojih je svaka opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od sljedećih: (1) deuterij, (2) atom halogena, (3) hidroksi skupina, (4) C1-6 alkil skupina koja je opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od atoma halogena i C6-14 aril skupine, (5) C3-10 cikloalkil skupina, (6) C1-6 alkoksi skupina koja je opcionalno supstituirana sa C3-10 cikloalkil skupinom, (7) C6-14 aril skupina koja je opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od atoma halogena, cijano skupine, C1-6 alkil skupine koja je opcionalno supstituirana s 1 do 3 atoma halogena, C1-6 alkoksi skupine koja je opcionalno supstituirana s 1 do 3 atoma halogena i hidroksi skupine, (8) C6-14 ariloksi skupina, (9) tri-C1-6 alkilsililoksi skupina, (10) pirazolil skupina, tiazolil skupina, piridil skupina, pirimidinil skupina, kinazolinil skupina, benzotiazolil skupina ili izokinolinil skupina, od kojih je svaka opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od atoma halogena, C1-6 alkil skupine i C1-6 alkoksi skupine, i (11) C6-14 aril-karbonil skupina; i R3 je C1-6 alkil skupina ili mono- ili di-C1-6 alkilamino skupina, ili njegova sol.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen formulom: [image] u kojoj su R1, R2 i R3 isti kao što su definirani u patentnom zahtjevu 1, ili njegova sol.
3. Spoj prema patentnom zahtjevu 1, naznačen time, da R1 je (1) atom vodika, (2) C1-6 alkil-karbonil skupina koja je opcionalno supstituirana s hidroksi skupinom, (3) ciklopropankarbonil skupina, (4) C1-6 alkoksi-karbonil skupina, ili (5) mono- ili di-C1-6 alkil-karbamoil skupina; R2 je (A) cikloheksil skupina koja je opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od sljedećih: (1) C1-6 alkil skupina, i (2) fenil skupina koja je opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od atoma halogena, C1-6 alkil skupine opcionalno supstituirane s 1 do 3 atoma halogena i C1-6 alkoksi skupine, ili (B) piperidinil skupina koja je opcionalno supstituirana s 1 do 3 pirimidinil skupine; i R3 je C1-6 alkil skupina ili di-C1-6 alkilamino skupina, ili njegova sol.
4. Spoj prema patentnom zahtjevu 1, naznačen time, da R1 je (1) C1-6 alkil-karbonil skupina koja je opcionalno supstituirana s hidroksi skupinom, (2) C1-6 alkoksi-karbonil skupina, ili (3) mono- ili di-C1-6 alkil-karbamoil skupina; R2 je cikloheksil skupina koja je opcionalno supstituirana s 1 do 3 supstituenta koji se biraju od sljedećih: (1) C1-6 alkil skupina, i (2) fenil skupina koja je opcionalno supstituirana s 1 do 3 atoma halogena; i R2 je C1-6 alkil skupina, ili njegova sol.
5. Spoj prema patentnom zahtjevu 1, naznačen time, da je metil (2R,3S)-3-((metilsulfonil)amino)-2-(((cis-4-fenilcikloheksil)oksi)metil)piperidin-1-karboksilat ili njegova sol.
6. Spoj prema patentnom zahtjevu 1, naznačen time, da je N-(2R,3S)-1-glikoloil-2-(((cis-4-(2,3,6-trifluorofenil)cikloheksil)oksi)metil)piperidin-3-il)metansulfonamid ili njegova sol.
7. Spoj prema patentnom zahtjevu 1, naznačen time, da je (2R,3S)-N-etil-2-(((cis-4-izopropilcikloheksil)oksi)metil)-3-((metilsulfonil)amino)piperidin-1-karboksamid ili njegova sol.
8. Lijek, naznačen time, da sadrži spoj prema patentnom zahtjevu 1, ili njegovu sol.
9. Spoj prema patentnom zahtjevu 1 ili njegova sol, naznačen time, da je za uporabu u profilaksi ili liječenju narkolepsije.
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