HRP20210899T1 - Derivat piridona koji ima tetrahidropiranil metil grupu - Google Patents

Derivat piridona koji ima tetrahidropiranil metil grupu Download PDF

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HRP20210899T1
HRP20210899T1 HRP20210899TT HRP20210899T HRP20210899T1 HR P20210899 T1 HRP20210899 T1 HR P20210899T1 HR P20210899T T HRP20210899T T HR P20210899TT HR P20210899 T HRP20210899 T HR P20210899T HR P20210899 T1 HRP20210899 T1 HR P20210899T1
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cancer
crystal
angstroms
wavelength
irradiation
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HRP20210899TT
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Noriyasu Haginoya
Takashi Suzuki
Miho Hayakawa
Masahiro Ota
Tomoharu Tsukada
Katsuhiro Kobayashi
Yosuke Ando
Takeshi Jimbo
Koichi Nakamura
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Daiichi Sankyo Company, Limited
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Claims (34)

1. Spoj predstavljen općom formulom (I) ili farmaceutski prihvatljiva sol istog: [image] pri čemu W, X, i Y svako nezavisno predstavlja atom dušika, C-H, C-F, ili C-Cl, Z predstavlja atom dušika, C-H, C-F, C-Cl, C-C1-C6 alkil ili C-C1-C6 alkoksi grupu, R1 predstavlja grupu predstavljenu sljedećom formulom (II-1) ili (II-2): [image] pri čemu u formuli (II-1), Q predstavlja atom dušika, C-H, ili C-F, T predstavlja atom dušika ili C-H, U predstavlja atom dušika ili C-H, i R6 predstavlja atom halogena, C1-C6 alkil grupu, C3-C6 cikloalkil grupu, cijano grupu, ili trifluorometoksi grupu, i u formuli (II-2), V predstavlja atom sumpora ili atom kisika, i R7 predstavlja C1-C6 alkil grupu, R2 predstavlja atom vodika, atom halogena, C1-C6 alkil grupu, C1-C6 alkoksi grupu, ili cijano grupu, R3 predstavlja atom vodika ili C1-C6 alkil grupu, R4 predstavlja atom vodika, atom halogena, ili C1-C6 alkil grupu, i R5 predstavlja atom vodika ili grupu predstavljenu sljedećom formulom (III-1), (III-2), (III-3), ili (III-4): [image] pri čemu u formuli (III-1), R8 i R12 svako nezavisno predstavlja atom vodika ili atom deuterija, R9 predstavlja atom vodika, atom halogena, ili C1-C6 alkoksi grupu, R10 predstavlja atom vodika, C1-C6 alkil grupu po izboru supstituiranu heterocikloalkil grupom, ili C1-C6 alkoksi grupu po izboru supstituiranu heterocikloalkil grupom po izboru supstituiranu C1-C6 alkil grupom, i R11 predstavlja atom vodika, C1-C6 alkoksi grupu, ili deuterijem supstituiranu C1-C6 alkoksi grupu, u formuli (III-2), R13 predstavlja C1-C6 alkil grupu po izboru supstituiranu heterocikloalkil grupom, ili heterocikloalkil grupu, u formuli (III-3), R14 predstavlja atom vodika ili C1-C6 alkil grupu, R15 predstavlja atom vodika, C1-C6 alkil grupu, ili C1-C6 alkoksi grupu, i R16 predstavlja atom vodika ili atom halogena, i u formuli (III-4), R17 predstavlja C1-C6 alkoksi grupu, i R18 predstavlja C1-C6 alkoksi grupu.
2. Spoj prema patentnom zahtjevu 1 koje je N-[4-(2-Amino-5-{4-[(2R)-1,4-dioksan-2-ilmetoksi]-3-metoksifenil}piridin-3-il)fenil]-5-(4-metilfenil)-4-okso-1-(tetrahidro-2H-piran-4-ilmetil)-1,4-dihidropiridin-3-karboksamid predstavljen sljedećom formulom: [image] ili farmaceutski prihvatljiva sol istog.
3. Spoj prema patentnom zahtjevu 1 koje je N-[4-(2-Amino-5-{4-[(2S)-1,4-dioksan-2-ilmetoksi]-3-metoksifenil}piridin-3-il)fenil]-5-(4-metilfenil)-4-okso-1-(tetrahidro-2H-piran-4-ilmetil)-1,4-dihidropiridin-3-karboksamid predstavljen sljedećom formulom: [image] ili farmaceutski prihvatljiva sol istog.
4. Spoj prema patentnom zahtjevu 1 koje je N-{4-[2-Amino-5-(3,4-dimetoksifenil)piridin-3-il]fenil}-5-(4-metilfenil)-4-okso-1-(tetrahidro-2H-piran-4-ilmetil)-1,4-dihidropiridin-3-karboksamid predstavljen sljedećom formulom: [image] ili farmaceutski prihvatljiva sol istog.
5. Spoj prema patentnom zahtjevu 1 koje je N-[4-(2-Amino-5-{4-[(2R)-1,4-dioksan-2-ilmetoksi]-3-metoksifenil}piridin-3-il)-3-fluorofenil]-5-metil-4'-okso-1'-(tetrahidro-2H-piran-4-ilmetil)-1',4'-dihidro-2,3'-bipiridin-5'-karboksamid predstavljen sljedećom formulom: [image] ili farmaceutski prihvatljiva sol istog.
6. Spoj prema patentnom zahtjevu 1 koje je odabrano iz grupe koja se sastoji od: N-[4-(2-Amino-5-{4-[(2S)-1,4-dioksan-2-ilmetoksi]-3-metoksifenil}piridin-3-il)-3-fluorofenil]-5-metil-4'-okso-1'-(tetrahidro-2H-piran-4-ilmetil)-1',4'-dihidro-2,3'-bipiridin-5'-karboksamida predstavljenog sljedećom formulom: [image] ili farmaceutski prihvatljive soli istog; N-{4-[2-Amino-5-(1-etil-1H-pirazol-4-il)piridin-3-il]-3-fluorofenil}-5-(4-metilfenil)-4-okso-1-(tetrahidro-2H-piran-4-ilmetil)-1,4-dihidropiridin-3-karboksamida predstavljenog sljedećom formulom: [image] ili farmaceutski prihvatljive soli istog; N-(4-{2-Amino-5-[1-(tetrahidro-2H-piran-4-il)-1H-pirazol-4-il]piridin-3-il}-3-fluorofenil)-5-(4-metilfenil)-4-okso-1-(tetrahidro-2H-piran-4-ilmetil)-1,4-dihidropiridin-3-karboksamida predstavljenog sljedećom formulom: [image] ili farmaceutski prihvatljive soli istog; N-[6-(2-Amino-5-{4-[(2R)-1,4-dioksan-2-ilmetoksi]-3-metoksifenil}piridin-3-il)piridazin-3-il]-5-(5-metiltiofen-2-il)-4-okso-1-(tetrahidro-2H-piran-4-ilmetil)-1,4-dihidropiridin-3-karboksamida predstavljenog sljedećom formulom: [image] ili farmaceutski prihvatljive soli istog; i N-[6-(2-Amino-5-{3-metoksi-4-[2-(morfolin-4-il)etoksi]fenil}piridin-3-il)piridazin-3-il]-5-(4-metilfenil)-4-okso-1-(tetrahidro-2H-piran-4-ilmetil)-1,4-dihidropiridin-3-karboksamida predstavljenog sljedećom formulom: [image] ili farmaceutski prihvatljive soli istog.
7. Hidrobromid, nitrat, sulfat, fosfat, metansulfonat, etansulfonat, benzensulfonat, ili p-toluensulfonat spoja prema patentnom zahtjevu 2.
8. Metansulfonat spoja prema patentnom zahtjevu 4.
9. Metansulfonat, fosfat, naftalen-1,5-disulfonat, ili sulfat spoja prema patentnom zahtjevu 5.
10. Kristal metansulfonata prema patentnom zahtjevu 7, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.74, 7.56, 8.96, 11.38, 12.36, 14.78, 15.60, 16.16, 18.70, i 24.10 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
11. Kristal hidrobromida prema patentnom zahtjevu 7, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.84, 7.72, 9.40, 11.62, 14.92, 15.48, 16.70, 18.88, 19.32, i 24.40 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
12. Kristal nitrata prema patentnom zahtjevu 7, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.82, 7.66, 9.28, 9.52, 11.54, 15.26, 15.54, 16.62, 19.24, i 24.56 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
13. Kristal sulfata prema patentnom zahtjevu 7, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.74, 7.56, 8.92, 9.58, 11.36, 12.38, 14.68, 15.64, 16.06, i 24.38 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
14. Kristal fosfata prema patentnom zahtjevu 7, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.74, 7.56, 8.80, 9.56, 11.34, 14.56, 15.74, 23.68, 24.34, i 24.68 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
15. Kristal etansulfonata prema patentnom zahtjevu 7, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 6.72, 7.90, 12.02, 13.40, 16.90, 17.88, 19.00, 19.80, 21.26, i 24.18 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
16. Kristal benzensulfonata prema patentnom zahtjevu 7, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 9.22, 10.60, 10.82, 11.10, 13.40, 15.78, 17.50, 18.66, 21.02, i 26.10 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
17. Kristal p-toluensulfonata prema patentnom zahtjevu 7, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 4.18, 5.12, 13.44, 14.98, 16.96, 17.44, 18.92, 19.72, 20.16, i 23.04 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
18. Kristal fosfata prema patentnom zahtjevu 9, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 4.28, 8.42, 8.64, 10.54, 12.72, 13.48, 15.90, 17.00. 17.46, i 21.26 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
19. Kristal sulfata prema patentnom zahtjevu 9, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.66, 6.42, 7.32, 9.76, 11.00, 12.88, 18.42, 19.62, 20.54, i 24.22 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
20. Kristal sulfata prema patentnom zahtjevu 9, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.64, 6.40, 7.32, 9.76, 17.38, 18.42, 19.64, 20.56, 22.90, i 24.20 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
21. Kristal sulfata prema patentnom zahtjevu 9, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.64, 6.40, 7.30, 9.76, 17.34, 18.38, 19.34, 20.56, 21.52, i 22.94 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
22. Kristal sulfata prema patentnom zahtjevu 9, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.62, 6.38, 7.28, 9.74, 17.30, 18.36, 19.54, 20.52, 22.86, i 24.14 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
23. Kristal sulfata prema patentnom zahtjevu 9, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.64, 6.40, 7.30, 9.76, 12.86, 18.40, 19.62, 20.54, 22.92, i 24.20 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
24. Kristal sulfata prema patentnom zahtjevu 9, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 3.64, 6.36, 7.30, 18.36, 19.04, 19.42, 19.70, 20.12, 20.42, i 21.32 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
25. Kristal sulfata prema patentnom zahtjevu 9, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 5.62, 7.18, 9.22, 10.36, 15.56, 16.40, i 20.86 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
26. Kristal naftalen-1,5-disulfonata prema patentnom zahtjevu 9, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 6.14, 6.98, 11.24, 14.84, 17.48, 19.54, 20.94, 22.38, 23.20, i 24.70 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
27. Kristal naftalen-1,5-disulfonata prema patentnom zahtjevu 9, pri čemu kristal pokazuje karakteristične pikove pri difrakcijskim kutovima 2θ = 9.24, 9.58, 14.00, 14.46, 16.70, 17.02, 18.22, 20.24, 21.64, i 25.52 u obrascu rendgenske difrakcije na prahu dobivenom ozračivanjem sa bakrenim Kα zračenjem (valna dužina λ = 1.54 angstrema).
28. Axl inhibitor koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 6 ili farmaceutski prihvatljivu sol istog.
29. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 6 ili farmaceutski prihvatljivu sol istog i farmaceutski prihvatljiv nosač.
30. Medikament koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 6 ili farmaceutski prihvatljivu sol istog kao aktivni sastojak.
31. Spoj prema bilo kojem od patentnih zahtjeva 1 do 6 ili farmaceutski prihvatljiva sol istog, farmaceutska kompozicija prema patentnom zahtjevu 29 ili medikament prema patentnom zahtjevu 30 za primjenu u terapiji.
32. Spoj prema bilo kojem od patentnih zahtjeva 1 do 6 ili farmaceutski prihvatljiva sol istog, farmaceutska kompozicija prema patentnom zahtjevu 29 ili medikament prema patentnom zahtjevu 30 za primjenu u liječenju hiperproliferativne bolesti.
33. Spoj prema bilo kojem od patentnih zahtjeva 1 do 6 ili farmaceutski prihvatljiva sol istog, farmaceutska kompozicija prema patentnom zahtjevu 29 ili medikament prema patentnom zahtjevu 30 za primjenu u liječenju raka, prevenciji metastaze raka, prevladavanje rezistencije raka na lijek, ili inhibiciji stjecanja rezistencije raka na lijek.
34. Spoj, farmaceutska kompozicija ili medikament za primjenu u liječenju raka, prevenciji metastaze raka, prevladavanju rezistencije raka na lijek, ili inhibiciji stjecanja rezistencije raka na lijek prema patentnom zahtjevu 33, pri čemu je rak izabran od raka dojke, raka debelog crijeva, raka prostate, raka pluća, raka želuca, raka jajnika, raka endometrija, raka bubrega, hepatocelularnog raka, raka tiroidne žljezde, raka materice, raka jednjaka, raka skvamoznih stanica, leukemije, osteosarkoma, melanoma, glioblastoma, neuroblastoma, i raka gušterače.
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