HRP20211922T1 - Postupci i intermedijeri za pripravu jak inhibitora - Google Patents

Postupci i intermedijeri za pripravu jak inhibitora Download PDF

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Publication number
HRP20211922T1
HRP20211922T1 HRP20211922TT HRP20211922T HRP20211922T1 HR P20211922 T1 HRP20211922 T1 HR P20211922T1 HR P20211922T T HRP20211922T T HR P20211922TT HR P20211922 T HRP20211922 T HR P20211922T HR P20211922 T1 HRP20211922 T1 HR P20211922T1
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Croatia
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compound
formula
image
salt
reaction
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HRP20211922TT
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English (en)
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Pingli Liu
Dengjin Wang
Yongzhong Wu
Ganfeng Cao
Michael Xia
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Incyte Holdings Corporation
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50382653&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20211922(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Holdings Corporation filed Critical Incyte Holdings Corporation
Publication of HRP20211922T1 publication Critical patent/HRP20211922T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/26—Catalysts comprising hydrides, coordination complexes or organic compounds containing in addition, inorganic metal compounds not provided for in groups B01J31/02 - B01J31/24
    • B01J31/28—Catalysts comprising hydrides, coordination complexes or organic compounds containing in addition, inorganic metal compounds not provided for in groups B01J31/02 - B01J31/24 of the platinum group metals, iron group metals or copper
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (26)

1. Spoj, naznačen time, da je predstavljen Formulom VII: [image] ili njegova sol, u kojoj: svaki od R1 i R2 je neovisno H ili C1-6 alkil; ili R1 i R2, zajedno s dva atoma kisika s kojima su vezani i atom bora s kojim su vezani atomi kisika, tvore 5-člani do 6-člani heterocikloalkilni prsten koji je opcionalno supstituiran s 1, 2, 3 ili 4 C1-4 alkil skupine.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen Formulom VIIa: [image] ili njegova sol.
3. Postupak, naznačen time, da obuhvaća: reakciju spoja Formulom VIII: [image] sa spojem Formule IX: [image] u prisutnosti veznog sredstva za tvorbu spoja prema patentnom zahtjevu 1; pri čemu: svaki od R1 i R2 je neovisno H ili C1-6 alkil; ili R1 i R2, zajedno s dva atoma kisika s kojima su vezani i atom bora s kojim su vezani atomi kisika, tvore 5-člani do 6-člani heterocikloalkilni prsten koji je opcionalno supstituiran s 1, 2, 3 ili 4 C1-4 alkil skupine.
4. Postupak prema patentnom zahtjevu 3, naznačen time, da vezno sredstvo je 1,8-diazabiciklo[5,4,0]undecen.
5. Postupak prema bilo kojem od patentnih zahtjeva 3 do 4, naznačen time, da se upotrebljava 1,05 do oko 1,2 ekvivalenta veznog sredstva na temelju spoja Formule VIII.
6. Postupak prema bilo kojem od patentnih zahtjeva 3 do 5, naznačen time, da se reakcija spoja Formule VIII sa spojem Formule IX: (a) provodi u komponenti otapala koja sadrži acetonitril; ili (b) provodi u komponenti otapala koja sadrži acetonitril na temperaturi od oko 40 ºC do oko 60 ºC.
7. Postupak prema bilo kojem od patentnih zahtjeva 3 do 6, naznačen time, da se upotrebljava 1 do 1,2 ekvivalenta spoja Formule IX na temelju spoja Formule VIII.
8. Postupak prema patentnom zahtjevu 3, naznačen time, da postupak obuhvaća reakciju spoja Formule VIII: [image] sa spojem Formule IXa: [image] u prisutnosti veznog sredstva za tvorbu spoja Formule VIIa: [image]
9. Postupak prema patentnom zahtjevu 8, naznačen time, da vezno sredstvo je 1,8-diazabiciklo[5,4,0]undecen.
10. Postupak prema bilo kojem od patentnih zahtjeva 8 ili 9, naznačen time, da se upotrebljava 1,05 do oko 1,2 ekvivalenta veznog sredstva na temelju spoja Formule VIII.
11. Postupak prema bilo kojem od patentnih zahtjeva 8 do 10, naznačen time, da se reakcija spoja Formule VIII sa spojem Formule IXa: (a) provodi u komponenti otapala koja sadrži acetonitril; ili (b) provodi u komponenti otapala koja sadrži acetonitril na temperaturi od oko 40 ºC do oko 60 ºC.
12. Postupak prema bilo kojem od patentnih zahtjeva 8 do 11, naznačen time, da se upotrebljava 1 do 1,2 ekvivalenta spoja Formule IXa na temelju spoja Formule VIII.
13. Postupak prema bilo kojem od patentnih zahtjeva 8 do 12, naznačen time, da nadalje obuhvaća reakciju spoja Formule VIIa sa spojem Formule IVa: [image] pod uvjetima Suzuki vezanja u svrhu tvorbe spoja Formule I: [image] pri čemu uvjeti Suzuki vezanja obuhvaćaju zagrijavanje reakcijske smjese koja sadrži spoj Formule VIIa, spoj Formule IVa, katalizator Suzuki vezanja, bazu i drugu komponentu otapala.
14. Postupak prema patentnom zahtjevu 13, naznačen time, da katalizator je tetrakis(trifenilfosfin)paladij(0).
15. Postupak prema patentnom zahtjevu 13 ili zahtjevu 14, naznačen time, da baza je natrijev bikarbonat.
16. Postupak prema patentnom zahtjevu 15, naznačen time, da je natrijev bikarbonat prisutan u 4 ekvivalenta ili više na temelju spoja Formule VIIa.
17. Postupak prema bilo kojem od patentnih zahtjeva 13 do 16, naznačen time, da druga komponenta otapala sadrži 1,4-dioksan i vodu.
18. Postupak prema patentnom zahtjevu 17, naznačen time, da se 1,4-dioksan i voda nalaze u volumenskom omjeru 1:1.
19. Postupak prema bilo kojem od patentnih zahtjeva 13 do 18, naznačen time, da se spojevi Formule VIIa i IVa nalaze u molarnom omjeru od oko 1:1.
20. Postupak prema patentnom zahtjevu 8, naznačen time, da nadalje obuhvaća reakciju spoja Formulle VIIa sa spojem Formule IVa: [image] pod uvjetima Suzuki vezanja u svrhu tvorbe spoja Formule I: [image] pri čemu uvjeti Suzuki vezanja obuhvaćaju zagrijavanje reakcijske smjese koja sadrži spoj Formule VIIa, spoj Formule IVa, tetrakis(trifenilfosfin)paladij(0), natrijev bikarbonat, i drugu komponentu otapala, pri čemu druga komponenta otapala sadrži vodu i 1,4-dioksan.
21. Spoj, naznačen time, da je predstavljen Formulom VIII: [image] ili njegova sol.
22. Postupak priprave spoja prema patentnom zahtjevu 21, ili njegove soli, naznačen time, da obuhvaća reakciju spoja Formule VI: [image] sa spojem Formule X: [image] ili njegovom soli, u prisutnosti redukcijskog sredstva.
23. Postupak prema patentnom zahtjevu 22, naznačen time, da spoj Formule X, ili njegova sol, jest 2-(azetidin-3-iliden)acetonitril hidroklorid.
24. Postupak prema patentnom zahtjevu 22 ili zahtjevu 23, naznačen time, da redukcijsko sredstvo je: (a) natrijev cijanoborohidrid ili natrijev triacetoksiborohidrid; ili (b) natrijev triacetoksiborohidrid.
25. Postupak prema bilo kojem od patentnih zahtjeva 22 do 24, naznačen time, da se: (a) oko 1,5 do oko 2,5 ekvivalenata redukcijskog sredstva upotrebljava na temelju spoja Formule X, ili njegove soli; ili (b) oko 2 ekvivalenta redukcijskog sredstva upotrebljava na temelju spoja spoja Formule X, ili njegove soli.
26. Postupak prema bilo kojem od patentnih zahtjeva 22 do 25, naznačen time, da se reakcija spoja Formule VI i spoja Formule X, ili njegove soli, provodi u komponenti otapala koja sadrži diklorometan.
HRP20211922TT 2013-03-06 2014-03-05 Postupci i intermedijeri za pripravu jak inhibitora HRP20211922T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361773659P 2013-03-06 2013-03-06
EP18204165.7A EP3489239B1 (en) 2013-03-06 2014-03-05 Processes and intermediates for making a jak inhibitor

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HRP20211922T1 true HRP20211922T1 (hr) 2022-03-04

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HRP20190233TT HRP20190233T1 (hr) 2013-03-06 2019-02-05 Postupci i intermedijeri za dobivanje inhibitora jak

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US (3) US8987443B2 (hr)
EP (3) EP2964650B1 (hr)
JP (2) JP6397831B2 (hr)
KR (2) KR102236232B1 (hr)
CN (1) CN105189509B (hr)
AR (2) AR095018A1 (hr)
AU (1) AU2014225938B2 (hr)
BR (2) BR112015021458B1 (hr)
CA (2) CA2903418C (hr)
CL (2) CL2015002468A1 (hr)
CR (2) CR20190518A (hr)
CY (2) CY1121512T1 (hr)
DK (1) DK2964650T3 (hr)
EA (2) EA201891157A1 (hr)
ES (2) ES2707355T3 (hr)
HK (1) HK1218540A1 (hr)
HR (2) HRP20211922T1 (hr)
HU (2) HUE042466T2 (hr)
IL (3) IL240891A0 (hr)
LT (2) LT2964650T (hr)
ME (1) ME03350B (hr)
MX (2) MX2015011667A (hr)
NZ (2) NZ711976A (hr)
PE (2) PE20151902A1 (hr)
PH (1) PH12015501958B1 (hr)
PL (2) PL2964650T3 (hr)
PT (2) PT3489239T (hr)
RS (2) RS58547B1 (hr)
SG (2) SG10201707259PA (hr)
SI (2) SI3489239T1 (hr)
TR (1) TR201820520T4 (hr)
TW (1) TWI634121B (hr)
UA (2) UA120162C2 (hr)
WO (1) WO2014138168A1 (hr)
ZA (1) ZA201908345B (hr)

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KR102236232B1 (ko) 2021-04-05
LT2964650T (lt) 2019-04-25
CA3091179C (en) 2023-01-17
IL259723A (en) 2018-07-31
RS62867B1 (sr) 2022-02-28
HUE057262T2 (hu) 2022-04-28
CN105189509B (zh) 2017-12-19
US8987443B2 (en) 2015-03-24
CY1125072T1 (el) 2023-03-24
EP2964650B1 (en) 2018-12-05

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