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HRP20210338T1 - Kombinacije fgfr-i cmet-inhibitora za liječenje raka - Google Patents

Kombinacije fgfr-i cmet-inhibitora za liječenje raka Download PDF

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Publication number
HRP20210338T1
HRP20210338T1 HRP20210338TT HRP20210338T HRP20210338T1 HR P20210338 T1 HRP20210338 T1 HR P20210338T1 HR P20210338T T HRP20210338T T HR P20210338TT HR P20210338 T HRP20210338 T HR P20210338T HR P20210338 T1 HRP20210338 T1 HR P20210338T1
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Croatia
Prior art keywords
cancer
methyl
combination
pyrazol
pharmaceutically acceptable
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HRP20210338TT
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English (en)
Inventor
Eleonora JOVCHEVA
Timothy Pietro Suren Perera
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Astex Therapeutics Ltd.
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Publication of HRP20210338T1 publication Critical patent/HRP20210338T1/hr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (19)

1. Kombinacija prvog spoja odabranog od N-(3,5-dimetoksifenil)-N'-(1-metiletil)-N-[3-(1-metil-1H-pirazol-4-il)kvinoksalin-6-il]etan-1,2-diamina ili njegove farmaceutski prihvatljive soli ili njegovog solvata, i N-(2-fluoro-3,5-dimetoksifenil)-N-(1H-imidazol-2-ilmetil)-3-(1-metil-1H-pirazol-4-il)pirido[2,3-b]pirazin-6-amina ili njegove farmaceutski prihvatljive soli ili njegovog solvata; i drugog spoja koji je cMet inhibitor.
2. Kombinacija u skladu sa patentnim zahtjevom 1 naznačena time što je prvi spoj N-(3,5-dimetoksifenil)-N'-(1-metiletil)-N-[3-(1-metil-1H-pirazol-4-il)kvinoksalin-6-il]etan-1,2-diamin ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
3. Kombinacija u skladu sa patentnim zahtjevom 2 naznačena time što je prvi spoj N-(3,5-dimetoksifenil)-N'-(1-metiletil)-N-[3-(1-metil-1H-pirazol-4-il)kvinoksalin-6-il]etan-1,2-diamin baza.
4. Kombinacija u skladu sa patentnim zahtjevom 1 naznačena time što je prvi spoj N-(2-fluoro-3,5-dimetoksifenil)-N-(1H-imidazol-2-ilmetil)-3-(1-metil-1H-pirazol-4-il)pirido[2,3-b]pirazin-6-amin ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
5. Kombinacija u skladu sa patentnim zahtjevom 4 naznačena time što je prvi spoj N-(2-fluoro-3,5-dimetoksifenil)-N-(1H-imidazol-2-ilmetil)-3-(1-metil-1H-pirazol-4-il)pirido[2,3-b]pirazin-6-amin baza.
6. Kombinacija u skladu sa bilo kojim od prethodnih patentnih zahtjeva naznačena time što je cMet inhibitor odabran od 6-{difluoro[6-(1-metil-1H-pirazol-4-il)[1,2,4]triazolo[4,3-b]piridazin-3-il]metil}kvinolina ili njegove farmaceutski prihvatljive soli ili njegovog solvata, i 6-[difluoro(6-piridin-4-il[1,2,4]triazolo[4,3-b] piridazin-3-il)metil]kvinolina ili njegove farmaceutski prihvatljive soli ili njegovog solvata.
7. Kombinacija u skladu sa patentnim zahtjevom 6 naznačena time što je cMet inhibitor 6-{difluoro[6-(1-metil-1H-pirazol-4-il)[1,2,4]triazolo[4,3-b]piridazin-3-il]metil}kvinolin ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
8. Kombinacija u skladu sa patentnim zahtjevom 7 naznačena time što je cMet inhibitor 6-{difluoro[6-(1-metil-1H-pirazol-4-il)[1,2,4]triazolo[4,3-b]piridazin-3-il]metil}kvinolin baza.
9. Kombinacija u skladu sa patentnim zahtjevom 6 naznačena time što je cMet inhibitor 6-[difluoro(6-piridin-4-il[1,2,4]triazolo[4,3-b]piridazin-3-il)metil]kvinolin ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
10. Kombinacija u skladu sa patentnim zahtjevom 9 naznačena time što je cMet inhibitor 6-[difluoro(6-piridin-4-il[1,2,4]triazolo[4,3-b]piridazin-3-il)metil]kvinolin baza.
11. Farmaceutski pripravak koji sadrži farmaceutski prihvatljiv nosač i kombinaciju kao što je zahtijevano u bilo kojem od prethodnih patentnih zahtjeva.
12. Kombinacija kao što je zahtijevano u bilo kojem od patentnih zahtjeva 1 do 10 ili farmaceutski pripravak kao što je zahtijevano u patentnom zahtjevu 11 za uporabu kao lijek.
13. Kombinacija kao što je zahtijevano u bilo kojem od patentnih zahtjeva 1 do 10 ili farmaceutski pripravak kao što je zahtijevano u patentnom zahtjevu 11 za uporabu u profilaksi ili liječenju, posebno za uporabu u liječenju, raka.
14. Kombinacija ili farmaceutski pripravak za uporabu u liječenju raka u skladu sa patentnim zahtjevom 13 naznačeni time što je rak rak pluća, mjehura, dojke, želuca ili hepatocelularni rak.
15. Kombinacija ili farmaceutski pripravak za uporabu u skladu sa patentnim zahtjevom 14 naznačeni time što (i) rak je rak mjehura; (ii) rak je rak mjehura sa FGFR3 kromosomskom translokacijom; ili (iii) rak je rak mjehura sa FGFR3 točkastom mutacijom.
16. Kombinacija ili farmaceutski pripravak za uporabu u liječenju raka u skladu sa patentnim zahtjevom 13 naznačeni time što (i) rak je tumor sa mutantom FGFR1, FGFR2, FGFR3 ili FGFR4; ili (ii) rak je tumor sa mutantom dobivanja funkcije FGFR2 ili FGFR3; ili (iii) rak je tumor sa prekomjernom ekspresijom FGFR1.
17. Kombinacija ili farmaceutski pripravak za uporabu u liječenju raka u skladu sa patentnim zahtjevom 13 naznačeni time što je rak rak mjehura, urotelijalni rak, metastatski urotelijalni rak, kirurški neopoziv urotelijalni rak, rak dojke, glioblastom, rak pluća, nesitnostanićni rak pluća, rak pločastih stanica pluća, adenokarcinom pluća, pulmonarni adenokarcinom, sitnostanićni rak pluća, rak jajnika, rak endometrija, rak grlića materice, sarkom mekog tkiva, rak pločastih stanica glave i vrata, rak želuca, rak jednjaka, karcinom pločastih stanica jednjaka, adenokarcinom jednjaka, kolangiokarcinom, hepatocelularni karcinom.
18. Kombinacija ili farmaceutski pripravak za uporabu u skladu sa patentnim zahtjevom 17 naznačeni time što je rak urotelijalni kancer, metastatski urotelijalni rak, kirurški neopoziv urotelijalni rak.
19. Farmaceutski proizvod koji sadrži kombinaciju u skladu sa bilo kojim od patentnih zahtjeva 1 do 10 kao kombinirani preparat za istovremenu, odvojenu ili uzastopnu uporabu u liječenju raka.
HRP20210338TT 2014-03-26 2015-03-26 Kombinacije fgfr-i cmet-inhibitora za liječenje raka HRP20210338T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14161835 2014-03-26
PCT/EP2015/056512 WO2015144804A1 (en) 2014-03-26 2015-03-26 Combinations
EP15721129.3A EP3122358B1 (en) 2014-03-26 2015-03-26 Combinations of fgfr- and cmet-inhibitors for the treatment of cancer

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HRP20210338T1 true HRP20210338T1 (hr) 2021-04-30

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US (3) US10085982B2 (hr)
EP (2) EP3122358B1 (hr)
JP (2) JP6752715B2 (hr)
KR (1) KR102479693B1 (hr)
CN (1) CN106458999B (hr)
AU (1) AU2015238301B2 (hr)
BR (1) BR112016022056B1 (hr)
CA (1) CA2943682C (hr)
CY (1) CY1123930T1 (hr)
DK (1) DK3122358T3 (hr)
ES (2) ES2856482T3 (hr)
HR (1) HRP20210338T1 (hr)
HU (1) HUE053654T2 (hr)
LT (1) LT3122358T (hr)
MA (2) MA55696A (hr)
MX (1) MX370099B (hr)
PL (1) PL3122358T3 (hr)
PT (1) PT3122358T (hr)
RS (1) RS61536B1 (hr)
RU (1) RU2715236C2 (hr)
SI (1) SI3122358T1 (hr)
SM (1) SMT202100115T1 (hr)
WO (1) WO2015144804A1 (hr)

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