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RU2016141569A - Комбинации - Google Patents

Комбинации Download PDF

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Publication number
RU2016141569A
RU2016141569A RU2016141569A RU2016141569A RU2016141569A RU 2016141569 A RU2016141569 A RU 2016141569A RU 2016141569 A RU2016141569 A RU 2016141569A RU 2016141569 A RU2016141569 A RU 2016141569A RU 2016141569 A RU2016141569 A RU 2016141569A
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RU
Russia
Prior art keywords
methyl
combination according
pyrazol
pharmaceutically acceptable
solvate
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RU2016141569A
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English (en)
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RU2016141569A3 (ru
RU2715236C2 (ru
Inventor
Элеонора ЙОВХЕВА
Тимоти Пьетро Сурен Перера
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Астекс Терапьютикс Лтд
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Publication of RU2016141569A publication Critical patent/RU2016141569A/ru
Publication of RU2016141569A3 publication Critical patent/RU2016141569A3/ru
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Publication of RU2715236C2 publication Critical patent/RU2715236C2/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures 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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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 (16)

1. Комбинация первого соединения, выбранного из N-(3,5-диметоксифенил)-N'-(1-метилэтил)-N-[3-(1-метил-1H-пиразол-4-ил)хиноксалин-6-ил]этан-1,2-диамина или его фармацевтически приемлемой соли или его сольвата и N-(2-фтор-3,5-диметоксифенил)-N-(1H-имидазол-2-илметил)-3-(1-метил-1H-пиразол-4-ил)пиридо[2,3-b]пиразин-6-амина или его фармацевтически приемлемой соли или его сольвата; и второго соединения, которое является ингибитором cMet.
2. Комбинация по п.1, где первое соединение является N-(3,5-диметоксифенил)-N'-(1-метилэтил)-N-[3-(1-метил-1H-пиразол-4-ил)хиноксалин-6-ил]этан-1,2-диамином или его фармацевтически приемлемой солью или его сольватом.
3. Комбинация по п.2, где первое соединение является N-(3,5-диметоксифенил)-N'-(1-метилэтил)-N-[3-(1-метил-1H-пиразол-4-ил)хиноксалин-6-ил]этан-1,2-диамином в форме основания.
4. Комбинация по п.1, где первое соединение является N-(2-фтор-3,5-диметоксифенил)-N-(1H-имидазол-2-илметил)-3-(1-метил-1H-пиразол-4-ил)пиридо[2,3-b]пиразин-6-амином или его фармацевтически приемлемой солью или его сольватом.
5. Комбинация по п.4, где первое соединение является N-(2-фтор-3,5-диметоксифенил)-N-(1H-имидазол-2-илметил)-3-(1-метил-1H-пиразол-4-ил)пиридо[2,3-b]пиразин-6-амином в форме основания.
6. Комбинация по любому из предыдущих пунктов, где ингибитор cMet выбран из 6-{дифтор[6-(1-метил-1H-пиразол-4-ил)[1,2,4]триа-золо[4,3-b]пиридазин-3-ил]метил}хинолина или его фармацевтически приемлемой соли или его сольвата и 6-[дифтор(6-пиридин-4-ил[1,2,4]триазоло[4,3-b]пиридазин-3-ил)метил]хинолина или его фармацевтически приемлемой соли или его сольвата.
7. Комбинация по п.6, где ингибитор cMet является 6-{дифтор[6-(1-метил-1H-пиразол-4-ил)[1,2,4]триазоло[4,3-b]пиридазин-3-ил]метил}хинолином или его фармацевтически приемлемой солью или его сольватом.
8. Комбинация по п.7, где ингибитор cMet является 6-{дифтор[6-(1-метил-1H-пиразол-4-ил)[1,2,4]триазоло[4,3-b]пиридазин-3-ил]метил}хинолином в форме основания.
9. Комбинация по п.6, где ингибитор cMet является 6-[дифтор(6-пиридин-4-ил[1,2,4]триазоло[4,3-b]пиридазин-3-ил)метил]хинолином или его фармацевтически приемлемой солью или его сольватом.
10. Комбинация по п.9, где ингибитор cMet является 6-[дифтор(6-пиридин-4-ил[1,2,4]триазоло[4,3-b]пиридазин-3-ил)метил]хинолином в форме основания.
11. Фармацевтическая композиция, содержащая фармацевтически приемлемый носитель и комбинацию по любому из предыдущих пунктов.
12. Комбинация по любому из пп.1-10 или фармацевтическая композиция по п.11 для применения в качестве лекарственного средства.
13. Применение комбинации по любому из пп.1-10 или фармацевтической композиции по п.11 для производства лекарственного средства для профилактики или лечения, в частности лечения рака.
14. Способ профилактики или лечения рака, включающий введение субъекту, нуждающемуся в этом, комбинации по любому из пп.1-10 или фармацевтической композиции по п.11.
15. Применение по п.13 или способ по п.14 для лечения рака легкого, мочевого пузыря, молочной железы, желудка или гепатоцеллюлярного рака.
16. Фармацевтический продукт, включающий комбинацию по любому из пп.1-10 в качестве комбинированного препарата для одновременного, раздельного или последовательного применения в лечении рака.
RU2016141569A 2014-03-26 2015-03-26 Комбинации RU2715236C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14161835 2014-03-26
EP14161835.5 2014-03-26
PCT/EP2015/056512 WO2015144804A1 (en) 2014-03-26 2015-03-26 Combinations

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RU2016141569A true RU2016141569A (ru) 2018-04-26
RU2016141569A3 RU2016141569A3 (ru) 2018-11-02
RU2715236C2 RU2715236C2 (ru) 2020-02-26

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US (3) US10085982B2 (ru)
EP (2) EP3848034A1 (ru)
JP (2) JP6752715B2 (ru)
KR (1) KR102479693B1 (ru)
CN (1) CN106458999B (ru)
AU (1) AU2015238301B2 (ru)
BR (1) BR112016022056B1 (ru)
CA (1) CA2943682C (ru)
CY (1) CY1123930T1 (ru)
DK (1) DK3122358T3 (ru)
ES (1) ES2856482T3 (ru)
HR (1) HRP20210338T1 (ru)
HU (1) HUE053654T2 (ru)
LT (1) LT3122358T (ru)
MA (2) MA39784B1 (ru)
MX (1) MX370099B (ru)
PL (1) PL3122358T3 (ru)
PT (1) PT3122358T (ru)
RS (1) RS61536B1 (ru)
RU (1) RU2715236C2 (ru)
SI (1) SI3122358T1 (ru)
WO (1) WO2015144804A1 (ru)

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