RU2016140626A - Комбинация ингибитора EGFR и ингибитора MEK для применения в лечении рака, вызванного мутировавшим NRAS - Google Patents

Комбинация ингибитора EGFR и ингибитора MEK для применения в лечении рака, вызванного мутировавшим NRAS Download PDF

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RU2016140626A
RU2016140626A RU2016140626A RU2016140626A RU2016140626A RU 2016140626 A RU2016140626 A RU 2016140626A RU 2016140626 A RU2016140626 A RU 2016140626A RU 2016140626 A RU2016140626 A RU 2016140626A RU 2016140626 A RU2016140626 A RU 2016140626A
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egfr inhibitor
inhibitor
nras
use according
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RU2016140626A
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RU2016140626A3 (ru
RU2683276C2 (ru
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Даррен Энтони Эдвард КРОСС
Кэтрин Энн ЭБЕРЛЕЙН
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Астразенека Аб
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    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • A61K31/41641,3-Diazoles
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    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4458Non condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
    • AHUMAN NECESSITIES
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    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Pulmonology (AREA)
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  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Claims (8)

1. Ингибитор EGFR (рецептор эпидермального фактора роста) для применения в лечении рака, вызванного мутировавшим NRAS (вирусный онкоген RAS нейробластомы), где ингибитор EGFR вводят в комбинации с ингибитором MEK (MAP (митогенактивируемая) протеинкиназа/регулируемая внеклеточными сигналами киназа-киназа), и мутация NRAS выбрана из E63K, G12V, G12R, G12A, G12D, G12S и G12C или роста копийности гена NRAS.
2. Ингибитор EGFR для применения по п. 1, где ингибитор EGFR выбран из гефитиниба, эрлотиниба, афатиниба, AZD9291 и CO1686 или их фармацевтически приемлемой соли.
3. Ингибитор EGFR для применения по пп. 1 или 2, где ингибитор EGFR выбран из AZD9291 и CO1686 или их фармацевтически приемлемой соли.
4. Ингибитор EGFR для применения по любому из пп. 1-3, где ингибитор MEK выбран из селуметиниба, траметиниба, MEK-162 и кобиметиниба или их фармацевтически приемлемой соли.
5. Ингибитор EGFR для применения по любому из пп. 1-4, где рак, вызванный мутировавшим NRAS, представляет собой вызванный мутировавшим NRAS немелкоклеточный рак легких.
6. Ингибитор EGFR для применения по любому из пп. 1-5, где мутация NRAS выбрана из E63K, G12V и G12R или роста копийности гена NRAS.
7. Ингибитор EGFR для применения по любому из пп. 1-6, где ингибитор EGFR представляет собой AZD9291 или его фармацевтически приемлемую соль.
8. Ингибитор EGFR для применения по любому из пп. 1-7, где ингибитор MEK представляет собой селуметиниб или его фармацевтически приемлемую соль.
RU2016140626A 2014-04-04 2015-04-02 Комбинация ингибитора EGFR и ингибитора MEK для применения в лечении рака, вызванного мутировавшим NRAS RU2683276C2 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201461975088P 2014-04-04 2014-04-04
US61/975,088 2014-04-04
US201462013573P 2014-06-18 2014-06-18
US62/013,573 2014-06-18
PCT/GB2015/051042 WO2015150826A1 (en) 2014-04-04 2015-04-02 Combination of egfr inhibitor and mek inhibitor for use in the treatment of nras mutated cancer

Publications (3)

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RU2016140626A true RU2016140626A (ru) 2018-05-07
RU2016140626A3 RU2016140626A3 (ru) 2018-10-23
RU2683276C2 RU2683276C2 (ru) 2019-03-27

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US (2) US20200237758A1 (ru)
EP (1) EP3125885B1 (ru)
JP (1) JP6549147B2 (ru)
KR (1) KR102406334B1 (ru)
CN (1) CN106456774A (ru)
AU (1) AU2015242407B2 (ru)
CA (1) CA2943402C (ru)
DK (1) DK3125885T3 (ru)
ES (1) ES2890556T3 (ru)
HU (1) HUE055747T2 (ru)
MA (1) MA39841A (ru)
MX (1) MX369111B (ru)
PL (1) PL3125885T3 (ru)
RU (1) RU2683276C2 (ru)
WO (1) WO2015150826A1 (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2780168C1 (ru) * 2019-02-18 2022-09-20 Корея Инститьют Оф Сайенс Энд Текнолоджи Новое производное пиридо [3,4-d] пиримидин-8-она, обладающее ингибирующей протеинкиназы активностью, и фармацевтическая композиция для предупреждения, облегчения или лечения рака, содержащее указанное выше

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KR102444835B1 (ko) 2016-05-26 2022-09-19 리커리엄 아이피 홀딩스, 엘엘씨 Egfr 억제제 화합물
WO2018218633A1 (en) * 2017-06-02 2018-12-06 Beijing Percans Oncology Co. Ltd. Combination therapies for treating cancers
WO2019195959A1 (en) 2018-04-08 2019-10-17 Cothera Biosciences, Inc. Combination therapy for cancers with braf mutation

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EP1492568A1 (en) * 2002-04-08 2005-01-05 SmithKline Beecham Corporation Cancer treatment method comprising administration of an erb-family inhibitor and a raf and/or ras inhibitor
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2780168C1 (ru) * 2019-02-18 2022-09-20 Корея Инститьют Оф Сайенс Энд Текнолоджи Новое производное пиридо [3,4-d] пиримидин-8-она, обладающее ингибирующей протеинкиназы активностью, и фармацевтическая композиция для предупреждения, облегчения или лечения рака, содержащее указанное выше

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KR20160135362A (ko) 2016-11-25
RU2016140626A3 (ru) 2018-10-23
PL3125885T3 (pl) 2021-12-06
WO2015150826A1 (en) 2015-10-08
DK3125885T3 (da) 2021-09-27
EP3125885B1 (en) 2021-06-30
JP6549147B2 (ja) 2019-07-24
CA2943402C (en) 2022-12-13
RU2683276C2 (ru) 2019-03-27
KR102406334B1 (ko) 2022-06-07
US20200237758A1 (en) 2020-07-30
AU2015242407B2 (en) 2017-11-09
JP2017511341A (ja) 2017-04-20
MX2016013048A (es) 2017-04-27
AU2015242407A1 (en) 2016-10-13
CA2943402A1 (en) 2015-10-08
US20210177844A1 (en) 2021-06-17
HUE055747T2 (hu) 2021-12-28
EP3125885A1 (en) 2017-02-08
CN106456774A (zh) 2017-02-22
MX369111B (es) 2019-10-29
ES2890556T3 (es) 2022-01-20
MA39841A (fr) 2017-02-08

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