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RU2015137610A - Способы лечения и профилактики лекарственной резистентности злокачественных опухолей - Google Patents

Способы лечения и профилактики лекарственной резистентности злокачественных опухолей Download PDF

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RU2015137610A
RU2015137610A RU2015137610A RU2015137610A RU2015137610A RU 2015137610 A RU2015137610 A RU 2015137610A RU 2015137610 A RU2015137610 A RU 2015137610A RU 2015137610 A RU2015137610 A RU 2015137610A RU 2015137610 A RU2015137610 A RU 2015137610A
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antagonist
individual
effective amount
egfr
egfr antagonist
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RU2015137610A
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RU2015137610A3 (ru
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Роберт Л. ЯУХ
Сяофэнь Е
Ави АШКЕНАЗИ
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Дженентек, Инк.
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/177Receptors; Cell surface antigens; Cell surface determinants
    • A61K38/179Receptors; Cell surface antigens; Cell surface determinants for growth factors; for growth regulators
    • 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
    • A61K31/517Pyrimidines; 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
    • 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
    • A61K31/535Heterocyclic 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Cell Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (21)

1. Способ лечения злокачественной опухоли у индивидуума, включающий одновременное введение индивидууму (а) антагониста сигнализации FGFR и (b) антагониста EGFR.
2. Способ по п. 1, в котором соответствующие количества антагониста сигнализации FGFR и антагониста EGFR эффективны для увеличения периода чувствительности злокачественной опухоли и/или задержки развития резистентности злокачественной опухоли к антагонисту EGFR.
3. Способ по п. 1, в котором соответствующие количества антагониста сигнализации FGFR и антагониста EGFR эффективны для повышения чувствительности злокачественной опухоли и/или восстановления чувствительности к антагонисту EGFR.
4. Способ воздействия на злокачественную клетку, в котором злокачественная клетка опухоли устойчива к воздействию антагонистом EGFR у индивидуума, включающий введение индивидууму эффективного количества антагониста сигнализации FGFR и эффективного количества антагониста EGFR.
5. Способ лечения резистентной к антагонисту EGFR злокачественной опухоли у индивидуума, включающий введение индивидууму эффективного количества антагониста сигнализации FGFR и эффективного количества антагониста EGFR.
6. Способ повышения чувствительности и/или восстановления чувствительности к антагонисту EGFR, включающий введение индивидууму эффективного количества антагониста сигнализации FGFR и эффективного количества антагониста EGFR.
7. Способ повышения эффективности лечения злокачественной опухоли, включающий антагонист EGFR у индивидуума, способ включает одновременное введение индивидууму (а) эффективного количества антагониста сигнализации FGFR и (b) эффективного количества антагониста EGFR.
8. Способ задержки и/или профилактики развития резистентной к антагонисту EGFR злокачественной опухоли у индивидуума, включающий одновременное введение индивидууму (а) эффективного количества антагониста сигнализации FGFR и (b) эффективного количества антагониста EGFR.
9. Способ лечения индивидуума со злокачественной опухолью, которая характеризуется повышенной вероятностью развития резистентности к антагонисту EGFR, включающий одновременное введение индивидууму (а) эффективного количества антагониста сигнализации FGFR и (b) эффективного количества антагониста EGFR.
10. Способ повышения чувствительности к антагонисту EGFR у индивидуума со злокачественной опухолью, включающий одновременное введение индивидууму (а) эффективного количества антагониста сигнализации FGFR и (b) эффективного количества антагониста EGFR.
11. Способ продления периода чувствительности к антагонисту EGFR у индивидуума со злокачественной опухолью, включающий одновременное введение индивидууму (а) эффективного количества антагониста сигнализации FGFR и (b) эффективного количества антагониста EGFR.
12. Способ увеличения продолжительности ответа на антагонист EGFR у индивидуума со злокачественной опухолью, включающий одновременное введение индивидууму (а) эффективного количества антагониста сигнализации FGFR и (b) эффективного количества антагониста EGFR.
13. Способ по любому из пп. 1-12, в котором злокачественная опухоль представляет собой рак легких (например, немелкоклеточный рак легких (NSCLC)).
14. Способ по любому из пп. 1-12, в котором злокачественная опухоль претерпела эпителиально-мезенхимальный переход.
15. Способ по любому из пп. 1-12, в котором антагонист сигнализации FGFR представляет собой антитело-ингибитор, низкомолекулярный ингибитор, связующий полипептид-ингибитор и/или полинуклеотид-антагонист.
16. Способ по любому из пп. 1-12, в котором антагонист сигнализации FGFR представляет собой антагонист сигнализации FGFR1.
17. Способ по любому из пп. 1-12, в котором антагонист сигнализации FGFR1 связывается с одним или несколькими из FGFR1b, FGFR1c, FGF1, FGF2, FGF3, FGF4, FGF5, FGF6 и FGF10.
18. Способ по п. 15, в котором антагонист сигнализации FGFR представляет собой связующий полипептид-ингибитор и связующий полипептид-ингибитор содержит связанную с Fc FGFR область внеклеточного домена.
19. Способ по п. 15, в котором антагонист сигнализации FGFR представляет собой малую молекулу и малая молекула представляет собой N-[2-[[4-(диэтиламино)бутил]амино]-6-(3,5-диметоксифенил)пиридо-[2,3-(3]пиримидин-7-ил]-N'-(1,1-димитилэтил)мочевину или ее фармацевтически приемлемую соль.
20. Способ по любому из пп. 1-12, 18 и 19, в котором антагонист EGFR представляет собой N-(3-этинилфенил)-6,7-бис(2-метоксиэтокси)-4-хиназолинамин и/или его фармацевтически приемлемую соль.
21. Способ по любому из пп. 1-12, 18 и 19, в котором антагонист EGFR представляет собой N-(3-хлор-4-фторфенил)-7-метокси-6-(3-морфолин-4-илпропокси)хиназолин-4-амин или его фармацевтически приемлемую соль.
RU2015137610A 2013-03-06 2014-03-06 Способы лечения и профилактики лекарственной резистентности злокачественных опухолей RU2015137610A (ru)

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US201361773720P 2013-03-06 2013-03-06
US61/773,720 2013-03-06
PCT/US2014/021120 WO2014138364A2 (en) 2013-03-06 2014-03-06 Methods of treating and preventing cancer drug resistance

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RU2015137610A3 RU2015137610A3 (ru) 2018-03-13

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US (1) US9925240B2 (ru)
EP (1) EP2964260A2 (ru)
JP (1) JP2016510751A (ru)
KR (1) KR20150123250A (ru)
CN (1) CN105246511A (ru)
BR (1) BR112015021423A2 (ru)
CA (1) CA2902263A1 (ru)
HK (1) HK1213180A1 (ru)
MX (1) MX2015011428A (ru)
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