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RU2014120792A - Способ лечения стромальных опухолей желудочно-кишечного тракта - Google Patents

Способ лечения стромальных опухолей желудочно-кишечного тракта Download PDF

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Publication number
RU2014120792A
RU2014120792A RU2014120792/15A RU2014120792A RU2014120792A RU 2014120792 A RU2014120792 A RU 2014120792A RU 2014120792/15 A RU2014120792/15 A RU 2014120792/15A RU 2014120792 A RU2014120792 A RU 2014120792A RU 2014120792 A RU2014120792 A RU 2014120792A
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Prior art keywords
gist
combination
inhibitor
imatinib
pharmaceutically acceptable
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RU2014120792/15A
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English (en)
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Джон Е. МОНАХАН
Фан Ли
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Новартис Аг
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Application filed by Новартис Аг filed Critical Новартис Аг
Publication of RU2014120792A publication Critical patent/RU2014120792A/ru

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    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)

Abstract

1. Способ лечения GIST у пациента человека, включающий введение пациенту человеку, нуждающемуся в лечении, эффективной в отношении GIST дозы сочетания (a) ингибитора c-kit и (b) ингибитора PI3K или ингибитора FGFR, или их соответствующих фармацевтически приемлемых солей.2. Способ по п. 1, в котором в качестве ингибитора c-kit выбирают иматиниб, нилотиниб и маситиниб, или их соответствующие фармацевтически приемлемые соли.3. Комбинация, включающая для лечения GIST, (a) ингибитор c-kit и (b) ингибитор PI3K или ингибитор FGFR, или их соответствующие фармацевтически приемлемые соли.4. Способ по п. 1 или 2 или комбинация по п. 3, где GIST прогрессирует после терапии иматинибом.5. Способ по п. 1 или 2 или комбинация по п. 3, где GIST прогрессирует после терапии иматинибом и сунитинибом.6. Способ по п. 2, в котором иматиниб применяют в суточной дозе, составляющей от 300 до 600 мг.7. Способ по любому из пп. 1 или 2 или комбинация по п. 3, где в качестве ингибитора PI3K выбирают 2-метил-2-[4-(3-метил-2-оксо-8-хинолин-3-ил-2,3-дигидро-имидазо[4,5-c]хинолин-1-ил)-фенил]-пропионитрил, 5-(2,6-ди-морфолин-4-ил-пиримидин-4-ил)-4-трифторметил-пиридин-2-иламин и 2-амид 1-({4-метил-5-[2-(2,2,2-трифтор-1,1-диметил-этил)-пиридин-4-ил]-тиазол-2-ил}-амид) (S)-пирролидин-1,2-дикарбоновой кислоты или их соответствующие фармацевтически приемлемые соли.

Claims (7)

1. Способ лечения GIST у пациента человека, включающий введение пациенту человеку, нуждающемуся в лечении, эффективной в отношении GIST дозы сочетания (a) ингибитора c-kit и (b) ингибитора PI3K или ингибитора FGFR, или их соответствующих фармацевтически приемлемых солей.
2. Способ по п. 1, в котором в качестве ингибитора c-kit выбирают иматиниб, нилотиниб и маситиниб, или их соответствующие фармацевтически приемлемые соли.
3. Комбинация, включающая для лечения GIST, (a) ингибитор c-kit и (b) ингибитор PI3K или ингибитор FGFR, или их соответствующие фармацевтически приемлемые соли.
4. Способ по п. 1 или 2 или комбинация по п. 3, где GIST прогрессирует после терапии иматинибом.
5. Способ по п. 1 или 2 или комбинация по п. 3, где GIST прогрессирует после терапии иматинибом и сунитинибом.
6. Способ по п. 2, в котором иматиниб применяют в суточной дозе, составляющей от 300 до 600 мг.
7. Способ по любому из пп. 1 или 2 или комбинация по п. 3, где в качестве ингибитора PI3K выбирают 2-метил-2-[4-(3-метил-2-оксо-8-хинолин-3-ил-2,3-дигидро-имидазо[4,5-c]хинолин-1-ил)-фенил]-пропионитрил, 5-(2,6-ди-морфолин-4-ил-пиримидин-4-ил)-4-трифторметил-пиридин-2-иламин и 2-амид 1-({4-метил-5-[2-(2,2,2-трифтор-1,1-диметил-этил)-пиридин-4-ил]-тиазол-2-ил}-амид) (S)-пирролидин-1,2-дикарбоновой кислоты или их соответствующие фармацевтически приемлемые соли.
RU2014120792/15A 2011-10-28 2012-10-24 Способ лечения стромальных опухолей желудочно-кишечного тракта RU2014120792A (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161552633P 2011-10-28 2011-10-28
US61/552,633 2011-10-28
PCT/US2012/061532 WO2013063000A1 (en) 2011-10-28 2012-10-24 Method of treating gastrointestinal stromal tumors

Publications (1)

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RU2014120792A true RU2014120792A (ru) 2015-12-10

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US (1) US20140288073A1 (ru)
EP (1) EP2770999A1 (ru)
JP (1) JP2014532647A (ru)
KR (1) KR20140096035A (ru)
CN (1) CN103889422A (ru)
AU (1) AU2012328979B2 (ru)
BR (1) BR112014009993A2 (ru)
CA (1) CA2853095A1 (ru)
CL (1) CL2014001062A1 (ru)
IL (1) IL231943A0 (ru)
MX (1) MX2014005130A (ru)
RU (1) RU2014120792A (ru)
SG (1) SG11201400543TA (ru)
TN (1) TN2014000093A1 (ru)
TW (1) TW201332550A (ru)
WO (1) WO2013063000A1 (ru)
ZA (1) ZA201401622B (ru)

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JP2014532647A (ja) 2014-12-08
CL2014001062A1 (es) 2014-10-10
TN2014000093A1 (en) 2015-07-01
TW201332550A (zh) 2013-08-16
NZ622155A (en) 2015-12-24
AU2012328979B2 (en) 2016-04-21
AU2012328979A1 (en) 2014-05-15
ZA201401622B (en) 2015-12-23
CN103889422A (zh) 2014-06-25
IL231943A0 (en) 2014-05-28
MX2014005130A (es) 2014-08-27
EP2770999A1 (en) 2014-09-03
WO2013063000A1 (en) 2013-05-02
CA2853095A1 (en) 2013-05-02
US20140288073A1 (en) 2014-09-25
SG11201400543TA (en) 2014-08-28
BR112014009993A2 (pt) 2017-04-25
KR20140096035A (ko) 2014-08-04

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