CN102596937B - 作为蛋白激酶抑制剂的化合物和组合物 - Google Patents

作为蛋白激酶抑制剂的化合物和组合物 Download PDF

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Publication number
CN102596937B
CN102596937B CN201080038235.XA CN201080038235A CN102596937B CN 102596937 B CN102596937 B CN 102596937B CN 201080038235 A CN201080038235 A CN 201080038235A CN 102596937 B CN102596937 B CN 102596937B
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amino
pyrimidine
imidazoles
phenyl
cyclopropyl
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Chinese (zh)
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CN102596937A (zh
Inventor
A·Q·科斯塔勒斯
S·黄
J(X)·金
刘佐胜
S·佩基
D·蓬
J·泰卢
张琼
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Novartis AG
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Novartis AG
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    • 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
    • A61K31/505Pyrimidines; 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201080038235.XA 2009-08-28 2010-08-26 作为蛋白激酶抑制剂的化合物和组合物 Active CN102596937B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US23808309P 2009-08-28 2009-08-28
US61/238,083 2009-08-28
US31306110P 2010-03-11 2010-03-11
US61/313,061 2010-03-11
PCT/EP2010/062495 WO2011023773A1 (en) 2009-08-28 2010-08-26 Compounds and compositions as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
CN102596937A CN102596937A (zh) 2012-07-18
CN102596937B true CN102596937B (zh) 2014-02-12

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CN201080038235.XA Active CN102596937B (zh) 2009-08-28 2010-08-26 作为蛋白激酶抑制剂的化合物和组合物

Country Status (19)

Country Link
US (3) US8242260B2 (OSRAM)
EP (1) EP2470528B1 (OSRAM)
JP (1) JP5726190B2 (OSRAM)
KR (1) KR101714107B1 (OSRAM)
CN (1) CN102596937B (OSRAM)
AR (1) AR077977A1 (OSRAM)
AU (1) AU2010288455B2 (OSRAM)
BR (1) BR112012004448A2 (OSRAM)
CA (1) CA2771673C (OSRAM)
EA (1) EA020479B1 (OSRAM)
ES (1) ES2527176T3 (OSRAM)
IN (1) IN2012DN00869A (OSRAM)
JO (1) JO3007B1 (OSRAM)
MX (1) MX2012002542A (OSRAM)
PL (1) PL2470528T3 (OSRAM)
PT (1) PT2470528E (OSRAM)
TW (1) TWI487701B (OSRAM)
UY (1) UY32859A (OSRAM)
WO (1) WO2011023773A1 (OSRAM)

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US20150232452A1 (en) * 2012-09-19 2015-08-20 Ruga Corporation Novel raf kinase inhibitors
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
CA2912568A1 (en) * 2013-05-30 2014-12-04 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
EP3013815B1 (en) 2013-06-25 2017-05-03 Bristol-Myers Squibb Company Carbazole carboxamide compounds useful as kinase inhibitors
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JP2017506618A (ja) * 2013-08-28 2017-03-09 メディベイション テクノロジーズ, インコーポレイテッド 複素環式化合物および使用方法
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HK1243021A1 (zh) 2014-10-14 2018-07-06 The Regents Of The University Of California 使用cdk9和brd4抑制剂来抑制炎症
CN104402920B (zh) * 2014-11-27 2018-04-03 河南科技学院 一种合成2‑卤代‑3‑频那醇硼酸酯‑5‑氯苯胺的方法
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WO2018146253A1 (en) 2017-02-10 2018-08-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway
AU2018262891B2 (en) 2017-05-02 2021-04-01 Novartis Ag Combination therapy
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WO2020124397A1 (en) * 2018-12-19 2020-06-25 Inventisbio Shanghai Ltd. C-terminal src kinase inhibitors
AU2020276695A1 (en) 2019-05-13 2021-12-23 Novartis Ag New crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as Raf inhibitors for the treatment of cancer
WO2022036176A1 (en) * 2020-08-13 2022-02-17 Albert Einstein College Of Medicine N-cyclyl-sulfonamides useful for inhibiting raf
KR20240167846A (ko) 2022-03-28 2024-11-28 니캉 테라퓨틱스 인코포레이티드 사이클린 의존적 키나제 2 억제제로서의 설폰아미도 유도체
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Also Published As

Publication number Publication date
US8859548B2 (en) 2014-10-14
KR20120092577A (ko) 2012-08-21
BR112012004448A2 (pt) 2017-05-30
JP5726190B2 (ja) 2015-05-27
US20110052578A1 (en) 2011-03-03
AU2010288455A1 (en) 2012-02-23
AU2010288455B2 (en) 2013-01-31
WO2011023773A1 (en) 2011-03-03
US20140011825A1 (en) 2014-01-09
PT2470528E (pt) 2014-12-29
AR077977A1 (es) 2011-10-05
US8242260B2 (en) 2012-08-14
MX2012002542A (es) 2012-04-02
CA2771673A1 (en) 2011-03-03
KR101714107B1 (ko) 2017-03-08
UY32859A (es) 2011-03-31
TWI487701B (zh) 2015-06-11
PL2470528T3 (pl) 2015-03-31
JO3007B1 (ar) 2016-09-05
CA2771673C (en) 2016-07-12
ES2527176T3 (es) 2015-01-21
EP2470528A1 (en) 2012-07-04
IN2012DN00869A (OSRAM) 2015-07-10
CN102596937A (zh) 2012-07-18
US8563553B2 (en) 2013-10-22
EA020479B1 (ru) 2014-11-28
TW201111365A (en) 2011-04-01
EA201200323A1 (ru) 2012-09-28
EP2470528B1 (en) 2014-10-01
US20120225899A1 (en) 2012-09-06
JP2013503139A (ja) 2013-01-31

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