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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China
Prior art keywords
amino
pyrimidine
phenyl
cyclopropyl
chloro
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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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs 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

Family

ID=42829939

Family Applications (1)

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

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AR077975A1 (es) 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
ES2576061T3 (es) 2010-02-25 2016-07-05 Dana-Farber Cancer Institute, Inc. Mutaciones de BRAF que confieren resistencia a inhibidores de BRAF
US9498471B2 (en) 2011-10-20 2016-11-22 The Regents Of The University Of California Use of CDK9 inhibitors to reduce cartilage degradation
RU2622015C2 (ru) 2011-11-11 2017-06-08 Новартис Аг Способ лечения пролиферативного заболевания
SI2782557T1 (sl) 2011-11-23 2019-02-28 Array Biopharma, Inc., Farmacevtske formulacije
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
WO2014047330A1 (en) * 2012-09-19 2014-03-27 Jean-Michel Vernier Novel raf kinase inhibitors
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
CN105228983A (zh) 2013-05-30 2016-01-06 普莱希科公司 用于激酶调节的化合物及其适应症
TWI648272B (zh) 2013-06-25 2019-01-21 美商必治妥美雅史谷比公司 經取代之四氫咔唑及咔唑甲醯胺化合物
AU2014302550A1 (en) 2013-06-25 2016-02-11 Bristol-Myers Squibb Company Carbazole carboxamide compounds useful as kinase inhibitors
SI3038622T1 (en) * 2013-08-28 2018-08-31 Medivation Technologies Llc Heterocyclic compounds and methods of use
GB2517988A (en) * 2013-09-09 2015-03-11 Redx Pharma Ltd Compounds
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
CA3000633C (en) 2014-10-14 2023-10-03 The Regents Of The University Of California Use of cdk9 and brd4 inhibitors to inhibit inflammation
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
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
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
CA3057969A1 (en) 2017-05-02 2018-11-08 Novartis Ag Combination therapy
WO2019133810A1 (en) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
WO2020124397A1 (en) * 2018-12-19 2020-06-25 Inventisbio Shanghai Ltd. C-terminal src kinase inhibitors
EP3969449B1 (en) 2019-05-13 2025-02-12 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
US20230303551A1 (en) * 2020-08-13 2023-09-28 Albert Einstein College Of Medicine N-cyclyl-sulfonamides useful for inhibiting raf
CN119053595A (zh) 2022-03-28 2024-11-29 尼坎治疗公司 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰氨基衍生物
CN119790053A (zh) 2022-06-08 2025-04-08 霖康疗法公司 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰胺衍生物
WO2025072462A1 (en) 2023-09-27 2025-04-03 Nikang Therapeutics, Inc. Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors

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WO2009115572A2 (en) * 2008-03-21 2009-09-24 Novartis Ag Novel heterocyclic compounds and uses therof
WO2009137391A2 (en) * 2008-05-06 2009-11-12 Smithkline Beecham Corporation Benzene sulfonamide thiazole and oxazole compounds

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AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
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Also Published As

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

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