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

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

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JO3002B1 (ar) 2009-08-28 2016-09-05 Irm Llc مركبات و تركيبات كمثبطات كيناز بروتين
WO2011106298A1 (en) 2010-02-25 2011-09-01 Dana-Farber Cancer Institute, Inc. Braf mutations conferring resistance to braf inhibitors
US9498471B2 (en) 2011-10-20 2016-11-22 The Regents Of The University Of California Use of CDK9 inhibitors to reduce cartilage degradation
WO2013070996A1 (en) 2011-11-11 2013-05-16 Novartis Ag Method of treating a proliferative disease
EP2782557B1 (en) 2011-11-23 2018-09-12 Array Biopharma, Inc. Pharmaceutical formulations
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
CA2912568A1 (en) * 2013-05-30 2014-12-04 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
CN105473573B (zh) 2013-06-25 2018-03-16 百时美施贵宝公司 用作激酶抑制剂的咔唑甲酰胺化合物
UY35625A (es) 2013-06-25 2014-12-31 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos como inhibidores de quinasa
DK3038622T3 (en) * 2013-08-28 2018-07-16 Medivation Tech Llc HETEROCYCLIC RELATIONS AND PROCEDURES FOR 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
CA3037456A1 (en) 2016-09-19 2018-03-22 Novartis Ag Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
US11471538B2 (en) 2017-02-10 2022-10-18 INSERM (Institut National de la Santéet de la Recherche Medicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the MAPK pathway
IL270224B1 (en) 2017-05-02 2024-04-01 Novartis Ag Combination therapy employing trametinib and a defined raf inhibitor
EP3732285A1 (en) 2017-12-28 2020-11-04 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
EP4563150A3 (en) 2019-05-13 2025-07-23 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
US20230303551A1 (en) * 2020-08-13 2023-09-28 Albert Einstein College Of Medicine N-cyclyl-sulfonamides useful for inhibiting raf
US12331026B2 (en) 2022-03-28 2025-06-17 Nikang Therapeutics, Inc. Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors
WO2023240024A1 (en) 2022-06-08 2023-12-14 Nikang Therapeutics, Inc. Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors
WO2025072462A1 (en) 2023-09-27 2025-04-03 Nikang Therapeutics, Inc. Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors

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WO2009137391A2 (en) * 2008-05-06 2009-11-12 Smithkline Beecham Corporation Benzene sulfonamide thiazole and oxazole compounds

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Also Published As

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

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