CN103080107A - 作为蛋白激酶抑制剂的杂芳基化合物和组合物 - Google Patents

作为蛋白激酶抑制剂的杂芳基化合物和组合物 Download PDF

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Publication number
CN103080107A
CN103080107A CN201180040746XA CN201180040746A CN103080107A CN 103080107 A CN103080107 A CN 103080107A CN 201180040746X A CN201180040746X A CN 201180040746XA CN 201180040746 A CN201180040746 A CN 201180040746A CN 103080107 A CN103080107 A CN 103080107A
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CN
China
Prior art keywords
compound
chloro
pyrimidin
phenyl
mmol
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Pending
Application number
CN201180040746XA
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English (en)
Chinese (zh)
Inventor
A·M·马德拉
D·蓬
A·史密斯
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Novartis AG
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Novartis AG
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Publication of CN103080107A publication Critical patent/CN103080107A/zh
Pending legal-status Critical Current

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Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201180040746XA 2010-06-25 2011-06-23 作为蛋白激酶抑制剂的杂芳基化合物和组合物 Pending CN103080107A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US35860310P 2010-06-25 2010-06-25
US61/358,603 2010-06-25
US36853410P 2010-07-28 2010-07-28
US61/368,534 2010-07-28
PCT/EP2011/060561 WO2011161216A1 (en) 2010-06-25 2011-06-23 Heteroaryl compounds and compositions as protein kinase inhibitors

Publications (1)

Publication Number Publication Date
CN103080107A true CN103080107A (zh) 2013-05-01

Family

ID=44280749

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180040746XA Pending CN103080107A (zh) 2010-06-25 2011-06-23 作为蛋白激酶抑制剂的杂芳基化合物和组合物

Country Status (11)

Country Link
US (1) US20130096149A1 (https=)
EP (1) EP2585454A1 (https=)
JP (1) JP2013529619A (https=)
KR (2) KR20130048293A (https=)
CN (1) CN103080107A (https=)
AU (1) AU2011268906A1 (https=)
BR (1) BR112012032884A2 (https=)
CA (1) CA2803055A1 (https=)
EA (1) EA201201676A1 (https=)
MX (1) MX2012015100A (https=)
WO (1) WO2011161216A1 (https=)

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CN111320548A (zh) * 2020-04-24 2020-06-23 浦拉司科技（上海）有限责任公司 抗癌药物中间体2-氟-3-氨基苯甲酸甲酯的合成方法
CN114746419A (zh) * 2019-12-05 2022-07-12 国家医疗保健研究所 N-(3-(5-(嘧啶-4-基)噻唑-4-基)苯基)磺酰胺化合物及其用作braf抑制剂的用途
CN116724021A (zh) * 2021-01-20 2023-09-08 巴斯夫欧洲公司 多氟化芳基和杂芳基羧酰胺的合成

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WO2012113774A1 (en) 2011-02-24 2012-08-30 Nerviano Medical Sciences S.R.L. Thiazolylphenyl-benzenesulfonamido derivatives as kinase inhibitors
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
WO2014172639A1 (en) * 2013-04-19 2014-10-23 Ruga Corporation Raf kinase inhibitors
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
EP3515909A1 (en) 2016-09-23 2019-07-31 Cellipse Lim kinase inhibitors, pharmaceutical composition and method of use in limk-mediated diseases
ES2952265T3 (es) 2017-05-02 2023-10-30 Novartis Ag Terapia combinada que comprende un inhibidor de Raf y trametinib
WO2020124397A1 (en) * 2018-12-19 2020-06-25 Inventisbio Shanghai Ltd. C-terminal src kinase inhibitors
ES3025633T3 (en) 2019-05-13 2025-06-09 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
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

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US20090298815A1 (en) * 2008-05-06 2009-12-03 Jerry Leroy Adams Benzene Sulfonamide Thiazole and Oxazole Compounds
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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114746419A (zh) * 2019-12-05 2022-07-12 国家医疗保健研究所 N-(3-(5-(嘧啶-4-基)噻唑-4-基)苯基)磺酰胺化合物及其用作braf抑制剂的用途
CN114746419B (zh) * 2019-12-05 2023-10-24 国家医疗保健研究所 N-(3-(5-(嘧啶-4-基)噻唑-4-基)苯基)磺酰胺化合物及其用作braf抑制剂的用途
CN111320548A (zh) * 2020-04-24 2020-06-23 浦拉司科技（上海）有限责任公司 抗癌药物中间体2-氟-3-氨基苯甲酸甲酯的合成方法
CN111320548B (zh) * 2020-04-24 2022-10-18 浦拉司科技（上海）有限责任公司 抗癌药物中间体2-氟-3-氨基苯甲酸甲酯的合成方法
CN116724021A (zh) * 2021-01-20 2023-09-08 巴斯夫欧洲公司 多氟化芳基和杂芳基羧酰胺的合成

Also Published As

Publication number Publication date
EP2585454A1 (en) 2013-05-01
KR20140117684A (ko) 2014-10-07
WO2011161216A1 (en) 2011-12-29
CA2803055A1 (en) 2011-12-29
KR20130048293A (ko) 2013-05-09
AU2011268906A1 (en) 2013-01-31
BR112012032884A2 (pt) 2016-11-08
MX2012015100A (es) 2013-05-01
JP2013529619A (ja) 2013-07-22
US20130096149A1 (en) 2013-04-18
EA201201676A1 (ru) 2013-06-28

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Application publication date: 20130501