CN102770426B - 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
CN102770426B
CN102770426B CN201180008135.7A CN201180008135A CN102770426B CN 102770426 B CN102770426 B CN 102770426B CN 201180008135 A CN201180008135 A CN 201180008135A CN 102770426 B CN102770426 B CN 102770426B
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CN
China
Prior art keywords
alkyl
base
compound
halogen
methyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
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CN201180008135.7A
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English (en)
Chinese (zh)
Other versions
CN102770426A (zh
Inventor
J·E·泰卢
S·潘
Y·万
Y·谢
X·王
S·黄
Z·刘
Q·张
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis International Pharmaceutical Ltd
Novartis AG
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IRM LLC
Novartis AG
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Publication of CN102770426A publication Critical patent/CN102770426A/zh
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Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201180008135.7A 2010-02-05 2011-02-04 作为蛋白激酶抑制剂的化合物和组合物 Expired - Fee Related CN102770426B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30181010P 2010-02-05 2010-02-05
US61/301,810 2010-02-05
PCT/US2011/023812 WO2011097526A1 (en) 2010-02-05 2011-02-04 Compounds and compositions as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
CN102770426A CN102770426A (zh) 2012-11-07
CN102770426B true CN102770426B (zh) 2016-03-23

Family

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Family Applications (1)

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CN201180008135.7A Expired - Fee Related CN102770426B (zh) 2010-02-05 2011-02-04 作为蛋白激酶抑制剂的化合物和组合物

Country Status (5)

Country Link
US (1) US9181238B2 (enExample)
EP (1) EP2531498B1 (enExample)
JP (1) JP5728499B2 (enExample)
CN (1) CN102770426B (enExample)
WO (1) WO2011097526A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011097526A1 (en) * 2010-02-05 2011-08-11 Irm Llc Compounds and compositions as protein kinase inhibitors
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
CN105283454B (zh) * 2013-04-12 2019-10-29 阿萨纳生物科技有限责任公司 作为ras/raf/mek/erk和pi3k/akt/pten/mtor通路双重抑制剂的喹唑啉和氮杂喹唑啉
WO2014179498A1 (en) * 2013-04-30 2014-11-06 Genentech, Inc. Serine/threonine kinase inhibitors
WO2014206344A1 (en) 2013-06-28 2014-12-31 Beigene, Ltd. Fused tricyclic amide compounds as multiple kinase inhibitors
EP3579872A1 (en) 2017-02-10 2019-12-18 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
CA3086765A1 (en) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
TWI831829B (zh) 2018-09-12 2024-02-11 美商建南德克公司 苯氧基-吡啶基-嘧啶化合物及使用方法
CN109078189A (zh) * 2018-10-23 2018-12-25 黄泳华 含有蛋白激酶抑制剂与白藜芦醇的组合物
CN109157660A (zh) * 2018-10-28 2019-01-08 黄泳华 含有蛋白激酶抑制剂与西地那非的组合物
WO2020142612A1 (en) * 2019-01-03 2020-07-09 Genentech, Inc. Pyrido-pyrimidinone and pteridinone compounds as inhibitors of endoribonuclease inositol requiring enzyme i (ire i alpha) for the treatment of cancer diseases.
IL310931A (en) * 2021-09-10 2024-04-01 Black Diamond Therapeutics Inc 6-aza-quinoline derivatives and related uses

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1341098A (zh) * 1999-01-13 2002-03-20 拜尔有限公司 用ω－羧基芳基取代的二苯脲作为raf激酶抑制剂
CN1863774A (zh) * 2003-10-08 2006-11-15 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物

Family Cites Families (15)

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US6358932B1 (en) 1994-05-31 2002-03-19 Isis Pharmaceticals, Inc. Antisense oligonucleotide inhibition of raf gene expression
US6391636B1 (en) 1994-05-31 2002-05-21 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
US6037136A (en) 1994-10-24 2000-03-14 Cold Spring Harbor Laboratory Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto
US5717100A (en) 1995-10-06 1998-02-10 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
IL127210A0 (en) 1996-05-23 1999-09-22 Applied Research Systems Compounds inhibiting the binding of raf-1 or 13-3-3 proteins to the beta-chain of il-2 pharmaceutical compositions containing them and their use
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
US6187799B1 (en) 1997-05-23 2001-02-13 Onyx Pharmaceuticals Inhibition of raf kinase activity using aryl ureas
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
US6204467B1 (en) 1998-03-24 2001-03-20 Ford Global Technologies, Inc. Method and apparatus for resistive welding
US7351834B1 (en) 1999-01-13 2008-04-01 Bayer Pharmaceuticals Corporation ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US6756410B2 (en) 2000-08-30 2004-06-29 Kamal D. Mehta Induction of LDL receptor expression by extracellular-signal regulated kinase, ERK-1/2
WO2007067444A1 (en) 2005-12-08 2007-06-14 Millennium Pharmaceuticals, Inc. Bicyclic compounds with kinase inhibitory activity
EP2076513A1 (en) 2006-10-20 2009-07-08 Irm Llc Compositions and methods for modulating c-kit and pdgfr receptors
WO2011097526A1 (en) * 2010-02-05 2011-08-11 Irm Llc Compounds and compositions as protein kinase inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1341098A (zh) * 1999-01-13 2002-03-20 拜尔有限公司 用ω－羧基芳基取代的二苯脲作为raf激酶抑制剂
CN1863774A (zh) * 2003-10-08 2006-11-15 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物

Also Published As

Publication number Publication date
US9181238B2 (en) 2015-11-10
JP5728499B2 (ja) 2015-06-03
EP2531498A1 (en) 2012-12-12
US20130143899A1 (en) 2013-06-06
JP2013518904A (ja) 2013-05-23
WO2011097526A1 (en) 2011-08-11
EP2531498B1 (en) 2016-07-13
CN102770426A (zh) 2012-11-07

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C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C41 Transfer of patent application or patent right or utility model
TA01 Transfer of patent application right

Effective date of registration: 20160104

Address after: Basel, Switzerland

Applicant after: NOVARTIS AG

Address before: British Bermuda, Hamilton

Applicant before: Novartis international pharmaceuticals Ltd.

Applicant before: Novartis AG

Effective date of registration: 20160104

Address after: British Bermuda, Hamilton

Applicant after: Novartis international pharmaceuticals Ltd.

Applicant after: NOVARTIS AG

Address before: British Bermuda, Hamilton

Applicant before: IRM LLC

Applicant before: Novartis AG

C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20160323

Termination date: 20190204

CF01 Termination of patent right due to non-payment of annual fee