AU2017359276B2 - Selective inhibitors of genotoxic stress-induced IKK/NF-κΒ pathways - Google Patents

Selective inhibitors of genotoxic stress-induced IKK/NF-κΒ pathways Download PDF

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AU2017359276B2
AU2017359276B2 AU2017359276A AU2017359276A AU2017359276B2 AU 2017359276 B2 AU2017359276 B2 AU 2017359276B2 AU 2017359276 A AU2017359276 A AU 2017359276A AU 2017359276 A AU2017359276 A AU 2017359276A AU 2017359276 B2 AU2017359276 B2 AU 2017359276B2
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alkyl
halogen
alkoxy
amine
methoxy
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AU2017359276A1 (en
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Peter Lindemann
Marc Nazare
Silke RADETZKI
Claus Scheidereit
Jens Peter VON KRIES
Michael WILLENBROCK
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Max Delbrueck Centrum fuer Molekulare in der Helmholtz Gemeinschaft
Forschungsverbund Berlin FVB eV
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Max Delbrueck Centrum fuer Molekulare in der Helmholtz Gemeinschaft
Forschungsverbund Berlin FVB eV
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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
AU2017359276A 2016-11-14 2017-11-14 Selective inhibitors of genotoxic stress-induced IKK/NF-κΒ pathways Active AU2017359276B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16198731.8 2016-11-14
EP16198731.8A EP3321264A1 (en) 2016-11-14 2016-11-14 Selective inhibitors of genotoxic stress-induced ikk/nf-kb pathways
PCT/EP2017/079181 WO2018087389A1 (en) 2016-11-14 2017-11-14 SELECTIVE INHIBITORS OF GENOTOXIC STRESS-INDUCED IKK/NF-kB PATHWAYS

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AU2017359276A1 AU2017359276A1 (en) 2019-05-16
AU2017359276B2 true AU2017359276B2 (en) 2022-02-17

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AU2017359276A Active AU2017359276B2 (en) 2016-11-14 2017-11-14 Selective inhibitors of genotoxic stress-induced IKK/NF-κΒ pathways

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US (1) US11028084B2 (enExample)
EP (2) EP3321264A1 (enExample)
JP (2) JP7307677B2 (enExample)
CN (1) CN109963850A (enExample)
AU (1) AU2017359276B2 (enExample)
CA (1) CA3041832A1 (enExample)
WO (1) WO2018087389A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3321264A1 (en) * 2016-11-14 2018-05-16 Max-Delbrück-Centrum für Molekulare Medizin in der Helmholtz-Gemeinschaft Selective inhibitors of genotoxic stress-induced ikk/nf-kb pathways
CN113913515A (zh) * 2020-07-10 2022-01-11 上海吉凯基因医学科技股份有限公司 人eme1基因的用途及相关产品
CN111781358A (zh) * 2020-07-13 2020-10-16 张瑜 Xab2蛋白作为卵巢癌预后和/或预测铂类耐药标志物
CN116829560A (zh) * 2020-12-14 2023-09-29 金奥克斯治疗有限公司 催产素受体调节剂
AU2023397973A1 (en) * 2022-12-13 2025-07-03 Flare Therapeutics Inc. Compounds and composition for targeting tp53-y220c mutants
EP4467141A1 (en) 2023-05-24 2024-11-27 Max-Delbrück-Centrum für Molekulare Medizin in der Helmholtz-Gemeinschaft Pyrazolo-quinolines as selective inhibitors of genotoxic stress-induced ikk/nf- kb pathways for cancer therapy

Citations (9)

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WO2004106335A1 (en) * 2003-06-02 2004-12-09 Xinjiang Huashidan Pharmaceutical Research Co., Ltd Harmine derivatives, intermediates used in their preparation, preparation processes and use thereof
WO2007097981A2 (en) * 2006-02-16 2007-08-30 Millennium Pharmaceuticals, Inc. Alpha carbolines and uses thereof
WO2007119600A1 (en) * 2006-03-23 2007-10-25 Otsuka Pharmaceutical Co., Ltd. Carbazole compound
WO2009121063A2 (en) * 2008-03-28 2009-10-01 Altiris Therapeutics Chemokine receptor modulators
WO2011011186A2 (en) * 2009-07-22 2011-01-27 The Board Of Trustees Of The University Of Illinois Hdac inhibitors and therapeutic methods using the same
CN102146080A (zh) * 2010-02-10 2011-08-10 新疆华世丹药业股份有限公司 β-咔啉碱衍生物类化合物及其应用
US20120039804A1 (en) * 2010-06-04 2012-02-16 Philippe Diaz Novel Tricyclic Modulators of Cannabinoid Receptors
WO2013064460A1 (en) * 2011-11-02 2013-05-10 Bayer Intellectual Property Gmbh Compounds with nematicidal activity
WO2014041125A1 (en) * 2012-09-13 2014-03-20 Baden-Württemberg Stiftung Gmbh Specific inhibitors of protein p21 as therapeutic agents

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US3663559A (en) * 1969-12-03 1972-05-16 Union Carbide Corp Preparation of oxo-furo-pyridines from furylvinyl isocyanates
CA2932121A1 (en) * 2007-11-30 2009-06-11 Newlink Genetics Corporation Ido inhibitors
CA2785233C (en) * 2009-12-28 2018-10-09 Audiocure Pharma Gmbh .beta.-carbolines for treatment of hearing damages and vertigo
CN111012779A (zh) * 2011-10-25 2020-04-17 新疆华世丹药物研究有限责任公司 去氢骆驼蓬碱衍生物在制备抗菌药物中的应用
EP3321264A1 (en) 2016-11-14 2018-05-16 Max-Delbrück-Centrum für Molekulare Medizin in der Helmholtz-Gemeinschaft Selective inhibitors of genotoxic stress-induced ikk/nf-kb pathways

Patent Citations (10)

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Publication number Priority date Publication date Assignee Title
WO2004106335A1 (en) * 2003-06-02 2004-12-09 Xinjiang Huashidan Pharmaceutical Research Co., Ltd Harmine derivatives, intermediates used in their preparation, preparation processes and use thereof
EP1634881A1 (en) * 2003-06-02 2006-03-15 Xinjiang Huashidan Pharmaceutical Research Co., Ltd. Harmine derivatives, intermediates used in their preparation, preparation processes and use thereof
WO2007097981A2 (en) * 2006-02-16 2007-08-30 Millennium Pharmaceuticals, Inc. Alpha carbolines and uses thereof
WO2007119600A1 (en) * 2006-03-23 2007-10-25 Otsuka Pharmaceutical Co., Ltd. Carbazole compound
WO2009121063A2 (en) * 2008-03-28 2009-10-01 Altiris Therapeutics Chemokine receptor modulators
WO2011011186A2 (en) * 2009-07-22 2011-01-27 The Board Of Trustees Of The University Of Illinois Hdac inhibitors and therapeutic methods using the same
CN102146080A (zh) * 2010-02-10 2011-08-10 新疆华世丹药业股份有限公司 β-咔啉碱衍生物类化合物及其应用
US20120039804A1 (en) * 2010-06-04 2012-02-16 Philippe Diaz Novel Tricyclic Modulators of Cannabinoid Receptors
WO2013064460A1 (en) * 2011-11-02 2013-05-10 Bayer Intellectual Property Gmbh Compounds with nematicidal activity
WO2014041125A1 (en) * 2012-09-13 2014-03-20 Baden-Württemberg Stiftung Gmbh Specific inhibitors of protein p21 as therapeutic agents

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ALMERICO, A. M. et al., "A3 adenosine receptor: Homology modelling and 3D-QSAR studies", J. Mol. Graphics Modell., 2013, vol. 42, pages 60-72 *
CHEN, Q. et al., "Antitumor and neurotoxic effects of novel harmine derivatives and structure-activity relationship analysis", Int. J. Cancer, 2005, vol. 114, no. 5, pages 675-682 *
CLEMO, G. R. et al., "The Constitution of Yohimbine. Part II", J. Chem. Soc., 1949, pages 487-492 *
DU, H. et al., "Synthesis and biological evaluation of N9-substituted harmine derivatives as potential anticancer agents", Bioorg. Med. Chem. Lett., July 2016, vol. 26, no. 16, pages 4015-4019 *
HSU, M. et al., "Cell apoptosis induced by a synthetic carbazole compound LCY-2-CHO is mediated through activation of caspase and mitochondrial pathways", Biochem. Pharmacol., 2005, vol. 70, no. 1, pages 102-112 *
LAMCHOURI, F. et al., "Quantitative structure-activity relationship of antitumor and neurotoxic [beta]-carbolines alkaloids: nine harmine derivatives", Res. Chem. Intermed., 2012, vol. 39, no. 5, pages 2219-2236 *
LIN, Y. et al., Eur. J. Med. Chem., January 2016, vol. 110, pages 98-114 *
MANDOUR, A. H. et al., "Synthesis, anti-inflammatory, analgesic and anticonvulsant activities of 1,8-dihydro-1-aryl-8-alkyl pyrazolo(3,4-b)indoles", Acta Pharm., 2010, vol. 60, no. 1, pages 73-88 *
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SILVA, C. M. B. L. et al., Chem. Pharm. Bull., 2012, vol. 60, no. 11, pages 1372-1379 *
ZHANG, G. et al., "Synthesis and structure-activity relationships of N2-alkylated quaternary beta-carbolines as novel antitumor agents", Eur. J. Med. Chem., 2013, vol. 65, pages 21-31 *

Also Published As

Publication number Publication date
JP2019535709A (ja) 2019-12-12
EP3538529B1 (en) 2022-01-19
JP7701403B2 (ja) 2025-07-01
CA3041832A1 (en) 2018-05-17
EP3538529A1 (en) 2019-09-18
AU2017359276A1 (en) 2019-05-16
US11028084B2 (en) 2021-06-08
US20190276452A1 (en) 2019-09-12
WO2018087389A1 (en) 2018-05-17
JP2023101521A (ja) 2023-07-21
JP7307677B2 (ja) 2023-07-12
CN109963850A (zh) 2019-07-02
EP3321264A1 (en) 2018-05-16

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