CA2987978C - Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases - Google Patents

Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases Download PDF

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Publication number
CA2987978C
CA2987978C CA2987978A CA2987978A CA2987978C CA 2987978 C CA2987978 C CA 2987978C CA 2987978 A CA2987978 A CA 2987978A CA 2987978 A CA2987978 A CA 2987978A CA 2987978 C CA2987978 C CA 2987978C
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methoxy
substituents
optionally substituted
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French (fr)
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CA2987978A1 (en
Inventor
Xabier Aguirre Ena
Julen Oyarzabal Santamarina
Felipe Prosper Cardoso
Maria Obdulia Rabal Gracia
Juan Roberto Rodriguez Madoz
Edurne San Jose Eneriz
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Fundacion para la Investigacion Medica Aplicada
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Fundacion para la Investigacion Medica Aplicada
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CA2987978A 2014-06-16 2015-03-30 Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases Active CA2987978C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14382230.2 2014-06-16
EP14382230 2014-06-16
PCT/EP2015/056860 WO2015192981A1 (en) 2014-06-16 2015-03-30 Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases

Publications (2)

Publication Number Publication Date
CA2987978A1 CA2987978A1 (en) 2015-12-23
CA2987978C true CA2987978C (en) 2022-08-16

Family

ID=51136403

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2987978A Active CA2987978C (en) 2014-06-16 2015-03-30 Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases

Country Status (9)

Country Link
US (1) US9840500B2 (enExample)
EP (1) EP3154957B1 (enExample)
JP (1) JP6527534B2 (enExample)
CN (1) CN106536509B (enExample)
AU (1) AU2015276537B2 (enExample)
CA (1) CA2987978C (enExample)
DK (1) DK3154957T3 (enExample)
ES (1) ES2769648T3 (enExample)
WO (1) WO2015192981A1 (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019501904A (ja) * 2015-12-14 2019-01-24 ファンダシオン パラ ラ インベスティガシオン メディカ アプリカダFundacion Para La Investigasion Medica Aplicada Dnaメチルトランスフェラーゼの阻害剤としての2,4,6,7−四置換キノリン化合物
LT3442947T (lt) * 2016-04-15 2023-09-11 Epizyme, Inc. Aminu pakeisti arilo arba heteroarilo junginiai, kaip ehmt1 ir ehmt2 inhibitoriai
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
US11278550B2 (en) 2016-05-17 2022-03-22 Duke University Compositions and methods for the treatment of Prader-Willi syndrome
US11433068B2 (en) * 2016-09-08 2022-09-06 The General Hospital Corporation Treatment of cancers having alterations within the SWI/SNF chromatin remodeling complex
WO2018119208A1 (en) 2016-12-22 2018-06-28 Global Blood Therapeutics, Inc. Histone methyltransferase inhibitors
US11103549B2 (en) 2016-12-22 2021-08-31 Asddr, Llc Use of histone methyltransferase inhibitors and histone deacetylase inhibitors for therapy of Phelan-McDermid Syndrome
EP3600318A4 (en) * 2017-03-31 2021-06-09 Epizyme, Inc. METHOD OF USING EHMT2 INHIBITORS
CA3060416A1 (en) 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
ES2949402T3 (es) 2017-06-09 2023-09-28 Global Blood Therapeutics Inc Compuestos de azaindol como inhibidores de la histona metiltransferasa
WO2018229139A1 (en) 2017-06-14 2018-12-20 Fundación Para La Investigación Médica Aplicada Novel compounds for use in cancer
US11584734B2 (en) 2017-08-15 2023-02-21 Global Blood Therapeutics, Inc. Tricyclic compounds as histone methyltransferase inhibitors
ES3016407T3 (en) 2017-08-15 2025-05-09 Global Blood Therapeutics Inc Tricyclic compounds as histone methyl-transferase inhibitors
US20210260040A1 (en) * 2017-10-18 2021-08-26 Epizyme, Inc. Methods of using ehmt2 inhibitors in treating or preventing blood disorders
AU2018353122B2 (en) * 2017-10-18 2023-11-23 Epizyme, Inc. Amine-substituted heterocyclic compounds as EHMT2 inhibitors, salts thereof, and methods of synthesis thereof
EP3807248A4 (en) * 2018-05-29 2021-10-27 Council of Scientific and Industrial Research BICYCLIC TOPOISOMERASE I INHIBITOR COMPOUNDS, THEIR PREPARATION AND USE
WO2019243236A1 (en) 2018-06-18 2019-12-26 Fundación Para La Investigación Médica Aplicada New anticancer drug combinations
CN112390791B (zh) * 2019-08-14 2023-08-01 复旦大学 一类dna甲基转移酶1荧光探针及其用途
IL300351A (en) * 2020-08-07 2023-04-01 Athos Therapeutics Inc Small molecules for the treatment of autoimmune diseases and cancer
US11351149B2 (en) 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds
CN115160294B (zh) * 2022-06-27 2023-09-29 中山大学 一种G9a/GLP共价抑制剂及其制备方法及应用

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DE69840025D1 (de) 1997-07-03 2008-10-30 Donald E Macfarlane Assoziierter antworten
AU6051800A (en) * 1999-06-16 2001-01-02 University Of Iowa Research Foundation, The Antagonism of immunostimulatory cpg-oligonucleotides by 4-aminoquinolines and other weak bases
EP1088818B1 (en) 1999-10-01 2004-11-03 F. Hoffmann-La Roche Ag Quinolin-4-yl derivatives
US6440995B1 (en) * 1999-10-01 2002-08-27 Hoffman-La Roche Inc. Quinolin-4-yl derivatives
AU2002361846A1 (en) * 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
AU2003297460A1 (en) * 2002-12-19 2004-07-14 Scios, Inc. TREATMENT OF OBESITY AND ASSOCIATED CONDITIONS WITH TGF-Beta INHIBITORS
WO2004112710A2 (en) * 2003-06-17 2004-12-29 Millennium Pharmaceuticals, Inc. COMPOSITIONS AND METHODS FOR INHIBITING TGF-ß
CN101535295A (zh) * 2006-10-12 2009-09-16 休普基因公司 用于调节dna甲基化的喹啉衍生物
JP2010506856A (ja) 2006-10-12 2010-03-04 スーパージェン, インコーポレイテッド Dnaメチル化を調整するためのキノリン誘導体
US7790746B2 (en) 2007-10-12 2010-09-07 Supergen, Inc. Quinoline derivatives for modulating DNA methylation
WO2010151791A1 (en) * 2009-06-25 2010-12-29 Amgen Inc. Heterocyclic compounds and their uses
AU2010283229B2 (en) * 2009-08-12 2015-04-02 Kyoto University Method for inducing differentiation of pluripotent stem cells into neural precursor cells
US8987301B2 (en) * 2009-11-07 2015-03-24 Merck Patent Gmbh Heteroarylaminoquinolines as TGF-beta receptor kinase inhibitors
US20140357594A1 (en) 2011-10-24 2014-12-04 Glaxosmithkline Intellectual Property (No.2) Limited New compounds
US9932317B2 (en) * 2012-03-19 2018-04-03 Imperial Innovations Limited Quinazoline compounds and their use in therapy
EP2730558A1 (en) 2012-11-08 2014-05-14 Ikerchem, S.L. Indole derivatives, pharmaceutical compositions containing such indoles and their use as DNA methylation modulators
US9264060B2 (en) * 2012-11-09 2016-02-16 St-Ericsson Sa Analog to digital conversion method with offset tracking and correction and analog to digital converter implementing the same
EP2961741B1 (en) * 2013-03-01 2017-04-05 Fundacion para la Investigacion Medica Aplicada Novel compounds as dual inhibitors of phosphodiesterases and histone deacetylases

Also Published As

Publication number Publication date
JP6527534B2 (ja) 2019-06-05
DK3154957T3 (da) 2020-02-17
AU2015276537B2 (en) 2019-03-14
US9840500B2 (en) 2017-12-12
JP2017524668A (ja) 2017-08-31
EP3154957A1 (en) 2017-04-19
ES2769648T3 (es) 2020-06-26
WO2015192981A1 (en) 2015-12-23
EP3154957B1 (en) 2019-11-20
US20170121316A1 (en) 2017-05-04
CA2987978A1 (en) 2015-12-23
AU2015276537A1 (en) 2017-01-05
CN106536509B (zh) 2020-06-09
CN106536509A (zh) 2017-03-22

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