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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English (en)
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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

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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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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 (24)

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AU2016372280A1 (en) * 2015-12-14 2018-07-12 Fundación Para La Investigación Médica Aplicada 2,4,6,7-tetrasubstituted quinoline compounds as inhibitors of DNA methyltransferases
IL307931A (en) * 2016-04-15 2023-12-01 Epizyme Inc Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors
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
WO2017201199A1 (en) * 2016-05-17 2017-11-23 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
WO2018119065A1 (en) 2016-12-22 2018-06-28 Asddr, Llc Use of histone methyltransferase inhibitors and histone deacetylase inhibitors for therapy of phelan-mcdermid syndrome
EP4063358B1 (en) * 2016-12-22 2024-05-22 Global Blood Therapeutics, Inc. Histone methyltransferase inhibitors
WO2018183923A1 (en) * 2017-03-31 2018-10-04 Epizyme, Inc. Methods of using ehmt2 inhibitors
WO2018195450A1 (en) 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
BR112019025770A2 (pt) 2017-06-09 2020-06-23 Global Blood Therapeutics, Inc. Compostos de azaindol como inibidores de histona metiltransferase
WO2018229139A1 (en) 2017-06-14 2018-12-20 Fundación Para La Investigación Médica Aplicada Novel compounds for use in cancer
WO2019036384A1 (en) 2017-08-15 2019-02-21 Global Blood Therapeutics, Inc. TRICYCLIC COMPOUNDS AS HISTONE INHIBITORS METHYLTRANSFERASES
ES3016407T3 (en) 2017-08-15 2025-05-09 Global Blood Therapeutics Inc Tricyclic compounds as histone methyl-transferase inhibitors
IL301746B2 (en) * 2017-10-18 2025-01-01 Epizyme Inc Amine-modified heterocyclic compounds as EHMT2 inhibitors, their salts and a method for their synthesis
CA3081946A1 (en) * 2017-10-18 2019-04-25 Epizyme, Inc. Methods of using ehmt2 inhibitors in preventing or treating blood disorders
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
WO2022013684A1 (en) 2020-07-11 2022-01-20 Pfizer Inc. Antiviral heteroaryl ketone derivatives
CA3188260A1 (en) * 2020-08-07 2022-02-10 Dimitrios Iliopoulos 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
CN120965666B (zh) * 2025-10-21 2026-02-17 四川大学华西医院 一种喹啉类化合物、制备方法和用途及其药物组合物

Family Cites Families (18)

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US6221882B1 (en) * 1997-07-03 2001-04-24 University Of Iowa Research Foundation Methods for inhibiting immunostimulatory DNA associated responses
EP1377554A1 (en) * 1999-06-16 2004-01-07 University Of Iowa Research Foundation Antagonism of immunostimulatory cpg-oligonucleotides by 4-aminoquinolines and other weak bases
US6440995B1 (en) * 1999-10-01 2002-08-27 Hoffman-La Roche Inc. Quinolin-4-yl derivatives
EP1088818B1 (en) * 1999-10-01 2004-11-03 F. Hoffmann-La Roche Ag Quinolin-4-yl derivatives
WO2003055866A1 (en) 2001-12-21 2003-07-10 Bayer Pharmaceuticals Corporation Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
US20040192583A1 (en) * 2002-12-19 2004-09-30 Satyanarayana Medicherla Treatment of obesity and associated conditions with TGF-beta inhibitors
EP1633718B1 (en) * 2003-06-17 2012-06-06 Millennium Pharmaceuticals, Inc. COMPOSITIONS AND METHODS FOR INHIBITING TGF-s
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
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
US7790746B2 (en) 2007-10-12 2010-09-07 Supergen, Inc. Quinoline derivatives for modulating DNA methylation
KR20140015121A (ko) * 2009-06-25 2014-02-06 암젠 인크 헤테로사이클릭 화합물 및 이의 용도
CA2770753C (en) * 2009-08-12 2019-01-15 Kyoto University Method for inducing differentiation of pluripotent stem cells into neural precursor cells
WO2011054433A1 (en) * 2009-11-07 2011-05-12 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
EP2828250B1 (en) * 2012-03-19 2021-03-10 Imperial College 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
CA2908482A1 (en) * 2013-03-01 2014-09-04 Fundacion Para La Investigacion Medica Aplicada Novel compounds as dual inhibitors of phosphodiesterases and histone deacetylases

Also Published As

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

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