AU2015276537B2 - 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
AU2015276537B2
AU2015276537B2 AU2015276537A AU2015276537A AU2015276537B2 AU 2015276537 B2 AU2015276537 B2 AU 2015276537B2 AU 2015276537 A AU2015276537 A AU 2015276537A AU 2015276537 A AU2015276537 A AU 2015276537A AU 2015276537 B2 AU2015276537 B2 AU 2015276537B2
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amino
methoxy
quinolyl
phenyl
optionally substituted
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AU2015276537A1 (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
    • 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
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (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)
  • 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)
AU2015276537A 2014-06-16 2015-03-30 Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases Active AU2015276537B2 (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
AU2015276537A1 AU2015276537A1 (en) 2017-01-05
AU2015276537B2 true AU2015276537B2 (en) 2019-03-14

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2015276537A Active AU2015276537B2 (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 (OSRAM)
EP (1) EP3154957B1 (OSRAM)
JP (1) JP6527534B2 (OSRAM)
CN (1) CN106536509B (OSRAM)
AU (1) AU2015276537B2 (OSRAM)
CA (1) CA2987978C (OSRAM)
DK (1) DK3154957T3 (OSRAM)
ES (1) ES2769648T3 (OSRAM)
WO (1) WO2015192981A1 (OSRAM)

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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
JP7041070B2 (ja) * 2016-04-15 2022-03-23 エピザイム，インコーポレイティド Ｅｈｍｔ１およびｅｈｍｔ２阻害剤としてのアミン置換アリールまたはヘテロアリール化合物
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
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
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
ES2910108T3 (es) * 2016-12-22 2022-05-11 Global Blood Therapeutics Inc Inhibidores de la histona metiltransferasa
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
AU2018243749A1 (en) * 2017-03-31 2019-11-21 Epizyme, Inc. Methods of using EHMT2 inhibitors
CN110621316B (zh) 2017-04-21 2024-01-26 Epizyme股份有限公司 用ehmt2抑制剂进行的组合疗法
MX2019014759A (es) 2017-06-09 2020-02-12 Global Blood Therapeutics Inc Compuestos de azaindol como inhibidores de metiltransferasa de histona.
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
CN111372927A (zh) 2017-08-15 2020-07-03 全球血液疗法股份有限公司 作为组蛋白甲基转移酶抑制剂的三环化合物
JP2021500334A (ja) * 2017-10-18 2021-01-07 エピザイム，インコーポレイティド Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法
KR20200101332A (ko) * 2017-10-18 2020-08-27 에피자임, 인코포레이티드 혈액 장애 예방 또는 치료에 있어서의 ehmt2 저해제의 사용 방법
US12172991B2 (en) * 2018-05-29 2024-12-24 Council Of Scientific & Industrial Research Bicycle topoisomerase i inhibiting compounds, process for preparation and use thereof
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
WO2022031939A1 (en) * 2020-08-07 2022-02-10 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
CN120965666A (zh) * 2025-10-21 2025-11-18 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

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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
WO2011054433A1 (en) * 2009-11-07 2011-05-12 Merck Patent Gmbh Heteroarylaminoquinolines as tgf-beta receptor kinase inhibitors

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UY32742A (es) * 2009-06-25 2010-12-31 Amgen Inc Compuestos heterocíclicos y sus usos
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Patent Citations (3)

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EP1088818A1 (en) * 1999-10-01 2001-04-04 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
WO2011054433A1 (en) * 2009-11-07 2011-05-12 Merck Patent Gmbh Heteroarylaminoquinolines as tgf-beta receptor kinase inhibitors

Also Published As

Publication number Publication date
US20170121316A1 (en) 2017-05-04
JP2017524668A (ja) 2017-08-31
CA2987978A1 (en) 2015-12-23
CN106536509A (zh) 2017-03-22
ES2769648T3 (es) 2020-06-26
AU2015276537A1 (en) 2017-01-05
CN106536509B (zh) 2020-06-09
DK3154957T3 (da) 2020-02-17
CA2987978C (en) 2022-08-16
WO2015192981A1 (en) 2015-12-23
JP6527534B2 (ja) 2019-06-05
EP3154957B1 (en) 2019-11-20
EP3154957A1 (en) 2017-04-19
US9840500B2 (en) 2017-12-12

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