JP6527534B2 - ヒストンメチルトランスフェラーゼ及びｄｎａメチルトランスフェラーゼの二重阻害剤としての新規化合物 - Google Patents

ヒストンメチルトランスフェラーゼ及びｄｎａメチルトランスフェラーゼの二重阻害剤としての新規化合物 Download PDF

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JP6527534B2
JP6527534B2 JP2016573017A JP2016573017A JP6527534B2 JP 6527534 B2 JP6527534 B2 JP 6527534B2 JP 2016573017 A JP2016573017 A JP 2016573017A JP 2016573017 A JP2016573017 A JP 2016573017A JP 6527534 B2 JP6527534 B2 JP 6527534B2
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ring
amino
methoxy
quinolyl
substituents
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JP2017524668A (ja
JP2017524668A5 (enExample
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エナ，ザビエル アギーレ
エナ，ザビエル アギーレ
サンタマリーナ，フレン オヤルサバル
サンタマリーナ，フレン オヤルサバル
カルドーソ，フェリペ プロスペル
カルドーソ，フェリペ プロスペル
グラシア，マリア オブドゥリア ラバル
グラシア，マリア オブドゥリア ラバル
マドス，フアン ロベルト ロドリゲス
マドス，フアン ロベルト ロドリゲス
ホセ エネリス，エドゥルネ サン
ホセ エネリス，エドゥルネ サン
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Fundacion Para La Investigasion Medica Aplicada
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    • 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
    • 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

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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)
JP2016573017A 2014-06-16 2015-03-30 ヒストンメチルトランスフェラーゼ及びｄｎａメチルトランスフェラーゼの二重阻害剤としての新規化合物 Active JP6527534B2 (ja)

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 (3)

Publication Number Publication Date
JP2017524668A JP2017524668A (ja) 2017-08-31
JP2017524668A5 JP2017524668A5 (enExample) 2018-04-12
JP6527534B2 true JP6527534B2 (ja) 2019-06-05

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JP2016573017A Active JP6527534B2 (ja) 2014-06-16 2015-03-30 ヒストンメチルトランスフェラーゼ及びｄｎａメチルトランスフェラーゼの二重阻害剤としての新規化合物

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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)

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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
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
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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
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CA2987978C (en) 2022-08-16
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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