JP2016520645A - Zesteホモログ2エンハンサー阻害剤 - Google Patents

Zesteホモログ2エンハンサー阻害剤 Download PDF

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Publication number
JP2016520645A
JP2016520645A JP2016517732A JP2016517732A JP2016520645A JP 2016520645 A JP2016520645 A JP 2016520645A JP 2016517732 A JP2016517732 A JP 2016517732A JP 2016517732 A JP2016517732 A JP 2016517732A JP 2016520645 A JP2016520645 A JP 2016520645A
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JP
Japan
Prior art keywords
alkyl
methyl
amino
pyrido
dione
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Ceased
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JP2016517732A
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English (en)
Japanese (ja)
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JP2016520645A5 (enExample
Inventor
スティーブン、デイビッド、ナイト
ルイス、ビンセント、ラフランス、ザ、サード
ケネス、シー.マクナルティ
ステュアート、ポール、ロメリル
マーク、アンドリュー、シーフェルド
デイビッド、ティー.フォスベナー
ブライアン、ダブリュ.キング
メイ、リー
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GlaxoSmithKline Intellectual Property No 2 Ltd
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GlaxoSmithKline Intellectual Property No 2 Ltd
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Publication of JP2016520645A publication Critical patent/JP2016520645A/ja
Publication of JP2016520645A5 publication Critical patent/JP2016520645A5/ja
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2016517732A 2013-06-06 2014-06-06 Zesteホモログ2エンハンサー阻害剤 Ceased JP2016520645A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361831649P 2013-06-06 2013-06-06
US61/831,649 2013-06-06
US201461949399P 2014-03-07 2014-03-07
US61/949,399 2014-03-07
US201461977666P 2014-04-10 2014-04-10
US61/977,666 2014-04-10
PCT/IB2014/062025 WO2014195919A1 (en) 2013-06-06 2014-06-06 Enhancer of zeste homolog 2 inhibitors

Publications (2)

Publication Number Publication Date
JP2016520645A true JP2016520645A (ja) 2016-07-14
JP2016520645A5 JP2016520645A5 (enExample) 2017-07-13

Family

ID=50980343

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016517732A Ceased JP2016520645A (ja) 2013-06-06 2014-06-06 Zesteホモログ2エンハンサー阻害剤

Country Status (10)

Country Link
US (1) US20160122342A1 (enExample)
EP (1) EP3004096A1 (enExample)
JP (1) JP2016520645A (enExample)
KR (1) KR20160018594A (enExample)
CN (1) CN105452246A (enExample)
AU (1) AU2014276417B2 (enExample)
BR (1) BR112015030515A2 (enExample)
CA (1) CA2914414A1 (enExample)
RU (1) RU2015155595A (enExample)
WO (1) WO2014195919A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021501191A (ja) * 2017-11-01 2021-01-14 シージャーズォアン サガシティ ニュー ドラッグ デベロップメント カンパニー リミテッド Wee1阻害剤としての大環状化合物及びその使用
JP2022505756A (ja) * 2018-10-26 2022-01-14 シージャーヂュアン・サガシティー・ニュー・ドラッグ・デヴェロップメント・カンパニー・リミテッド Wee1阻害剤としてのピリミドピラゾロン類誘導体及びその使用

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ706836A (en) 2012-10-15 2019-02-22 Epizyme Inc Methods of treating cancer
UY36758A (es) * 2015-06-30 2016-12-30 Glaxosmithkline Ip No 2 Ltd Inhibidores del potenciador del homólogo zeste 2
US10493076B2 (en) 2015-08-24 2019-12-03 Epizyme, Inc. Method for treating cancer
EP3370725A4 (en) * 2015-11-06 2019-07-03 Epizyme, Inc. PEDIATRIC DOSAGE FOR THE TREATMENT OF CANCER WITH AN EZH2 INHIBITOR
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
CN108117564B (zh) * 2017-12-20 2020-09-04 苏州百灵威超精细材料有限公司 一种制备穴醚222的工艺方法
HUE059536T2 (hu) 2018-01-31 2022-11-28 Mirati Therapeutics Inc PRC2-inhibitorok
CN110229151B (zh) * 2018-03-06 2021-09-10 上海海和药物研究开发股份有限公司 吲嗪类化合物、其制备方法及用途
CN112399857A (zh) 2018-07-09 2021-02-23 盲人庇护基金会 Prc2亚单位的抑制治疗眼失调
EP3831822A4 (en) * 2018-07-27 2022-03-23 Suzhou Sinovent Pharmaceuticals Co., Ltd. POLYSUBSTITUTED BENZENE COMPOUND AND METHOD FOR PREPARING IT AND ITS USE
EP3959214A1 (en) 2019-04-22 2022-03-02 Mirati Therapeutics, Inc. Naphthyridine derivatives as prc2 inhibitors
CN111909157B (zh) * 2019-05-07 2023-02-03 南京药石科技股份有限公司 Ezh2抑制剂及其用途
CN114269748A (zh) 2019-06-05 2022-04-01 米拉蒂医疗股份有限公司 作为用于治疗癌症的PRC2抑制剂的咪唑并[1,2-c]嘧啶衍生物

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012075080A1 (en) * 2010-12-01 2012-06-07 Glaxosmithkline Llc Indoles
WO2012142504A1 (en) * 2011-04-13 2012-10-18 Epizyme, Inc. Aryl-or heteroaryl-substituted benzene compounds
WO2012156756A2 (en) * 2011-05-19 2012-11-22 Centro Nacional De Investigaciones Oncológicas (Cnio) New compounds
WO2013173441A2 (en) * 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102970869B (zh) * 2010-05-07 2014-07-16 葛兰素史密斯克莱有限责任公司 吲哚

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012075080A1 (en) * 2010-12-01 2012-06-07 Glaxosmithkline Llc Indoles
WO2012142504A1 (en) * 2011-04-13 2012-10-18 Epizyme, Inc. Aryl-or heteroaryl-substituted benzene compounds
WO2012156756A2 (en) * 2011-05-19 2012-11-22 Centro Nacional De Investigaciones Oncológicas (Cnio) New compounds
WO2013173441A2 (en) * 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
VERMA, SHARAD K. ET AL.: "Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase", ACS MEDICINAL CHEMISTRY LETTERS, vol. 3, no. 12, JPN6018014135, 2012, pages 1091 - 1096, ISSN: 0003780936 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021501191A (ja) * 2017-11-01 2021-01-14 シージャーズォアン サガシティ ニュー ドラッグ デベロップメント カンパニー リミテッド Wee1阻害剤としての大環状化合物及びその使用
US11613545B2 (en) 2017-11-01 2023-03-28 Wuxi Biocity Biopharmaceutics Co., Ltd. Macrocyclic compound serving as Wee1 inhibitor and applications thereof
JP7290638B2 (ja) 2017-11-01 2023-06-13 ウーシー・バイオシティ・バイオファーマシューティクス・カンパニー・リミテッド Wee1阻害剤としての大環状化合物及びその使用
JP2022505756A (ja) * 2018-10-26 2022-01-14 シージャーヂュアン・サガシティー・ニュー・ドラッグ・デヴェロップメント・カンパニー・リミテッド Wee1阻害剤としてのピリミドピラゾロン類誘導体及びその使用
JP7481336B2 (ja) 2018-10-26 2024-05-10 ウーシー・バイオシティ・バイオファーマシューティクス・カンパニー・リミテッド Wee1阻害剤としてのピリミドピラゾロン類誘導体及びその使用
US12180184B2 (en) 2018-10-26 2024-12-31 Wuxi Biocity Biopharmaceutics Co., Ltd. Pyrimidopyrazolone derivative as Wee1 inhibitor and use thereof

Also Published As

Publication number Publication date
RU2015155595A (ru) 2017-07-14
AU2014276417B2 (en) 2016-11-24
AU2014276417A1 (en) 2015-12-17
WO2014195919A1 (en) 2014-12-11
US20160122342A1 (en) 2016-05-05
CN105452246A (zh) 2016-03-30
EP3004096A1 (en) 2016-04-13
BR112015030515A2 (pt) 2017-07-25
CA2914414A1 (en) 2014-12-11
KR20160018594A (ko) 2016-02-17

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