JP7541538B2 - 癌を処置するためのｐｒｃ２阻害剤としてのイミダゾ［１，２－ｃ］ピリミジン誘導体 - Google Patents

癌を処置するためのｐｒｃ２阻害剤としてのイミダゾ［１，２－ｃ］ピリミジン誘導体 Download PDF

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JP7541538B2
JP7541538B2 JP2021572409A JP2021572409A JP7541538B2 JP 7541538 B2 JP7541538 B2 JP 7541538B2 JP 2021572409 A JP2021572409 A JP 2021572409A JP 2021572409 A JP2021572409 A JP 2021572409A JP 7541538 B2 JP7541538 B2 JP 7541538B2
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methyl
mmol
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JP2022535577A (ja
JP2022535577A5 (cg-RX-API-DMAC10.html
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マルクス，マシュー，アーノルド
ケチャム，ジョン，マイケル
バーンズ，アーロン，クレイグ
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ミラティ セラピューティクス，インク．
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2021572409A 2019-06-05 2020-06-03 癌を処置するためのｐｒｃ２阻害剤としてのイミダゾ［１，２－ｃ］ピリミジン誘導体 Active JP7541538B2 (ja)

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US201962857515P 2019-06-05 2019-06-05
US62/857,515 2019-06-05
PCT/US2020/035891 WO2020247475A1 (en) 2019-06-05 2020-06-03 Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer

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JP2022535577A JP2022535577A (ja) 2022-08-09
JP2022535577A5 JP2022535577A5 (cg-RX-API-DMAC10.html) 2023-05-08
JP7541538B2 true JP7541538B2 (ja) 2024-08-28

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EP (1) EP3980422A1 (cg-RX-API-DMAC10.html)
JP (1) JP7541538B2 (cg-RX-API-DMAC10.html)
KR (1) KR20220027933A (cg-RX-API-DMAC10.html)
CN (1) CN114269748A (cg-RX-API-DMAC10.html)
AU (1) AU2020288563A1 (cg-RX-API-DMAC10.html)
CA (1) CA3142711A1 (cg-RX-API-DMAC10.html)
IL (1) IL288529A (cg-RX-API-DMAC10.html)
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Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3746446T3 (da) 2018-01-31 2022-06-27 Mirati Therapeutics Inc PRC2-inhibitorer
US12421228B2 (en) 2019-04-22 2025-09-23 Mirati Therapeutics, Inc. Naphthyridine derivatives as PRC2 inhibitors
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
CN114907385B (zh) * 2021-02-10 2026-07-21 上海翱路生物医药科技有限公司 氮杂芳基化合物、其制备方法及应用
TW202312995A (zh) * 2021-08-11 2023-04-01 大陸商上海青煜醫藥科技有限公司 氮雜芳基化合物、其製備方法及應用
US20240398811A1 (en) * 2021-09-24 2024-12-05 Oric Pharmaceuticals, Inc. Prc2 inhibitors for use in treating blood disorders
WO2023049723A1 (en) * 2021-09-24 2023-03-30 Oric Pharmaceuticals, Inc. Prc2 inhibitors for use in treating blood disorders
WO2024123669A1 (en) * 2022-12-05 2024-06-13 Oric Pharmaceuticals, Inc. Treatment of prostate cancer having androgen receptor variants
WO2024215699A1 (en) * 2023-04-11 2024-10-17 Oric Pharmaceuticals, Inc. Treatment of t-cell lymphoma
EP4753714A1 (en) * 2023-08-04 2026-06-10 Oric Pharmaceuticals, Inc. Treatment of prostate cancer

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017221100A1 (en) 2016-06-20 2017-12-28 Novartis Ag Imidazopyrimidine compounds useful for the treatment of cancer
JP2018500342A (ja) 2014-12-23 2018-01-11 ノバルティス アーゲー トリアゾロピリミジン化合物およびその使用
WO2019062435A1 (zh) 2017-09-28 2019-04-04 中国科学院上海药物研究所 三氮唑并嘧啶、三氮唑并吡啶化合物及其组合物用于治疗prc2介导的疾病

Family Cites Families (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
WO2010021381A1 (ja) 2008-08-22 2010-02-25 武田薬品工業株式会社 縮合複素環誘導体およびその用途
US8846935B2 (en) 2010-05-07 2014-09-30 Glaxosmithkline Llc Indazoles
MX2012012966A (es) 2010-05-07 2013-01-22 Glaxosmithkline Llc Indoles.
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
WO2012068589A2 (en) 2010-11-19 2012-05-24 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
AU2011341441A1 (en) 2010-12-03 2013-06-20 Epizyme, Inc. Modulators of histone methyltransferase, and methods of use thereof
WO2012118812A2 (en) 2011-02-28 2012-09-07 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
JO3363B1 (ar) 2011-04-13 2019-03-13 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TW201733984A (zh) 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
WO2012154760A1 (en) 2011-05-10 2012-11-15 Gilead Sciences, Inc. Fused heterocyclic compounds as sodium channel modulators
US9730925B2 (en) 2011-09-30 2017-08-15 Glaxomithkline Llc Methods of treating cancer
CA2853501A1 (en) 2011-10-27 2013-05-02 Memorial Sloan-Kettering Cancer Center Methyltransferase inhibitors for treating cancer
WO2013075084A1 (en) 2011-11-18 2013-05-23 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
US9206128B2 (en) 2011-11-18 2015-12-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9085583B2 (en) 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2836216B1 (en) 2012-04-13 2022-06-08 Epizyme, Inc. Combination therapy for treating cancer
US9562041B2 (en) 2012-05-16 2017-02-07 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
US9105490B2 (en) 2012-09-27 2015-08-11 Taiwan Semiconductor Manufacturing Company, Ltd. Contact structure of semiconductor device
JP6254169B2 (ja) 2012-09-28 2017-12-27 ファイザー・インク ベンズアミドおよびヘテロベンズアミド化合物
BR112015008480A2 (pt) 2012-10-15 2017-07-04 Epizyme Inc compostos de benzeno substituído
KR20190105669A (ko) 2012-10-15 2019-09-17 에피자임, 인코포레이티드 암을 치료하는 방법
RU2015127822A (ru) 2012-12-13 2017-01-16 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Ингибиторы энхансера гомолога 2 белка zeste
CA2894216A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone compounds
CA2894222A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
PL2953941T3 (pl) 2013-02-11 2017-11-30 Constellation Pharmaceuticals, Inc. Modulatory enzymów modyfikujących metyl, ich kompozycje i zastosowania
US20160031907A1 (en) 2013-03-15 2016-02-04 Epizyme, Inc. Substituted Benzene Compounds
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9243001B2 (en) 2013-03-15 2016-01-26 Epizyme, Inc. Substituted benzene compounds
US9045477B2 (en) 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
EP2970306A4 (en) 2013-03-15 2016-08-03 Epizyme Inc SUBSTITUTED 6.5-CONDENSED BICYCLIC HETEROARYL COMPOUNDS
HK1214815A1 (zh) 2013-04-30 2016-08-05 Glaxosmithkline Intellectual Property (No. 2) Limited Zeste增强子同源物2的抑制剂
CA2914414A1 (en) 2013-06-06 2014-12-11 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
CA2917463A1 (en) 2013-07-10 2015-01-15 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
EP3022184B1 (en) 2013-07-19 2017-09-27 Epizyme, Inc. Substituted benzene compounds
US9624205B2 (en) 2013-07-19 2017-04-18 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
US9969716B2 (en) 2013-08-15 2018-05-15 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
US9738630B2 (en) 2013-11-19 2017-08-22 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
WO2015077194A1 (en) 2013-11-22 2015-05-28 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
US20160361309A1 (en) 2014-02-26 2016-12-15 Glaxosmithkline Intellectual Property (No.2) Limited Methods of treating cancer patients responding to ezh2 inhibitor gsk126
AU2015225775B2 (en) 2014-03-07 2017-06-15 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of Zeste Homolog 2 inhibitors
PL3121175T3 (pl) 2014-03-17 2020-06-01 Daiichi Sankyo Company, Limited Pochodne 1,3-benzodioksolu jako inhibitory ezh1 i/lub ezh2
AP2016009605A0 (en) 2014-06-17 2016-12-31 Pfizer Substituted dihydroisoquinolinone compounds
WO2015193768A1 (en) 2014-06-17 2015-12-23 Pfizer Inc. Aryl fused lactams as ezh2 modulators
MA40848A (fr) 2014-10-28 2021-05-05 Glaxosmithkline Ip No 2 Ltd Inhibiteurs d'ezh2 (enhancer of zeste homolog 2)
CA2964629A1 (en) 2014-11-06 2016-05-12 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
BR112017009440A2 (pt) 2014-11-06 2017-12-19 Dana Farber Cancer Inst Inc uso de composições que modulam a estrutura de cromatina quanto à doença do enxerto versus hospedeiro (gvhd)
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ｅｚｈ２抑制劑
WO2016102493A1 (en) 2014-12-22 2016-06-30 Bayer Pharma Aktiengesellschaft Imidazopyridine ezh2 inhibitors
IL236420A (en) 2014-12-23 2016-06-30 Ron Schneider Methods and systems for producing an enlarged 3D image
EP3250552B1 (en) 2015-01-30 2019-03-27 Genentech, Inc. Therapeutic compounds and uses thereof
US20180037568A1 (en) 2015-02-13 2018-02-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ｅｚｈ２抑制劑
SI3378859T1 (sl) 2015-11-19 2020-03-31 Jiangsu Hengrui Medicine Co., Ltd., Derivat benzofurana, postopek za njegovo pripravo in njegova uporaba v medicini
EP3386513A2 (en) 2015-12-07 2018-10-17 Epizyme Inc Inhibitors of ezh2 and methods of use thereof
WO2017174023A1 (zh) 2016-04-08 2017-10-12 南京明德新药研发股份有限公司 作为ezh2抑制剂的联苯化合物
WO2017184999A1 (en) 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
WO2017191545A1 (en) 2016-05-05 2017-11-09 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
US9957274B2 (en) 2016-05-06 2018-05-01 Abbvie Inc. Indane inhibitors of EED and methods of their use
US11786533B2 (en) 2016-06-01 2023-10-17 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
US11147819B2 (en) 2016-06-17 2021-10-19 Epizyme, Inc. EZH2 inhibitors for treating cancer
US10689378B2 (en) 2016-06-20 2020-06-23 Novartis Ag Triazolopyridine compounds and uses thereof
JP7042812B2 (ja) 2016-06-20 2022-03-28 ノバルティス アーゲー トリアゾロピリミジン化合物の結晶形態
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
CN109942556A (zh) 2017-12-21 2019-06-28 上海青煜医药科技有限公司 嘧啶酮化合物及其应用
DK3746446T3 (da) 2018-01-31 2022-06-27 Mirati Therapeutics Inc PRC2-inhibitorer
CN110156787B (zh) 2018-02-13 2021-11-02 中国科学院上海药物研究所 一种三氮唑并嘧啶衍生化合物、包含其的药物组合物及其用途
CN110563722A (zh) 2018-06-06 2019-12-13 上海青煜医药科技有限公司 吡啶或哒嗪并环化合物及其应用
US12421228B2 (en) 2019-04-22 2025-09-23 Mirati Therapeutics, Inc. Naphthyridine derivatives as PRC2 inhibitors
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018500342A (ja) 2014-12-23 2018-01-11 ノバルティス アーゲー トリアゾロピリミジン化合物およびその使用
WO2017221100A1 (en) 2016-06-20 2017-12-28 Novartis Ag Imidazopyrimidine compounds useful for the treatment of cancer
WO2019062435A1 (zh) 2017-09-28 2019-04-04 中国科学院上海药物研究所 三氮唑并嘧啶、三氮唑并吡啶化合物及其组合物用于治疗prc2介导的疾病

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KR20220027933A (ko) 2022-03-08
US20250179082A1 (en) 2025-06-05
EP3980422A1 (en) 2022-04-13
JP2022535577A (ja) 2022-08-09
AU2020288563A1 (en) 2022-01-06
WO2020247475A1 (en) 2020-12-10
IL288529A (en) 2022-01-01
US20220274990A1 (en) 2022-09-01
US12252493B2 (en) 2025-03-18
CN114269748A (zh) 2022-04-01
CA3142711A1 (en) 2020-12-10

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