WO2013067300A1 - Méthode de traitement - Google Patents

Méthode de traitement Download PDF

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Publication number
WO2013067300A1
WO2013067300A1 PCT/US2012/063239 US2012063239W WO2013067300A1 WO 2013067300 A1 WO2013067300 A1 WO 2013067300A1 US 2012063239 W US2012063239 W US 2012063239W WO 2013067300 A1 WO2013067300 A1 WO 2013067300A1
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
methyl
mmol
indazole
cycloalkyl
Prior art date
Application number
PCT/US2012/063239
Other languages
English (en)
Inventor
Anna K. BASSIL
Soren BEINKE
Rabinder Kumar Prinjha
Original Assignee
Glaxosmithkline Intellectual Property (No. 2) Limited
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxosmithkline Intellectual Property (No. 2) Limited filed Critical Glaxosmithkline Intellectual Property (No. 2) Limited
Publication of WO2013067300A1 publication Critical patent/WO2013067300A1/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y201/00—Transferases transferring one-carbon groups (2.1)
    • C12Y201/01—Methyltransferases (2.1.1)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/1003—Transferases (2.) transferring one-carbon groups (2.1)
    • C12N9/1007—Methyltransferases (general) (2.1.1.)

Abstract

La présente invention concerne une méthode de traitement de maladies immunes inflammatoires médiées par les lymphocytes T ou de maladies d'hypersensibilité médiées par les lymphocytes T, la méthode consistant à administrer à un être humain nécessitant ce traitement une quantité efficace d'un composé qui inhibe EZH2 et/ou EZH1, ou un sel pharmaceutiquement acceptable de ce composé.
PCT/US2012/063239 2011-11-04 2012-11-02 Méthode de traitement WO2013067300A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161555656P 2011-11-04 2011-11-04
US61/555,656 2011-11-04

Publications (1)

Publication Number Publication Date
WO2013067300A1 true WO2013067300A1 (fr) 2013-05-10

Family

ID=48192802

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2012/063239 WO2013067300A1 (fr) 2011-11-04 2012-11-02 Méthode de traitement

Country Status (1)

Country Link
WO (1) WO2013067300A1 (fr)

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015506985A (ja) * 2012-02-10 2015-03-05 コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． メチル基変更酵素の調節物質、組成物及びその使用
WO2015077194A1 (fr) * 2013-11-22 2015-05-28 Bristol-Myers Squibb Company Inhibiteurs de la lysine méthyltransférase
US9051269B2 (en) 2011-11-18 2015-06-09 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US20150344459A1 (en) * 2012-12-21 2015-12-03 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
US9527837B2 (en) 2014-12-05 2016-12-27 Eli Lilly And Company Inhibitors of EZH2
US9718838B2 (en) 2015-08-27 2017-08-01 Eli Lilly And Company Inhibitors of EZH2
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9969716B2 (en) 2013-08-15 2018-05-15 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
WO2018210296A1 (fr) * 2017-05-18 2018-11-22 江苏恒瑞医药股份有限公司 Utilisation d'un inhibiteur d'ezh2 combiné à un inhibiteur de btk dans la préparation d'un médicament pour le traitement d'une tumeur
WO2018210302A1 (fr) 2017-05-18 2018-11-22 江苏恒瑞医药股份有限公司 Formes cristallines du chlore libre dérivé du benzofurane et son procédé de préparation
US10239843B2 (en) 2014-12-12 2019-03-26 Cancer Research Technology Limited 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
US10457640B2 (en) 2016-10-19 2019-10-29 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of EZH2
US10508086B2 (en) 2014-12-19 2019-12-17 Cancer Research Technology Limited PARG inhibitory compounds
US10577350B2 (en) 2015-08-28 2020-03-03 Constellation Pharmaceuticals, Inc. Crystalline forms of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
US10633371B2 (en) 2016-04-22 2020-04-28 Dana-Farber Cancer Institute, Inc. EZH2 inhibitors and uses thereof
US10759787B2 (en) 2015-11-19 2020-09-01 Jiangsu Hengrui Medicine Co., Ltd. Benzofuran derivative, preparation method thereof and use thereof in medicine
EP3885343A1 (fr) 2014-11-06 2021-09-29 Dana-Farber Cancer Institute, Inc. Composés d'indole comme inhibiteurs de ezh2 et utilisations associées
WO2023244918A1 (fr) 2022-06-13 2023-12-21 Treeline Biosciences, Inc. Agents de dégradation bifonctionnels de quinolone bcl6
WO2023244917A1 (fr) 2022-06-13 2023-12-21 Treeline Biosciences, Inc. Agents dégradant bcl6 hétérobifonctionnels 1,8-naphthyridin-2-one

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005034845A2 (fr) * 2003-09-12 2005-04-21 Supergen, Inc. Compositions et methodes de traitement du cancer
WO2007053114A1 (fr) * 2005-10-31 2007-05-10 S*Bio Pte Ltd Méthode permettant de prévoir une réponse aux inhibiteurs hdac
WO2010090723A2 (fr) * 2009-02-04 2010-08-12 University Of Georgia Research Foundation, Inc. Procédés d'inhibition de fibrogenèse et de traitement de maladie fibrotique
US20110064664A1 (en) * 2007-10-08 2011-03-17 The Board Of Regents Of The University Of Texas System Methods and compositions involving chitosan nanoparticles

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005034845A2 (fr) * 2003-09-12 2005-04-21 Supergen, Inc. Compositions et methodes de traitement du cancer
WO2007053114A1 (fr) * 2005-10-31 2007-05-10 S*Bio Pte Ltd Méthode permettant de prévoir une réponse aux inhibiteurs hdac
US20110064664A1 (en) * 2007-10-08 2011-03-17 The Board Of Regents Of The University Of Texas System Methods and compositions involving chitosan nanoparticles
WO2010090723A2 (fr) * 2009-02-04 2010-08-12 University Of Georgia Research Foundation, Inc. Procédés d'inhibition de fibrogenèse et de traitement de maladie fibrotique

Cited By (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9051269B2 (en) 2011-11-18 2015-06-09 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9409865B2 (en) 2011-11-18 2016-08-09 Constellation_Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9980952B2 (en) 2012-02-10 2018-05-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
USRE47428E1 (en) 2012-02-10 2019-06-11 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
JP2015506985A (ja) * 2012-02-10 2015-03-05 コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． メチル基変更酵素の調節物質、組成物及びその使用
US9371331B2 (en) 2012-02-10 2016-06-21 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9469646B2 (en) 2012-02-10 2016-10-18 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US10016405B2 (en) 2012-02-10 2018-07-10 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US10150759B2 (en) 2012-12-21 2018-12-11 Epizyme, Inc. 1,4-pyridone bicycic heteroaryl compounds
US20150344459A1 (en) * 2012-12-21 2015-12-03 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
US9701666B2 (en) * 2012-12-21 2017-07-11 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9969716B2 (en) 2013-08-15 2018-05-15 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
US9822103B2 (en) 2013-11-22 2017-11-21 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
WO2015077194A1 (fr) * 2013-11-22 2015-05-28 Bristol-Myers Squibb Company Inhibiteurs de la lysine méthyltransférase
US11236082B2 (en) 2014-11-06 2022-02-01 Dana-Farber Cancer Institute, Inc. EZH2 inhibitors and uses thereof
EP3885343A1 (fr) 2014-11-06 2021-09-29 Dana-Farber Cancer Institute, Inc. Composés d'indole comme inhibiteurs de ezh2 et utilisations associées
US9527837B2 (en) 2014-12-05 2016-12-27 Eli Lilly And Company Inhibitors of EZH2
US10239843B2 (en) 2014-12-12 2019-03-26 Cancer Research Technology Limited 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
US10995073B2 (en) 2014-12-19 2021-05-04 Cancer Research Technology Limited PARG inhibitory compounds
US10508086B2 (en) 2014-12-19 2019-12-17 Cancer Research Technology Limited PARG inhibitory compounds
US9718838B2 (en) 2015-08-27 2017-08-01 Eli Lilly And Company Inhibitors of EZH2
US10577350B2 (en) 2015-08-28 2020-03-03 Constellation Pharmaceuticals, Inc. Crystalline forms of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
US11059811B2 (en) 2015-11-19 2021-07-13 Jiangsu Hengrui Medicine Co., Ltd. Benzofuran derivative, preparation method thereof and use thereof in medicine
US10759787B2 (en) 2015-11-19 2020-09-01 Jiangsu Hengrui Medicine Co., Ltd. Benzofuran derivative, preparation method thereof and use thereof in medicine
US10633371B2 (en) 2016-04-22 2020-04-28 Dana-Farber Cancer Institute, Inc. EZH2 inhibitors and uses thereof
US10457640B2 (en) 2016-10-19 2019-10-29 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of EZH2
WO2018210302A1 (fr) 2017-05-18 2018-11-22 江苏恒瑞医药股份有限公司 Formes cristallines du chlore libre dérivé du benzofurane et son procédé de préparation
KR20200007851A (ko) * 2017-05-18 2020-01-22 지앙수 헨그루이 메디슨 컴퍼니 리미티드 종양 치료용 약물의 제조에 있어서의 ezh2 억제제 및 btk 억제제의 조합물의 용도
US11065239B2 (en) 2017-05-18 2021-07-20 Jiangsu Hengrui Medicine Co., Ltd. Use of EZH2 inhibitor combined with BTK inhibitor in preparing drug for treating tumor
CN109937041A (zh) * 2017-05-18 2019-06-25 江苏恒瑞医药股份有限公司 一种ezh2抑制剂与btk抑制剂联合在制备治疗肿瘤的药物中的用途
US11155537B2 (en) 2017-05-18 2021-10-26 Jiangsu Hengrui Medicine Co., Ltd. Crystal of benzofuran derivative free base and preparation method
RU2762893C2 (ru) * 2017-05-18 2021-12-23 Цзянсу Хэнжуй Медсин Ко., Лтд. Применение ингибитора ezh2 в комбинации с ингибитором btk в получении лекарственного средства для лечения опухоли
WO2018210296A1 (fr) * 2017-05-18 2018-11-22 江苏恒瑞医药股份有限公司 Utilisation d'un inhibiteur d'ezh2 combiné à un inhibiteur de btk dans la préparation d'un médicament pour le traitement d'une tumeur
CN109937041B (zh) * 2017-05-18 2022-04-12 江苏恒瑞医药股份有限公司 一种ezh2抑制剂与btk抑制剂联合在制备治疗肿瘤的药物中的用途
KR102635949B1 (ko) 2017-05-18 2024-02-14 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 종양 치료용 약물의 제조에 있어서의 ezh2 억제제 및 btk 억제제의 조합물의 용도
WO2023244918A1 (fr) 2022-06-13 2023-12-21 Treeline Biosciences, Inc. Agents de dégradation bifonctionnels de quinolone bcl6
WO2023244917A1 (fr) 2022-06-13 2023-12-21 Treeline Biosciences, Inc. Agents dégradant bcl6 hétérobifonctionnels 1,8-naphthyridin-2-one

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