KR102120883B1 - 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태 - Google Patents

인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태 Download PDF

Info

Publication number
KR102120883B1
KR102120883B1 KR1020147030684A KR20147030684A KR102120883B1 KR 102120883 B1 KR102120883 B1 KR 102120883B1 KR 1020147030684 A KR1020147030684 A KR 1020147030684A KR 20147030684 A KR20147030684 A KR 20147030684A KR 102120883 B1 KR102120883 B1 KR 102120883B1
Authority
KR
South Korea
Prior art keywords
cancer
degrees
polymorph
compound
methyl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
KR1020147030684A
Other languages
English (en)
Korean (ko)
Other versions
KR20150002730A (ko
Inventor
케빈 웨인 쿤츠
관춘 황
형욱 최
크리스틴 샌더스
스티븐 마티유
아라니 찬다
프랭크 팡
Original Assignee
에피자임, 인코포레이티드
에자이 알앤드디 매니지먼트 가부시키가이샤
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 에피자임, 인코포레이티드, 에자이 알앤드디 매니지먼트 가부시키가이샤 filed Critical 에피자임, 인코포레이티드
Priority to KR1020207015664A priority Critical patent/KR102438340B1/ko
Publication of KR20150002730A publication Critical patent/KR20150002730A/ko
Application granted granted Critical
Publication of KR102120883B1 publication Critical patent/KR102120883B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
KR1020147030684A 2012-04-13 2013-04-11 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태 Active KR102120883B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020207015664A KR102438340B1 (ko) 2012-04-13 2013-04-11 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261624215P 2012-04-13 2012-04-13
US61/624,215 2012-04-13
PCT/US2013/036193 WO2013155317A1 (en) 2012-04-13 2013-04-11 Salt form of a human hi stone methyltransf erase ezh2 inhibitor

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020207015664A Division KR102438340B1 (ko) 2012-04-13 2013-04-11 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태

Publications (2)

Publication Number Publication Date
KR20150002730A KR20150002730A (ko) 2015-01-07
KR102120883B1 true KR102120883B1 (ko) 2020-06-09

Family

ID=49328166

Family Applications (4)

Application Number Title Priority Date Filing Date
KR1020147030684A Active KR102120883B1 (ko) 2012-04-13 2013-04-11 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태
KR1020247041285A Pending KR20250005505A (ko) 2012-04-13 2013-04-11 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태
KR1020227029511A Active KR102744039B1 (ko) 2012-04-13 2013-04-11 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태
KR1020207015664A Active KR102438340B1 (ko) 2012-04-13 2013-04-11 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태

Family Applications After (3)

Application Number Title Priority Date Filing Date
KR1020247041285A Pending KR20250005505A (ko) 2012-04-13 2013-04-11 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태
KR1020227029511A Active KR102744039B1 (ko) 2012-04-13 2013-04-11 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태
KR1020207015664A Active KR102438340B1 (ko) 2012-04-13 2013-04-11 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태

Country Status (26)

Country Link
US (7) US9394283B2 (https=)
EP (4) EP3184523B1 (https=)
JP (3) JP6255382B2 (https=)
KR (4) KR102120883B1 (https=)
CN (2) CN104603130B (https=)
AU (2) AU2013245878B2 (https=)
BR (1) BR112014025508B1 (https=)
CA (1) CA2870005C (https=)
CY (2) CY1119383T1 (https=)
DK (3) DK3184523T3 (https=)
ES (3) ES2745016T3 (https=)
HR (2) HRP20170295T1 (https=)
HU (3) HUE031976T2 (https=)
IL (4) IL296199B2 (https=)
IN (1) IN2014DN09068A (https=)
LT (2) LT2836491T (https=)
MX (2) MX384641B (https=)
NZ (1) NZ700761A (https=)
PL (3) PL3184523T3 (https=)
PT (3) PT3184523T (https=)
RS (2) RS55690B1 (https=)
RU (1) RU2658911C2 (https=)
SG (3) SG10201608577RA (https=)
SI (2) SI2836491T1 (https=)
SM (2) SMT201900501T1 (https=)
WO (1) WO2013155317A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220123339A (ko) * 2012-04-13 2022-09-06 에피자임, 인코포레이티드 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3363B1 (ar) 2011-04-13 2019-03-13 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
EP2780013A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
NZ628762A (en) 2012-02-10 2016-07-29 Constellation Pharmaceuticals Inc Modulators of methyl modifying enzymes, compositions and uses thereof
SG10201912111TA (en) 2012-04-13 2020-02-27 Epizyme Inc Combination therapy for treating cancer
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
MX2015004721A (es) 2012-10-15 2016-01-25 Epizyme Inc Compuestos de benceno sustituidos.
KR20230156450A (ko) 2012-10-15 2023-11-14 에피자임, 인코포레이티드 암을 치료하는 방법
WO2014151142A1 (en) 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2991980B1 (en) 2013-04-30 2019-01-02 Glaxosmithkline Intellectual Property (No. 2) Limited Enhancer of zeste homolog 2 inhibitors
KR20160030221A (ko) 2013-07-10 2016-03-16 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 제스트 인핸서 상동체 2 억제제
EP3033334A1 (en) 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
MA38949A1 (fr) 2013-10-16 2017-07-31 Eisai R&D Man Co Ltd Forme saline d'hydrochlorure pour inhibition d'ezh2
WO2015058125A1 (en) * 2013-10-18 2015-04-23 Epizyme, Inc. Method of treating cancer
US9738630B2 (en) 2013-11-19 2017-08-22 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
CN116019921A (zh) 2013-12-06 2023-04-28 Epizyme股份有限公司 用于治疗癌症的组合疗法
BR112016029492A2 (pt) 2014-06-17 2017-10-17 Eisai R&D Man Co Ltd método para tratamento de linfoma não hodgkin
CA2952830C (en) 2014-06-20 2022-11-01 Constellation Pharmaceuticals, Inc. Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
EA201790845A1 (ru) 2014-10-16 2017-08-31 Эпизайм, Инк. Способ лечения рака
HUE062159T2 (hu) * 2014-11-17 2023-10-28 Epizyme Inc Módszer a rák kezelésére N-((4,6-dimetil-2-oxo-l,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2H -pirán-4-il)amino)-4-metil-4'-(morfolinmetil)-[1,1'-bifenil]-3-karboxamiddal
AR102767A1 (es) 2014-12-05 2017-03-22 Lilly Co Eli Inhibidores de ezh2
WO2016172199A1 (en) 2015-04-20 2016-10-27 Epizyme, Inc. Combination therapy for treating cancer
AU2016275051A1 (en) 2015-06-10 2017-12-07 Epizyme, Inc. EZH2 inhibitors for treating lymphoma
WO2017035234A1 (en) 2015-08-24 2017-03-02 Epizyme, Inc. Method for treating cancer
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ezh2抑制劑
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
EP3407978A4 (en) 2016-01-29 2020-01-15 Epizyme Inc POLYTHERAPY FOR THE TREATMENT OF CANCER
CA3025933A1 (en) * 2016-06-01 2017-12-07 Epizyme, Inc. Use of ezh2 inhibitors for treating cancer
WO2017218953A1 (en) 2016-06-17 2017-12-21 Epizyme, Inc. Ezh2 inhibitors for treating cancer
US10457640B2 (en) 2016-10-19 2019-10-29 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of EZH2
US11214561B2 (en) * 2017-01-25 2022-01-04 Ancureall Pharmaceutical (Shanghai) Co., Ltd. Histone methyltransferase EZH2 inhibitor, preparation method and pharmaceutical use thereof
WO2018183885A1 (en) 2017-03-31 2018-10-04 Epizyme, Inc. Combination therapy for treating cancer
AU2018275123A1 (en) 2017-06-02 2020-01-30 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
CN111093660A (zh) 2017-09-05 2020-05-01 Epizyme股份有限公司 用于治疗癌症的组合疗法
CA3104209A1 (en) 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
WO2021016414A1 (en) 2019-07-24 2021-01-28 Constellation Pharmaceuticals, Inc. Crystalline forms of 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-n-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide
JP2022545467A (ja) 2019-08-22 2022-10-27 ジュノー セラピューティクス インコーポレイテッド T細胞療法とzesteホモログ2エンハンサー(EZH2)阻害剤との併用療法および関連方法
IL294108A (en) * 2019-12-20 2022-08-01 Epizyme Inc Crystalline hydrobromide salt of a ezh2 inhibitor, its preparation and pharmaceutical composition useful for the treatment of cancer
WO2022208552A1 (en) * 2021-03-31 2022-10-06 Msn Laboratories Private Limited, R&D Center Crystalline forms of [1,1'-Biphenyl]-3-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-, hydrobromide (1:1) and process for its preparation thereof
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011140324A1 (en) 2010-05-07 2011-11-10 Glaxosmithkline Llc Indoles

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0733729A (ja) 1993-07-26 1995-02-03 Kirin Brewery Co Ltd N−シアノ−n′−置換−アリールカルボキシイミダミド化合物の製造法
EP0686625B1 (en) 1993-12-27 1999-05-26 Eisai Co., Ltd. Anthranilic acid derivative
DE19516776A1 (de) 1995-05-10 1996-11-14 Boehringer Ingelheim Int Chromatin-Regulatorgene
US5741819A (en) 1995-06-07 1998-04-21 3-Dimensional Pharmaceuticals, Inc. Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors
JP3906935B2 (ja) 1995-12-18 2007-04-18 杏林製薬株式会社 N−置換ジオキソチアゾリジルベンズアミド誘導体及びその製造法
AU6060099A (en) 1998-09-30 2000-04-17 Procter & Gamble Company, The 2-substituted ketoamides
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
ES2330719T3 (es) 2000-12-28 2009-12-15 SHIONOGI & CO., LTD. Derivados de 2-piridona con afinidad para el receptor cannabinoide de tipo 2.
US7700293B2 (en) 2001-08-02 2010-04-20 The Regents Of The University Of Michigan Expression profile of prostate cancer
TW200303304A (en) * 2002-02-18 2003-09-01 Astrazeneca Ab Chemical compounds
PT1477186E (pt) 2002-02-19 2010-02-11 Shionogi & Co Antipruriginosos
TW200306155A (en) 2002-03-19 2003-11-16 Du Pont Benzamides and advantageous compositions thereof for use as fungicides
US7442685B2 (en) 2003-06-13 2008-10-28 The University Of North Carolina At Chapel Hill DOT1 histone methyltransferases as a target for identifying therapeutic agents for leukemia
MXPA06010520A (es) 2004-03-30 2007-03-26 Chiron Corp Derivados de tiofeno sustituidos como agentes anticancerosos.
DE602005017781D1 (de) 2004-06-01 2009-12-31 Univ North Carolina Rekonstituierter histon-methyltransferase-komplex und verfahren zur identifizierung von modulatoren dafür
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
WO2006130720A2 (en) 2005-06-02 2006-12-07 University Of North Carolina At Chapel Hill Purification, characterization and reconstitution of a ubiquitin e3 ligase
FR2889526B1 (fr) 2005-08-04 2012-02-17 Aventis Pharma Sa 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation
PE20110285A1 (es) 2005-10-19 2011-06-04 Gruenenthal Chemie Derivados de sulfonamidofenil propionamida como ligandos del receptor vaniloide del subtipo 1
JP4931930B2 (ja) 2005-10-21 2012-05-16 メルク・シャープ・エンド・ドーム・コーポレイション カリウムチャネル阻害剤
EP1941060B1 (en) 2005-10-28 2012-02-29 The University of North Carolina At Chapel Hill Protein demethylases comprising a jmjc domain
AU2006325746A1 (en) 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
JP5167149B2 (ja) 2006-01-20 2013-03-21 ザ・ユニヴァーシティ・オヴ・ノース・キャロライナ・アト・チャペル・ヒル 白血病の診断および治療ターゲット
CA2650329A1 (en) 2006-05-15 2008-06-19 Irm Llc Terephthalamate compounds and compositions, and their use as hiv integrase inhibitors
EP2040711A2 (en) 2006-05-18 2009-04-01 Amphora Discovery Corporation 2-oxo-1,2-dihydroquinoline derivatives, compositions, and uses thereof as antiproliferative agents
US8022246B2 (en) 2006-10-10 2011-09-20 The Burnham Institute For Medical Research Neuroprotective compositions and methods
AU2008219166B2 (en) 2007-02-16 2013-05-16 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors
US8338437B2 (en) 2007-02-28 2012-12-25 Methylgene Inc. Amines as small molecule inhibitors
WO2008113006A1 (en) 2007-03-14 2008-09-18 Xenon Pharmaceuticals Inc. Methods of using quinolinone compounds in treating sodium channel-mediated diseases or conditions
DE102007017884A1 (de) 2007-04-13 2008-10-16 Grünethal GmbH Neue Vanilloid-Rezeptor Liganden und ihre Verwendung zur Herstellung von Arzneimitteln
US20090012031A1 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan EZH2 Cancer Markers
DE102007047737A1 (de) * 2007-10-05 2009-04-30 Merck Patent Gmbh Piperidin- und Piperazinderivate
CA2703909A1 (en) 2007-10-31 2009-05-07 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
AU2008337286B2 (en) 2007-12-19 2014-08-07 Cancer Research Technology Limited Pyrido[2,3-b]pyrazine-8-substituted compounds and their use
WO2009124137A2 (en) 2008-04-01 2009-10-08 Mount Sinai School Of Medicine Of New York University Method of suppressing gene transcription through histone lysine methylation
US20100113415A1 (en) 2008-05-29 2010-05-06 Rajapakse Hemaka A Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer
EP2335779A1 (en) 2008-08-08 2011-06-22 New York Blood Center Small Molecule Inhibitors of Retroviral Assembly & Maturation
FR2934995B1 (fr) 2008-08-14 2010-08-27 Sanofi Aventis Composes d'azetidines polysubstitues, leur preparation et leur application en therapeutique
US20120065247A1 (en) 2009-03-27 2012-03-15 Discoverybiomed, Inc. Modulating ires-mediated translation
US20110021362A1 (en) 2009-07-20 2011-01-27 Constellation Pharmaceuticals Agents for stimulating activity of methyl modifying enzymes and methods of use thereof
WO2011082044A1 (en) 2009-12-30 2011-07-07 Avon Products, Inc. Topical lightening composition and uses thereof
JP5889875B2 (ja) 2010-05-07 2016-03-22 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーGlaxoSmithKline LLC アザインダゾール
US8846935B2 (en) * 2010-05-07 2014-09-30 Glaxosmithkline Llc Indazoles
BR112013005806B1 (pt) 2010-09-10 2022-05-10 Epizyme, Inc Métodos para detectar se um indivíduo é um candidato para o tratamento com ou responsivo a um inibidor de ezh2 e usos terapêuticos do dito inibidor de ezh2
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
US20130310379A1 (en) 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
ES2607064T3 (es) 2010-12-01 2017-03-29 Glaxosmithkline Llc Indoles
EP2646454B1 (en) 2010-12-03 2015-07-08 Epizyme, Inc. 7-deazapurine modulators of histone methyltransferase, and methods of use thereof
ES2951688T3 (es) 2011-02-28 2023-10-24 Epizyme Inc Compuestos de heteroarilo biciclico fusionados en 6,5 sustituidos
TWI598336B (zh) 2011-04-13 2017-09-11 雅酶股份有限公司 經取代之苯化合物
JO3363B1 (ar) 2011-04-13 2019-03-13 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
EP3536314A1 (en) 2012-03-12 2019-09-11 Epizyme, Inc. Inhibitors of human ezh2, and methods of use thereof
PT3184523T (pt) * 2012-04-13 2019-09-26 Eisai R&D Man Co Ltd Bromidrato de n-((4,6-dimetil-2-oxo-l,2-di-hidropiridin- 3-il)metil)-5-(etil(tetra-hidro-2h-piran-4-il)amino)-4- metil-4¿-(morfolinometil)-[l,1¿-bofenil]-3-carboxamida para utilização no tratamento de uma doença proliferativa celular do sistema hematológico
SG10201912111TA (en) 2012-04-13 2020-02-27 Epizyme Inc Combination therapy for treating cancer
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
KR20230156450A (ko) 2012-10-15 2023-11-14 에피자임, 인코포레이티드 암을 치료하는 방법
MA38949A1 (fr) 2013-10-16 2017-07-31 Eisai R&D Man Co Ltd Forme saline d'hydrochlorure pour inhibition d'ezh2

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011140324A1 (en) 2010-05-07 2011-11-10 Glaxosmithkline Llc Indoles

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220123339A (ko) * 2012-04-13 2022-09-06 에피자임, 인코포레이티드 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태
KR102744039B1 (ko) * 2012-04-13 2024-12-17 에피자임, 인코포레이티드 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태

Also Published As

Publication number Publication date
IL282732B (en) 2022-12-01
AU2013245878A1 (en) 2014-10-30
EP3184523A1 (en) 2017-06-28
JP2015512942A (ja) 2015-04-30
SG10201912109QA (en) 2020-02-27
MX384641B (es) 2025-03-14
US20180243316A1 (en) 2018-08-30
EP3184523B1 (en) 2019-06-19
JP6255382B2 (ja) 2017-12-27
KR20200066380A (ko) 2020-06-09
JP2018199740A (ja) 2018-12-20
BR112014025508B1 (pt) 2020-11-17
CA2870005A1 (en) 2013-10-17
US12251386B2 (en) 2025-03-18
US20190269692A1 (en) 2019-09-05
EP2836491A1 (en) 2015-02-18
IL266165A (en) 2019-06-30
CA2870005C (en) 2021-06-22
KR20220123339A (ko) 2022-09-06
WO2013155317A1 (en) 2013-10-17
IL282732A (en) 2021-06-30
JP6634058B2 (ja) 2020-01-22
KR102438340B1 (ko) 2022-08-30
KR102744039B1 (ko) 2024-12-17
DK2836491T3 (en) 2017-03-06
ES2745016T3 (es) 2020-02-27
US11491163B2 (en) 2022-11-08
EP2836491A4 (en) 2015-09-16
US9872862B2 (en) 2018-01-23
SG11201406468YA (en) 2015-01-29
AU2018200168B2 (en) 2019-08-29
NZ700761A (en) 2016-09-30
EP2836491B1 (en) 2016-12-07
CN104603130A (zh) 2015-05-06
SMT201700132T1 (it) 2017-05-08
HUE045353T2 (hu) 2019-12-30
PT3184523T (pt) 2019-09-26
CY1119383T1 (el) 2018-02-14
CN104603130B (zh) 2018-04-27
IL296199B1 (en) 2024-08-01
CN108358899A (zh) 2018-08-03
IL235045A0 (en) 2014-12-31
DK3184523T3 (da) 2019-08-19
IL266165B (en) 2021-06-30
IN2014DN09068A (https=) 2015-05-22
US20170143729A1 (en) 2017-05-25
KR20250005505A (ko) 2025-01-09
HUE060881T2 (hu) 2023-04-28
US20150065503A1 (en) 2015-03-05
IL296199B2 (en) 2024-12-01
US20230140327A1 (en) 2023-05-04
LT2836491T (lt) 2017-03-27
AU2013245878B2 (en) 2017-10-12
MX362339B (es) 2019-01-11
HRP20170295T1 (hr) 2017-04-21
PL3628670T3 (pl) 2023-02-20
SI3184523T1 (sl) 2020-04-30
DK3628670T3 (da) 2022-12-05
SI2836491T1 (sl) 2017-06-30
US20210137936A1 (en) 2021-05-13
RS59392B1 (sr) 2019-11-29
SG10201608577RA (en) 2016-12-29
US20250268905A1 (en) 2025-08-28
LT3184523T (lt) 2020-02-10
SMT201900501T1 (it) 2019-11-13
CN108358899B (zh) 2021-07-27
PT3628670T (pt) 2022-12-02
US10821113B2 (en) 2020-11-03
AU2018200168A1 (en) 2018-02-01
US10245269B2 (en) 2019-04-02
ES2617379T3 (es) 2017-06-16
EP4190777A1 (en) 2023-06-07
RU2658911C2 (ru) 2018-06-26
HRP20191653T1 (hr) 2020-02-21
PL3184523T3 (pl) 2019-12-31
US9394283B2 (en) 2016-07-19
IL235045B (en) 2019-05-30
EP3628670B1 (en) 2022-10-12
RU2014145544A (ru) 2016-06-10
RS55690B1 (sr) 2017-07-31
CY1122883T1 (el) 2022-03-24
PL2836491T3 (pl) 2017-08-31
HUE031976T2 (en) 2017-08-28
ES2931316T3 (es) 2022-12-28
MX2014012380A (es) 2015-07-23
KR20150002730A (ko) 2015-01-07
IL296199A (en) 2022-11-01
JP2018002742A (ja) 2018-01-11
IL282732B2 (en) 2023-04-01
PT2836491T (pt) 2017-02-08
EP3628670A1 (en) 2020-04-01

Similar Documents

Publication Publication Date Title
KR102120883B1 (ko) 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태
HK40087682A (en) Hbr salt form for ezh2 inhibition
HK40026825B (en) Salt form for ezh2 inhibition
HK40026825A (en) Salt form for ezh2 inhibition

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

R17-X000 Change to representative recorded

St.27 status event code: A-3-3-R10-R17-oth-X000

A201 Request for examination
AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

AMND Amendment
P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

R17-X000 Change to representative recorded

St.27 status event code: A-3-3-R10-R17-oth-X000

E601 Decision to refuse application
PE0601 Decision on rejection of patent

St.27 status event code: N-2-6-B10-B15-exm-PE0601

X091 Application refused [patent]
AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PX0901 Re-examination

St.27 status event code: A-2-3-E10-E12-rex-PX0901

PX0701 Decision of registration after re-examination

St.27 status event code: A-3-4-F10-F13-rex-PX0701

X701 Decision to grant (after re-examination)
A107 Divisional application of patent
PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-OTH-PR1001 (AS PROVIDED BY THE NATIONAL OFFICE)

Year of fee payment: 6