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JO3363B1 - مركبات بنزين مستبدلة بأريل أو أريل غير متجانس - Google Patents

مركبات بنزين مستبدلة بأريل أو أريل غير متجانس

Info

Publication number
JO3363B1
JO3363B1 JOP/2012/0087A JOP20120087A JO3363B1 JO 3363 B1 JO3363 B1 JO 3363B1 JO P20120087 A JOP20120087 A JO P20120087A JO 3363 B1 JO3363 B1 JO 3363B1
Authority
JO
Jordan
Prior art keywords
aryl
compounds
benzene compounds
relates
present
Prior art date
Application number
JOP/2012/0087A
Other languages
English (en)
Inventor
Kenneth William Duncan
K Knutson Sarah
Masashi Seki
Syuji Shirotori
Richard Chesworth
Heike Keilhack
Christine Klaus
Kevin Wayne Kuntz
Natalie Warholic
Original Assignee
Epizyme Inc
Eisai R&D Man Co Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46045109&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JO3363(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Epizyme Inc, Eisai R&D Man Co Ltd filed Critical Epizyme Inc
Application granted granted Critical
Publication of JO3363B1 publication Critical patent/JO3363B1/ar

Links

Classifications

    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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  • Chemical & Material Sciences (AREA)
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

يتعلق الاختراع الحالي بمركبات بنزين بها استبدال بأريل أو أريل غير متجانسة. كما يتعلق الاختراع الحالي بتركيبات صيدلانية تحتوي على هذه المركبات وطرق لعلاج السرطان عن طريق إعطاء هذه المركبات والتركيبات الصيدلانية إلى حالات مرضية في حاجة إليها. كما يتعلق الاختراع الحالي باستخدام هذه المركبات بغرض البحث أو أغراض أخرى غير علاجية.
JOP/2012/0087A 2011-04-13 2012-04-10 مركبات بنزين مستبدلة بأريل أو أريل غير متجانس JO3363B1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161474821P 2011-04-13 2011-04-13
US201161499595P 2011-06-21 2011-06-21

Publications (1)

Publication Number Publication Date
JO3363B1 true JO3363B1 (ar) 2019-03-13

Family

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Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130102477A1 (en) 2010-06-23 2013-04-25 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
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
JO3438B1 (ar) * 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TWI598336B (zh) * 2011-04-13 2017-09-11 雅酶股份有限公司 經取代之苯化合物
WO2013049770A2 (en) 2011-09-30 2013-04-04 Glaxosmithkline Llc Methods of treating cancer
WO2013075084A1 (en) 2011-11-18 2013-05-23 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
EP2812001B1 (en) 2012-02-10 2017-06-14 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2825161B1 (en) * 2012-03-12 2019-01-02 Epizyme, Inc. Inhibitors of human ezh2, and methods of use thereof
US9394283B2 (en) * 2012-04-13 2016-07-19 Epizyme, Inc. Salt form of a human histone methyltransferase EZH2 inhibitor
SG10201912111TA (en) 2012-04-13 2020-02-27 Epizyme Inc Combination therapy for treating cancer
US9562041B2 (en) 2012-05-16 2017-02-07 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
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
KR102057365B1 (ko) 2012-10-15 2019-12-18 에피자임, 인코포레이티드 치환된 벤젠 화합물
KR20190105669A (ko) 2012-10-15 2019-09-17 에피자임, 인코포레이티드 암을 치료하는 방법
KR20150095779A (ko) * 2012-12-13 2015-08-21 글락소스미스클라인 엘엘씨 제스트 인핸서 상동체 2 억제제
US20150313906A1 (en) * 2012-12-19 2015-11-05 Glaxosmithkline Llc Combination
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
CA2894216A1 (en) * 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone compounds
WO2014100665A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
ME02730B (me) * 2013-02-11 2017-10-20 Constellation Pharmaceuticals Inc Modulatori enzima koji modifikuju metil, njihove kompozicije i upotreba
US9365527B2 (en) 2013-03-14 2016-06-14 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970137A1 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
EP2970181B1 (en) 2013-03-14 2017-06-07 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
JP2016518336A (ja) 2013-03-14 2016-06-23 エピザイム，インコーポレイティド Ｐｒｍｔ１阻害剤としてのピラゾール誘導体およびその使用
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9598374B2 (en) 2013-03-14 2017-03-21 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970220A2 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153030A2 (en) 2013-03-14 2014-09-25 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
US9447079B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. PRMT1 inhibitors and uses thereof
WO2014153214A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyl transferase inhibtors and uses thereof
US9023883B2 (en) 2013-03-14 2015-05-05 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9243001B2 (en) 2013-03-15 2016-01-26 Epizyme, Inc. Substituted benzene compounds
EP2970281A4 (en) 2013-03-15 2016-08-03 Epizyme Inc SUBSTITUTED BENZOL COMPOUNDS
EP2970305B1 (en) 2013-03-15 2017-02-22 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
CA2910873A1 (en) 2013-04-30 2014-11-06 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
JP2016520645A (ja) * 2013-06-06 2016-07-14 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｎｏ．２ Ｌｉｍｉｔｅｄ Ｚｅｓｔｅホモログ２エンハンサー阻害剤
US9556157B2 (en) 2013-07-10 2017-01-31 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
WO2015010049A1 (en) * 2013-07-19 2015-01-22 Epizyme, Inc. Substituted benzene compounds
US9624205B2 (en) 2013-07-19 2017-04-18 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
EP3033334A1 (en) 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
WO2015057859A1 (en) * 2013-10-16 2015-04-23 Epizyme, Inc. Hydrochloride salt form for ezh2 inhibition
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
ES2863996T3 (es) 2013-12-06 2021-10-13 Epizyme Inc Terapia de combinación para el tratamiento del cáncer
CN105037360B (zh) * 2014-04-28 2016-08-17 四川大学 吡啶酮衍生物及其制备方法和用途
KR20230031963A (ko) 2014-06-17 2023-03-07 에피자임, 인코포레이티드 림프종 치료를 위한 ｅｚｈ2 억제제
EA031892B1 (ru) 2014-06-17 2019-03-29 Пфайзер Инк. Замещенные дигидроизохинолиноновые соединения для лечения аномального клеточного роста, ассоциированного с активностью ezh2
US20170217941A1 (en) 2014-06-25 2017-08-03 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
AU2015331729A1 (en) 2014-10-16 2017-04-13 Epizyme, Inc. Method for treating cancer
CN107148419A (zh) * 2014-10-28 2017-09-08 葛兰素史密斯克莱知识产权（第2 号）有限公司 Zeste增强子同源物2抑制剂
BR112017009671A2 (pt) 2014-11-06 2017-12-26 Dana Farber Cancer Inst Inc inibidores de ezh2 e usos destes
ES2947819T3 (es) 2014-11-17 2023-08-21 Epizyme Inc Método para el tratamiento del cáncer con N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2H-piran-4-il)amino)-4-metil-4'-(morfolinometil)-[1,1'-bifenil]-3-carboxamida
AR102767A1 (es) 2014-12-05 2017-03-22 Lilly Co Eli Inhibidores de ezh2
SG10201902664RA (en) * 2015-04-20 2019-04-29 Epizyme Inc Combination therapy for treating cancer
AU2016275051A1 (en) 2015-06-10 2017-12-07 Epizyme, Inc. EZH2 inhibitors for treating lymphoma
UY36758A (es) * 2015-06-30 2016-12-30 Glaxosmithkline Ip No 2 Ltd Inhibidores del potenciador del homólogo zeste 2
EA201890567A1 (ru) 2015-08-24 2018-08-31 Эпизайм, Инк. Способ лечения рака
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
EP3371175A4 (en) * 2015-10-06 2019-09-25 Epizyme Inc METHOD FOR THE TREATMENT OF MEDULLOBLASTOMY WITH AN EZH2 INHIBITOR
WO2017079757A1 (en) * 2015-11-06 2017-05-11 Epizyme, Inc. Pediatric dosing for treatment of cancer with an ezh2 inhibitor
PL3378859T3 (pl) 2015-11-19 2020-04-30 Jiangsu Hengrui Medicine Co., Ltd. Pochodna benzofuranu, sposób jej wytwarzania i jej zastosowanie w medycynie
CN105440023A (zh) * 2015-12-10 2016-03-30 江苏理工学院 Epz-6438的合成方法
TWI773657B (zh) 2015-12-18 2022-08-11 美商亞德利克斯公司 作爲非全身ｔｇｒ５促效劑之經取代之4-苯基吡啶化合物
US12084472B2 (en) 2015-12-18 2024-09-10 Ardelyx, Inc. Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists
CA3011186A1 (en) 2016-01-29 2017-08-03 Epizyme, Inc. Combination therapy for treating cancer
SG10201913331VA (en) 2016-03-15 2020-03-30 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
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
CA3018270A1 (en) * 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
US10987353B2 (en) 2016-05-04 2021-04-27 The Wistar Institute Of Anatomy And Biology Methods of treating cancers overexpressing CARM1 with EZH2 inhibitors and platinum-based antineoplastic drugs
AU2017260854B2 (en) 2016-05-05 2020-01-30 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of Zeste Homolog 2 inhibitors
AU2017273726B2 (en) 2016-06-01 2023-10-19 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
MA45406A (fr) 2016-06-17 2019-04-24 Epizyme Inc Inhibiteurs d'ezh2 pour traiter le cancer
EP3529242A1 (en) 2016-10-19 2019-08-28 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
EP3548032A2 (en) 2016-12-02 2019-10-09 Epizyme, Inc. Combination therapy for treating cancer
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
CN108314677B (zh) 2017-01-17 2020-06-30 安徽中科拓苒药物科学研究有限公司 一种ezh2抑制剂及其用途
KR20190105602A (ko) 2017-01-19 2019-09-17 다이이찌 산쿄 가부시키가이샤 Htlv-1 관련 척수증을 치료하는 것에 사용하기 위한 의약 조성물
WO2018137639A1 (zh) * 2017-01-25 2018-08-02 恩瑞生物医药科技（上海）有限公司 一种组蛋白甲基转移酶ezh2抑制剂、其制备方法及其医药用途
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
US11642346B2 (en) 2017-03-31 2023-05-09 Epizyme, Inc. Combination therapy for treating cancer
US11672800B2 (en) * 2017-04-21 2023-06-13 Epizyme, Inc. Combination therapies with EHMT2 inhibitors
BR112019021023A2 (pt) 2017-05-18 2020-05-05 Jiangsu Hengrui Medicine Co cristal de base livre de derivado de benzofurano e método de preparação.
US11602529B2 (en) 2017-06-02 2023-03-14 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
WO2018231973A1 (en) 2017-06-13 2018-12-20 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
JP7399079B2 (ja) * 2017-09-05 2023-12-15 エピザイム，インコーポレイティド 癌を処置するための併用療法
JP7201400B2 (ja) 2017-11-14 2023-01-10 ファイザー・インク Ｅｚｈ２阻害剤組合せ療法
PT4043466T (pt) 2018-01-31 2024-10-14 Mirati Therapeutics Inc Inibidores de prc2
CN108640842B (zh) * 2018-04-04 2021-06-04 大连九信精细化工有限公司 一种2-溴-5-氟硝基苯的合成方法
JP7461304B2 (ja) * 2018-06-07 2024-04-03 メルク・シャープ・アンド・ドーム・エルエルシー スガマデクスの製造方法
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
WO2020020374A1 (zh) * 2018-07-27 2020-01-30 苏州信诺维医药科技有限公司 多取代苯环化合物、制备方法及其用途
KR102689665B1 (ko) 2019-02-19 2024-07-31 한미약품 주식회사 신규한 헤테로트리시클릭 유도체 화합물 및 이의 용도
JP7395807B2 (ja) * 2019-03-25 2023-12-12 上海華匯拓医薬科技有限公司 アミド類化合物の調製方法及びその医薬分野の使用
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
CN115551842B (zh) * 2020-06-08 2024-04-23 南京明德新药研发有限公司 联苯类化合物
US20230382898A1 (en) * 2020-10-13 2023-11-30 Evopoint Biosciences Co., Ltd. Crystal form of multi-substituted benzene ring compound maleate, and preparation method therefor and use thereof
CN114907300B (zh) * 2021-02-08 2024-05-28 上海医药工业研究院 他泽司他关键中间体的制备方法及其中间体
CN114907299B (zh) * 2021-02-08 2024-06-25 上海医药工业研究院 他泽司他关键中间体的盐型、其制备方法及其中间体
CN113292489B (zh) * 2021-06-16 2022-08-30 泓博智源(开原)药业有限公司 二氯代二烷基烟腈的制备方法
CN113527275A (zh) * 2021-07-20 2021-10-22 成都师范学院 一种sklb1039化合物及其制备方法和应用
CN113582863B (zh) * 2021-08-19 2023-05-26 沈阳农业大学 一种氨乙基联苯类化合物及其制备方法和用途
KR20230081459A (ko) 2021-11-30 2023-06-07 엘젠테라퓨틱스 주식회사 헤테로사이클릭이 치환된 신규한 3-페닐피리딘과 4-페닐피리딘 유도체 및 이의 용도
US20250049802A1 (en) 2021-12-14 2025-02-13 Pfizer Inc. Combination therapies and uses for treating cancer
CN119095624A (zh) 2022-04-27 2024-12-06 第一三共株式会社 抗体-药物缀合物与ezh1和/或ezh2抑制剂的组合
IL317228A (en) 2022-06-13 2025-01-01 Treeline Biosciences Inc BCL6 quinolone bifunctional joints
IL317217A (en) 2022-06-13 2025-01-01 Treeline Biosciences Inc BCL6 heterobifunctional 8,1-naphthyridin-2-one joints
CN115197202B (zh) * 2022-07-15 2024-01-26 四川大学 一种ezh2共价抑制剂及其制备方法和应用

Family Cites Families (106)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
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
HUT74450A (en) 1993-12-27 1996-12-30 Eisai Co Ltd Anthranilic acid derivative and pharmaceutical compns. contg. such compds.
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
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
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
BR9914207A (pt) 1998-09-30 2001-07-03 Procter & Gamble Ceto-amidas 2-substituìdas
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
KR20030070082A (ko) * 2000-12-28 2003-08-27 시오노기세이야쿠가부시키가이샤 칸나비노이드 2형 수용체 친화 작용을 갖는 피리돈 유도체
WO2002060492A1 (en) * 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
US7700293B2 (en) 2001-08-02 2010-04-20 The Regents Of The University Of Michigan Expression profile of prostate cancer
US7998986B2 (en) 2001-12-21 2011-08-16 Exelixis Patent Company Llc Modulators of LXR
JPWO2003070277A1 (ja) 2002-02-19 2005-06-09 塩野義製薬株式会社 抗掻痒剤
TW200306155A (en) 2002-03-19 2003-11-16 Du Pont Benzamides and advantageous compositions thereof for use as fungicides
EP1575596B1 (en) 2002-12-27 2016-06-22 Sucampo AG Derivatives of prostaglandins for treating irritable bowel syndrome and/or functional dyspepsia
JP4695588B2 (ja) 2003-02-26 2011-06-08 スージェン， インク． プロテインキナーゼ阻害剤としてのアミノヘテロアリール化合物
US7405295B2 (en) * 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
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
JP4869068B2 (ja) 2003-06-19 2012-02-01 スミスクライン ビーチャム コーポレーション 化合物
KR101139557B1 (ko) * 2003-07-23 2012-04-30 바이엘 파마슈티칼스 코포레이션 질환 및 상태의 치료 및 예방을 위한 플루오로 치환오메가-카르복시아릴 디페닐 우레아
KR100924737B1 (ko) 2003-08-26 2009-11-04 슬로안-케테링인스티튜트퍼캔서리서치 Ｈｄａｃ 억제제를 이용한 암의 치료 방법
US20050059682A1 (en) 2003-09-12 2005-03-17 Supergen, Inc., A Delaware Corporation Compositions and methods for treatment of cancer
CA2558545C (en) 2004-03-11 2012-10-16 Actelion Pharmaceuticals Ltd Indol-1-yl-acetic acid derivatives
CN1286973C (zh) 2004-04-12 2006-11-29 上海第二医科大学附属瑞金医院 一种组蛋白甲基转移酶及其制备方法
WO2005118796A2 (en) 2004-06-01 2005-12-15 The University Of North Carolina At Chapel Hill Reconstituted histone methyltransferase complex and methods of identifying modulators thereof
JO2787B1 (ar) 2005-04-27 2014-03-15 امجين إنك, مشتقات الاميد البديلة وطرق استخدامها
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
PT1940821E (pt) 2005-10-19 2013-05-29 Gruenenthal Gmbh Novos ligandos do receptor de vanilóide e seu uso para a produção de medicamentos
ATE510822T1 (de) 2005-10-21 2011-06-15 Merck Sharp & Dohme Kaliumkanalinhibitoren
CA2622615A1 (en) 2005-10-28 2007-05-10 The University Of North Carolina At Chapel Hill Protein demethylases comprising a jmjc domain
CA2631236C (en) 2005-12-01 2019-10-29 Medical Prognosis Institute Methods and devices for identifying biomarkers of treatment response and use thereof to predict treatment efficacy
EP1966141A1 (en) 2005-12-14 2008-09-10 Brystol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
EP1974055A4 (en) 2006-01-20 2010-01-27 Univ North Carolina DIAGNOSTIC AND THERAPEUTIC OBJECTIVES AGAINST LEUKEMIA
MX2008014616A (es) 2006-05-15 2008-11-28 Irm Llc Compuestos y composiciones de tereftalamato, y su uso como inhibidores de integrasa de vih.
US20070287706A1 (en) 2006-05-18 2007-12-13 Dickson John K Jr Certain substituted quinolones, compositions, and uses thereof
JP2010505958A (ja) 2006-10-10 2010-02-25 バーンハム インスティトゥート フォー メディカル リサーチ 神経防護作用組成物および方法
JP2010519204A (ja) 2007-02-16 2010-06-03 アムジエン・インコーポレーテツド 窒素含有複素環ケトン類およびそれらのｃ−Ｍｅｔ阻害薬としての使用
WO2008104077A1 (en) 2007-02-28 2008-09-04 Methylgene Inc. Small molecule inhibitors of protein arginine methyltransferases (prmts)
WO2008109534A1 (en) * 2007-03-02 2008-09-12 Mdrna, Inc. Nucleic acid compounds for inhibiting ezh2 gene expression and uses thereof
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
WO2009006577A2 (en) * 2007-07-03 2009-01-08 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
US8110572B2 (en) 2007-07-16 2012-02-07 Abbott Laboratories Inhibitors of protein kinases
WO2009058298A1 (en) * 2007-10-31 2009-05-07 Merck & Co., Inc. P2x3, receptor antagonists for treatment of pain
PL2229391T3 (pl) 2007-12-19 2015-02-27 Cancer Research Tech Ltd Pirydo[2,3-b]pirazyno-8-podstawione związki i ich zastosowanie
ES2531396T3 (es) 2008-01-23 2015-03-13 Bristol Myers Squibb Co Proceso para preparar compuestos de piridinona
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
UY31982A (es) * 2008-07-16 2010-02-26 Boehringer Ingelheim Int Derivados de 1,2-dihidropiridin-3-carboxamidas n-sustituidas
EP2323660A2 (en) 2008-08-08 2011-05-25 New York Blood Center Small molecule inhibitors of retroviral assembly and maturation
FR2934995B1 (fr) 2008-08-14 2010-08-27 Sanofi Aventis Composes d'azetidines polysubstitues, leur preparation et leur application en therapeutique
KR20110130504A (ko) * 2009-03-24 2011-12-05 사노피 ９ｈ-피롤로〔２,３-ｂ:５,４-ｃ'〕디피리딘 아자카르볼린 유도체, 그의 제조법, 및 그의 치료 용도
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
CA2784899A1 (en) 2009-12-30 2011-07-07 Avon Products, Inc. Topical lightening composition and uses thereof
LT2566327T (lt) * 2010-05-07 2017-05-25 Glaxosmithkline Llc Indolai
US8846935B2 (en) * 2010-05-07 2014-09-30 Glaxosmithkline Llc Indazoles
WO2012005805A1 (en) * 2010-05-07 2012-01-12 Glaxosmithkline Llc Azaindazoles
US20130102477A1 (en) 2010-06-23 2013-04-25 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
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
WO2012075080A1 (en) 2010-12-01 2012-06-07 Glaxosmithkline Llc Indoles
RU2013130253A (ru) 2010-12-03 2015-01-10 Эпизайм, Инк. 7-деазапуриновые регуляторы метилтрансферазы гистонов и способы их применения
EP2681216B1 (en) 2011-02-28 2017-09-27 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TWI598336B (zh) * 2011-04-13 2017-09-11 雅酶股份有限公司 經取代之苯化合物
WO2013049770A2 (en) 2011-09-30 2013-04-04 Glaxosmithkline Llc Methods of treating cancer
EP2825161B1 (en) * 2012-03-12 2019-01-02 Epizyme, Inc. Inhibitors of human ezh2, and methods of use thereof
US9394283B2 (en) 2012-04-13 2016-07-19 Epizyme, Inc. Salt form of a human histone methyltransferase EZH2 inhibitor
SG10201912111TA (en) 2012-04-13 2020-02-27 Epizyme Inc Combination therapy for treating cancer
US9562041B2 (en) 2012-05-16 2017-02-07 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
KR102057365B1 (ko) 2012-10-15 2019-12-18 에피자임, 인코포레이티드 치환된 벤젠 화합물
KR20190105669A (ko) 2012-10-15 2019-09-17 에피자임, 인코포레이티드 암을 치료하는 방법
WO2014100665A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
EP2970306A4 (en) 2013-03-15 2016-08-03 Epizyme Inc SUBSTITUTED 6.5-CONDENSED BICYCLIC HETEROARYL COMPOUNDS
US9045477B2 (en) 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
US9243001B2 (en) 2013-03-15 2016-01-26 Epizyme, Inc. Substituted benzene compounds
US9624205B2 (en) 2013-07-19 2017-04-18 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2015010049A1 (en) 2013-07-19 2015-01-22 Epizyme, Inc. Substituted benzene compounds
WO2015057859A1 (en) 2013-10-16 2015-04-23 Epizyme, Inc. Hydrochloride salt form for ezh2 inhibition
ES2863996T3 (es) 2013-12-06 2021-10-13 Epizyme Inc Terapia de combinación para el tratamiento del cáncer
KR20230031963A (ko) 2014-06-17 2023-03-07 에피자임, 인코포레이티드 림프종 치료를 위한 ｅｚｈ2 억제제
AU2015331729A1 (en) 2014-10-16 2017-04-13 Epizyme, Inc. Method for treating cancer
ES2947819T3 (es) 2014-11-17 2023-08-21 Epizyme Inc Método para el tratamiento del cáncer con N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2H-piran-4-il)amino)-4-metil-4'-(morfolinometil)-[1,1'-bifenil]-3-carboxamida
SG10201902664RA (en) 2015-04-20 2019-04-29 Epizyme Inc Combination therapy for treating cancer
AU2016275051A1 (en) 2015-06-10 2017-12-07 Epizyme, Inc. EZH2 inhibitors for treating lymphoma
EA201890567A1 (ru) 2015-08-24 2018-08-31 Эпизайм, Инк. Способ лечения рака
US20180296563A1 (en) 2015-09-25 2018-10-18 Epizyme, Inc. Method of treating malignant rhabdoid tumor of the ovary (mrto)/small cell cancer of the ovary of the hypercalcemic type(sccoht) with an ezh2 inhibitor
EP3371601A1 (en) 2015-11-05 2018-09-12 Epizyme Inc Flow cytometry for monitoring histone h3 methylation status
CA3007492A1 (en) 2015-12-07 2017-06-15 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
CA3011186A1 (en) 2016-01-29 2017-08-03 Epizyme, Inc. Combination therapy for treating cancer
WO2017139404A1 (en) 2016-02-08 2017-08-17 Epizyme, Inc. Methods of treating cancer
AU2017273726B2 (en) 2016-06-01 2023-10-19 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
MA45406A (fr) 2016-06-17 2019-04-24 Epizyme Inc Inhibiteurs d'ezh2 pour traiter le cancer
EP3548032A2 (en) 2016-12-02 2019-10-09 Epizyme, Inc. Combination therapy for treating cancer
EP3576729A4 (en) 2017-02-02 2021-04-14 Epizyme, Inc. CANCER TREATMENT MODALITIES
US11642346B2 (en) 2017-03-31 2023-05-09 Epizyme, Inc. Combination therapy for treating cancer
US11602529B2 (en) 2017-06-02 2023-03-14 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
WO2018231973A1 (en) 2017-06-13 2018-12-20 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
JP7399079B2 (ja) 2017-09-05 2023-12-15 エピザイム，インコーポレイティド 癌を処置するための併用療法
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
CA3177444A1 (en) 2020-05-28 2021-12-02 Carly CAMPBELL Use of ezh2 inhibitors for treating cancer

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