SG194447A1 - Aryl-or heteroaryl-substituted benzene compounds - Google Patents

Aryl-or heteroaryl-substituted benzene compounds Download PDF

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Publication number
SG194447A1
SG194447A1 SG2013075478A SG2013075478A SG194447A1 SG 194447 A1 SG194447 A1 SG 194447A1 SG 2013075478 A SG2013075478 A SG 2013075478A SG 2013075478 A SG2013075478 A SG 2013075478A SG 194447 A1 SG194447 A1 SG 194447A1
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SG
Singapore
Prior art keywords
heteroaryl
aryl
compounds
substituted benzene
benzene compounds
Prior art date
Application number
SG2013075478A
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English (en)
Inventor
Kevin Wayne Kuntz
Richard Chesworth
Kenneth William Duncan
Heike Keilhack
Natalie Warholic
Christine Klaus
Masashi Seki
Syuji Shirotori
Satoshi Kawano
Timothy James Nelson Wigle
Original Assignee
Epizyme Inc
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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=SG194447(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Epizyme Inc filed Critical Epizyme Inc
Publication of SG194447A1 publication Critical patent/SG194447A1/en

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    • 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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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    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/52Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C229/54Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
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    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
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    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
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SG2013075478A 2011-04-13 2012-04-13 Aryl-or heteroaryl-substituted benzene compounds SG194447A1 (en)

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US201161474821P 2011-04-13 2011-04-13
US201161499595P 2011-06-21 2011-06-21
PCT/US2012/033648 WO2012142504A1 (en) 2011-04-13 2012-04-13 Aryl-or heteroaryl-substituted benzene compounds

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US (15) US8410088B2 (enExample)
EP (5) EP3486234B1 (enExample)
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Families Citing this family (115)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2841142C (en) 2010-06-23 2020-12-15 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
AU2011298987B2 (en) 2010-09-10 2017-09-28 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
US9175331B2 (en) * 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
TW201733984A (zh) 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
EP2760452A4 (en) * 2011-09-30 2015-04-01 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
US9085583B2 (en) 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
TR201904660T4 (tr) * 2012-03-12 2019-05-21 Epizyme Inc İnsan EZH2 inhibitörleri ve bunun kullanım yöntemleri.
DK3184523T3 (da) 2012-04-13 2019-08-19 Epizyme Inc N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4' -(morphofinomethyl)-[1,1'-biphenyl]-3-carboxamidhydrobromid til anvendelse i behandlingen af en sygdom med celleproliferation i det hæmatologiske system.
IL308807B2 (en) * 2012-04-13 2025-08-01 Epizyme Inc Combination therapy for treating cancer
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
US20150239842A1 (en) * 2012-09-28 2015-08-27 Pfizer Inc. Benzamide and heterobenzamide compounds
CN110898067A (zh) * 2012-10-15 2020-03-24 Epizyme股份有限公司 癌症治疗方法
PE20150886A1 (es) 2012-10-15 2015-06-04 Epizyme Inc Compuestos de benceno sustituidos
BR112015014090A2 (pt) * 2012-12-13 2017-07-11 Glaxosmithkline Llc intensificador de inibidores de zeste homólogo 2
US20150313906A1 (en) * 2012-12-19 2015-11-05 Glaxosmithkline Llc Combination
AU2013361079B2 (en) 2012-12-21 2018-07-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
US20150344427A1 (en) * 2012-12-21 2015-12-03 Epizyme, Inc. 1,4-pyridone compounds
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
KR102219441B1 (ko) * 2013-02-11 2021-02-23 콘스텔레이션 파마슈티칼스, 인크. 메틸 변형 효소 조절제, 이의 조성물 및 용도
WO2014178954A1 (en) 2013-03-14 2014-11-06 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153090A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives asprmt1 inhibitors and uses thereof
HK1220916A1 (zh) 2013-03-14 2017-05-19 基因泰克公司 治疗癌症和预防癌症药物抗性的方法
WO2014153100A2 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153208A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014144659A1 (en) 2013-03-14 2014-09-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
BR112015022785A2 (pt) 2013-03-14 2017-07-18 Epizyme Inc composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt
WO2014153172A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9765035B2 (en) 2013-03-14 2017-09-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
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
EP2970281A4 (en) 2013-03-15 2016-08-03 Epizyme Inc SUBSTITUTED BENZOL COMPOUNDS
ES2717680T3 (es) 2013-04-30 2019-06-24 Glaxosmithkline Ip No 2 Ltd Potenciador de inhibidores del homólogo de Zeste 2
RU2015155595A (ru) * 2013-06-06 2017-07-14 Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед Ингибиторы энхансера zeste гомолога 2 область техники, к которой относится изобретение
US9556157B2 (en) 2013-07-10 2017-01-31 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
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
EP3033334A1 (en) 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
SG11201602269QA (en) * 2013-10-16 2016-04-28 Epizyme Inc Hydrochloride salt form for ezh2 inhibition
WO2015077193A1 (en) 2013-11-19 2015-05-28 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
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
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
PE20161552A1 (es) 2014-06-17 2017-01-11 Pfizer Compuestos de dihidroisoquinolinona sustituida
PL3157527T3 (pl) 2014-06-17 2023-08-07 Epizyme, Inc. Inhibitory ezh2 do leczenia chłoniaka
WO2015200650A1 (en) 2014-06-25 2015-12-30 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
HRP20191414T1 (hr) 2014-08-21 2019-11-01 Boehringer Ingelheim Int Novi spojevi i derivati spiro[3h-indol-3,2'-pirolidin]-2(1h)-ona kao mdm1-p53-inhibitori
CN106794177A (zh) 2014-10-16 2017-05-31 Epizyme股份有限公司 治疗癌症的方法
RU2017118165A (ru) * 2014-10-28 2018-11-29 Глэксосмитклайн Интеллекчуал Проперти (Но.2) Лимитед Ингибиторы энхансера гомолога 2 zestes
CN107105651A (zh) 2014-11-06 2017-08-29 达纳-法伯癌症研究所股份有限公司 Ezh2抑制剂及其用途
BR112017010166A2 (en) 2014-11-17 2018-02-14 Epizyme, Inc. solid tumor treatment method, activity inhibition method, oral dosage form for treating a solid tumor, solid pharmaceutical formulation, process for preparing a pharmaceutical formulation, and solid pharmaceutical composition
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ezh2抑制劑
CN108135908A (zh) * 2015-04-20 2018-06-08 Epizyme股份有限公司 用于治疗癌症的组合疗法
JP6890097B2 (ja) 2015-06-10 2021-06-18 エピザイム,インコーポレイティド リンパ腫を処置するためのezh2阻害剤
UY36758A (es) * 2015-06-30 2016-12-30 Glaxosmithkline Ip No 2 Ltd Inhibidores del potenciador del homólogo zeste 2
CA2996412A1 (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
SG10201909413SA (en) 2015-10-06 2019-11-28 Epizyme Inc Method of treating medulloblastoma with an ezh2 inhibitor
HUE054985T2 (hu) 2015-10-09 2021-11-29 Boehringer Ingelheim Int Spiro[3H-indol-3,2'-pirrolidin]-2(1H)-on vegyületek és számrazékok, mint MDM2-P53 inhibitorok
US20190070188A1 (en) * 2015-11-06 2019-03-07 Epizyme, Inc. Pediatric dosing for treatment of cancer with an ezh2 inhibitor
LT3378859T (lt) 2015-11-19 2020-01-27 Jiangsu Hengrui Medicine Co., Ltd. Benzofurano darinys, jo gavimo būdas ir jo panaudojimas medicinoje
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
EA201892075A1 (ru) 2016-03-15 2019-04-30 Оризон Дженомикс, С.А. Комбинации ингибиторов lsd1 для применения для лечения солидных опухолей
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
WO2017192290A1 (en) 2016-05-04 2017-11-09 The Wistar Institute Of Anatomy And Biology Methods of treating cancers overexpressing carm1 with ezh2 inhibitors and platinum-based antineoplastic drugs
CA3023157A1 (en) 2016-05-05 2017-11-09 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
JP7121660B2 (ja) 2016-06-01 2022-08-18 エピザイム,インコーポレイティド 癌を処置するためのezh2阻害剤の使用
WO2017218953A1 (en) 2016-06-17 2017-12-21 Epizyme, Inc. Ezh2 inhibitors for treating cancer
WO2018075598A1 (en) 2016-10-19 2018-04-26 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
US11311524B2 (en) 2017-01-19 2022-04-26 Daiichi Sankyo Company, Limited Pharmaceutical composition used for treatment of HTLV-1-associated myelopathy
US11214561B2 (en) 2017-01-25 2022-01-04 Ancureall Pharmaceutical (Shanghai) Co., Ltd. Histone methyltransferase EZH2 inhibitor, preparation method and pharmaceutical use thereof
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
WO2018183885A1 (en) 2017-03-31 2018-10-04 Epizyme, Inc. Combination therapy for treating cancer
CN110621316B (zh) * 2017-04-21 2024-01-26 Epizyme股份有限公司 用ehmt2抑制剂进行的组合疗法
JP7257328B2 (ja) 2017-05-18 2023-04-13 ジエンス ヘンルイ メデイシンカンパニー リミテッド ベンゾフラン誘導体遊離塩基の結晶およびその製造方法
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
WO2019050924A1 (en) * 2017-09-05 2019-03-14 Epizyme, Inc. POLY THERAPY FOR THE TREATMENT OF CANCER
WO2019097369A1 (en) 2017-11-14 2019-05-23 Pfizer Inc. Ezh2 inhibitor combination therapies
WO2019152419A1 (en) 2018-01-31 2019-08-08 Mirati Therapeutics, Inc Prc2 inhibitors
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
AU2019281969B2 (en) * 2018-06-07 2024-03-07 Merck Sharp & Dohme Llc Processes for the preparation of sugammadex
JP2021531340A (ja) 2018-07-09 2021-11-18 フォンダシヨン、アジール、デ、アブグルスFondation Asile Des Aveugles 眼障害を治療するためのprc2サブユニットの阻害
JP7411256B2 (ja) * 2018-07-27 2024-01-11 エボポイント、バイオサイエンシズ、カンパニー、リミテッド 多置換ベンゼン環化合物、製造方法及びその用途
KR102689665B1 (ko) 2019-02-19 2024-07-31 한미약품 주식회사 신규한 헤테로트리시클릭 유도체 화합물 및 이의 용도
WO2020192652A1 (zh) * 2019-03-25 2020-10-01 上海华汇拓医药科技有限公司 酰胺类化合物制备方法及其在医药领域的应用
JP7624404B2 (ja) 2019-04-22 2025-01-30 ミラティ セラピューティクス,インク. Prc2阻害剤としてのナフチリジン誘導体
CA3137916A1 (en) 2019-05-06 2020-11-12 Ichan School Of Medicine At Mount Sinai Heterobifunctional compounds as degraders of hpk1
WO2020247475A1 (en) 2019-06-05 2020-12-10 Mirati Therapeutics, Inc. Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer
US20220298222A1 (en) 2019-08-22 2022-09-22 Juno Therapeutics, Inc. Combination therapy of a t cell therapy and an enhancer of zeste homolog 2 (ezh2) inhibitor and related methods
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
EP4556479A1 (en) 2020-08-13 2025-05-21 Hanmi Pharmaceutical Co., Ltd. Novel dioxoloisoquinolinone derivatives and use thereof
WO2022078307A1 (zh) * 2020-10-13 2022-04-21 苏州信诺维医药科技股份有限公司 多取代苯环化合物马来酸盐的晶型、其制备方法及其应用
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
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
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
WO2023111810A1 (en) 2021-12-14 2023-06-22 Pfizer Inc. Combination therapies and uses for treating cancer
JP2025513620A (ja) 2022-04-27 2025-04-24 第一三共株式会社 抗体-薬物コンジュゲートとezh1阻害剤および/またはezh2阻害剤との組合せ
CA3258412A1 (en) 2022-06-13 2023-12-21 Treeline Biosciences, Inc. HETEROBORCTIONAL BCL6 DEGRADING AGENTS 1,8-NAPHTHYRIDIN-2-ONE
IL317228A (en) 2022-06-13 2025-01-01 Treeline Biosciences Inc BCL6 quinolone bifunctional 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
CN1118595A (zh) 1993-12-27 1996-03-13 卫材株式会社 氨茴酸衍生物
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
JP2002525352A (ja) 1998-09-30 2002-08-13 ザ、プロクター、エンド、ギャンブル、カンパニー 2−置換ケトアミド
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
CA2433158C (en) * 2000-12-28 2011-05-10 Shionogi & Co., Ltd. Pyridone derivatives having a binding activity to the cannabinoid type 2 receptor
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
JP5082033B2 (ja) * 2001-12-21 2012-11-28 エグゼリクシス パテント カンパニー エルエルシー Lxrのモジュレーター
ATE447971T1 (de) 2002-02-19 2009-11-15 Shionogi & Co Antipruriginosa
TW200306155A (en) 2002-03-19 2003-11-16 Du Pont Benzamides and advantageous compositions thereof for use as fungicides
JP4889219B2 (ja) 2002-12-27 2012-03-07 スキャンポ・アーゲー 腹部不快感の処置のためのプロスタグランジン誘導体
WO2004076412A2 (en) 2003-02-26 2004-09-10 Sugen, Inc. Aminoheteroaryl compounds as protein kinase inhibitors
WO2005014599A1 (en) * 2003-06-04 2005-02-17 Cellular Genomics, Inc. 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
EP1633740B1 (en) 2003-06-19 2011-11-09 GlaxoSmithKline LLC 5-(acylamino)indazole derivatives as kinase inhibitors
EP1663978B1 (en) * 2003-07-23 2007-11-28 Bayer Pharmaceuticals Corporation Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions
PL379887A1 (pl) 2003-08-26 2006-11-27 Merck Hdac Research, Llc Sposób leczenia raka inhibitorami HDAC
US20050059682A1 (en) 2003-09-12 2005-03-17 Supergen, Inc., A Delaware Corporation Compositions and methods for treatment of cancer
BRPI0508579A (pt) 2004-03-11 2007-08-14 Actelion Pharmaceuticals Ltd composto, composição farmacêutica, e, uso de um composto
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
EP1765994B1 (en) 2004-06-01 2009-11-18 The University of North Carolina at Chapel Hill Reconstituted histone methyltransferase complex and methods of identifying modulators thereof
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
ATE494548T1 (de) 2005-06-02 2011-01-15 Univ North Carolina Reinigung, charakterisierung und wiederherstellung einer 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
DK1940821T3 (da) 2005-10-19 2013-06-10 Gruenenthal Gmbh Nye vanilloid-receptorligander og deres anvendelse til fremstilling af lægemidler.
NZ567000A (en) 2005-10-21 2010-03-26 Merck & Co Inc Potassium channel inhibitors
US20090203057A1 (en) 2005-10-28 2009-08-13 Yi Zhang Protein demethylases comprising a jmjc domain
EP1960551A2 (en) 2005-12-01 2008-08-27 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
AU2006336552B2 (en) 2006-01-20 2012-12-20 The University Of North Carolina At Chapel Hill Diagnostic and therapeutic targets for leukemia
RU2008149246A (ru) 2006-05-15 2010-06-20 Айрм Ллк (Bm) Соединение на основе терефталата, композиции и их применение в качестве ингибиторов интегразы вич
WO2007136592A2 (en) 2006-05-18 2007-11-29 Amphora Discovery Corporation 2-0x0-l,2-dihydr0quin0line derivatives, compositions, and uses thereof as antiproliferative agents
EP2086318A4 (en) 2006-10-10 2009-12-23 Burnham Inst Medical Research NEUROPROTECTIVE COMPOSITIONS AND CORRESPONDING 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
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
US20090012031A1 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan EZH2 Cancer Markers
EP2170834B1 (en) 2007-07-16 2014-01-08 AbbVie Inc. Indazoles, benzisoxazoles and benzisothiazoles as inhibitors of protein kinases
US8247401B2 (en) * 2007-10-31 2012-08-21 Merck Sharp & Dohme Corp. P2X3 receptor antagonists for treatment of pain
JP5511680B2 (ja) 2007-12-19 2014-06-04 キャンサー・リサーチ・テクノロジー・リミテッド ピリド[2,3−b]ピラジン−8−置換化合物及びその使用
CN101977905B (zh) * 2008-01-23 2014-07-02 百时美施贵宝公司 4-吡啶酮化合物及其对于癌症的用途
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
US8299093B2 (en) 2008-08-08 2012-10-30 New York Blood Center, Inc. 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
US20120208809A1 (en) * 2009-03-24 2012-08-16 Sanofi 9h-pyrrolo[2,3-b: 5,4-c'] dipyridine azacarboline derivatives, preparation thereof, and therapeutic use thereof
JP2012522013A (ja) 2009-03-27 2012-09-20 ザ ユーエービー リサーチ ファウンデーション 調節ires媒介翻訳
WO2011011366A2 (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
PH12012502194A1 (en) * 2010-05-07 2014-09-05 Glaxosmithkline Llc Indoles
ES2528269T3 (es) * 2010-05-07 2015-02-06 Glaxosmithkline Llc Azaindazoles
ES2534804T3 (es) 2010-05-07 2015-04-28 Glaxosmithkline Llc Indazoles
CA2841142C (en) 2010-06-23 2020-12-15 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
AU2011298987B2 (en) 2010-09-10 2017-09-28 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
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
BR112013013668A2 (pt) 2010-12-03 2016-09-06 Epizyme Inc moduladores 7-deazapurina de histona metiltransferase, e métodos de uso dos mesmos
EP2681216B1 (en) 2011-02-28 2017-09-27 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
TW201733984A (zh) * 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
EP2760452A4 (en) 2011-09-30 2015-04-01 Glaxosmithkline Llc METHODS OF TREATING CANCER
TR201904660T4 (tr) 2012-03-12 2019-05-21 Epizyme Inc İnsan EZH2 inhibitörleri ve bunun kullanım yöntemleri.
DK3184523T3 (da) 2012-04-13 2019-08-19 Epizyme Inc N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4' -(morphofinomethyl)-[1,1'-biphenyl]-3-carboxamidhydrobromid til anvendelse i behandlingen af en sygdom med celleproliferation i det hæmatologiske system.
IL308807B2 (en) 2012-04-13 2025-08-01 Epizyme Inc Combination therapy for treating cancer
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
CN110898067A (zh) 2012-10-15 2020-03-24 Epizyme股份有限公司 癌症治疗方法
PE20150886A1 (es) 2012-10-15 2015-06-04 Epizyme Inc Compuestos de benceno sustituidos
AU2013361079B2 (en) 2012-12-21 2018-07-26 Epizyme, Inc. 1,4-pyridone 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
EP2970306A4 (en) 2013-03-15 2016-08-03 Epizyme Inc SUBSTITUTED 6.5-CONDENSED BICYCLIC HETEROARYL COMPOUNDS
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
SG11201602269QA (en) 2013-10-16 2016-04-28 Epizyme Inc Hydrochloride salt form for ezh2 inhibition
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
PL3157527T3 (pl) 2014-06-17 2023-08-07 Epizyme, Inc. Inhibitory ezh2 do leczenia chłoniaka
CN106794177A (zh) 2014-10-16 2017-05-31 Epizyme股份有限公司 治疗癌症的方法
BR112017010166A2 (en) 2014-11-17 2018-02-14 Epizyme, Inc. solid tumor treatment method, activity inhibition method, oral dosage form for treating a solid tumor, solid pharmaceutical formulation, process for preparing a pharmaceutical formulation, and solid pharmaceutical composition
CN108135908A (zh) 2015-04-20 2018-06-08 Epizyme股份有限公司 用于治疗癌症的组合疗法
JP6890097B2 (ja) 2015-06-10 2021-06-18 エピザイム,インコーポレイティド リンパ腫を処置するためのezh2阻害剤
CA2996412A1 (en) 2015-08-24 2017-03-02 Epizyme, Inc. Method for treating cancer
CA2999898A1 (en) 2015-09-25 2017-03-30 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
WO2017079738A1 (en) 2015-11-05 2017-05-11 Epizyme, Inc. Flow cytometry for monitoring histone h3 methylation status
EP3386513A2 (en) 2015-12-07 2018-10-17 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
JP2019508406A (ja) 2016-02-08 2019-03-28 エピザイム,インコーポレイティド 癌を処置する方法
JP7121660B2 (ja) 2016-06-01 2022-08-18 エピザイム,インコーポレイティド 癌を処置するためのezh2阻害剤の使用
WO2017218953A1 (en) 2016-06-17 2017-12-21 Epizyme, Inc. Ezh2 inhibitors for treating cancer
EP3548032A2 (en) 2016-12-02 2019-10-09 Epizyme, Inc. Combination therapy for treating cancer
WO2018144798A1 (en) 2017-02-02 2018-08-09 Epizyme, Inc. Cancer treatment modalities
WO2018183885A1 (en) 2017-03-31 2018-10-04 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
WO2019050924A1 (en) 2017-09-05 2019-03-14 Epizyme, Inc. POLY THERAPY FOR THE TREATMENT OF CANCER
JP2023509385A (ja) 2019-12-20 2023-03-08 エピザイム インコーポレイテッド Ezh2阻害剤の結晶性ヒドロブロミド塩、その調製及びがんの治療に有用な医薬組成物
WO2021243060A1 (en) 2020-05-28 2021-12-02 Epizyme, Inc. Use of ezh2 inhibitors for treating cancer

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