IL288181B2 - Methods of treating cancer - Google Patents

Methods of treating cancer

Info

Publication number
IL288181B2
IL288181B2 IL288181A IL28818121A IL288181B2 IL 288181 B2 IL288181 B2 IL 288181B2 IL 288181 A IL288181 A IL 288181A IL 28818121 A IL28818121 A IL 28818121A IL 288181 B2 IL288181 B2 IL 288181B2
Authority
IL
Israel
Prior art keywords
ezh2 inhibitor
compound
cancer
ezh2
cancer treatment
Prior art date
Application number
IL288181A
Other languages
English (en)
Hebrew (he)
Other versions
IL288181B1 (en
IL288181A (en
Original Assignee
Epizyme Inc
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 Epizyme Inc filed Critical Epizyme Inc
Publication of IL288181A publication Critical patent/IL288181A/en
Publication of IL288181B1 publication Critical patent/IL288181B1/en
Publication of IL288181B2 publication Critical patent/IL288181B2/en

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
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • A61K31/445—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
    • C07D211/86—Oxygen atoms
    • 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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/156—Polymorphic or mutational markers
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/158—Expression markers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Immunology (AREA)
  • Analytical Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Pathology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
IL288181A 2012-10-15 2013-10-15 Methods of treating cancer IL288181B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201261714145P 2012-10-15 2012-10-15
US201261714140P 2012-10-15 2012-10-15
US201261714045P 2012-10-15 2012-10-15
US201361758972P 2013-01-31 2013-01-31
US201361780703P 2013-03-13 2013-03-13
US201361786277P 2013-03-14 2013-03-14
PCT/US2013/065112 WO2014062720A2 (en) 2012-10-15 2013-10-15 Methods of treating cancer

Publications (3)

Publication Number Publication Date
IL288181A IL288181A (en) 2022-01-01
IL288181B1 IL288181B1 (en) 2023-12-01
IL288181B2 true IL288181B2 (en) 2024-04-01

Family

ID=49519104

Family Applications (4)

Application Number Title Priority Date Filing Date
IL288181A IL288181B2 (en) 2012-10-15 2013-10-15 Methods of treating cancer
IL308613A IL308613A (en) 2012-10-15 2013-10-15 Cancer treatment methods
IL238254A IL238254B (en) 2012-10-15 2015-04-13 Cancer treatment methods
IL273517A IL273517A (en) 2012-10-15 2020-03-23 Cancer treatment methods

Family Applications After (3)

Application Number Title Priority Date Filing Date
IL308613A IL308613A (en) 2012-10-15 2013-10-15 Cancer treatment methods
IL238254A IL238254B (en) 2012-10-15 2015-04-13 Cancer treatment methods
IL273517A IL273517A (en) 2012-10-15 2020-03-23 Cancer treatment methods

Country Status (23)

Country Link
US (7) US9688665B2 (enExample)
EP (2) EP3659606A1 (enExample)
JP (5) JP6351182B2 (enExample)
KR (3) KR102021642B1 (enExample)
CN (2) CN105142642B (enExample)
AU (4) AU2013331368A1 (enExample)
BR (1) BR112015008447A2 (enExample)
CA (2) CA3177498A1 (enExample)
CY (1) CY1122186T1 (enExample)
ES (1) ES2750199T3 (enExample)
HR (1) HRP20191814T1 (enExample)
HU (1) HUE046790T2 (enExample)
IL (4) IL288181B2 (enExample)
LT (1) LT2908823T (enExample)
MX (2) MX376008B (enExample)
NZ (2) NZ706836A (enExample)
PL (1) PL2908823T3 (enExample)
PT (1) PT2908823T (enExample)
RS (1) RS59541B1 (enExample)
RU (2) RU2018145311A (enExample)
SI (1) SI2908823T1 (enExample)
SM (1) SMT201900593T1 (enExample)
WO (1) WO2014062720A2 (enExample)

Families Citing this family (61)

* 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
JO3438B1 (ar) 2011-04-13 2019-10-20 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
US9085583B2 (en) 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
PL3628670T3 (pl) 2012-04-13 2023-02-20 Epizyme, Inc. Postać soli dla inhibicji ezh2
MX376008B (es) 2012-10-15 2025-03-07 Epizyme Inc Inhibidor de ezh2 para usarse en el tratamiento de sarcoma epiteloide.
SG10201705989YA (en) 2012-10-15 2017-08-30 Epizyme Inc Substituted benzene compounds
EP3498701B1 (en) 2012-12-21 2023-02-22 Epizyme Inc Prmt5 inhibitors and uses thereof
EP2970305B1 (en) 2013-03-15 2017-02-22 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2015023915A1 (en) 2013-08-15 2015-02-19 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
SI3057962T1 (sl) 2013-10-16 2024-01-31 Epizyme, Inc. Oblika hidrokloridne soli za ezh2 inhibicijo
AU2014337121A1 (en) * 2013-10-18 2016-04-14 Epizyme, Inc. Method of treating cancer
KR20220165809A (ko) 2013-12-06 2022-12-15 에피자임, 인코포레이티드 암 치료를 위한 병용 요법
PL3157527T3 (pl) * 2014-06-17 2023-08-07 Epizyme, Inc. Inhibitory ezh2 do leczenia chłoniaka
MX384423B (es) 2014-06-19 2025-03-14 Memorial Sloan Kettering Cancer Center Biomarcadores para la respuesta a inhibidores del mejorador del homólogo 2 de zeste (ezh2).
CA2963149A1 (en) * 2014-10-16 2016-04-21 Epizyme, Inc. Method for treating cancer
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
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ｅｚｈ２抑制劑
EP3236962A2 (en) 2014-12-23 2017-11-01 University of Copenhagen Treatment of cancer by inhibiting ezh2 activity
MX391720B (es) * 2015-04-20 2025-03-21 Epizyme Inc Terapia combinada para tratar cáncer.
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
MX2018002344A (es) 2015-08-24 2018-07-06 Epizyme Inc Metodo para tratar el 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
AU2016325643B2 (en) * 2015-09-25 2022-07-21 Epizyme, Inc. Method of treating malignant rhabdoid tumor or small cell cancer of the ovary of the hypercalcemic type
KR20180058829A (ko) * 2015-10-06 2018-06-01 에피자임, 인코포레이티드 Ezh2 억제제로 수모세포종을 치료하는 방법
JP2018532761A (ja) * 2015-11-06 2018-11-08 エピザイム，インコーポレイティド Ｅｚｈ２阻害剤を用いた癌の処置のための小児投与
CN105440023A (zh) * 2015-12-10 2016-03-30 江苏理工学院 Epz-6438的合成方法
EP3407978A4 (en) 2016-01-29 2020-01-15 Epizyme Inc POLYTHERAPY FOR THE TREATMENT OF CANCER
WO2017139404A1 (en) * 2016-02-08 2017-08-17 Epizyme, Inc. Methods of treating cancer
WO2017201585A1 (en) * 2016-05-26 2017-11-30 Genea Ip Holdings Pty Ltd Modulators of dux4 for regulation of muscle function
CA3025933A1 (en) 2016-06-01 2017-12-07 Epizyme, Inc. Use of ezh2 inhibitors for treating cancer
WO2017214373A1 (en) * 2016-06-08 2017-12-14 Genentech, Inc. Diagnostic and therapeutic methods for cancer
JP2019521988A (ja) 2016-06-17 2019-08-08 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
WO2018034801A1 (en) * 2016-08-15 2018-02-22 The Wistar Institute Of Anatomy And Biology Methods of treating arid1a-mutated cancers with hdac6 inhibitors and ezh2 inhibitors
US11433068B2 (en) * 2016-09-08 2022-09-06 The General Hospital Corporation Treatment of cancers having alterations within the SWI/SNF chromatin remodeling complex
WO2018075598A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
CA3044691A1 (en) 2016-10-26 2018-05-03 Genea Biocells USA (Holdings), Inc. Improved generation of muscle lineage cells and therapeutic uses thereof
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
EP3576729A4 (en) * 2017-02-02 2021-04-14 Epizyme, Inc. CANCER TREATMENT MODALITIES
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
JP2020522687A (ja) 2017-06-02 2020-07-30 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
WO2019018635A1 (en) 2017-07-19 2019-01-24 Children's Medical Center Corporation COMPOSITIONS AND METHODS FOR TREATING DISEASES ASSOCIATED WITH IMPRESSIVE FAULT
KR102758037B1 (ko) 2017-08-18 2025-01-22 코테라 바이오사이언스 인코포레이티드 Tg02의 다형성 형태
EP3678663A4 (en) 2017-09-05 2021-06-02 Epizyme, Inc. POLYTHERAPY FOR CANCER TREATMENT
CA3082287C (en) 2017-11-14 2023-02-28 Pfizer Inc. Ezh2 inhibitor combination therapies
PT4043466T (pt) 2018-01-31 2024-10-14 Mirati Therapeutics Inc Inibidores de prc2
WO2020011607A1 (en) * 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
TWI798532B (zh) * 2019-03-25 2023-04-11 大陸商深圳微芯生物科技股份有限公司 Ｋｄｍ５ａ基因和ａｔｒｘ基因的應用
US20220154295A1 (en) * 2019-03-27 2022-05-19 The Johns Hopkins University Methods and materials for assessing and treating cancer
WO2020219606A1 (en) 2019-04-22 2020-10-29 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Use of erk5 inhibitors for treating gliomas in pediatric subjects
EP3959214A1 (en) 2019-04-22 2022-03-02 Mirati Therapeutics, Inc. Naphthyridine derivatives as prc2 inhibitors
WO2020247130A1 (en) * 2019-06-03 2020-12-10 Icahn School Of Medicine At Mount Sinai Compounds and methods for inhibiting cancers via rest inhibition
EP3980422A1 (en) 2019-06-05 2022-04-13 Mirati Therapeutics, Inc. Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer
CN114126651A (zh) 2019-06-28 2022-03-01 Als治疗发展学会 对二肽重复蛋白的抑制
US20230181543A1 (en) * 2020-02-28 2023-06-15 The Wistar Institute Of Anatomy And Biology Treatment of carm1-overexpressing and/or arid1a mutant cancers with ire-1/xbp-1 inhibitors
WO2021257842A1 (en) * 2020-06-18 2021-12-23 Epizyme, Inc. Smarca4 inhibition for the treatment of cancer
CN111773387A (zh) * 2020-07-08 2020-10-16 北京大学 一种通过改变bin1剪切体比例改善心脏横管结构的方法
US20240350508A1 (en) 2021-08-25 2024-10-24 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of ezh2 inhibitors for the treatment of aortic valve stenosis
CN116019916A (zh) * 2021-10-27 2023-04-28 蚌埠医学院第一附属医院 非小细胞肺癌靶点arid1a及其抑制剂在制备肺癌治疗药物中的用途

Family Cites Families (81)

* 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
US5455044A (en) 1993-05-14 1995-10-03 Depotech Corporation Method for treating neurological disorders
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
US7229774B2 (en) 2001-08-02 2007-06-12 Regents Of The University Of Michigan Expression profile of prostate cancer
EP1638541B1 (en) 2003-06-27 2010-05-19 Astellas Pharma Inc. Therapeutic agent for soft tissue sarcoma
WO2009006577A2 (en) * 2007-07-03 2009-01-08 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
US20120114670A1 (en) * 2007-10-02 2012-05-10 University Of Rochester Methods and compositions related to synergistic responses to oncogenic mutations
WO2009048958A2 (en) * 2007-10-08 2009-04-16 The Board Of Regents Of The University Of Texas System Methods and compositions involving chitosan nanoparticles
US20110251216A1 (en) 2010-02-19 2011-10-13 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
US8637509B2 (en) 2010-05-07 2014-01-28 Glaxosmithkline Llc Azaindazoles
EP2566327B1 (en) 2010-05-07 2017-03-29 Glaxosmithkline LLC Indoles
WO2011140325A1 (en) 2010-05-07 2011-11-10 Glaxosmithkline Llc Indazoles
WO2012071096A2 (en) * 2010-09-03 2012-05-31 The Johns Hopkins University Arid1a and ppp2r1a mutations in cancer
PL2614369T3 (pl) * 2010-09-10 2016-08-31 Epizyme Inc Sposób określania przydatności inhibitorów ludzkiego ezh2 w leczeniu
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
WO2012068589A2 (en) * 2010-11-19 2012-05-24 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
ES2607064T3 (es) 2010-12-01 2017-03-29 Glaxosmithkline Llc Indoles
JP2014511389A (ja) 2011-02-28 2014-05-15 エピザイム インコーポレイテッド 置換６，５−縮合二環式ヘテロアリール化合物
EP2694677A2 (en) 2011-04-04 2014-02-12 Netherland Cancer Institute Methods and compositions for predicting resistance to anticancer treatment with protein kinase inhibitors
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TW201733984A (zh) 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
EP2709629B1 (en) 2011-05-16 2017-10-11 Ulrike Nuber Novel cancer therapies and methods
EP2755962B1 (en) * 2011-09-13 2017-03-01 Glaxosmithkline LLC Azaindazoles
BR112014007603A2 (pt) 2011-09-30 2017-06-13 Glaxosmithkline Llc métodos de tratamento do câncer
WO2013059944A1 (en) 2011-10-28 2013-05-02 British Columbia Cancer Agency Branch Epigenetic regulators and uses thereof
US9085583B2 (en) 2012-02-10 2015-07-21 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
EP2828250B1 (en) * 2012-03-19 2021-03-10 Imperial College Innovations Limited Quinazoline compounds and their use in therapy
CN104768555B (zh) 2012-04-13 2018-10-30 Epizyme股份有限公司 用于治疗癌症的联合治疗
PL3628670T3 (pl) 2012-04-13 2023-02-20 Epizyme, Inc. Postać soli dla inhibicji ezh2
WO2013173441A2 (en) * 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
SG10201705989YA (en) 2012-10-15 2017-08-30 Epizyme Inc Substituted benzene compounds
MX376008B (es) 2012-10-15 2025-03-07 Epizyme Inc Inhibidor de ezh2 para usarse en el tratamiento de sarcoma epiteloide.
US20140120083A1 (en) 2012-11-01 2014-05-01 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
WO2014092905A1 (en) 2012-12-10 2014-06-19 Children's Medical Center Corporation Methods and assays for combination treatment of cancer
AU2013361060B2 (en) 2012-12-21 2018-04-19 Epizyme, Inc. 1,4-pyridone compounds
CA2894222A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
MA38341B1 (fr) 2013-02-11 2018-11-30 Constellation Pharmaceuticals Inc Modulateurs d'enzymes de modification par méthylation, compositions et utilisations associées
US9045477B2 (en) 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
US20160031907A1 (en) 2013-03-15 2016-02-04 Epizyme, Inc. Substituted Benzene Compounds
US9243001B2 (en) 2013-03-15 2016-01-26 Epizyme, Inc. Substituted benzene compounds
US9776996B2 (en) 2013-03-15 2017-10-03 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2014176047A1 (en) 2013-04-25 2014-10-30 Novartis Ag Markers for ezh2 inhibitors
HK1214815A1 (zh) 2013-04-30 2016-08-05 Glaxosmithkline Intellectual Property (No. 2) Limited Zeste增强子同源物2的抑制剂
CN105452246A (zh) 2013-06-06 2016-03-30 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的抑制剂
CN105473580A (zh) 2013-07-10 2016-04-06 葛兰素史密斯克莱知识产权（第2号）有限公司 Zeste同源物增强子2抑制剂
WO2015010049A1 (en) 2013-07-19 2015-01-22 Epizyme, Inc. Substituted benzene compounds
EP3022195A2 (en) 2013-07-19 2016-05-25 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
SI3057962T1 (sl) 2013-10-16 2024-01-31 Epizyme, Inc. Oblika hidrokloridne soli za ezh2 inhibicijo
AU2014337121A1 (en) 2013-10-18 2016-04-14 Epizyme, Inc. Method of treating cancer
KR20220165809A (ko) 2013-12-06 2022-12-15 에피자임, 인코포레이티드 암 치료를 위한 병용 요법
WO2015103431A1 (en) 2013-12-31 2015-07-09 Memorial Sloan-Kettering Cancer Center Compositions and methods for the diagnosis and treatment of ovarian cancers that are associated with reduced smarca4 gene expression or protein function
US20160361309A1 (en) 2014-02-26 2016-12-15 Glaxosmithkline Intellectual Property (No.2) Limited Methods of treating cancer patients responding to ezh2 inhibitor gsk126
WO2015132765A1 (en) 2014-03-07 2015-09-11 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
EA201691872A1 (ru) 2014-03-19 2017-04-28 Инфинити Фармасьютикалз, Инк. Гетероциклические соединения для применения в лечении pi3k-гамма-опосредованных расстройств
WO2015193768A1 (en) 2014-06-17 2015-12-23 Pfizer Inc. Aryl fused lactams as ezh2 modulators
PL3157527T3 (pl) 2014-06-17 2023-08-07 Epizyme, Inc. Inhibitory ezh2 do leczenia chłoniaka
MX384423B (es) 2014-06-19 2025-03-14 Memorial Sloan Kettering Cancer Center Biomarcadores para la respuesta a inhibidores del mejorador del homólogo 2 de zeste (ezh2).
EP3160940A4 (en) 2014-06-25 2018-05-02 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
BR112017004459A2 (pt) 2014-09-05 2017-12-05 Arqule Inc composições e métodos para o tratamento de distúrbios de proliferação
CA2963149A1 (en) * 2014-10-16 2016-04-21 Epizyme, Inc. Method for treating cancer
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
MX391720B (es) 2015-04-20 2025-03-21 Epizyme Inc Terapia combinada para tratar cáncer.
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
MX2018002344A (es) 2015-08-24 2018-07-06 Epizyme Inc Metodo para tratar el cancer.
AU2016325643B2 (en) 2015-09-25 2022-07-21 Epizyme, Inc. Method of treating malignant rhabdoid tumor or small cell cancer of the ovary of the hypercalcemic type
KR20180058829A (ko) 2015-10-06 2018-06-01 에피자임, 인코포레이티드 Ezh2 억제제로 수모세포종을 치료하는 방법
JP2018532761A (ja) 2015-11-06 2018-11-08 エピザイム，インコーポレイティド Ｅｚｈ２阻害剤を用いた癌の処置のための小児投与
CN108697716A (zh) 2015-12-07 2018-10-23 Epizyme股份有限公司 Ezh2抑制剂及其使用方法
EP3407978A4 (en) 2016-01-29 2020-01-15 Epizyme Inc POLYTHERAPY FOR THE TREATMENT OF CANCER
WO2017139404A1 (en) 2016-02-08 2017-08-17 Epizyme, Inc. Methods of treating cancer
CA3025933A1 (en) 2016-06-01 2017-12-07 Epizyme, Inc. Use of ezh2 inhibitors for treating cancer
WO2017214373A1 (en) 2016-06-08 2017-12-14 Genentech, Inc. Diagnostic and therapeutic methods for cancer
JP2019521988A (ja) 2016-06-17 2019-08-08 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
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
JP2020522687A (ja) 2017-06-02 2020-07-30 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
WO2018231973A1 (en) 2017-06-13 2018-12-20 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
EP3678663A4 (en) 2017-09-05 2021-06-02 Epizyme, Inc. POLYTHERAPY FOR CANCER TREATMENT
CA3162315A1 (en) 2019-12-20 2021-06-24 Marinus Jacobus Verwijs Crystalline hydrobromide salt of a ezh2 inhibitor, its preparation and pharmaceutical composition useful for the treatment of cancer
CN115666725A (zh) 2020-05-28 2023-01-31 Epizyme股份有限公司 Ezh2抑制剂用于治疗癌症的用途

Also Published As

Publication number Publication date
CA3177498A1 (en) 2014-04-24
AU2020205261A1 (en) 2020-08-06
NZ746054A (en) 2020-07-31
MX376008B (es) 2025-03-07
AU2018233004A1 (en) 2018-10-11
US20250163033A1 (en) 2025-05-22
KR102021642B1 (ko) 2019-09-16
IL288181B1 (en) 2023-12-01
JP6351182B2 (ja) 2018-07-04
WO2014062720A2 (en) 2014-04-24
US20190100514A1 (en) 2019-04-04
LT2908823T (lt) 2019-10-25
US20170305889A1 (en) 2017-10-26
JP2018062535A (ja) 2018-04-19
JP2021120420A (ja) 2021-08-19
CA2887243A1 (en) 2014-04-24
JP2020011971A (ja) 2020-01-23
JP2015536308A (ja) 2015-12-21
EP2908823A2 (en) 2015-08-26
US20200262823A1 (en) 2020-08-20
IL273517A (en) 2020-05-31
PL2908823T3 (pl) 2020-03-31
US9688665B2 (en) 2017-06-27
HUE046790T2 (hu) 2020-03-30
HK1213771A1 (en) 2016-07-15
AU2020205261B2 (en) 2023-09-14
IL288181A (en) 2022-01-01
US20140128393A1 (en) 2014-05-08
MX2020010535A (es) 2020-11-06
CY1122186T1 (el) 2020-11-25
KR20230156450A (ko) 2023-11-14
IL238254A0 (en) 2015-06-30
SMT201900593T1 (it) 2019-11-13
AU2018233004B2 (en) 2020-04-16
IL308613A (en) 2024-01-01
ES2750199T3 (es) 2020-03-25
NZ706836A (en) 2019-02-22
MX2015004771A (es) 2016-01-08
WO2014062720A3 (en) 2014-06-19
JP2024029066A (ja) 2024-03-05
EP2908823B1 (en) 2019-09-25
CN105142642B (zh) 2019-10-18
CN105142642A (zh) 2015-12-09
CA2887243C (en) 2024-04-09
IL238254B (en) 2020-04-30
RU2015118144A (ru) 2016-12-10
RU2677276C2 (ru) 2019-01-16
US12162865B2 (en) 2024-12-10
US20220315566A1 (en) 2022-10-06
AU2013331368A1 (en) 2015-04-30
BR112015008447A2 (pt) 2017-07-04
HRP20191814T1 (hr) 2019-12-27
KR20190105669A (ko) 2019-09-17
US20170305890A1 (en) 2017-10-26
AU2023282217A1 (en) 2024-01-04
PT2908823T (pt) 2019-11-04
KR20150086264A (ko) 2015-07-27
RU2018145311A (ru) 2019-02-18
RS59541B1 (sr) 2019-12-31
CN110898067A (zh) 2020-03-24
EP3659606A1 (en) 2020-06-03
SI2908823T1 (sl) 2019-11-29

Similar Documents

Publication Publication Date Title
IL288181B2 (en) Methods of treating cancer
de Sena Murteira Pinheiro et al. Molecular hybridization: a powerful tool for multitarget drug discovery
Oh et al. Tuberculosis drug discovery: A decade of hit assessment for defined targets
EP2809324B1 (en) Cdk8/cdk19 selective inhibitors and their use in anti-metastatic and chemopreventive methods for cancer
US11291666B2 (en) Uses
EP3863642A1 (en) Covalent targeting of e3 ligases
EA010652B1 (ru) Замещенные индолильные алкиламинопроизводные в качестве новых ингибиторов гистондеацетилазы
EA007908B1 (ru) Карбониламинопроизводные как новые ингибиторы гистондеацетилазы
EA200870373A1 (ru) Пиридил- и пиримидинилзамещённые производные пиррола, тиофена и фурана в качестве ингибиторов киназ
EA201201161A1 (ru) Пирролопиримидины в качестве ингибиторов cdk4/6
EA006707B1 (ru) Сульфонилпроизводные в качестве новых ингибиторов гистон-деацетилазы
RS51191B (sr) Derivati aminofenila kao novi inhibitori histon deacetilaze
Suthar et al. Design and synthesis of novel 4-(4-oxo-2-arylthiazolidin-3-yl) benzenesulfonamides as selective inhibitors of carbonic anhydrase IX over I and II with potential anticancer activity
Peng et al. Stellettin B Sensitizes Glioblastoma to DNA‐Damaging Treatments by Suppressing PI3K‐Mediated Homologous Recombination Repair
Hatae et al. Antiproliferative activity of O4-benzo [c] phenanthridine alkaloids against HCT-116 and HL-60 tumor cells
AU2013243097A1 (en) Combination products with tyrosine kinase inhibitors and their use
EA011932B1 (ru) Производные замещенного пропенилпиперазина в качестве новых ингибиторов гистондеацетилазы
Sun et al. H2S scavenger as a broad-spectrum strategy to deplete bacteria-derived H2S for antibacterial sensitization
EP2819662B1 (en) Reprogramming effector protein interactions to correct epigenetic defects in cancer
WO2016054237A2 (en) Poly (adp-ribose) polymerase 1 inhibitors structurally unrelated to nad
Chen et al. A new synthetic ursolic acid derivative IUA with anti-tumor efficacy against osteosarcoma cells via inhibition of JNK signaling pathway
Song et al. Discovery of potent and selective rhodanine type IKKβ inhibitors by hit-to-lead strategy
WO2013042124A1 (en) Use of strigolactones and strigolactone analogs for treating proliferative conditions
Luo et al. Potent antitumor activity of 10-methoxy-9-nitrocamptothecin
Stubbs et al. ALK2 and JAK2 inhibition for improved treatment of anemia in myelofibrosis patients: Preclinical profile of an ALK2 inhibitor Zilurgisertib in combination with Ruxolitinib