[go: up one dir, main page]

TR201904660T4 - İnsan EZH2 inhibitörleri ve bunun kullanım yöntemleri. - Google Patents

İnsan EZH2 inhibitörleri ve bunun kullanım yöntemleri. Download PDF

Info

Publication number
TR201904660T4
TR201904660T4 TR2019/04660T TR201904660T TR201904660T4 TR 201904660 T4 TR201904660 T4 TR 201904660T4 TR 2019/04660 T TR2019/04660 T TR 2019/04660T TR 201904660 T TR201904660 T TR 201904660T TR 201904660 T4 TR201904660 T4 TR 201904660T4
Authority
TR
Turkey
Prior art keywords
methods
ezh2
inhibition
mutant forms
certain
Prior art date
Application number
TR2019/04660T
Other languages
English (en)
Inventor
Wayne Kuntz Kevin
Kathleen Knutson Sarah
James Nelson Wigle Timothy
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
Priority claimed from US13/418,242 external-priority patent/US9175331B2/en
Application filed by Epizyme Inc filed Critical Epizyme Inc
Publication of TR201904660T4 publication Critical patent/TR201904660T4/tr

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
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/4433—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
    • 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
    • A61K31/4439—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
    • 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
    • A61K31/444—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
    • 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
    • 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
    • A61K31/495—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
    • 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
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/55—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/1003—Transferases (2.) transferring one-carbon groups (2.1)
    • C12N9/1007—Methyltransferases (general) (2.1.1.)
    • 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
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57407—Specifically defined cancers
    • G01N33/57426—Specifically defined cancers leukemia
    • 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
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/52—Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Analytical Chemistry (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Pathology (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Physics & Mathematics (AREA)
  • General Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Cell Biology (AREA)
  • Neurology (AREA)
  • Food Science & Technology (AREA)
  • General Physics & Mathematics (AREA)
  • Biophysics (AREA)

Abstract

Buluş, histon H3 (H3-K27) üzerinde lizin 27?nin mono- ila tri-metilasyonunu katalize eden PRC2 kompleksinin katalitik alt birimi olan insan histon metiltransferaz EZH2?nin doğal suşu ve belli mutant formlarının inhibisyonu ile ilgilidir. Bir düzenlemede inhibisyon, belli kanserler ile bağlantılı olan H3-K27?nin trimetilasyonu inhibe edilecek şekilde EZH2?nin mutant formuna yönelik olarak selektiftir. Yöntemler, foliküler lenfoma ve diffüz büyük B hücreli lenfomayı (DLBCL) içeren kanserleri tedavi etmek üzere kullanılabilir. Ayrıca, EZH2?nin mutant formlarının küçük moleküllü selektif inhibitörlerinin tanımlanmasına yönelik yöntemler ve aynı zamanda bir öznede bir EZH2 inhibitörüne karşı yanıt verebilme yeteneğinin belirlenmesine yönelik yöntemler sağlanır.
TR2019/04660T 2012-03-12 2013-03-12 İnsan EZH2 inhibitörleri ve bunun kullanım yöntemleri. TR201904660T4 (tr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US13/418,242 US9175331B2 (en) 2010-09-10 2012-03-12 Inhibitors of human EZH2, and methods of use thereof

Publications (1)

Publication Number Publication Date
TR201904660T4 true TR201904660T4 (tr) 2019-05-21

Family

ID=47913638

Family Applications (1)

Application Number Title Priority Date Filing Date
TR2019/04660T TR201904660T4 (tr) 2012-03-12 2013-03-12 İnsan EZH2 inhibitörleri ve bunun kullanım yöntemleri.

Country Status (14)

Country Link
EP (2) EP3536314A1 (tr)
JP (2) JP6321619B2 (tr)
KR (4) KR20230145531A (tr)
CN (2) CN110420327B (tr)
AU (4) AU2013232229B2 (tr)
CA (2) CA2867282C (tr)
DK (1) DK2825161T3 (tr)
ES (1) ES2718900T3 (tr)
HU (1) HUE042271T2 (tr)
PL (1) PL2825161T3 (tr)
PT (1) PT2825161T (tr)
RU (2) RU2019132222A (tr)
TR (1) TR201904660T4 (tr)
WO (1) WO2013138361A1 (tr)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011160206A1 (en) 2010-06-23 2011-12-29 Morin Ryan D 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
EP2812001B1 (en) 2012-02-10 2017-06-14 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
SG10201608577RA (en) 2012-04-13 2016-12-29 Epizyme Inc Salt form of a human hi stone methyltransf erase ezh2 inhibitor
EP2836216B1 (en) 2012-04-13 2022-06-08 Epizyme, Inc. Combination therapy for treating cancer
CA2884848C (en) * 2012-09-28 2017-08-22 Pfizer Inc. Benzamide and heterobenzamide compounds
AU2013331368A1 (en) 2012-10-15 2015-04-30 Epizyme, Inc. Methods of treating cancer
NZ706738A (en) * 2012-10-15 2018-10-26 Epizyme Inc Substituted benzene compounds
WO2014151142A1 (en) 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP3033334A1 (en) 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
LT3057962T (lt) 2013-10-16 2023-12-11 Epizyme, Inc. Hidrochlorido druskos forma, skirta ezh2 inhibavimui
WO2015058125A1 (en) * 2013-10-18 2015-04-23 Epizyme, Inc. Method of treating cancer
ES2863996T3 (es) 2013-12-06 2021-10-13 Epizyme Inc Terapia de combinación para el tratamiento del cáncer
WO2015128837A1 (en) * 2014-02-26 2015-09-03 Glaxosmithkline Intellectual Property (No.2) Limited Methods of treating cancer patients responding to ezh2 inhibitor gsk126
JP6779793B2 (ja) * 2014-06-17 2020-11-04 エピザイム，インコーポレイティド リンパ腫を治療するためのｅｚｈ２阻害剤
AU2015276899B2 (en) 2014-06-19 2021-08-12 Memorial Sloan-Kettering Cancer Center Biomarkers for response to EZH2 inhibitors
KR102397720B1 (ko) 2014-10-16 2022-05-13 에피자임, 인코포레이티드 암을 치료하기 위한 방법
EP3885343A1 (en) 2014-11-06 2021-09-29 Dana-Farber Cancer Institute, Inc. Indole compounds as ezh2 inhibitors and uses thereof
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
US10220036B2 (en) 2014-12-23 2019-03-05 Novartis Ag Triazolopyrimidine compounds and uses thereof
WO2016172332A1 (en) * 2015-04-22 2016-10-27 The University Of North Carolina At Chapel Hill A novel compound for the treatment of ewing sarcoma and high-throughput assays for identifying small molecules that modulate aberrant chromatin accessibility
MX387885B (es) 2015-06-10 2025-03-19 Epizyme Inc Inhibidores de ezh2 para tratar linfomas.
WO2017035234A1 (en) 2015-08-24 2017-03-02 Epizyme, Inc. Method for treating cancer
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ｅｚｈ２抑制劑
US10577350B2 (en) 2015-08-28 2020-03-03 Constellation Pharmaceuticals, Inc. Crystalline forms of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
MX2018003663A (es) * 2015-09-25 2018-08-14 Epizyme Inc Metodo de tratamiento de tumor rabdoide maligno del ovario (mrto) /cancer microcitico del ovario del tipo hipercalcemico (sccoht) con un inhibidor de ezh2.
EP3371601A1 (en) * 2015-11-05 2018-09-12 Epizyme Inc Flow cytometry for monitoring histone h3 methylation status
US10633371B2 (en) * 2016-04-22 2020-04-28 Dana-Farber Cancer Institute, Inc. EZH2 inhibitors and uses thereof
EP3463355B1 (en) * 2016-05-26 2024-08-28 Sonic Master Limited Modulators of dux4 for regulation of muscle function
EP3464643A4 (en) 2016-06-01 2020-04-01 Epizyme Inc USE OF EZH2 INHIBITORS FOR THE TREATMENT OF CANCER
MA45406A (fr) 2016-06-17 2019-04-24 Epizyme Inc Inhibiteurs d'ezh2 pour traiter le cancer
CA3027246A1 (en) 2016-06-20 2017-12-28 Novartis Ag Crystalline forms of triazolopyrimidine compound
JP2019522049A (ja) 2016-06-20 2019-08-08 ノバルティス アーゲー トリアゾロピリジン化合物及びその使用
JP2019524872A (ja) 2016-06-20 2019-09-05 ノバルティス アーゲー 癌の治療に有用なイミダゾピリミジン化合物
WO2018075598A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
WO2018076060A1 (en) 2016-10-26 2018-05-03 Genea Ip Holdings Pty Ltd Improved generation of muscle lineage cells and therapeutic uses thereof
CN108699029B (zh) * 2016-11-11 2021-07-30 上海海雁医药科技有限公司 4,5,6-三取代吲唑类衍生物、其制法与医药上的用途
CN106963765B (zh) * 2017-03-28 2020-04-07 上海交通大学医学院附属第九人民医院 Ezh2抑制剂化合物在制备治疗眼部黑色素瘤的药物中的应用
US11642346B2 (en) 2017-03-31 2023-05-09 Epizyme, Inc. Combination therapy for treating cancer
AU2018275123A1 (en) 2017-06-02 2020-01-30 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
TWI785098B (zh) 2017-08-18 2022-12-01 開曼群島商科賽睿生命科學公司 Tg02之多晶型
CA3074720A1 (en) 2017-09-05 2019-03-14 Epizyme, Inc. Combination therapy for treating cancer
WO2019204998A1 (zh) * 2018-04-25 2019-10-31 北京肿瘤医院 Ezh2抑制剂在治疗粘膜型黑色素瘤中的应用
MY204088A (en) * 2018-06-03 2024-08-07 Excelsior Pharmatech Labs Method for treating non-compaction cardiomyopathy
CA3106589A1 (en) * 2018-07-27 2020-01-30 Suzhou Sinovent Pharma Co., Ltd. Polysubstituted benzene compound and preparation method and use thereof
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
CN110960525A (zh) * 2019-11-26 2020-04-07 济南大学 新型eed-ezh2相互作用抑制剂的确定和评价
CN113024516B (zh) * 2021-03-29 2022-05-17 中国药科大学 双靶点parp/ezh2抑制剂、制备方法及用途
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
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
CN119143880A (zh) * 2024-09-20 2024-12-17 上海交通大学医学院附属第九人民医院 抗ezh2蛋白抗体及其应用

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
US7700293B2 (en) * 2001-08-02 2010-04-20 The Regents Of The University Of Michigan Expression profile of prostate cancer
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
ES2324435B1 (es) * 2005-10-27 2010-05-31 Fundacion Para El Estudio De La Hematologia Y Hemoterapia De Aragon (Fehha) Procedimiento y dispositivo de analisis in vitro de mrna de genes implicados en neoplasias hematologicas.
WO2008101118A2 (en) * 2007-02-14 2008-08-21 The Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services A gene expression signature identifying pro-angiogenic genes in ovarian tumor endothelial cell isolates
WO2009006577A2 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
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
WO2012005805A1 (en) 2010-05-07 2012-01-12 Glaxosmithkline Llc Azaindazoles
US8846935B2 (en) 2010-05-07 2014-09-30 Glaxosmithkline Llc Indazoles
PT2566327T (pt) 2010-05-07 2017-05-26 Glaxosmithkline Llc Indoles
RU2765155C2 (ru) * 2010-09-10 2022-01-26 Эпизайм, Инк. Ингибиторы ezh2 человека и способы их применения
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

Also Published As

Publication number Publication date
AU2013232229B2 (en) 2017-11-23
CN110420327B (zh) 2022-05-03
JP2018083821A (ja) 2018-05-31
KR102267502B1 (ko) 2021-06-24
JP2015511603A (ja) 2015-04-20
HUE042271T2 (hu) 2019-06-28
KR20220139453A (ko) 2022-10-14
CN104540500B (zh) 2019-02-22
KR102453519B1 (ko) 2022-10-11
RU2704445C2 (ru) 2019-10-28
PT2825161T (pt) 2019-04-29
JP6592071B2 (ja) 2019-10-16
AU2013232229A1 (en) 2014-10-02
HK1205938A1 (en) 2015-12-31
PL2825161T3 (pl) 2019-06-28
AU2018201176A1 (en) 2018-03-08
CA3177515A1 (en) 2013-09-19
RU2014141045A (ru) 2016-05-10
KR20210079384A (ko) 2021-06-29
DK2825161T3 (en) 2019-04-08
AU2021202119A1 (en) 2021-05-06
WO2013138361A1 (en) 2013-09-19
CA2867282C (en) 2024-04-02
CA2867282A1 (en) 2013-09-19
EP2825161A1 (en) 2015-01-21
AU2019250181A1 (en) 2019-11-07
EP3536314A1 (en) 2019-09-11
KR102587175B1 (ko) 2023-10-06
CN110420327A (zh) 2019-11-08
JP6321619B2 (ja) 2018-05-09
EP2825161B1 (en) 2019-01-02
CN104540500A (zh) 2015-04-22
RU2019132222A (ru) 2021-06-03
KR20140147836A (ko) 2014-12-30
KR20230145531A (ko) 2023-10-17
ES2718900T3 (es) 2019-07-05

Similar Documents

Publication Publication Date Title
TR201904660T4 (tr) İnsan EZH2 inhibitörleri ve bunun kullanım yöntemleri.
WO2012034132A3 (en) Inhibitors of human ezh2, and methods of use thereof
PH12021550758A1 (en) The use of inhibitors of bruton`s tyrosine kinase (btk)
ECSP13012461A (es) Ensayos biomarcadores para detectar o medir inhibición de actividad quinasa tor
PH12020500103A1 (en) Use of cas protein, method for detecting target nucleic acid molecule, and kit
EP3734281A3 (en) Therapeutic and diagnostic methods relating to cancer stem cells
TR201907783T4 (tr) Benzosulfonamit türevleri, bileşimleri ve kanser hücrelerinin metastazının önlenmesinde kullanımları.
BR112014007821A2 (pt) método para determinar a localização, tamanho, e composição fluida de um acúmulo de hidrocarboneto abaixo da superfície
TN2012000485A1 (en) Predictive markers useful in the treatment of fragile x syndrome (fxs)
WO2012061510A3 (en) Methods of predicting cancer cell response to therapeutic agents
PH12013502490A1 (en) Lysyl oxidase-like 2 assay and methods of use thereof
BR112012007555A2 (pt) biomarcadores para prever a sensibilidade e resposta de doenças mediadas por quinase de proteína ck2 a inibidores de ck2
MX371379B (es) Deteccion de la actividad de corte de una enzima.
DE602005016800D1 (de) Hif-prolylhydroxylase-aktivitätstest
GB201206977D0 (en) An enzyme detection device
BR112015012331A2 (pt) autenticação social
EA201401201A1 (ru) Способ
BR112017011903A2 (pt) processo para avaliação do desempenho catalítico de um sólido poroso
BR112016004450A2 (pt) métodos para tratar uma doença, para aumentar a eficácia de um tratamento, para adiar e/ou prevenir desenvolvimento da reincidência e/ou resistência de uma doença, para aumentar a sensibilidade a um inibidor, para estender o período de sensibilidade a um inibidor e para estender a duração de resposta a um inibidor
BR112012017221B8 (pt) método para o processamento de dados de subsuperfície, e sistema para processamento de dados de subsuperfície
AR104805A1 (es) Métodos y composiciones para evaluar la capacidad de respuesta de los cánceres a los inhibidores de bet
BRPI0513596A (pt) anticorpo enriquecido para detecção de infecção micobacteriana, métodos de uso e teste diagnóstico empregando o mesmo
WO2009094556A3 (en) Identification of predictive markers of response to dasatinib in human colon cancer
WO2015157624A3 (en) A novel isoform of anaplastic lymphoma kinase and its uses
MX373640B (es) Ensayos de aclaramiento de sustratos para enzimas lisosomales.