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JO3438B1 - مركبات بنزين مستبدلة بأريل أو أريل غير متجانس - Google Patents

مركبات بنزين مستبدلة بأريل أو أريل غير متجانس

Info

Publication number
JO3438B1
JO3438B1 JOP/2018/0104A JOP20180104A JO3438B1 JO 3438 B1 JO3438 B1 JO 3438B1 JO P20180104 A JOP20180104 A JO P20180104A JO 3438 B1 JO3438 B1 JO 3438B1
Authority
JO
Jordan
Prior art keywords
compounds
heteroaryl
aryl substituted
relates
present
Prior art date
Application number
JOP/2018/0104A
Other languages
English (en)
Inventor
K Knutson Sarah
Natalie Warholic
Syuji Shirotori
Christine Klaus
Richard Chesworth
Kenneth William Duncan
Kevin Wayne Kuntz
Masashi Seki
Heike Keilhack
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46045109&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JO3438(B1) "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 JOP20180104A1 publication Critical patent/JOP20180104A1/ar
Application granted granted Critical
Publication of JO3438B1 publication Critical patent/JO3438B1/ar

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • 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
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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—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
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring

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  • Animal Behavior & Ethology (AREA)
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Abstract

يتعلق الاختراع الحالي بمركبات بنزين بها استبدال بأريل أو أريل غير متجانسة. كما يتعلق الاختراع الحالي بتركيبات صيدلانية تحتوي على هذه المركبات وطرق لعلاج السرطان عن طريق إعطاء هذه المركبات والتركيبات الصيدلانية إلى حالات مرضية في حاجة إليها. كما يتعلق الاختراع الحالي باستخدام هذه المركبات بغرض البحث أو أغراض أخرى غير علاجية.
JOP/2018/0104A 2011-04-13 2011-04-13 مركبات بنزين مستبدلة بأريل أو أريل غير متجانس JO3438B1 (ar)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
JOP20180104A1 JOP20180104A1 (ar) 2019-01-30
JO3438B1 true JO3438B1 (ar) 2019-10-20

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Families Citing this family (114)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130102477A1 (en) 2010-06-23 2013-04-25 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
US9175331B2 (en) * 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
DK2614369T3 (en) 2010-09-10 2016-05-02 Epizyme Inc METHOD FOR DETERMINING THE SUITABILITY OF HUMAN EZH2 INHIBITORS TREATED
TWI598336B (zh) 2011-04-13 2017-09-11 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
KR20140082742A (ko) * 2011-09-30 2014-07-02 글락소스미스클라인 엘엘씨 암을 치료하는 방법
US9051269B2 (en) 2011-11-18 2015-06-09 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
PL2825161T3 (pl) * 2012-03-12 2019-06-28 Epizyme, Inc. Inhibitory ludzkiej ezh2 i sposoby ich zastosowania
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
IL282732B2 (en) * 2012-04-13 2023-04-01 Eisai R&D Man Co Ltd Salt form of human histone methyltransferase inhibitor 2ezh
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
EP2900653A1 (en) * 2012-09-28 2015-08-05 Pfizer Inc. Benzamide and heterobenzamide compounds
ES2750199T3 (es) * 2012-10-15 2020-03-25 Epizyme Inc Métodos para tratar el cáncer
JP6461803B2 (ja) 2012-10-15 2019-01-30 エピザイム，インコーポレイティド 置換ベンゼン化合物
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
US20150344427A1 (en) * 2012-12-21 2015-12-03 Epizyme, Inc. 1,4-pyridone compounds
AU2013361079B2 (en) 2012-12-21 2018-07-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
SG11201506077XA (en) * 2013-02-11 2015-08-28 Constellation Pharmaceuticals Inc Modulators of methyl modifying enzymes, compositions and uses thereof
CA2903264A1 (en) 2013-03-14 2014-11-06 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
WO2014153235A2 (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
EP2970136A1 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Arginine methyl transferase inhibtors and uses thereof
WO2014153208A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153226A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US20160039767A1 (en) 2013-03-14 2016-02-11 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
WO2014153100A2 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153172A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
EP2970135B1 (en) 2013-03-14 2018-07-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
WO2014153030A2 (en) 2013-03-14 2014-09-25 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
US9243001B2 (en) 2013-03-15 2016-01-26 Epizyme, Inc. Substituted benzene compounds
EP2970305B1 (en) 2013-03-15 2017-02-22 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2014172044A1 (en) 2013-03-15 2014-10-23 Epizyme, Inc. Substituted benzene compounds
AU2014261075B2 (en) 2013-04-30 2017-01-19 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
EP3004096A1 (en) * 2013-06-06 2016-04-13 Glaxosmithkline Intellectual Property (No. 2) Limited Enhancer of zeste homolog 2 inhibitors
CA2917463A1 (en) * 2013-07-10 2015-01-15 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
US10150764B2 (en) 2013-07-19 2018-12-11 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
EP3076977B1 (en) 2013-12-06 2021-03-03 Epizyme, Inc. Combination therapy for treating cancer
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
MY185765A (en) * 2014-06-17 2021-06-06 Pfizer Substituted dihydroisoquinolinone compounds
ES2948442T3 (es) 2014-06-17 2023-09-12 Epizyme Inc Inhibidores de EZH2 para el tratamiento de linfoma
EP3160940A4 (en) 2014-06-25 2018-05-02 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
MX383635B (es) 2014-10-16 2025-03-14 Epizyme Inc Método para tratar el cáncer.
EP3212639A1 (en) * 2014-10-28 2017-09-06 Glaxosmithkline Intellectual Property (No. 2) Limited Enhancer of zeste homolog 2 inhibitors
CN113444086B (zh) 2014-11-06 2024-04-30 达纳-法伯癌症研究所股份有限公司 Ezh2抑制剂及其用途
CN116650500A (zh) 2014-11-17 2023-08-29 Epizyme股份有限公司 治疗癌症的方法
AR102767A1 (es) 2014-12-05 2017-03-22 Lilly Co Eli Inhibidores de ezh2
US10456407B2 (en) 2015-04-20 2019-10-29 Epizyme, Inc. Combination therapy for treating cancer
AU2016275051A1 (en) 2015-06-10 2017-12-07 Epizyme, Inc. EZH2 inhibitors for treating lymphoma
UY36758A (es) * 2015-06-30 2016-12-30 Glaxosmithkline Ip No 2 Ltd Inhibidores del potenciador del homólogo zeste 2
US10493076B2 (en) 2015-08-24 2019-12-03 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
CA3000983A1 (en) 2015-10-06 2017-04-13 The Regents Of The University Of Colorado, A Body Corporate Method of treating medulloblastoma with an ezh2 inhibitor
EP3359542B1 (en) 2015-10-09 2021-03-17 Boehringer Ingelheim International GmbH Spiro[3h-indole-3,2´-pyrrolidin]-2(1h)-one compounds and derivatives as mdm2-p53 inhibitors
EP3370725A4 (en) * 2015-11-06 2019-07-03 Epizyme, Inc. PEDIATRIC DOSAGE FOR THE TREATMENT OF CANCER WITH AN EZH2 INHIBITOR
MX380122B (es) 2015-11-19 2025-03-11 Jiangsu Hengrui Medicine Co Derivado benzofurano, su metodo de preparacion, y sus usos en medicinas.
CN105440023A (zh) * 2015-12-10 2016-03-30 江苏理工学院 Epz-6438的合成方法
TW202246215A (zh) 2015-12-18 2022-12-01 美商亞德利克斯公司 作為非全身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
JP2019503391A (ja) 2016-01-29 2019-02-07 エピザイム，インコーポレイティド 癌を処置するための併用療法
IL261721B (en) 2016-03-15 2022-07-01 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
WO2017174023A1 (zh) * 2016-04-08 2017-10-12 南京明德新药研发股份有限公司 作为ezh2抑制剂的联苯化合物
CA3018270A1 (en) * 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
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
CR20180521A (es) 2016-05-05 2019-01-15 Glaxosmithkline Ip No 2 Ltd Inhibidores del potenciador del homólogo zeste 2
AU2017273726B2 (en) 2016-06-01 2023-10-19 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
MA45406A (fr) 2016-06-17 2019-04-24 Epizyme Inc Inhibiteurs d'ezh2 pour traiter le cancer
CA3039059A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
US20200078362A1 (en) 2016-12-02 2020-03-12 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
BR112019014924A2 (pt) * 2017-01-19 2020-03-31 St. Marianna University School Of Medicine Composição farmacêutica usada para o tratamento de mielopatia associada ao htlv-1
CN110191879A (zh) * 2017-01-25 2019-08-30 恩瑞生物医药科技（上海）有限公司 一种组蛋白甲基转移酶ezh2抑制剂、其制备方法及其医药用途
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
WO2018183885A1 (en) 2017-03-31 2018-10-04 Epizyme, Inc. Combination therapy for treating cancer
CN118021814A (zh) * 2017-04-21 2024-05-14 Epizyme股份有限公司 用ehmt2抑制剂进行的组合疗法
KR102612379B1 (ko) 2017-05-18 2023-12-12 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 벤조푸란 유도체 자유 염기의 결정 및 제조 방법
CN110944628A (zh) 2017-06-02 2020-03-31 Epizyme股份有限公司 使用ezh2抑制剂治疗癌症
US20230201212A1 (en) 2017-06-13 2023-06-29 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
CA3074720A1 (en) * 2017-09-05 2019-03-14 Epizyme, Inc. Combination therapy for treating cancer
SG11202003477QA (en) 2017-11-14 2020-05-28 Pfizer Ezh2 inhibitor combination therapies
PL3746446T3 (pl) 2018-01-31 2022-08-29 Mirati Therapeutics, Inc. Inhibitory PRC2
CN108640842B (zh) * 2018-04-04 2021-06-04 大连九信精细化工有限公司 一种2-溴-5-氟硝基苯的合成方法
WO2019236436A1 (en) * 2018-06-07 2019-12-12 Merck Sharp & Dohme Corp. Processes for the preparation of sugammadex
CN112399857A (zh) 2018-07-09 2021-02-23 盲人庇护基金会 Prc2亚单位的抑制治疗眼失调
CN111683936B (zh) * 2018-07-27 2021-08-20 苏州信诺维医药科技股份有限公司 多取代苯环化合物、制备方法及其用途
KR102689665B1 (ko) 2019-02-19 2024-07-31 한미약품 주식회사 신규한 헤테로트리시클릭 유도체 화합물 및 이의 용도
JP7396369B2 (ja) * 2019-03-25 2023-12-12 上海華匯拓医薬科技有限公司 アミド系化合物の調製方法及びその医学分野での使用
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
EP3980422A1 (en) 2019-06-05 2022-04-13 Mirati Therapeutics, Inc. Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer
CN114555112A (zh) 2019-08-22 2022-05-27 朱诺治疗学股份有限公司 T细胞疗法和zeste增强子同源物2(ezh2)抑制剂的组合疗法及相关方法
CN115551842B (zh) * 2020-06-08 2024-04-23 南京明德新药研发有限公司 联苯类化合物
EP4556479A1 (en) 2020-08-13 2025-05-21 Hanmi Pharmaceutical Co., Ltd. Novel dioxoloisoquinolinone derivatives and use thereof
CA3195479A1 (en) * 2020-10-13 2022-04-21 Xufan WANG Crystal form of multi-substituted benzene ring compound maleate, and preparation method therefor and use thereof
CN114907300B (zh) * 2021-02-08 2024-05-28 上海医药工业研究院 他泽司他关键中间体的制备方法及其中间体
CN114907299B (zh) * 2021-02-08 2024-06-25 上海医药工业研究院 他泽司他关键中间体的盐型、其制备方法及其中间体
CN113292489B (zh) * 2021-06-16 2022-08-30 泓博智源(开原)药业有限公司 二氯代二烷基烟腈的制备方法
CN113527275A (zh) * 2021-07-20 2021-10-22 成都师范学院 一种sklb1039化合物及其制备方法和应用
CN113582863B (zh) * 2021-08-19 2023-05-26 沈阳农业大学 一种氨乙基联苯类化合物及其制备方法和用途
KR20230081459A (ko) 2021-11-30 2023-06-07 엘젠테라퓨틱스 주식회사 헤테로사이클릭이 치환된 신규한 3-페닐피리딘과 4-페닐피리딘 유도체 및 이의 용도
WO2023111810A1 (en) 2021-12-14 2023-06-22 Pfizer Inc. Combination therapies and uses for treating cancer
EP4514391A1 (en) 2022-04-27 2025-03-05 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate with ezh1 and/or ezh2 inhibitor
EP4536649A1 (en) 2022-06-13 2025-04-16 Treeline Biosciences, Inc. Quinolone bcl6 bifunctional degraders
IL317217A (en) 2022-06-13 2025-01-01 Treeline Biosciences Inc BCL6 heterobifunctional 8,1-naphthyridin-2-one joints
CN115197202B (zh) * 2022-07-15 2024-01-26 四川大学 一种ezh2共价抑制剂及其制备方法和应用

Family Cites Families (106)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
JPH0733729A (ja) 1993-07-26 1995-02-03 Kirin Brewery Co Ltd Ｎ−シアノ−ｎ′−置換−アリールカルボキシイミダミド化合物の製造法
KR100189863B1 (ko) 1993-12-27 1999-06-01 나이또 하루오 안트라닐산 유도체
DE19516776A1 (de) 1995-05-10 1996-11-14 Boehringer Ingelheim Int Chromatin-Regulatorgene
US5741819A (en) 1995-06-07 1998-04-21 3-Dimensional Pharmaceuticals, Inc. Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
JP3906935B2 (ja) 1995-12-18 2007-04-18 杏林製薬株式会社 Ｎ−置換ジオキソチアゾリジルベンズアミド誘導体及びその製造法
BR9914207A (pt) 1998-09-30 2001-07-03 Procter & Gamble Ceto-amidas 2-substituìdas
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
WO2002053543A1 (fr) 2000-12-28 2002-07-11 Shionogi & Co., Ltd. Derive de pyridone ayant une affinite pour le recepteur cannabinoide de type 2
EP1363702A4 (en) * 2001-01-30 2007-08-22 Cytopia Pty Ltd PROCESS FOR INHIBITING KINASES
US7700293B2 (en) 2001-08-02 2010-04-20 The Regents Of The University Of Michigan Expression profile of prostate cancer
EP1465869B1 (en) 2001-12-21 2013-05-15 Exelixis Patent Company LLC Modulators of lxr
EP1477186B1 (en) 2002-02-19 2009-11-11 Shionogi & Co., Ltd. Antipruritics
TW200306155A (en) 2002-03-19 2003-11-16 Du Pont Benzamides and advantageous compositions thereof for use as fungicides
BRPI0317740B8 (pt) 2002-12-27 2021-05-25 Sucampo Ag uso do composto 13,14-diidro-15-ceto-16,16-diflúorprostaglandina e1
EA010727B1 (ru) * 2003-02-26 2008-10-30 Суджен, Инк. Аминогетероарильные соединения в качестве ингибиторов протеинкиназ
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
ES2374272T3 (es) 2003-06-19 2012-02-15 Glaxosmithkline Llc Derivados de 5-(acilamino)indazol como inhibidores de quinasas.
US8637553B2 (en) * 2003-07-23 2014-01-28 Bayer Healthcare Llc Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions
DE602004026321D1 (de) 2003-08-26 2010-05-12 Merck Hdac Res Llc Verwendung von SAHA zur Behandlung von Mesotheliom
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
ATE449168T1 (de) 2004-06-01 2009-12-15 Univ North Carolina Rekonstituierter histon-methyltransferase-komplex und verfahren zur identifizierung von modulatoren dafür
JO2787B1 (ar) 2005-04-27 2014-03-15 امجين إنك, مشتقات الاميد البديلة وطرق استخدامها
WO2006130720A2 (en) 2005-06-02 2006-12-07 University Of North Carolina At Chapel Hill Purification, characterization and reconstitution of a ubiquitin e3 ligase
FR2889526B1 (fr) 2005-08-04 2012-02-17 Aventis Pharma Sa 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation
US8710233B2 (en) 2005-10-19 2014-04-29 Gruenenthal Gmbh Vanilloid receptor ligands and use thereof for the production of pharmaceutical preparations
WO2007050347A1 (en) 2005-10-21 2007-05-03 Merck & Co., Inc. Potassium channel inhibitors
AU2006308957B2 (en) 2005-10-28 2012-04-12 The University Of North Carolina At Chapel Hill Protein demethylases comprising a JmjC domain
CA2631236C (en) 2005-12-01 2019-10-29 Medical Prognosis Institute Methods and devices for identifying biomarkers of treatment response and use thereof to predict treatment efficacy
US8163749B2 (en) 2005-12-14 2012-04-24 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
EP2730661A1 (en) 2006-01-20 2014-05-14 The University of North Carolina at Chapel Hill Diagnostic and therapeutic targets for leukemia
US20100016379A1 (en) 2006-05-15 2010-01-21 Irm Llc Terephthalamate Compounds and Compositions, and Their Use as HIV Integrase Inhibitors
EP2040711A2 (en) 2006-05-18 2009-04-01 Amphora Discovery Corporation 2-oxo-1,2-dihydroquinoline derivatives, compositions, and uses thereof as antiproliferative agents
JP2010505958A (ja) 2006-10-10 2010-02-25 バーンハム インスティトゥート フォー メディカル リサーチ 神経防護作用組成物および方法
AU2008219166B2 (en) * 2007-02-16 2013-05-16 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors
WO2008104077A1 (en) 2007-02-28 2008-09-04 Methylgene Inc. Small molecule inhibitors of protein arginine methyltransferases (prmts)
WO2008109534A1 (en) * 2007-03-02 2008-09-12 Mdrna, Inc. Nucleic acid compounds for inhibiting ezh2 gene expression and uses thereof
WO2008113006A1 (en) 2007-03-14 2008-09-18 Xenon Pharmaceuticals Inc. Methods of using quinolinone compounds in treating sodium channel-mediated diseases or conditions
DE102007017884A1 (de) 2007-04-13 2008-10-16 Grünethal GmbH Neue Vanilloid-Rezeptor Liganden und ihre Verwendung zur Herstellung von Arzneimitteln
US20090012031A1 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan EZH2 Cancer Markers
CN101754955A (zh) 2007-07-16 2010-06-23 雅培制药有限公司 作为蛋白激酶抑制剂的吲唑、苯并异*唑和苯并异噻唑化合物
EP2215049B1 (en) * 2007-10-31 2019-06-12 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
CN101945869B (zh) 2007-12-19 2014-06-18 癌症研究技术有限公司 吡啶并[2,3-b]吡嗪-8-取代化合物及其用途
KR101608096B1 (ko) * 2008-01-23 2016-03-31 브리스톨-마이어스 스큅 컴퍼니 ４-피리디논 화합물 및 암을 위한 그의 용도
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
EP2335779A1 (en) 2008-08-08 2011-06-22 New York Blood Center Small Molecule Inhibitors of Retroviral Assembly & Maturation
FR2934995B1 (fr) 2008-08-14 2010-08-27 Sanofi Aventis Composes d'azetidines polysubstitues, leur preparation et leur application en therapeutique
AU2009342734A1 (en) * 2009-03-24 2011-10-13 Sanofi 9H-pyrrolo[2,3-b: 5,4-c'] dipyridine azacarboline derivatives, preparation thereof, and therapeutic use thereof
EP2411007A4 (en) 2009-03-27 2012-12-05 Uab Research Foundation MODULATION OF MEDIATION TRANSLATION BY IRES SEQUENCES
US20110021362A1 (en) 2009-07-20 2011-01-27 Constellation Pharmaceuticals Agents for stimulating activity of methyl modifying enzymes and methods of use thereof
US8329149B2 (en) 2009-12-30 2012-12-11 Avon Products, Inc. Topical lightening composition and uses thereof
HUE034787T2 (en) * 2010-05-07 2018-02-28 Glaxosmithkline Llc Indoles
JP5889875B2 (ja) 2010-05-07 2016-03-22 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ アザインダゾール
US8846935B2 (en) * 2010-05-07 2014-09-30 Glaxosmithkline Llc Indazoles
US20130102477A1 (en) 2010-06-23 2013-04-25 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
DK2614369T3 (en) 2010-09-10 2016-05-02 Epizyme Inc METHOD FOR DETERMINING THE SUITABILITY OF HUMAN EZH2 INHIBITORS TREATED
WO2012068589A2 (en) 2010-11-19 2012-05-24 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
EP2646020B1 (en) 2010-12-01 2016-09-21 Glaxosmithkline LLC Indoles
AU2011336272A1 (en) 2010-12-03 2013-06-20 Epizyme, Inc. 7-deazapurine modulators of histone methyltransferase, and methods of use thereof
EP3323820B1 (en) 2011-02-28 2023-05-10 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
TWI598336B (zh) 2011-04-13 2017-09-11 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
KR20140082742A (ko) 2011-09-30 2014-07-02 글락소스미스클라인 엘엘씨 암을 치료하는 방법
PL2825161T3 (pl) 2012-03-12 2019-06-28 Epizyme, Inc. Inhibitory ludzkiej ezh2 i sposoby ich zastosowania
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
IL282732B2 (en) 2012-04-13 2023-04-01 Eisai R&D Man Co Ltd Salt form of human histone methyltransferase inhibitor 2ezh
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
ES2750199T3 (es) 2012-10-15 2020-03-25 Epizyme Inc Métodos para tratar el cáncer
JP6461803B2 (ja) 2012-10-15 2019-01-30 エピザイム，インコーポレイティド 置換ベンゼン化合物
AU2013361079B2 (en) 2012-12-21 2018-07-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
US9243001B2 (en) 2013-03-15 2016-01-26 Epizyme, Inc. Substituted benzene compounds
WO2014144747A1 (en) 2013-03-15 2014-09-18 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
US9045477B2 (en) 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
US9624205B2 (en) 2013-07-19 2017-04-18 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
US10150764B2 (en) 2013-07-19 2018-12-11 Epizyme, Inc. Substituted benzene compounds
SG11201602269QA (en) 2013-10-16 2016-04-28 Epizyme Inc Hydrochloride salt form for ezh2 inhibition
EP3076977B1 (en) 2013-12-06 2021-03-03 Epizyme, Inc. Combination therapy for treating cancer
ES2948442T3 (es) 2014-06-17 2023-09-12 Epizyme Inc Inhibidores de EZH2 para el tratamiento de linfoma
MX383635B (es) 2014-10-16 2025-03-14 Epizyme Inc Método para tratar el cáncer.
CN116650500A (zh) 2014-11-17 2023-08-29 Epizyme股份有限公司 治疗癌症的方法
US10456407B2 (en) 2015-04-20 2019-10-29 Epizyme, Inc. Combination therapy for treating cancer
AU2016275051A1 (en) 2015-06-10 2017-12-07 Epizyme, Inc. EZH2 inhibitors for treating lymphoma
US10493076B2 (en) 2015-08-24 2019-12-03 Epizyme, Inc. Method for treating cancer
CN108349958B (zh) 2015-09-25 2022-02-15 Epizyme股份有限公司 用ezh2抑制剂治疗mrto/sccoht的方法
EP3674709A1 (en) 2015-11-05 2020-07-01 Epizyme Inc Flow cytometry for monitoring histone h3 methylation status
CA3007492A1 (en) 2015-12-07 2017-06-15 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
JP2019503391A (ja) 2016-01-29 2019-02-07 エピザイム，インコーポレイティド 癌を処置するための併用療法
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
AU2017273726B2 (en) 2016-06-01 2023-10-19 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
MA45406A (fr) 2016-06-17 2019-04-24 Epizyme Inc Inhibiteurs d'ezh2 pour traiter le cancer
US20200078362A1 (en) 2016-12-02 2020-03-12 Epizyme, Inc. Combination therapy for treating cancer
AU2018217139A1 (en) 2017-02-02 2019-08-22 Epizyme, Inc. Cancer treatment modalities
WO2018183885A1 (en) 2017-03-31 2018-10-04 Epizyme, Inc. Combination therapy for treating cancer
CN110944628A (zh) 2017-06-02 2020-03-31 Epizyme股份有限公司 使用ezh2抑制剂治疗癌症
US20230201212A1 (en) 2017-06-13 2023-06-29 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
CA3074720A1 (en) 2017-09-05 2019-03-14 Epizyme, Inc. Combination therapy for treating 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
CA3177444A1 (en) 2020-05-28 2021-12-02 Carly CAMPBELL Use of ezh2 inhibitors for treating cancer

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