TW201733984A - 經取代之苯化合物 - Google Patents

經取代之苯化合物 Download PDF

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Publication number
TW201733984A
TW201733984A TW106103833A TW106103833A TW201733984A TW 201733984 A TW201733984 A TW 201733984A TW 106103833 A TW106103833 A TW 106103833A TW 106103833 A TW106103833 A TW 106103833A TW 201733984 A TW201733984 A TW 201733984A
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TW
Taiwan
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group
alkyl
cycloalkyl
membered heterocycloalkyl
optionally substituted
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TW106103833A
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English (en)
Chinese (zh)
Inventor
凱文 光斯
理查 雀思沃斯
肯尼斯 鄧肯
海克 肯亥克
克里斯汀 克勞斯
納塔利 渥哈利克
莎瑞 康納森
關雅史
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雅酶股份有限公司
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Publication of TW201733984A publication Critical patent/TW201733984A/zh

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    • 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
    • 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
    • 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
    • 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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Peptides Or Proteins (AREA)
TW106103833A 2011-04-13 2012-04-12 經取代之苯化合物 TW201733984A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161474825P 2011-04-13 2011-04-13
US201161505676P 2011-07-08 2011-07-08

Publications (1)

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TW201733984A true TW201733984A (zh) 2017-10-01

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TW106103833A TW201733984A (zh) 2011-04-13 2012-04-12 經取代之苯化合物
TW101112996A TWI598336B (zh) 2011-04-13 2012-04-12 經取代之苯化合物

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US (2) US9376422B2 (enExample)
EP (3) EP3165520B1 (enExample)
JP (1) JP2014513084A (enExample)
KR (1) KR101975613B1 (enExample)
CN (1) CN104066718B (enExample)
AR (1) AR086839A1 (enExample)
AU (2) AU2012242604B2 (enExample)
BR (1) BR112013026308B1 (enExample)
CA (1) CA2832846C (enExample)
DK (1) DK2697198T3 (enExample)
ES (1) ES2590489T3 (enExample)
HK (1) HK1202534A1 (enExample)
HU (1) HUE030722T2 (enExample)
IL (1) IL228746B (enExample)
MX (1) MX344530B (enExample)
PL (1) PL2697198T3 (enExample)
PT (1) PT2697198T (enExample)
RU (2) RU2629118C2 (enExample)
TW (2) TW201733984A (enExample)
WO (1) WO2012142513A1 (enExample)

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2841142C (en) 2010-06-23 2020-12-15 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
AU2011298987B2 (en) 2010-09-10 2017-09-28 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
WO2013075084A1 (en) * 2011-11-18 2013-05-23 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
US9085583B2 (en) 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
IL308807B2 (en) 2012-04-13 2025-08-01 Epizyme Inc Combination therapy for treating cancer
DK3184523T3 (da) 2012-04-13 2019-08-19 Epizyme Inc N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4' -(morphofinomethyl)-[1,1'-biphenyl]-3-carboxamidhydrobromid til anvendelse i behandlingen af en sygdom med celleproliferation i det hæmatologiske system.
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
US20150239842A1 (en) * 2012-09-28 2015-08-27 Pfizer Inc. Benzamide and heterobenzamide compounds
PE20150886A1 (es) * 2012-10-15 2015-06-04 Epizyme Inc Compuestos de benceno sustituidos
CN110898067A (zh) * 2012-10-15 2020-03-24 Epizyme股份有限公司 癌症治疗方法
TWI494424B (zh) * 2012-11-20 2015-08-01 Dow Global Technologies Llc 可蒸餾燃料標記物
BR112015014090A2 (pt) * 2012-12-13 2017-07-11 Glaxosmithkline Llc intensificador de inibidores de zeste homólogo 2
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
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
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
BR112015022785A2 (pt) 2013-03-14 2017-07-18 Epizyme Inc composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt
US9765035B2 (en) 2013-03-14 2017-09-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153208A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153100A2 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153090A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives asprmt1 inhibitors and uses thereof
WO2014178954A1 (en) 2013-03-14 2014-11-06 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
WO2014144659A1 (en) 2013-03-14 2014-09-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
WO2014153172A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
RS59790B1 (sr) 2013-03-15 2020-02-28 G1 Therapeutics Inc Privremena zaštita normalnih ćelija tokom hemoterapije
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2970281A4 (en) * 2013-03-15 2016-08-03 Epizyme Inc SUBSTITUTED BENZOL COMPOUNDS
ES2717680T3 (es) 2013-04-30 2019-06-24 Glaxosmithkline Ip No 2 Ltd Potenciador de inhibidores del homólogo de Zeste 2
US9556157B2 (en) 2013-07-10 2017-01-31 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
US9624205B2 (en) 2013-07-19 2017-04-18 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2015010049A1 (en) * 2013-07-19 2015-01-22 Epizyme, Inc. Substituted benzene compounds
EP3033334A1 (en) 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
SG11201602269QA (en) 2013-10-16 2016-04-28 Epizyme Inc Hydrochloride salt form for ezh2 inhibition
WO2015077193A1 (en) * 2013-11-19 2015-05-28 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
WO2015077194A1 (en) * 2013-11-22 2015-05-28 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
CN116019921A (zh) 2013-12-06 2023-04-28 Epizyme股份有限公司 用于治疗癌症的组合疗法
PE20161552A1 (es) 2014-06-17 2017-01-11 Pfizer Compuestos de dihidroisoquinolinona sustituida
PL3157527T3 (pl) 2014-06-17 2023-08-07 Epizyme, Inc. Inhibitory ezh2 do leczenia chłoniaka
WO2015200650A1 (en) 2014-06-25 2015-12-30 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
CN106794177A (zh) 2014-10-16 2017-05-31 Epizyme股份有限公司 治疗癌症的方法
RU2017118165A (ru) * 2014-10-28 2018-11-29 Глэксосмитклайн Интеллекчуал Проперти (Но.2) Лимитед Ингибиторы энхансера гомолога 2 zestes
BR112017010166A2 (en) 2014-11-17 2018-02-14 Epizyme, Inc. solid tumor treatment method, activity inhibition method, oral dosage form for treating a solid tumor, solid pharmaceutical formulation, process for preparing a pharmaceutical formulation, and solid pharmaceutical composition
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ｅｚｈ２抑制劑
US20180271857A1 (en) 2014-12-23 2018-09-27 University Of Copenhagen Treatment of cancer by inhibiting ezh2 activity
CN108135908A (zh) 2015-04-20 2018-06-08 Epizyme股份有限公司 用于治疗癌症的组合疗法
WO2016187394A1 (en) * 2015-05-19 2016-11-24 Van Wijnen Andre J Methods and materials for promoting bone formation
JP6890097B2 (ja) 2015-06-10 2021-06-18 エピザイム，インコーポレイティド リンパ腫を処置するためのｅｚｈ２阻害剤
CA2996412A1 (en) 2015-08-24 2017-03-02 Epizyme, Inc. Method for treating cancer
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
LT3378859T (lt) * 2015-11-19 2020-01-27 Jiangsu Hengrui Medicine Co., Ltd. Benzofurano darinys, jo gavimo būdas ir jo panaudojimas medicinoje
US12084472B2 (en) 2015-12-18 2024-09-10 Ardelyx, Inc. Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists
TWI773657B (zh) 2015-12-18 2022-08-11 美商亞德利克斯公司 作爲非全身ｔｇｒ５促效劑之經取代之4-苯基吡啶化合物
CA3011186A1 (en) 2016-01-29 2017-08-03 Epizyme, Inc. Combination therapy for treating cancer
AU2017251555B2 (en) * 2016-04-14 2021-04-29 Guangzhou Joyo Pharmatech Co., Ltd Pyridone derivative comprising heteroatomic ring butane substituent, for treating fibrosis and inflammatory diseases
JP7121660B2 (ja) 2016-06-01 2022-08-18 エピザイム，インコーポレイティド 癌を処置するためのｅｚｈ２阻害剤の使用
WO2017218953A1 (en) 2016-06-17 2017-12-21 Epizyme, Inc. Ezh2 inhibitors for treating cancer
WO2018075598A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
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
US11214561B2 (en) 2017-01-25 2022-01-04 Ancureall Pharmaceutical (Shanghai) Co., Ltd. Histone methyltransferase EZH2 inhibitor, preparation method and pharmaceutical use thereof
US11395821B2 (en) 2017-01-30 2022-07-26 G1 Therapeutics, Inc. Treatment of EGFR-driven cancer with fewer side effects
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
WO2018183885A1 (en) 2017-03-31 2018-10-04 Epizyme, Inc. Combination therapy for treating cancer
CN110621316B (zh) * 2017-04-21 2024-01-26 Epizyme股份有限公司 用ehmt2抑制剂进行的组合疗法
JP7257328B2 (ja) 2017-05-18 2023-04-13 ジエンス ヘンルイ メデイシンカンパニー リミテッド ベンゾフラン誘導体遊離塩基の結晶およびその製造方法
US11602529B2 (en) 2017-06-02 2023-03-14 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
WO2019050924A1 (en) 2017-09-05 2019-03-14 Epizyme, Inc. POLY THERAPY FOR THE TREATMENT OF CANCER
WO2019091450A1 (zh) 2017-11-10 2019-05-16 江苏恒瑞医药股份有限公司 一种苯并呋喃衍生物的制备方法
WO2019097369A1 (en) 2017-11-14 2019-05-23 Pfizer Inc. Ezh2 inhibitor combination therapies
WO2019152419A1 (en) 2018-01-31 2019-08-08 Mirati Therapeutics, Inc Prc2 inhibitors
JP2021531340A (ja) 2018-07-09 2021-11-18 フォンダシヨン、アジール、デ、アブグルスFondation Asile Des Aveugles 眼障害を治療するためのｐｒｃ２サブユニットの阻害
JP7411256B2 (ja) * 2018-07-27 2024-01-11 エボポイント、バイオサイエンシズ、カンパニー、リミテッド 多置換ベンゼン環化合物、製造方法及びその用途
MX2021007536A (es) 2018-12-21 2021-09-23 Les Laboratoires Servier Sas Formas de sal y cristalinas de un compuesto organico y composiciones farmaceuticas del mismo.
WO2020192652A1 (zh) 2019-03-25 2020-10-01 上海华汇拓医药科技有限公司 酰胺类化合物制备方法及其在医药领域的应用
JP7624404B2 (ja) 2019-04-22 2025-01-30 ミラティ セラピューティクス，インク． Ｐｒｃ２阻害剤としてのナフチリジン誘導体
WO2020247475A1 (en) 2019-06-05 2020-12-10 Mirati Therapeutics, Inc. Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer
GB201908453D0 (en) * 2019-06-12 2019-07-24 Enterprise Therapeutics Ltd Compounds for treating respiratory disease
US20220298222A1 (en) 2019-08-22 2022-09-22 Juno Therapeutics, Inc. Combination therapy of a t cell therapy and an enhancer of zeste homolog 2 (ezh2) inhibitor and related methods
CN113248481B (zh) * 2021-04-19 2023-03-24 中山大学 Ezh2共价不可逆抑制剂、制备方法及其用途
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
IL317228A (en) 2022-06-13 2025-01-01 Treeline Biosciences Inc BCL6 quinolone bifunctional joints
CA3258412A1 (en) 2022-06-13 2023-12-21 Treeline Biosciences, Inc. HETEROBORCTIONAL BCL6 DEGRADING AGENTS 1,8-NAPHTHYRIDIN-2-ONE

Family Cites Families (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
JPH0733729A (ja) 1993-07-26 1995-02-03 Kirin Brewery Co Ltd Ｎ−シアノ−ｎ′−置換−アリールカルボキシイミダミド化合物の製造法
CN1118595A (zh) 1993-12-27 1996-03-13 卫材株式会社 氨茴酸衍生物
DE19516776A1 (de) 1995-05-10 1996-11-14 Boehringer Ingelheim Int Chromatin-Regulatorgene
US5741819A (en) 1995-06-07 1998-04-21 3-Dimensional Pharmaceuticals, Inc. Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
JP3906935B2 (ja) 1995-12-18 2007-04-18 杏林製薬株式会社 Ｎ−置換ジオキソチアゾリジルベンズアミド誘導体及びその製造法
JP2002525352A (ja) 1998-09-30 2002-08-13 ザ、プロクター、エンド、ギャンブル、カンパニー ２−置換ケトアミド
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
CA2433158C (en) 2000-12-28 2011-05-10 Shionogi & Co., Ltd. Pyridone derivatives having a binding activity to the cannabinoid type 2 receptor
US7700293B2 (en) 2001-08-02 2010-04-20 The Regents Of The University Of Michigan Expression profile of prostate cancer
ATE447971T1 (de) 2002-02-19 2009-11-15 Shionogi & Co Antipruriginosa
TW200306155A (en) 2002-03-19 2003-11-16 Du Pont Benzamides and advantageous compositions thereof for use as fungicides
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
TWI324926B (en) * 2004-04-23 2010-05-21 Bristol Myers Squibb Co Monocyclic heterocycles as kinase inhibitors
EP1765994B1 (en) 2004-06-01 2009-11-18 The University of North Carolina at Chapel Hill Reconstituted histone methyltransferase complex and methods of identifying modulators thereof
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
ATE494548T1 (de) 2005-06-02 2011-01-15 Univ North Carolina Reinigung, charakterisierung und wiederherstellung einer ubiquitin-e3-ligase
FR2889526B1 (fr) 2005-08-04 2012-02-17 Aventis Pharma Sa 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation
DK1940821T3 (da) 2005-10-19 2013-06-10 Gruenenthal Gmbh Nye vanilloid-receptorligander og deres anvendelse til fremstilling af lægemidler.
NZ567000A (en) 2005-10-21 2010-03-26 Merck & Co Inc Potassium channel inhibitors
US20090203057A1 (en) 2005-10-28 2009-08-13 Yi Zhang Protein demethylases comprising a jmjc domain
EP1966141A1 (en) 2005-12-14 2008-09-10 Brystol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
AU2006336552B2 (en) 2006-01-20 2012-12-20 The University Of North Carolina At Chapel Hill Diagnostic and therapeutic targets for leukemia
RU2008149246A (ru) 2006-05-15 2010-06-20 Айрм Ллк (Bm) Соединение на основе терефталата, композиции и их применение в качестве ингибиторов интегразы вич
WO2007136592A2 (en) * 2006-05-18 2007-11-29 Amphora Discovery Corporation 2-0x0-l,2-dihydr0quin0line derivatives, compositions, and uses thereof as antiproliferative agents
EP2086318A4 (en) 2006-10-10 2009-12-23 Burnham Inst Medical Research NEUROPROTECTIVE COMPOSITIONS AND CORRESPONDING METHODS
AU2008219166B2 (en) 2007-02-16 2013-05-16 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors
US8338437B2 (en) 2007-02-28 2012-12-25 Methylgene Inc. Amines as small molecule inhibitors
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
US8247401B2 (en) 2007-10-31 2012-08-21 Merck Sharp & Dohme Corp. P2X3 receptor antagonists for treatment of pain
JP5511680B2 (ja) 2007-12-19 2014-06-04 キャンサー・リサーチ・テクノロジー・リミテッド ピリド［２，３−ｂ］ピラジン−８−置換化合物及びその使用
CN101977905B (zh) 2008-01-23 2014-07-02 百时美施贵宝公司 4-吡啶酮化合物及其对于癌症的用途
WO2009124137A2 (en) 2008-04-01 2009-10-08 Mount Sinai School Of Medicine Of New York University Method of suppressing gene transcription through histone lysine methylation
US20100113415A1 (en) 2008-05-29 2010-05-06 Rajapakse Hemaka A Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer
US8299093B2 (en) * 2008-08-08 2012-10-30 New York Blood Center, Inc. Small molecule inhibitors of retroviral assembly and maturation
FR2934995B1 (fr) 2008-08-14 2010-08-27 Sanofi Aventis Composes d'azetidines polysubstitues, leur preparation et leur application en therapeutique
CA2738583A1 (en) 2008-10-01 2010-04-08 Ludwig Institute For Cancer Research Methods for the treatment of cancer
JP2012522013A (ja) 2009-03-27 2012-09-20 ザ ユーエービー リサーチ ファウンデーション 調節ｉｒｅｓ媒介翻訳
WO2011011366A2 (en) 2009-07-20 2011-01-27 Constellation Pharmaceuticals Agents for stimulating activity of methyl modifying enzymes and methods of use thereof
CA2784899A1 (en) 2009-12-30 2011-07-07 Avon Products, Inc. Topical lightening composition and uses thereof
ES2528269T3 (es) 2010-05-07 2015-02-06 Glaxosmithkline Llc Azaindazoles
PH12012502194A1 (en) 2010-05-07 2014-09-05 Glaxosmithkline Llc Indoles
ES2534804T3 (es) 2010-05-07 2015-04-28 Glaxosmithkline Llc Indazoles
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
AU2011298987B2 (en) 2010-09-10 2017-09-28 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
US20130310379A1 (en) 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
ES2607064T3 (es) 2010-12-01 2017-03-29 Glaxosmithkline Llc Indoles
BR112013013668A2 (pt) 2010-12-03 2016-09-06 Epizyme Inc moduladores 7-deazapurina de histona metiltransferase, e métodos de uso dos mesmos
EP2681216B1 (en) 2011-02-28 2017-09-27 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
EP2727328B8 (en) 2011-06-28 2020-02-26 NCR Corporation Image processing to prevent access to private information
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
PE20150886A1 (es) 2012-10-15 2015-06-04 Epizyme Inc Compuestos de benceno sustituidos

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