ES2590489T3 - Compuestos de benceno sustituidos - Google Patents

Compuestos de benceno sustituidos Download PDF

Info

Publication number
ES2590489T3
ES2590489T3 ES12716968.8T ES12716968T ES2590489T3 ES 2590489 T3 ES2590489 T3 ES 2590489T3 ES 12716968 T ES12716968 T ES 12716968T ES 2590489 T3 ES2590489 T3 ES 2590489T3
Authority
ES
Spain
Prior art keywords
alkyl
halo
membered heterocycloalkyl
amino
optionally substituted
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES12716968.8T
Other languages
English (en)
Spanish (es)
Inventor
Kevin Wayne Kuntz
Richard Chesworth
Kenneth William DUNCAN
Heike KEILHACK
Natalie WARHOLIC
Christine KLAUS
Masashi Seki
Sarah K. KNUTSON
Timothy James Nelson WIGLE
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Epizyme Inc
Original Assignee
Epizyme Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Epizyme Inc filed Critical Epizyme Inc
Application granted granted Critical
Publication of ES2590489T3 publication Critical patent/ES2590489T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic 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
    • C07D407/02Heterocyclic 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
    • C07D407/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/113Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Landscapes

  • 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)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
ES12716968.8T 2011-04-13 2012-04-13 Compuestos de benceno sustituidos Active ES2590489T3 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161474825P 2011-04-13 2011-04-13
US201161474825P 2011-04-13
US201161505676P 2011-07-08 2011-07-08
US201161505676P 2011-07-08
PCT/US2012/033662 WO2012142513A1 (en) 2011-04-13 2012-04-13 Substituted benzene compounds

Publications (1)

Publication Number Publication Date
ES2590489T3 true ES2590489T3 (es) 2016-11-22

Family

ID=46000399

Family Applications (1)

Application Number Title Priority Date Filing Date
ES12716968.8T Active ES2590489T3 (es) 2011-04-13 2012-04-13 Compuestos de benceno sustituidos

Country Status (20)

Country Link
US (2) US9376422B2 (enExample)
EP (3) EP2697198B1 (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
US20130102477A1 (en) 2010-06-23 2013-04-25 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
BR112013005806B1 (pt) 2010-09-10 2022-05-10 Epizyme, Inc Métodos para detectar se um indivíduo é um candidato para o tratamento com ou responsivo a um inibidor de ezh2 e usos terapêuticos do dito inibidor de ezh2
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
EP2780013A4 (en) * 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
JP5989805B2 (ja) 2012-02-10 2016-09-07 コンステレーション・ファーマシューティカルズ・インコーポレイテッドConstellation Pharmaceuticals,Inc. メチル基変更酵素の調節物質、組成物及びその使用
NZ729643A (en) 2012-04-13 2018-02-23 Epizyme Inc Combination therapy for treating cancer
HUE045353T2 (hu) 2012-04-13 2019-12-30 Epizyme Inc N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)-metil)-5-(etil-(tetrahidro-2H-pirán-4-il) -amino)-4-metil-4'-(morfolino-metil)-[1,1'-bifenil]-3-karboxamid-hidrobromid a hematológiai rendszer egy sejtszaporodásos rendellenességének kezelésében való alkalmazásra
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
CA2884848C (en) * 2012-09-28 2017-08-22 Pfizer Inc. Benzamide and heterobenzamide compounds
MX376008B (es) * 2012-10-15 2025-03-07 Epizyme Inc Inhibidor de ezh2 para usarse en el tratamiento de sarcoma epiteloide.
CA2887562C (en) 2012-10-15 2021-01-12 Epizyme, Inc. Substituted benzene compounds
TWI494424B (zh) * 2012-11-20 2015-08-01 Dow Global Technologies Llc 可蒸餾燃料標記物
CN104968646B (zh) 2012-12-13 2017-09-05 葛兰素史密斯克莱有限责任公司 Zeste同源物增强子2的抑制剂
UA111305C2 (uk) * 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
WO2014100665A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
EP2935214B1 (en) 2012-12-21 2019-02-20 Epizyme, Inc. 1,4-pyridone compounds
US9776972B2 (en) 2013-03-14 2017-10-03 Epizyme Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9394258B2 (en) 2013-03-14 2016-07-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US20160031839A1 (en) 2013-03-14 2016-02-04 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
US9023883B2 (en) 2013-03-14 2015-05-05 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US8952026B2 (en) 2013-03-14 2015-02-10 Epizyme, Inc. PRMT1 inhibitors and uses thereof
KR102028793B1 (ko) 2013-03-14 2019-10-07 에피자임, 인코포레이티드 아르기닌 메틸기 전이효소 억제제 및 이의 용도
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970181B1 (en) 2013-03-14 2017-06-07 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014144847A2 (en) 2013-03-15 2014-09-18 G1 Therapeutics, Inc. Hspc-sparing treatments for rb-positive abnormal cellular proliferation
EP2970281A4 (en) * 2013-03-15 2016-08-03 Epizyme Inc SUBSTITUTED BENZOL COMPOUNDS
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
ES2717680T3 (es) * 2013-04-30 2019-06-24 Glaxosmithkline Ip No 2 Ltd Potenciador de inhibidores del homólogo de Zeste 2
JP2016523955A (ja) * 2013-07-10 2016-08-12 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー2、リミテッドGlaxosmithkline Intellectual Property No.2 Limited Zesteホモログ2エンハンサー阻害剤
WO2015010078A2 (en) 2013-07-19 2015-01-22 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
US10150764B2 (en) 2013-07-19 2018-12-11 Epizyme, Inc. Substituted benzene compounds
US9969716B2 (en) 2013-08-15 2018-05-15 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
US9738630B2 (en) 2013-11-19 2017-08-22 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
US9822103B2 (en) 2013-11-22 2017-11-21 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
ES2863996T3 (es) 2013-12-06 2021-10-13 Epizyme Inc Terapia de combinación para el tratamiento del cáncer
TN2016000529A1 (en) * 2014-06-17 2018-04-04 Pfizer Substituted dihydroisoquinolinone compounds
CA2952074C (en) 2014-06-17 2022-08-30 Epizyme, Inc. Ezh2 inhibitors for treating lymphoma
WO2015200650A1 (en) 2014-06-25 2015-12-30 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
CN112168967A (zh) 2014-10-16 2021-01-05 Epizyme股份有限公司 治疗癌症的方法
CN107148419A (zh) * 2014-10-28 2017-09-08 葛兰素史密斯克莱知识产权(第2 号)有限公司 Zeste增强子同源物2抑制剂
IL296080B2 (en) 2014-11-17 2023-12-01 Eisai R&D Man Co Ltd Method for treating cancer
AR102767A1 (es) 2014-12-05 2017-03-22 Lilly Co Eli Inhibidores de ezh2
EP3236962A2 (en) 2014-12-23 2017-11-01 University of Copenhagen Treatment of cancer by inhibiting ezh2 activity
AU2016252546A1 (en) 2015-04-20 2017-11-02 Epizyme, Inc. Combination therapy for treating cancer
US20180133211A1 (en) * 2015-05-19 2018-05-17 Mayo Foundation For Medical Education And Research Methods and materials for promoting bone formation
CN107635965A (zh) 2015-06-10 2018-01-26 Epizyme股份有限公司 用于治疗淋巴瘤的ezh2抑制剂
EA201890567A1 (ru) 2015-08-24 2018-08-31 Эпизайм, Инк. Способ лечения рака
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ezh2抑制劑
WO2017040190A1 (en) 2015-08-28 2017-03-09 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
EP3378859B1 (en) * 2015-11-19 2019-10-30 Jiangsu Hengrui Medicine Co., Ltd. Benzofuran derivative, preparation method thereof and use thereof in medicine
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
EP3444247B1 (en) * 2016-04-14 2022-11-30 Guangzhou Joyo Pharmatech Co., Ltd Pyridone derivative comprising oxetane substituent, for treating fibrosis and inflammatory diseases
US11786533B2 (en) 2016-06-01 2023-10-17 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
US11147819B2 (en) 2016-06-17 2021-10-19 Epizyme, Inc. EZH2 inhibitors for treating cancer
US10457640B2 (en) 2016-10-19 2019-10-29 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
US11672800B2 (en) * 2017-04-21 2023-06-13 Epizyme, Inc. Combination therapies with EHMT2 inhibitors
EP3626715A4 (en) 2017-05-18 2021-03-24 Jiangsu Hengrui Medicine Co., Ltd. CRYSTAL OF A BENZOFURAND DERIVATIVE-FREE BASE AND MANUFACTURING PROCESS
WO2018223030A1 (en) 2017-06-02 2018-12-06 Epizyme, Inc. Use of ezh2 inhibitors for treating cancer
CA3074720A1 (en) 2017-09-05 2019-03-14 Epizyme, Inc. Combination therapy for treating cancer
JP7295105B6 (ja) 2017-11-10 2023-07-24 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 ベンゾフラン誘導体の製造方法
CA3082287C (en) 2017-11-14 2023-02-28 Pfizer Inc. Ezh2 inhibitor combination therapies
DK3746446T3 (da) 2018-01-31 2022-06-27 Mirati Therapeutics Inc PRC2-inhibitorer
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
EP3831822A4 (en) * 2018-07-27 2022-03-23 Suzhou Sinovent Pharmaceuticals Co., Ltd. POLYSUBSTITUTED BENZENE COMPOUND AND METHOD FOR PREPARING IT AND ITS USE
JP2022515239A (ja) 2018-12-21 2022-02-17 レ ラボラトワール セルヴィエ ソシエテ・パール・アクシオンス・サンプリフィエ 有機化合物の結晶および塩形態およびその医薬組成物
US12473298B2 (en) 2019-03-25 2025-11-18 Shanghai Synergy Pharmaceutical Sciences Co., Ltd. Amide compounds, preparation method therefor, and use thereof in the medical field
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
US12252493B2 (en) 2019-06-05 2025-03-18 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
EP4017527A1 (en) 2019-08-22 2022-06-29 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
AU2023292893A1 (en) 2022-06-13 2025-01-02 Treeline Biosciences, Inc. Quinolone bcl6 bifunctional degraders
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
FI953968A7 (fi) 1993-12-27 1995-10-19 Eisai Co Ltd Antraniiliset happojohdannaiset
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
CN1332722A (zh) 1998-09-30 2002-01-23 宝洁公司 2-取代的酮酰胺
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
US6977266B2 (en) 2000-12-28 2005-12-20 Shionogi & Co., Ltd. Pyridone derivatives having affinity for cannabinoid 2-type receptor
US7700293B2 (en) 2001-08-02 2010-04-20 The Regents Of The University Of Michigan Expression profile of prostate cancer
EP2130820A1 (en) 2002-02-19 2009-12-09 Shionogi & Co., Ltd. Antipruritics
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
EP2388258A1 (de) 2005-10-19 2011-11-23 Grünenthal GmbH Neue Vanilloidrezeptor-Liganden und ihre Verwendung zur Herstellung von Arzneimitteln
KR20080057296A (ko) 2005-10-21 2008-06-24 머크 앤드 캄파니 인코포레이티드 칼륨 채널 억제제
JP5078901B2 (ja) 2005-10-28 2012-11-21 ザ・ユニヴァーシティ・オヴ・ノース・キャロライナ・アト・チャペル・ヒル JmjCドメインを含むタンパク質デメチラーゼ
AU2006325746A1 (en) 2005-12-14 2007-06-21 Bristol-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
KR20080110905A (ko) 2006-05-15 2008-12-19 아이알엠 엘엘씨 테레프탈라메이트 화합물 및 조성물, 및 hiv 인테그라제억제제로서의 그들의 용도
WO2007136592A2 (en) * 2006-05-18 2007-11-29 Amphora Discovery Corporation 2-0x0-l,2-dihydr0quin0line 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
EP2114898A2 (en) 2007-02-16 2009-11-11 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
AU2008319308B2 (en) 2007-10-31 2013-01-31 Merck Sharp & Dohme Corp. P2X3, receptor antagonists for treatment of pain
EP2229391B1 (en) 2007-12-19 2014-08-06 Cancer Research Technology Limited Pyrido[2,3-b]pyrazine-8-substituted compounds and their use
EP2235001B1 (en) 2008-01-23 2014-12-24 Bristol-Myers Squibb Company Process for preparing pyridinone compounds
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
WO2010017355A2 (en) * 2008-08-08 2010-02-11 New York Blood Center 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
MX2011003363A (es) 2008-10-01 2011-04-27 Ludwig Inst Cancer Res Metodos para el tratamiento de cancer.
US20120065247A1 (en) 2009-03-27 2012-03-15 Discoverybiomed, Inc. Modulating ires-mediated translation
WO2011011366A2 (en) 2009-07-20 2011-01-27 Constellation Pharmaceuticals Agents for stimulating activity of methyl modifying enzymes and methods of use thereof
WO2011082044A1 (en) 2009-12-30 2011-07-07 Avon Products, Inc. Topical lightening composition and uses thereof
WO2011140325A1 (en) 2010-05-07 2011-11-10 Glaxosmithkline Llc Indazoles
BR112012028556A2 (pt) 2010-05-07 2014-04-01 Glaxosmithkline Llc Indóis
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
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
BR112013005806B1 (pt) 2010-09-10 2022-05-10 Epizyme, Inc Métodos para detectar se um indivíduo é um candidato para o tratamento com ou responsivo a um inibidor de ezh2 e usos terapêuticos do dito inibidor de ezh2
US20130310379A1 (en) 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
JP5908493B2 (ja) 2010-12-01 2016-04-26 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 インドール
AU2011336272A1 (en) 2010-12-03 2013-06-20 Epizyme, Inc. 7-deazapurine modulators of histone methyltransferase, and methods of use thereof
WO2012118812A2 (en) 2011-02-28 2012-09-07 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
EP3654627B1 (en) 2011-06-28 2025-08-06 NCR Voyix 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
CA2887562C (en) 2012-10-15 2021-01-12 Epizyme, Inc. Substituted benzene compounds

Also Published As

Publication number Publication date
RU2017126990A (ru) 2019-02-01
EP2697198B1 (en) 2016-06-08
AU2017218920A1 (en) 2017-09-07
HK1202534A1 (en) 2015-10-02
WO2012142513A1 (en) 2012-10-18
TW201305107A (zh) 2013-02-01
EP2697198A1 (en) 2014-02-19
MX2013011922A (es) 2014-04-10
PT2697198T (pt) 2016-09-13
TWI598336B (zh) 2017-09-11
RU2629118C2 (ru) 2017-08-24
IL228746B (en) 2019-08-29
EP3165520B1 (en) 2018-08-15
EP3470396A1 (en) 2019-04-17
IL228746A0 (en) 2013-12-31
KR101975613B1 (ko) 2019-05-07
CA2832846C (en) 2022-04-19
AU2012242604A1 (en) 2013-10-24
BR112013026308B1 (pt) 2024-01-02
CN104066718B (zh) 2017-08-29
KR20140034787A (ko) 2014-03-20
BR112013026308A2 (pt) 2022-07-19
PL2697198T3 (pl) 2016-12-30
AR086839A1 (es) 2014-01-29
CN104066718A (zh) 2014-09-24
US20140142083A1 (en) 2014-05-22
EP3165520A1 (en) 2017-05-10
HUE030722T2 (en) 2017-05-29
RU2017126990A3 (enExample) 2020-10-30
JP2014513084A (ja) 2014-05-29
CA2832846A1 (en) 2012-10-18
MX344530B (es) 2016-12-19
US9376422B2 (en) 2016-06-28
DK2697198T3 (en) 2016-09-19
AU2012242604B2 (en) 2017-05-25
RU2013150510A (ru) 2015-05-20
US20160332969A1 (en) 2016-11-17
TW201733984A (zh) 2017-10-01

Similar Documents

Publication Publication Date Title
ES2590489T3 (es) Compuestos de benceno sustituidos
ES2589555T3 (es) Compuestos de benceno sustituidos con arilo o heteroarilo
AR101558A1 (es) Difluoropirrolidinas como moduladores del receptor de orexina
AR094299A1 (es) Derivados de ftalazin-1(2h)-ona sustituidos
AR084553A1 (es) DERIVADOS IMIDAZOLICOS HETEROCICLICOS INHIBIDORES DE b-SECRETASA, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y USO DE LOS MISMOS PARA TRATAR ENFERMEDADES NEURODEGENERATIVAS, EN PARTICULAR ALZHEIMER
AR086729A1 (es) Composiciones pesticidas y los procesos relacionados con las mismas
ES2432821T3 (es) Compuestos de pirimidina, composiciones y métodos de utilización
AR100807A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
ES2721031T3 (es) Compuestos de dihidroisoquinolinona sustituidos
AR093184A1 (es) Compuesto de pirimidina sustituida como inhibidor de quinurenina-3-monooxigenasa y composicion farmaceutica que lo comprenden
AR080314A1 (es) Derivado de 1,3,4,8-tetrahidro-2h-pirido (1,2-a) pirazina y su uso como inhibidor de la hiv integrasa
NI201600170A (es) Pirazolopiridinas y pirazolopirimidinas
ES2722048T3 (es) Compuestos de triazolopirimidina y usos de los mismos
AR101175A1 (es) Imidazopiridinas e imidazopirazinas como inhibidores de lsd1
AR109709A1 (es) Inhibidores de la fosfatidilinositol 3-quinasa
CU20180146A7 (es) Compuestos derivados de (piperidin-1-ilo)(piperidin-4-ilo) sustituidos con hetero(arilo), un proceso para su preparación y composiciones farmacéuticas que los contienen
AR100809A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR095339A1 (es) Compuestos moduladores alostericos de la hemoglobina
AR091193A1 (es) HETEROCICLOS DE 5 MIEMBROS QUE CONTIENEN NITROGENO SUSTITUIDO POR CARBOXAMIDA O SULFONAMIDA COMO MODULADORES PARA EL RECEPTOR NUCLEAR HUERFANO RORg
AR089143A1 (es) Triazolopiridinas sustituidas con actividad inhibidora de ttk
AR109711A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR092809A1 (es) 3,5-diaminopirazol como inhibidor de quinasa
MX2017011650A (es) Inhibidores de kv1.3 y su aplicacion medica.
AR102079A1 (es) DERIVADOS BICÍCLICOS QUE TIENEN ACTIVIDAD COMO AGONISTAS ADRENÉRGICOS b2 Y COMO ANTAGONISTAS MUSCARÍNICOS M3
PE20161240A1 (es) Agentes anticancerosos y sus preparaciones