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PE20151981A1 - Pontenciador de inhibidores del homologo de zeste - Google Patents

Pontenciador de inhibidores del homologo de zeste

Info

Publication number
PE20151981A1
PE20151981A1 PE2015002298A PE2015002298A PE20151981A1 PE 20151981 A1 PE20151981 A1 PE 20151981A1 PE 2015002298 A PE2015002298 A PE 2015002298A PE 2015002298 A PE2015002298 A PE 2015002298A PE 20151981 A1 PE20151981 A1 PE 20151981A1
Authority
PE
Peru
Prior art keywords
zeste
pontencer
approval
inhibitor
dihydropidin
Prior art date
Application number
PE2015002298A
Other languages
English (en)
Inventor
Jr Charles William Blackledge
Joelle Lorraine Burgess
Neil W Johnson
Jiri Kasparec
Steven David Knight
Iii Louis V Lafrance
Xinrong Tian
William Henry Miller
Kenneth Allen Newlander
Stuart Paul Romeril
Mark Schulz
Dai-Shi Su
Juan I Luengo
Original Assignee
Glaxosmithkline Ip No 2 Ltd
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 Glaxosmithkline Ip No 2 Ltd filed Critical Glaxosmithkline Ip No 2 Ltd
Publication of PE20151981A1 publication Critical patent/PE20151981A1/es

Links

Classifications

    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D409/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/14—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)

Abstract

Esta invencion se refiere a compuestos de acuerdo con la formula (I) que son inhibidores del potenciador de homologo Zeste 2(EZH2), a composiciones farmaceuticas que los contienen, a procedimientos para su preparacion y a su uso en terapia para el tratamiento de canceres. Donde R es H, entre otros; R4 es H, entre otros; X es O, N, etc; Y es O, N, etc; Z es CR5; R1, R2 Y R3 son hidrogeno, alcoxi C1-C4, etc; R5 es alquilo C4-C8, etc; son compuestos preferidos: N-((4,6-dimetil-2-oxo-1,2-dihidropidin-3-il)metil)-4-isopropoxi-3-metiltiofen-2-carboxamida; N-((4,6-dimetil-2-oxo-1,2-dihidropidin-3-il)metil)-4-(etil(tetrahidro-2H-piran-4-il)amino)-3-metiltiofen-2-carboxamida; entre otros
PE2015002298A 2013-04-30 2014-04-25 Pontenciador de inhibidores del homologo de zeste PE20151981A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361817436P 2013-04-30 2013-04-30
US201361842038P 2013-07-02 2013-07-02
US201361907024P 2013-11-21 2013-11-21
US201461936460P 2014-02-06 2014-02-06

Publications (1)

Publication Number Publication Date
PE20151981A1 true PE20151981A1 (es) 2016-01-14

Family

ID=50877537

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015002298A PE20151981A1 (es) 2013-04-30 2014-04-25 Pontenciador de inhibidores del homologo de zeste

Country Status (20)

Country Link
US (2) US9505745B2 (es)
EP (1) EP2991980B1 (es)
JP (1) JP6373973B2 (es)
KR (1) KR20160003115A (es)
CN (1) CN105308038B (es)
AU (1) AU2014261075B2 (es)
BR (1) BR112015027527A2 (es)
CA (1) CA2910873A1 (es)
CL (1) CL2015003200A1 (es)
DO (1) DOP2015000270A (es)
EA (1) EA030196B1 (es)
ES (1) ES2717680T3 (es)
HK (1) HK1214815A1 (es)
MX (1) MX2015015144A (es)
NZ (1) NZ630205A (es)
PE (1) PE20151981A1 (es)
PH (1) PH12015502414A1 (es)
SG (1) SG11201508203TA (es)
WO (1) WO2014177982A1 (es)
ZA (1) ZA201507398B (es)

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AU2013216721B2 (en) * 2012-02-10 2017-09-28 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
MX376008B (es) 2012-10-15 2025-03-07 Epizyme Inc Inhibidor de ezh2 para usarse en el tratamiento de sarcoma epiteloide.
SG11201508203TA (en) * 2013-04-30 2015-11-27 Glaxosmithkline Ip No 2 Ltd Enhancer of zeste homolog 2 inhibitors
AU2014288839B2 (en) 2013-07-10 2017-02-02 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of Zeste Homolog 2 inhibitors
SMT202400446T1 (it) 2014-02-06 2024-11-15 Nxera Pharma Uk Ltd Composti aza biciclici come agonisti del recettore muscarinico
US20170334891A1 (en) * 2014-10-28 2017-11-23 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ｅｚｈ２抑制劑
TW201708210A (zh) * 2015-06-30 2017-03-01 葛蘭素史克智慧財產（第二）有限公司 Ｚｅｓｔｅ同源物２增強子之抑制劑
IL307260A (en) 2015-08-24 2023-11-01 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
EP3370725A4 (en) * 2015-11-06 2019-07-03 Epizyme, Inc. PEDIATRIC DOSAGE FOR THE TREATMENT OF CANCER WITH AN EZH2 INHIBITOR
ES2760510T3 (es) 2015-11-19 2020-05-14 Jiangsu Hengrui Medicine Co Derivado de benzofurano, método de preparación del mismo y uso del mismo en medicina
BR112018072740A2 (pt) * 2016-05-05 2019-02-19 Glaxosmithkline Intellectual Property (No. realçador de inibidores de homólogo 2 de zeste
US20170337814A1 (en) * 2016-05-20 2017-11-23 Donald Edward Morgan Safety alerting drivers device and system
EP3524602A1 (en) 2016-09-07 2019-08-14 Shanghai Haihe Pharmaceutical Co., Ltd. Pyrido five-element aromatic ring compound, preparation method therefor and use thereof
WO2018125983A1 (en) 2016-12-30 2018-07-05 Mitobridge, Inc. Oxopyridine derivatives useful as aminocarboxymuconate semialdehyde decarboxylase (acmsd) inhibitors
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
FI4043466T3 (fi) 2018-01-31 2024-10-30 Mirati Therapeutics Inc Prc2:n estäjiä
WO2020011607A1 (en) 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
EP3959214A1 (en) 2019-04-22 2022-03-02 Mirati Therapeutics, Inc. Naphthyridine derivatives as prc2 inhibitors
CA3133004A1 (en) * 2019-05-31 2020-12-03 Sichuan Haisco Pharmaceutical Co., Ltd. Btk inhibitor ring derivative, preparation method therefor and pharmaceutical application thereof
JP7541538B2 (ja) 2019-06-05 2024-08-28 ミラティ セラピューティクス，インク． 癌を処置するためのｐｒｃ２阻害剤としてのイミダゾ［１，２－ｃ］ピリミジン誘導体
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
CN110964200A (zh) * 2019-12-19 2020-04-07 新纳奇材料科技江苏有限公司 一种基于聚硅氧烷馏出物的羟基封端聚硅氧烷的制备方法
WO2021129629A1 (zh) * 2019-12-23 2021-07-01 四川海思科制药有限公司 Zeste增强子同源物2抑制剂及其用途
CN111233768B (zh) * 2020-03-18 2021-08-03 徐州圣元化工有限公司 一种3-(二氟甲基)-1-甲基-1h-吡唑-4-羧酸乙酯的制备方法
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof

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US7696352B2 (en) * 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
CN101341124A (zh) 2005-12-14 2009-01-07 布里斯托尔-迈尔斯斯奎布公司 可用作丝氨酸蛋白酶抑制剂的6元杂环
BR112012002336A2 (pt) * 2009-08-07 2016-05-31 Merck Patent Gmbh compostos aza-heterocíclicos
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SG11201508203TA (en) * 2013-04-30 2015-11-27 Glaxosmithkline Ip No 2 Ltd Enhancer of zeste homolog 2 inhibitors

Also Published As

Publication number Publication date
EP2991980A1 (en) 2016-03-09
DOP2015000270A (es) 2016-02-15
KR20160003115A (ko) 2016-01-08
EA030196B1 (ru) 2018-07-31
SG11201508203TA (en) 2015-11-27
CN105308038A (zh) 2016-02-03
HK1214815A1 (zh) 2016-08-05
MX2015015144A (es) 2016-02-18
US9790212B2 (en) 2017-10-17
AU2014261075B2 (en) 2017-01-19
US9505745B2 (en) 2016-11-29
CA2910873A1 (en) 2014-11-06
BR112015027527A2 (pt) 2017-07-25
CL2015003200A1 (es) 2016-04-22
ES2717680T3 (es) 2019-06-24
US20170029412A1 (en) 2017-02-02
US20160102083A1 (en) 2016-04-14
WO2014177982A1 (en) 2014-11-06
CN105308038B (zh) 2018-05-29
EP2991980B1 (en) 2019-01-02
ZA201507398B (en) 2017-01-25
AU2014261075A1 (en) 2015-11-05
JP2016517878A (ja) 2016-06-20
EA201592068A1 (ru) 2016-05-31
JP6373973B2 (ja) 2018-08-15
PH12015502414A1 (en) 2016-02-22
NZ630205A (en) 2017-03-31

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Legal Events

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