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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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NZ628762A (en) * 2012-02-10 2016-07-29 Constellation Pharmaceuticals Inc Modulators of methyl modifying enzymes, compositions and uses thereof
PE20151981A1 (es) * 2013-04-30 2016-01-14 Glaxosmithkline Ip No 2 Ltd Pontenciador de inhibidores del homologo de zeste
CN105473580A (zh) 2013-07-10 2016-04-06 葛兰素史密斯克莱知识产权（第2号）有限公司 Zeste同源物增强子2抑制剂
UA122121C2 (uk) 2014-02-06 2020-09-25 Хептерс Терап'Ютікс Лімітед Біциклічні азотовмісні сполуки як агоністи мускаринового м1 рецептора i/або м4 рецептора
EP3212639A1 (en) * 2014-10-28 2017-09-06 Glaxosmithkline Intellectual Property (No. 2) Limited Enhancer of zeste homolog 2 inhibitors
AR102767A1 (es) * 2014-12-05 2017-03-22 Lilly Co Eli Inhibidores de ezh2
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
EP3341080A4 (en) 2015-08-24 2019-03-20 Epizyme Inc METHOD FOR THE TREATMENT OF CANCER
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ｅｚｈ２抑制劑
US20190070188A1 (en) * 2015-11-06 2019-03-07 Epizyme, Inc. Pediatric dosing for treatment of cancer with an ezh2 inhibitor
WO2017084494A1 (zh) 2015-11-19 2017-05-26 江苏恒瑞医药股份有限公司 苯并呋喃类衍生物、其制备方法及其在医药上的应用
MX2018013519A (es) * 2016-05-05 2019-03-14 Glaxosmithkline Ip No 2 Ltd Inhibidores del potenciador del homologo zeste 2.
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
CA3089639C (en) 2018-01-31 2024-06-18 Mirati Therapeutics, Inc. Imidazo[1,2-c]pyrimidinyl compounds as 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
WO2020239103A1 (zh) * 2019-05-31 2020-12-03 四川海思科制药有限公司 一种btk抑制剂环衍生物及其制备方法和药学上的应用
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
CN114787143A (zh) * 2019-12-23 2022-07-22 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
US11878958B2 (en) 2022-05-25 2024-01-23 Ikena Oncology, Inc. MEK inhibitors and uses thereof

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US20080293716A1 (en) * 2004-01-30 2008-11-27 Smithkline Beecham Corporation Chemical Compounds
RU2006138036A (ru) * 2004-03-30 2008-05-10 Чирон Корпорейшн (Us) Производные замещенного тиофена в качестве противораковых средств
US7696352B2 (en) * 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
EP1966141A1 (en) 2005-12-14 2008-09-10 Brystol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
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ES2528269T3 (es) 2010-05-07 2015-02-06 Glaxosmithkline Llc Azaindazoles
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ES2534804T3 (es) * 2010-05-07 2015-04-28 Glaxosmithkline Llc Indazoles
ES2607064T3 (es) 2010-12-01 2017-03-29 Glaxosmithkline Llc Indoles
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JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TWI598336B (zh) 2011-04-13 2017-09-11 雅酶股份有限公司 經取代之苯化合物
JP2014534178A (ja) * 2011-09-30 2014-12-18 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 癌の処置方法
NZ628762A (en) 2012-02-10 2016-07-29 Constellation Pharmaceuticals Inc Modulators of methyl modifying enzymes, compositions and uses thereof
CN104603130B (zh) 2012-04-13 2018-04-27 Epizyme股份有限公司 人类组蛋白甲基转移酶ezh2抑制剂的盐形式
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
PE20151981A1 (es) * 2013-04-30 2016-01-14 Glaxosmithkline Ip No 2 Ltd Pontenciador de inhibidores del homologo de zeste

Also Published As

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

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Legal Events

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