KR20170098865A - Egfr 조정제로서의 치환된 2-아닐리노피리미딘 유도체 - Google Patents

Egfr 조정제로서의 치환된 2-아닐리노피리미딘 유도체 Download PDF

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KR20170098865A
KR20170098865A KR1020177019147A KR20177019147A KR20170098865A KR 20170098865 A KR20170098865 A KR 20170098865A KR 1020177019147 A KR1020177019147 A KR 1020177019147A KR 20177019147 A KR20177019147 A KR 20177019147A KR 20170098865 A KR20170098865 A KR 20170098865A
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South Korea
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pharmaceutically acceptable
prodrug
solvate
acceptable salt
cancer
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Korean (ko)
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지롱 펭
마이클 존 코스탄조
마이클 니콜라스 그레코
마이클 앨런 그린
빅토리아 린 와일드
돈 장
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베타 파마, 인크.
베타 파마 (상하이) 코., 엘티디.
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Publication of KR20170098865A publication Critical patent/KR20170098865A/ko
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020177019147A 2014-12-11 2015-12-11 Egfr 조정제로서의 치환된 2-아닐리노피리미딘 유도체 Ceased KR20170098865A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462090869P 2014-12-11 2014-12-11
US62/090,869 2014-12-11
US201562166883P 2015-05-27 2015-05-27
US62/166,883 2015-05-27
PCT/US2015/065286 WO2016094821A2 (en) 2014-12-11 2015-12-11 Substituted 2-anilinopyrimidine derivatives as egfr modulators

Publications (1)

Publication Number Publication Date
KR20170098865A true KR20170098865A (ko) 2017-08-30

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KR1020177019147A Ceased KR20170098865A (ko) 2014-12-11 2015-12-11 Egfr 조정제로서의 치환된 2-아닐리노피리미딘 유도체

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US (2) US10590111B2 (enExample)
EP (1) EP3229798A4 (enExample)
JP (2) JP6709786B2 (enExample)
KR (1) KR20170098865A (enExample)
CN (3) CN112375067B (enExample)
AU (1) AU2015360360B2 (enExample)
BR (1) BR112017012272A2 (enExample)
CA (1) CA2970185C (enExample)
CO (1) CO2017006962A2 (enExample)
EA (1) EA036453B1 (enExample)
HK (1) HK1245634A1 (enExample)
IL (1) IL252554A0 (enExample)
MX (1) MX382869B (enExample)
PH (1) PH12017501057A1 (enExample)
SG (2) SG11201704685TA (enExample)
TW (1) TWI618704B (enExample)
WO (1) WO2016094821A2 (enExample)

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CN111170998B (zh) 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
US10590111B2 (en) * 2014-12-11 2020-03-17 Beta Pharma, Inc. Substituted 2-anilinopyrimidine derivatives as EGFR modulators
US11052086B2 (en) * 2016-05-11 2021-07-06 Beta Pharma, Inc. 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
CN109311858B (zh) 2016-05-26 2021-12-03 里科瑞尔姆Ip控股有限责任公司 Egfr抑制剂化合物
EP3471730B1 (en) 2016-06-17 2021-10-20 Beta Pharma, Inc. Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof
CN106243044A (zh) * 2016-06-30 2016-12-21 浙江大学 含卤代丙烯酰胺侧链的嘧啶类衍生物及制备和应用
CN108602802B (zh) * 2016-07-26 2020-01-21 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
MX2019015177A (es) * 2017-06-16 2020-02-07 Beta Pharma Inc Formulaciones farmaceuticas de n-(2-(2-(dimetilamino)etoxi)-4-meto xi-5((4-(1-metil-1h-indol-3-il)pirimidin-2-il)amino)fenil)acrilam ida y las sales de ellas.
CN109503573A (zh) * 2017-09-14 2019-03-22 昆明圣加南生物科技有限公司 2-取代苯胺基嘧啶衍生物及其用途
CN107935995A (zh) * 2017-11-28 2018-04-20 中山大学 一种新型2‑苯胺基嘧啶衍生物及其在制备抗肿瘤药物中的应用
CN108017633A (zh) * 2018-01-30 2018-05-11 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-2-氟代丙烯酰胺衍生物及应用
PT3806898T (pt) * 2018-06-18 2025-12-02 UCB Biopharma SRL Antagonista de gremlin-1 para utilização no tratamento do cancro
IL281344B2 (en) 2018-09-10 2025-09-01 Mirati Therapeutics Inc Combination of adagrasib and cetuximab for cancer treatment
US12390464B2 (en) 2019-09-23 2025-08-19 Beta Pharma, Inc. Treatment of EGFR mutant-related cancers using a combination of EGFR and CDK4/6 inhibitors
WO2021094379A1 (en) 2019-11-12 2021-05-20 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
CA3166980A1 (en) 2020-01-20 2021-07-29 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
US20210369709A1 (en) 2020-05-27 2021-12-02 Astrazeneca Ab EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER
US20250136576A1 (en) * 2021-07-13 2025-05-01 ACEA Therapeutics, Inc. Heterocyclic Compounds and Uses Thereof
CN119278041A (zh) 2022-03-31 2025-01-07 阿斯利康(瑞典)有限公司 用于治疗癌症的与akt抑制剂组合的表皮生长因子受体(egfr)酪氨酸激酶抑制剂
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application in the treatment of cancer
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
US20240116926A1 (en) 2022-04-28 2024-04-11 Astrazeneca Ab Heteroaromatic compounds
AU2023262556A1 (en) 2022-04-28 2024-12-05 Astrazeneca Ab Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer
MA71241A (fr) 2022-06-27 2025-04-30 Astrazeneca Ab Combinaisons impliquant des inhibiteurs de tyrosine kinase du récepteur du facteur de croissance épidermique pour traiter le cancer
JP2025522965A (ja) 2022-07-08 2025-07-17 アストラゼネカ・アクチエボラーグ 癌の治療のためのhgf受容体阻害剤と組み合わせた上皮成長因子受容体チロシンキナーゼ阻害剤
WO2025238661A1 (en) * 2024-05-17 2025-11-20 Bdr Lifesciences Private Limited An improved process for the preparation of osimertinib

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JP5179509B2 (ja) * 2006-12-08 2013-04-10 エフ.ホフマン−ラ ロシュ アーゲー 置換ピリミジン類及びjnkモジュレーターとしてのこれらの使用
WO2010059711A1 (en) * 2008-11-18 2010-05-27 Wisconsin Alumni Research Foundation Sigma-1 receptor ligands and methods of use
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Egfr阻害剤及び疾患の治療方法
BR112013027734A2 (pt) * 2011-05-04 2017-08-08 Ariad Pharma Inc compostos para a inibição de proliferação celular em cânceres impulsionados pelo egfr, método e composição farmacêutica
EP2736895B1 (en) * 2011-07-27 2016-01-06 Astrazeneca AB 2-(2,4,5-substituted-anilino) pyrimidine derivatives as egfr modulators useful for treating cancer
AU2013204563B2 (en) * 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
CN104860941B (zh) 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
PE20170268A1 (es) 2014-06-19 2017-04-21 Ariad Pharma Inc Compuestos de heteroarilo para la inhibicion de cinasa
CN106458969A (zh) * 2014-08-25 2017-02-22 四川海思科制药有限公司 一种(取代的苯基)(取代的嘧啶)胺基衍生物及其制备方法和药物用途
CN105461695B (zh) * 2014-09-29 2018-03-27 齐鲁制药有限公司 嘧啶或三嗪衍生物及其制备方法和用途
CN111170998B (zh) 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
US10590111B2 (en) * 2014-12-11 2020-03-17 Beta Pharma, Inc. Substituted 2-anilinopyrimidine derivatives as EGFR modulators

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US11414401B2 (en) 2022-08-16
JP6709786B2 (ja) 2020-06-17
AU2015360360A1 (en) 2017-06-08
CA2970185C (en) 2023-10-17
CN112457298B (zh) 2024-05-07
CN112375067A (zh) 2021-02-19
CN112457298A (zh) 2021-03-09
SG10201909060SA (en) 2019-11-28
EA201790921A1 (ru) 2017-12-29
JP2017537114A (ja) 2017-12-14
IL252554A0 (en) 2017-07-31
CN112375067B (zh) 2024-03-15
EP3229798A4 (en) 2018-05-30
TW201632512A (zh) 2016-09-16
PH12017501057A1 (en) 2018-03-05
EA036453B1 (ru) 2020-11-12
AU2015360360B2 (en) 2020-06-25
BR112017012272A2 (pt) 2018-01-30
JP7181558B2 (ja) 2022-12-01
CN108024993A (zh) 2018-05-11
US20170362203A1 (en) 2017-12-21
CO2017006962A2 (es) 2017-10-20
US10590111B2 (en) 2020-03-17
MX382869B (es) 2025-03-13
WO2016094821A2 (en) 2016-06-16
TWI618704B (zh) 2018-03-21
EP3229798A2 (en) 2017-10-18
JP2020143131A (ja) 2020-09-10
MX2017007664A (es) 2018-01-23
CA2970185A1 (en) 2016-06-16
SG11201704685TA (en) 2017-07-28
WO2016094821A3 (en) 2016-08-25
CN108024993B (zh) 2020-11-06
HK1245634A1 (zh) 2018-08-31
US20200216421A1 (en) 2020-07-09

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