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)
Inventor
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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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 (https=)
EP (1) EP3229798A4 (https=)
JP (2) JP6709786B2 (https=)
KR (1) KR20170098865A (https=)
CN (3) CN108024993B (https=)
AU (1) AU2015360360B2 (https=)
BR (1) BR112017012272A2 (https=)
CA (1) CA2970185C (https=)
CO (1) CO2017006962A2 (https=)
EA (1) EA036453B1 (https=)
HK (1) HK1245634A1 (https=)
IL (1) IL252554A0 (https=)
MX (1) MX382869B (https=)
PH (1) PH12017501057A1 (https=)
SG (2) SG10201909060SA (https=)
TW (1) TWI618704B (https=)
WO (1) WO2016094821A2 (https=)

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CN108024993B (zh) * 2014-12-11 2020-11-06 贝达医药公司 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂
EP3454860B1 (en) * 2016-05-11 2025-09-17 Beta Pharma, Inc. 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
AU2017269335B2 (en) 2016-05-26 2021-07-01 Recurium Ip Holdings, Llc EGFR inhibitor compounds
BR112018075823A2 (pt) * 2016-06-17 2019-03-26 Beta Pharma, Inc. sais farmacêuticos de n-(2-(2-(dimetilamino)etoxi)-4-metoxi-5-((4-(1-metil-1h-indol-3-il)pirimidin-2-il)amino)fenil)acrilamida e suas formas cristalinas
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
JP6740452B2 (ja) * 2016-07-26 2020-08-12 深▲セン▼市塔吉瑞生物医▲薬▼有限公司Shenzhen TargetRx,Inc. プロテインチロシンキナーゼの活性を阻害するためのアミノピリミジン系化合物
CN110799191B (zh) 2017-06-16 2023-05-26 贝塔制药有限公司 N-(2-(2-(二甲氨基)乙氧基)-4-甲氧基-5-((4-(1-甲基-1h-吲哚-3-基)嘧啶-2-基)氨基)苯基)丙烯酰胺及其盐的药物制剂
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
PL3806898T3 (pl) * 2018-06-18 2026-02-23 UCB Biopharma SRL Antagonista gremlin-1 do zastosowania w leczeniu nowotworu
CA3112043A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
JP2022549272A (ja) * 2019-09-23 2022-11-24 ベータ・ファーマ・インコーポレイテッド Egfr阻害剤とcdk4/6阻害剤の組み合わせを用いたegfr変異に関連する癌の治療
US20210161897A1 (en) 2019-11-12 2021-06-03 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
JP2023510426A (ja) 2020-01-20 2023-03-13 アストラゼネカ・アクチエボラーグ 癌を治療するための上皮細胞増殖因子受容体チロシンキナーゼ阻害剤
US20210369709A1 (en) 2020-05-27 2021-12-02 Astrazeneca Ab EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER
WO2023287783A1 (en) * 2021-07-13 2023-01-19 ACEA Therapeutics, Inc. Heterocyclic compounds and uses thereof
IL315848A (en) 2022-03-31 2024-11-01 Astrazeneca Ab Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in combination with an AKT inhibitor for cancer treatment
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application in the treatment of cancer
WO2023209086A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds for treating cancer
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
PE20250268A1 (es) 2022-04-28 2025-01-29 Astrazeneca Ab Compuestos heteroaromaticos biciclicos condensados y uso en el tratamiento del cancer
EP4543920A1 (en) 2022-06-27 2025-04-30 Astrazeneca AB Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
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WO2025238661A1 (en) * 2024-05-17 2025-11-20 Bdr Lifesciences Private Limited An improved process for the preparation of osimertinib

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CN110526912B (zh) 2014-06-19 2023-02-14 武田药品工业株式会社 用于激酶抑制的杂芳基化合物
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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
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CN108024993B (zh) 2014-12-11 2020-11-06 贝达医药公司 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂

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

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