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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Ceased
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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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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 (OSRAM)
EP (1) EP3229798A4 (OSRAM)
JP (2) JP6709786B2 (OSRAM)
KR (1) KR20170098865A (OSRAM)
CN (3) CN112457298B (OSRAM)
AU (1) AU2015360360B2 (OSRAM)
BR (1) BR112017012272A2 (OSRAM)
CA (1) CA2970185C (OSRAM)
CO (1) CO2017006962A2 (OSRAM)
EA (1) EA036453B1 (OSRAM)
HK (1) HK1245634A1 (OSRAM)
IL (1) IL252554A0 (OSRAM)
MX (1) MX382869B (OSRAM)
PH (1) PH12017501057A1 (OSRAM)
SG (2) SG10201909060SA (OSRAM)
TW (1) TWI618704B (OSRAM)
WO (1) WO2016094821A2 (OSRAM)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105085489B (zh) * 2014-11-05 2019-03-01 益方生物科技(上海)有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
CN112457298B (zh) * 2014-12-11 2024-05-07 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
TW201740951A (zh) * 2016-05-11 2017-12-01 貝達醫藥公司 做為用於治療腦癌的治療劑之2-苯胺嘧啶
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
SG11201810976TA (en) 2016-06-17 2019-01-30 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
JP7045726B2 (ja) * 2017-06-16 2022-04-01 ベータ ファーマ,インコーポレイテッド N-(2-(2-(ジメチルアミノ)エトキシ)-4-メトキシ-5-((4-(1-メチル-1h-インドール-3-イル)ピリミジン-2-イル)アミノ)フェニル)アクリルアミドおよびその塩の医薬品製剤
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
JP7565219B2 (ja) * 2018-06-18 2024-10-10 ユーシービー バイオファルマ エスアールエル がんを予防及び治療するためのgremlin-1アンタゴニスト
US12336995B2 (en) 2018-09-10 2025-06-24 Mirati Therapeutics, Inc. Combination therapies
EP4034121A4 (en) 2019-09-23 2023-10-18 Beta Pharma, Inc. TREATMENT OF EGFR MUTANT-RELATED CANCERS USING A COMBINATION OF EGFR AND CDK4/6 INHIBITORS
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
EP4370212A1 (en) * 2021-07-13 2024-05-22 ACEA Therapeutics, Inc. Heterocyclic compounds and uses thereof
WO2023187037A1 (en) 2022-03-31 2023-10-05 Astrazeneca Ab Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application in the treatment of cancer
US20240116926A1 (en) 2022-04-28 2024-04-11 Astrazeneca Ab Heteroaromatic compounds
CA3249080A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab CONDENSED BICYCLIC HETEROAROMATIC COMPOUNDS AND THEIR USE IN CANCER TREATMENT
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
IL317733A (en) 2022-06-27 2025-02-01 Astrazeneca Ab Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for cancer treatment
CA3261476A1 (en) 2022-07-08 2024-01-11 Astrazeneca Ab Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Combination with HGF Receptor Inhibitors for the Treatment of Cancer

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100379734C (zh) * 1999-12-24 2008-04-09 阿文蒂斯药物有限公司 氮杂吲哚类化合物
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
BRPI0720003A2 (pt) * 2006-12-08 2018-09-18 Hoffmann La Roche pirimidinas substituídas e seu uso como moduladores de jnk
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
CN103501612B (zh) * 2011-05-04 2017-03-29 阿里亚德医药股份有限公司 抑制表皮生长因子受体导致的癌症中细胞增殖的化合物
ME02887B (me) * 2011-07-27 2018-04-20 Astrazeneca Ab 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka
JP6469567B2 (ja) * 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Egfr発動性がんの細胞増殖阻害用化合物
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
AP2017009690A0 (en) * 2014-06-19 2017-01-31 Ariad Pharma Inc Heteroaryl compounds for kinase inhibition
WO2016029839A1 (zh) 2014-08-25 2016-03-03 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
CN105085489B (zh) * 2014-11-05 2019-03-01 益方生物科技(上海)有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
CN112457298B (zh) * 2014-12-11 2024-05-07 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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CN108024993B (zh) 2020-11-06
HK1245634A1 (zh) 2018-08-31
US20170362203A1 (en) 2017-12-21
EP3229798A2 (en) 2017-10-18
US11414401B2 (en) 2022-08-16
CN112375067B (zh) 2024-03-15
CN112457298B (zh) 2024-05-07
WO2016094821A2 (en) 2016-06-16
CN108024993A (zh) 2018-05-11
TWI618704B (zh) 2018-03-21
US10590111B2 (en) 2020-03-17
IL252554A0 (en) 2017-07-31
CN112457298A (zh) 2021-03-09
EA036453B1 (ru) 2020-11-12
JP7181558B2 (ja) 2022-12-01
AU2015360360A1 (en) 2017-06-08
TW201632512A (zh) 2016-09-16
US20200216421A1 (en) 2020-07-09
SG11201704685TA (en) 2017-07-28
MX382869B (es) 2025-03-13
CO2017006962A2 (es) 2017-10-20
JP6709786B2 (ja) 2020-06-17
JP2020143131A (ja) 2020-09-10
EP3229798A4 (en) 2018-05-30
SG10201909060SA (en) 2019-11-28
CA2970185C (en) 2023-10-17
BR112017012272A2 (pt) 2018-01-30
AU2015360360B2 (en) 2020-06-25
WO2016094821A3 (en) 2016-08-25
CN112375067A (zh) 2021-02-19
MX2017007664A (es) 2018-01-23
EA201790921A1 (ru) 2017-12-29
CA2970185A1 (en) 2016-06-16
PH12017501057A1 (en) 2018-03-05
JP2017537114A (ja) 2017-12-14

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