EA201790921A1 - Замещенные производные 2-анилинпиримидина в качестве модуляторов egfr - Google Patents

Замещенные производные 2-анилинпиримидина в качестве модуляторов egfr

Info

Publication number
EA201790921A1
EA201790921A1 EA201790921A EA201790921A EA201790921A1 EA 201790921 A1 EA201790921 A1 EA 201790921A1 EA 201790921 A EA201790921 A EA 201790921A EA 201790921 A EA201790921 A EA 201790921A EA 201790921 A1 EA201790921 A1 EA 201790921A1
Authority
EA
Eurasian Patent Office
Prior art keywords
anilinpyrimidin
substituted derivatives
egfr modulators
egfr
modulators
Prior art date
Application number
EA201790921A
Other languages
English (en)
Other versions
EA036453B1 (ru
Inventor
Цзижун Пэн
Майкл Джон Костанцо
Майкл Николас Греко
Майкл Алан Грин
Виктория Линн Уайлд
Дунь Чжан
Original Assignee
Бета Фарма, Инк.
Бета Фарма (Шанхай) Ко., Лтд.
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 Бета Фарма, Инк., Бета Фарма (Шанхай) Ко., Лтд. filed Critical Бета Фарма, Инк.
Publication of EA201790921A1 publication Critical patent/EA201790921A1/ru
Publication of EA036453B1 publication Critical patent/EA036453B1/ru

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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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)

Abstract

В настоящей заявке предложены новые замещенные производные 2-анилинпиримидина и их фармацевтически приемлемые соли, сольваты, пролекарства и композиции, подходящие для лечения или предотвращения заболеваний или состояний, опосредованных рецепторами эпидермального фактора роста (EGFR), включая, но не ограничиваясь ими, различные виды рака.
EA201790921A 2014-12-11 2015-12-11 Замещенные производные 2-анилинпиримидина в качестве модуляторов egfr EA036453B1 (ru)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
EA201790921A1 true EA201790921A1 (ru) 2017-12-29
EA036453B1 EA036453B1 (ru) 2020-11-12

Family

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EA201790921A EA036453B1 (ru) 2014-12-11 2015-12-11 Замещенные производные 2-анилинпиримидина в качестве модуляторов egfr

Country Status (17)

Country Link
US (2) US10590111B2 (ru)
EP (1) EP3229798A4 (ru)
JP (2) JP6709786B2 (ru)
KR (1) KR20170098865A (ru)
CN (3) CN112375067B (ru)
AU (1) AU2015360360B2 (ru)
BR (1) BR112017012272A2 (ru)
CA (1) CA2970185C (ru)
CO (1) CO2017006962A2 (ru)
EA (1) EA036453B1 (ru)
HK (1) HK1245634A1 (ru)
IL (1) IL252554A0 (ru)
MX (1) MX2017007664A (ru)
PH (1) PH12017501057A1 (ru)
SG (2) SG10201909060SA (ru)
TW (1) TWI618704B (ru)
WO (1) WO2016094821A2 (ru)

Families Citing this family (24)

* 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
CN112375067B (zh) * 2014-12-11 2024-03-15 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
SG11201809931YA (en) * 2016-05-11 2018-12-28 Beta Pharma Inc 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
US10513509B2 (en) 2016-05-26 2019-12-24 Recurium Ip Holdings, Llc EGFR inhibitor compounds
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
CN110818690B (zh) * 2016-07-26 2021-08-10 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
WO2018232235A1 (en) * 2017-06-16 2018-12-20 Beta Pharma, Inc. Pharmaceutical formulations of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and salts thereof
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
AU2019289176A1 (en) * 2018-06-18 2020-12-24 Oxford University Innovation Limited Gremlin-1 antagonist for the prevention and treatment of cancer
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
WO2021094379A1 (en) 2019-11-12 2021-05-20 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
US20230056604A1 (en) 2020-01-20 2023-02-23 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
KR20240063865A (ko) * 2021-07-13 2024-05-10 아세아 테라퓨틱스 인코포레이티드 헤테로사이클릭 화합물 및 이의 용도
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
US20240116926A1 (en) 2022-04-28 2024-04-11 Astrazeneca Ab Heteroaromatic compounds
WO2023209084A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Condensed bicyclic heteroaromatic compounds and their use in 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
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
WO2024002938A1 (en) 2022-06-27 2024-01-04 Astrazeneca Ab Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
WO2024008929A1 (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
IL150388A0 (en) * 1999-12-24 2002-12-01 Aventis Pharma Ltd Azaindoles
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
MX2009005508A (es) * 2006-12-08 2009-06-03 Hoffmann La Roche Pirimidinas substituidas y su uso como moduladores de cinasas c-jun n-terminales.
WO2010059711A1 (en) * 2008-11-18 2010-05-27 Wisconsin Alumni Research Foundation Sigma-1 receptor ligands and methods of use
CA2760794C (en) * 2009-05-05 2017-07-25 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
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
HUE037645T2 (hu) * 2011-07-27 2018-09-28 Astrazeneca Ab Rák kezelésére alkalmas 2.(2,4,5-helyettesített-anilino)pirimidin származékok mint EGFR modulátorok
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
US10227342B2 (en) * 2014-06-19 2019-03-12 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
CN113121575A (zh) * 2014-08-25 2021-07-16 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
CN112375067B (zh) * 2014-12-11 2024-03-15 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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JP2020143131A (ja) 2020-09-10
CN112375067A (zh) 2021-02-19
EP3229798A4 (en) 2018-05-30
CN108024993B (zh) 2020-11-06
JP2017537114A (ja) 2017-12-14
US20170362203A1 (en) 2017-12-21
PH12017501057A1 (en) 2018-03-05
CN112457298B (zh) 2024-05-07
SG10201909060SA (en) 2019-11-28
CN108024993A (zh) 2018-05-11
KR20170098865A (ko) 2017-08-30
AU2015360360B2 (en) 2020-06-25
EP3229798A2 (en) 2017-10-18
JP7181558B2 (ja) 2022-12-01
US10590111B2 (en) 2020-03-17
SG11201704685TA (en) 2017-07-28
CO2017006962A2 (es) 2017-10-20
TWI618704B (zh) 2018-03-21
JP6709786B2 (ja) 2020-06-17
TW201632512A (zh) 2016-09-16
CA2970185A1 (en) 2016-06-16
EA036453B1 (ru) 2020-11-12
CN112375067B (zh) 2024-03-15
AU2015360360A1 (en) 2017-06-08
WO2016094821A3 (en) 2016-08-25
US11414401B2 (en) 2022-08-16
IL252554A0 (en) 2017-07-31
MX2017007664A (es) 2018-01-23
BR112017012272A2 (pt) 2018-01-30
HK1245634A1 (zh) 2018-08-31
WO2016094821A2 (en) 2016-06-16
US20200216421A1 (en) 2020-07-09
CN112457298A (zh) 2021-03-09
CA2970185C (en) 2023-10-17

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