AU2015360360B2 - Substituted 2-anilinopyrimidine derivatives as EGFR modulators - Google Patents

Substituted 2-anilinopyrimidine derivatives as EGFR modulators Download PDF

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Publication number
AU2015360360B2
AU2015360360B2 AU2015360360A AU2015360360A AU2015360360B2 AU 2015360360 B2 AU2015360360 B2 AU 2015360360B2 AU 2015360360 A AU2015360360 A AU 2015360360A AU 2015360360 A AU2015360360 A AU 2015360360A AU 2015360360 B2 AU2015360360 B2 AU 2015360360B2
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cancer
methyl
pharmaceutically acceptable
compound
hydrogen
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AU2015360360A1 (en
Inventor
Michael John COSTANZO
Michael Nicholas Greco
Michael Alan Green
Jirong Peng
Victoria Lynn Wilde
Don Zhang
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Beta Pharma (shanghai) Co Ltd
Beta Pharma Inc
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Beta Pharma Shanghai Co Ltd
Beta Pharma Inc
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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)
AU2015360360A 2014-12-11 2015-12-11 Substituted 2-anilinopyrimidine derivatives as EGFR modulators Active AU2015360360B2 (en)

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 (2)

Publication Number Publication Date
AU2015360360A1 AU2015360360A1 (en) 2017-06-08
AU2015360360B2 true AU2015360360B2 (en) 2020-06-25

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AU2015360360A Active AU2015360360B2 (en) 2014-12-11 2015-12-11 Substituted 2-anilinopyrimidine derivatives as EGFR modulators

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US (2) US10590111B2 (enExample)
EP (1) EP3229798A4 (enExample)
JP (2) JP6709786B2 (enExample)
KR (1) KR20170098865A (enExample)
CN (3) CN112457298B (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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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
WO2016094821A2 (en) * 2014-12-11 2016-06-16 Beta Pharma, Inc. Substituted 2-anilinopyrimidine derivatives as egfr modulators
MX2018013602A (es) 2016-05-11 2019-08-22 Beta Pharma Inc Derivados de 2-anilinopirimidina como agentes terapeuticos para el tratamiento de canceres cerebrales.
SG11201809751XA (en) 2016-05-26 2018-12-28 Zeno Royalties & Milestones Llc Egfr inhibitor compounds
TW201800404A (zh) * 2016-06-17 2018-01-01 貝達醫藥公司 N-(2-(2-(二甲基胺基)乙氧基)-4-甲氧基-5-((4-(1-甲基-1h-吲哚-3-基)嘧啶-2-基)胺基)苯基)丙烯醯胺及其結晶型式之醫藥鹽
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
TW201904577A (zh) 2017-06-16 2019-02-01 美商貝達醫藥公司 N-(2-(2-二甲胺基)乙氧基)-4-甲氧基-5-((4-(1-甲基-1h-吲哚-3-基)嘧啶-2-基)胺基)苯基)丙烯醯胺及其鹽之醫藥調配物
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
SG11202012312UA (en) * 2018-06-18 2021-01-28 UCB Biopharma SRL Gremlin-1 antagonist for the prevention and treatment of cancer
CA3112043A1 (en) 2018-09-10 2020-03-19 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
AU2021211871A1 (en) 2020-01-20 2022-09-08 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
JP2024527402A (ja) * 2021-07-13 2024-07-24 エイシア セラピューティクス, インコーポレイテッド 複素環式化合物およびその用途
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
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 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
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application in the treatment of cancer
KR20250029133A (ko) 2022-06-27 2025-03-04 아스트라제네카 아베 암 치료를 위한 표피성장인자 수용체 티로신 키나제 억제제를 포함하는 조합물
CN119654152A (zh) 2022-07-08 2025-03-18 阿斯利康(瑞典)有限公司 与hgf-受体抑制剂组合用于治疗癌症的表皮生长因子受体酪氨酸激酶抑制剂

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WO2001047922A2 (en) * 1999-12-24 2001-07-05 Aventis Pharma Limited Azaindoles
US20080146565A1 (en) * 2006-12-08 2008-06-19 Roche Palo Alto Llc JNK modulators
WO2010059711A1 (en) * 2008-11-18 2010-05-27 Wisconsin Alumni Research Foundation Sigma-1 receptor ligands and methods of use
WO2010129053A2 (en) * 2009-05-05 2010-11-11 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
US7943616B2 (en) * 2001-06-21 2011-05-17 Aventis Pharmaceuticals Inc. Azaindoles for inhibiting aurora2 and other kinases
US20120316135A1 (en) * 2011-05-04 2012-12-13 Ariad Pharmaceuticals, Inc. Compounds for Inhibiting Cell Proliferation in EGFR-Driven Cancers
WO2013014448A1 (en) * 2011-07-27 2013-01-31 Astrazeneca Ab 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer
WO2015195228A1 (en) * 2014-06-19 2015-12-23 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
WO2016070816A1 (zh) * 2014-11-05 2016-05-12 上海页岩科技有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途

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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
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
WO2016094821A2 (en) * 2014-12-11 2016-06-16 Beta Pharma, Inc. Substituted 2-anilinopyrimidine derivatives as egfr modulators

Patent Citations (10)

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WO2001047922A2 (en) * 1999-12-24 2001-07-05 Aventis Pharma Limited Azaindoles
US7943616B2 (en) * 2001-06-21 2011-05-17 Aventis Pharmaceuticals Inc. Azaindoles for inhibiting aurora2 and other kinases
US20080146565A1 (en) * 2006-12-08 2008-06-19 Roche Palo Alto Llc JNK modulators
WO2010059711A1 (en) * 2008-11-18 2010-05-27 Wisconsin Alumni Research Foundation Sigma-1 receptor ligands and methods of use
WO2010129053A2 (en) * 2009-05-05 2010-11-11 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
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CN112457298B (zh) 2024-05-07
PH12017501057A1 (en) 2018-03-05
MX382869B (es) 2025-03-13
SG11201704685TA (en) 2017-07-28
CA2970185A1 (en) 2016-06-16
CN112457298A (zh) 2021-03-09
CN112375067A (zh) 2021-02-19
US11414401B2 (en) 2022-08-16
US20170362203A1 (en) 2017-12-21
JP6709786B2 (ja) 2020-06-17
TW201632512A (zh) 2016-09-16
IL252554A0 (en) 2017-07-31
EP3229798A4 (en) 2018-05-30
TWI618704B (zh) 2018-03-21
JP7181558B2 (ja) 2022-12-01
BR112017012272A2 (pt) 2018-01-30
MX2017007664A (es) 2018-01-23
KR20170098865A (ko) 2017-08-30
JP2020143131A (ja) 2020-09-10
CN112375067B (zh) 2024-03-15
WO2016094821A2 (en) 2016-06-16
US20200216421A1 (en) 2020-07-09
US10590111B2 (en) 2020-03-17
CA2970185C (en) 2023-10-17
HK1245634A1 (zh) 2018-08-31
EA201790921A1 (ru) 2017-12-29
SG10201909060SA (en) 2019-11-28
JP2017537114A (ja) 2017-12-14
EP3229798A2 (en) 2017-10-18
CO2017006962A2 (es) 2017-10-20
CN108024993A (zh) 2018-05-11
CN108024993B (zh) 2020-11-06
EA036453B1 (ru) 2020-11-12
AU2015360360A1 (en) 2017-06-08
WO2016094821A3 (en) 2016-08-25

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Owner name: BETA PHARMA, INC.

Free format text: FORMER NAME(S): BETA PHARMA, INC.

Owner name: BETA PHARMA (SHANGHAI) CO., LTD.

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