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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-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) 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) SG10201909060SA (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
AU2015360360B2 (en) * 2014-12-11 2020-06-25 Beta Pharma (Shanghai) Co., Ltd. Substituted 2-anilinopyrimidine derivatives as EGFR modulators
AU2017264839B2 (en) * 2016-05-11 2021-08-05 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
WO2017218892A1 (en) * 2016-06-17 2017-12-21 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
SG11201911859QA (en) 2017-06-16 2020-01-30 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
AU2019289176B2 (en) * 2018-06-18 2026-02-19 Adelaide university Gremlin-1 antagonist for the prevention and treatment of cancer
CA3112043A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
AU2020352528A1 (en) * 2019-09-23 2022-04-21 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
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
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
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
AU2023262556A1 (en) 2022-04-28 2024-12-05 Astrazeneca Ab Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer
US20240116926A1 (en) 2022-04-28 2024-04-11 Astrazeneca Ab Heteroaromatic compounds
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
JP2025525410A (ja) 2022-06-27 2025-08-05 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成長因子受容体チロシンキナーゼ阻害剤を伴う組み合わせ
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
WO2025238661A1 (en) * 2024-05-17 2025-11-20 Bdr Lifesciences Private Limited An improved process for the preparation of osimertinib

Citations (9)

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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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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
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
AU2015360360B2 (en) * 2014-12-11 2020-06-25 Beta Pharma (Shanghai) Co., Ltd. Substituted 2-anilinopyrimidine derivatives as EGFR modulators

Patent Citations (10)

* Cited by examiner, † Cited by third party
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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
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
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WO2015195228A1 (en) * 2014-06-19 2015-12-23 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
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Publication number Publication date
CA2970185C (en) 2023-10-17
HK1245634A1 (zh) 2018-08-31
WO2016094821A2 (en) 2016-06-16
US20200216421A1 (en) 2020-07-09
SG10201909060SA (en) 2019-11-28
EA201790921A1 (ru) 2017-12-29
TWI618704B (zh) 2018-03-21
CN108024993B (zh) 2020-11-06
CN108024993A (zh) 2018-05-11
MX382869B (es) 2025-03-13
EP3229798A4 (en) 2018-05-30
CN112375067B (zh) 2024-03-15
EA036453B1 (ru) 2020-11-12
BR112017012272A2 (pt) 2018-01-30
KR20170098865A (ko) 2017-08-30
CN112375067A (zh) 2021-02-19
PH12017501057A1 (en) 2018-03-05
AU2015360360A1 (en) 2017-06-08
CN112457298A (zh) 2021-03-09
CA2970185A1 (en) 2016-06-16
JP7181558B2 (ja) 2022-12-01
JP2017537114A (ja) 2017-12-14
US11414401B2 (en) 2022-08-16
JP2020143131A (ja) 2020-09-10
WO2016094821A3 (en) 2016-08-25
SG11201704685TA (en) 2017-07-28
TW201632512A (zh) 2016-09-16
IL252554A0 (en) 2017-07-31
MX2017007664A (es) 2018-01-23
CO2017006962A2 (es) 2017-10-20
CN112457298B (zh) 2024-05-07
EP3229798A2 (en) 2017-10-18
US10590111B2 (en) 2020-03-17
JP6709786B2 (ja) 2020-06-17
US20170362203A1 (en) 2017-12-21

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Owner name: BETA PHARMA, INC.

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

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