CA2970185C - Substituted 2-anilinopyrimidine derivatives as egfr modulators - Google Patents

Substituted 2-anilinopyrimidine derivatives as egfr modulators Download PDF

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Publication number
CA2970185C
CA2970185C CA2970185A CA2970185A CA2970185C CA 2970185 C CA2970185 C CA 2970185C CA 2970185 A CA2970185 A CA 2970185A CA 2970185 A CA2970185 A CA 2970185A CA 2970185 C CA2970185 C CA 2970185C
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Prior art keywords
compound
cancer
pharmaceutically acceptable
solvate
acceptable salt
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CA2970185A
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English (en)
French (fr)
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CA2970185A1 (en
Inventor
Jirong Peng
Michael John COSTANZO
Michael Nicholas Greco
Michael Alan Green
Victoria Lynn Wilde
Don Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Beta Pharma (shanghai) Co Ltd
Beta Pharma Inc
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Beta Pharma (shanghai) Co Ltd
Beta Pharma Inc
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Publication of CA2970185A1 publication Critical patent/CA2970185A1/en
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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)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
CA2970185A 2014-12-11 2015-12-11 Substituted 2-anilinopyrimidine derivatives as egfr modulators Active CA2970185C (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
CA2970185A1 CA2970185A1 (en) 2016-06-16
CA2970185C true CA2970185C (en) 2023-10-17

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Application Number Title Priority Date Filing Date
CA2970185A Active CA2970185C (en) 2014-12-11 2015-12-11 Substituted 2-anilinopyrimidine derivatives as egfr modulators

Country Status (17)

Country Link
US (2) US10590111B2 (cg-RX-API-DMAC7.html)
EP (1) EP3229798A4 (cg-RX-API-DMAC7.html)
JP (2) JP6709786B2 (cg-RX-API-DMAC7.html)
KR (1) KR20170098865A (cg-RX-API-DMAC7.html)
CN (3) CN112375067B (cg-RX-API-DMAC7.html)
AU (1) AU2015360360B2 (cg-RX-API-DMAC7.html)
BR (1) BR112017012272A2 (cg-RX-API-DMAC7.html)
CA (1) CA2970185C (cg-RX-API-DMAC7.html)
CO (1) CO2017006962A2 (cg-RX-API-DMAC7.html)
EA (1) EA036453B1 (cg-RX-API-DMAC7.html)
HK (1) HK1245634A1 (cg-RX-API-DMAC7.html)
IL (1) IL252554A0 (cg-RX-API-DMAC7.html)
MX (1) MX382869B (cg-RX-API-DMAC7.html)
PH (1) PH12017501057A1 (cg-RX-API-DMAC7.html)
SG (2) SG10201909060SA (cg-RX-API-DMAC7.html)
TW (1) TWI618704B (cg-RX-API-DMAC7.html)
WO (1) WO2016094821A2 (cg-RX-API-DMAC7.html)

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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
EA201892311A1 (ru) * 2016-05-11 2019-06-28 Бета Фарма, Инк. Производные 2-анилинопиримидина в качестве терапевтических агентов для лечения рака мозга
JP7030066B2 (ja) 2016-05-26 2022-03-04 リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー Egfr阻害剤化合物
KR20190018494A (ko) * 2016-06-17 2019-02-22 베타 파마, 인크. N-(2-(2-(디메틸아미노)에톡시)-4-메톡시-5-((4-(1-메틸-1h-인돌-3-일)피리미딘-2-일)아미노)페닐)아크릴아미드의 제약 염 및 그의 결정질 형태
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
EP3638241B1 (en) 2017-06-16 2022-05-25 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
KR20210028191A (ko) * 2018-06-18 2021-03-11 유씨비 바이오파마 에스알엘 암을 예방 및 치료하기 위한 gremlin-1 길항제
CA3112043A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
CN114430681A (zh) * 2019-09-23 2022-05-03 贝达医药公司 使用egfr和cdk4/6抑制剂的组合治疗egfr突变相关的癌症
US20210161897A1 (en) 2019-11-12 2021-06-03 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
CN114980883A (zh) 2020-01-20 2022-08-30 阿斯利康(瑞典)有限公司 用于治疗癌症的表皮生长因子受体酪氨酸激酶抑制剂
US20210369709A1 (en) 2020-05-27 2021-12-02 Astrazeneca Ab EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER
AU2022312430A1 (en) * 2021-07-13 2024-02-29 ACEA Therapeutics, Inc. Heterocyclic compounds and uses thereof
AU2023246862A1 (en) 2022-03-31 2024-10-31 Astrazeneca Ab Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer
WO2023209086A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds for treating cancer
CA3249080A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab CONDENSED BICYCLIC HETEROAROMATIC COMPOUNDS AND THEIR USE IN CANCER TREATMENT
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
KR20250029133A (ko) 2022-06-27 2025-03-04 아스트라제네카 아베 암 치료를 위한 표피성장인자 수용체 티로신 키나제 억제제를 포함하는 조합물
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

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JP6709786B2 (ja) 2020-06-17
PH12017501057A1 (en) 2018-03-05
HK1245634A1 (zh) 2018-08-31
AU2015360360B2 (en) 2020-06-25
JP2020143131A (ja) 2020-09-10
CO2017006962A2 (es) 2017-10-20
CN112457298A (zh) 2021-03-09
CN108024993A (zh) 2018-05-11
US20170362203A1 (en) 2017-12-21
EP3229798A4 (en) 2018-05-30
IL252554A0 (en) 2017-07-31
CN112375067A (zh) 2021-02-19
TW201632512A (zh) 2016-09-16
CN112375067B (zh) 2024-03-15
EA036453B1 (ru) 2020-11-12
CA2970185A1 (en) 2016-06-16
WO2016094821A2 (en) 2016-06-16
MX382869B (es) 2025-03-13
AU2015360360A1 (en) 2017-06-08
CN112457298B (zh) 2024-05-07
MX2017007664A (es) 2018-01-23
CN108024993B (zh) 2020-11-06
US10590111B2 (en) 2020-03-17
BR112017012272A2 (pt) 2018-01-30
US11414401B2 (en) 2022-08-16
SG11201704685TA (en) 2017-07-28
WO2016094821A3 (en) 2016-08-25
SG10201909060SA (en) 2019-11-28
US20200216421A1 (en) 2020-07-09
TWI618704B (zh) 2018-03-21
KR20170098865A (ko) 2017-08-30
JP2017537114A (ja) 2017-12-14
EP3229798A2 (en) 2017-10-18
EA201790921A1 (ru) 2017-12-29
JP7181558B2 (ja) 2022-12-01

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