JP6709786B2 - Egfrモジュレーターとしての置換2−アミノピリミジン誘導体 - Google Patents

Egfrモジュレーターとしての置換2−アミノピリミジン誘導体 Download PDF

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JP6709786B2
JP6709786B2 JP2017530208A JP2017530208A JP6709786B2 JP 6709786 B2 JP6709786 B2 JP 6709786B2 JP 2017530208 A JP2017530208 A JP 2017530208A JP 2017530208 A JP2017530208 A JP 2017530208A JP 6709786 B2 JP6709786 B2 JP 6709786B2
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cancer
pharmaceutically acceptable
methyl
solvate
indol
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JP2017537114A5 (enExample
JP2017537114A (ja
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ペン,ジュロン
コスタンゾ,マイケル,ジョン
グレコ,マイケル,ニコラス
グリーン,マイケル,アラン
ワイルド,ビクトリア,リン
チャン,ドン
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ベータ ファーマ,インコーポレイテッド
ベータ ファーマ,インコーポレイテッド
ベータ ファーマ(シャンハイ)カンパニー,リミテッド
ベータ ファーマ(シャンハイ)カンパニー,リミテッド
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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)
JP2017530208A 2014-12-11 2015-12-11 Egfrモジュレーターとしての置換2−アミノピリミジン誘導体 Active JP6709786B2 (ja)

Applications Claiming Priority (5)

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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

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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) SG10201909060SA (enExample)
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JP2020143131A (ja) * 2014-12-11 2020-09-10 ベータ ファーマ,インコーポレイテッド Egfrモジュレーターとしての置換2−アミノピリミジン誘導体

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SG11201809931YA (en) * 2016-05-11 2018-12-28 Beta Pharma Inc 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
KR102444835B1 (ko) 2016-05-26 2022-09-19 리커리엄 아이피 홀딩스, 엘엘씨 Egfr 억제제 화합물
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
EP3492462B1 (en) * 2016-07-26 2023-08-30 Shenzhen TargetRx, Inc. Amino pyrimidine compound for inhibiting protein tyrosine kinase activity
US11180478B2 (en) * 2017-06-16 2021-11-23 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
MX2020013808A (es) * 2018-06-18 2021-05-27 UCB Biopharma SRL Antagonista de gremlina-1 para la prevencion y el tratamiento del cancer.
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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
KR20220130190A (ko) 2020-01-20 2022-09-26 아스트라제네카 아베 암 치료를 위한 표피성장인자 수용체 티로신 키나제 억제제
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
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
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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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Publication number Priority date Publication date Assignee Title
JP2020143131A (ja) * 2014-12-11 2020-09-10 ベータ ファーマ,インコーポレイテッド Egfrモジュレーターとしての置換2−アミノピリミジン誘導体
JP7181558B2 (ja) 2014-12-11 2022-12-01 ベータ ファーマ,インコーポレイテッド Egfrモジュレーターとしての置換2-アミノピリミジン誘導体

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CN112375067A (zh) 2021-02-19
CO2017006962A2 (es) 2017-10-20
BR112017012272A2 (pt) 2018-01-30
AU2015360360A1 (en) 2017-06-08
SG10201909060SA (en) 2019-11-28
MX2017007664A (es) 2018-01-23
US11414401B2 (en) 2022-08-16
WO2016094821A3 (en) 2016-08-25
JP2020143131A (ja) 2020-09-10
EP3229798A4 (en) 2018-05-30
CN112375067B (zh) 2024-03-15
CN108024993B (zh) 2020-11-06
PH12017501057A1 (en) 2018-03-05
CA2970185A1 (en) 2016-06-16
WO2016094821A2 (en) 2016-06-16
KR20170098865A (ko) 2017-08-30
TWI618704B (zh) 2018-03-21
US10590111B2 (en) 2020-03-17
TW201632512A (zh) 2016-09-16
EA036453B1 (ru) 2020-11-12
US20170362203A1 (en) 2017-12-21
CN112457298A (zh) 2021-03-09
IL252554A0 (en) 2017-07-31
MX382869B (es) 2025-03-13
EA201790921A1 (ru) 2017-12-29
US20200216421A1 (en) 2020-07-09
JP7181558B2 (ja) 2022-12-01
JP2017537114A (ja) 2017-12-14
CN112457298B (zh) 2024-05-07
EP3229798A2 (en) 2017-10-18
SG11201704685TA (en) 2017-07-28
HK1245634A1 (zh) 2018-08-31
CA2970185C (en) 2023-10-17
CN108024993A (zh) 2018-05-11
AU2015360360B2 (en) 2020-06-25

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