JP2021514400A - Ｅｇｆｒの阻害剤およびその使用法 - Google Patents

Ｅｇｆｒの阻害剤およびその使用法 Download PDF

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Publication number
JP2021514400A
JP2021514400A JP2020566548A JP2020566548A JP2021514400A JP 2021514400 A JP2021514400 A JP 2021514400A JP 2020566548 A JP2020566548 A JP 2020566548A JP 2020566548 A JP2020566548 A JP 2020566548A JP 2021514400 A JP2021514400 A JP 2021514400A
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JP
Japan
Prior art keywords
carbon atoms
egfr
formula
optionally substituted
heteroaryl
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Pending
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JP2020566548A
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English (en)
Japanese (ja)
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JPWO2019164948A5 (https=
JP2021514400A5 (https=
Inventor
ナサニエル・エス・グレイ
ドリス・ド・クレルク
ジェボン・ジャン
パシ・ジャンヌ
チリッチ・ト
マイケル・エク
ウンヨン・パク
デイヴィッド・ヘップナー
Original Assignee
デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド
デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド
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Application filed by デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド, デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド filed Critical デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド
Publication of JP2021514400A publication Critical patent/JP2021514400A/ja
Publication of JPWO2019164948A5 publication Critical patent/JPWO2019164948A5/ja
Publication of JP2021514400A5 publication Critical patent/JP2021514400A5/ja
Pending legal-status Critical Current

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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/38—[b, e]- or [b, f]-condensed with six-membered 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
    • C07D403/02—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
    • 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
    • C07D403/10—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 linked by a carbon chain containing aromatic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2020566548A 2018-02-20 2019-02-20 Ｅｇｆｒの阻害剤およびその使用法 Pending JP2021514400A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862632819P 2018-02-20 2018-02-20
US62/632,819 2018-02-20
US201862744086P 2018-10-10 2018-10-10
US62/744,086 2018-10-10
PCT/US2019/018773 WO2019164948A1 (en) 2018-02-20 2019-02-20 Inhibitors of egfr and methods of use thereof

Publications (3)

Publication Number Publication Date
JP2021514400A true JP2021514400A (ja) 2021-06-10
JPWO2019164948A5 JPWO2019164948A5 (https=) 2022-02-25
JP2021514400A5 JP2021514400A5 (https=) 2022-02-25

Family

ID=67687390

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2020566548A Pending JP2021514400A (ja) 2018-02-20 2019-02-20 Ｅｇｆｒの阻害剤およびその使用法

Country Status (6)

Country Link
US (1) US20200390783A1 (https=)
EP (1) EP3755690A4 (https=)
JP (1) JP2021514400A (https=)
AU (1) AU2019225806A1 (https=)
CA (1) CA3087288A1 (https=)
WO (1) WO2019164948A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021514399A (ja) * 2018-02-20 2021-06-10 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Ｅｇｆｒの阻害剤およびその使用法

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CN119317636A (zh) * 2023-03-07 2025-01-14 艾博生物科技(上海)有限公司 编码活化EGFR突变肽的免疫调节治疗性mRNA组合物
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Citations (13)

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US20040254159A1 (en) * 2003-02-27 2004-12-16 Hasvold Lisa A. Heterocyclic kinase inhibitors
WO2006061126A2 (en) * 2004-12-09 2006-06-15 F. Hoffmann-La Roche Ag Dibenzoxazepinone derivatives
US20070105835A1 (en) * 2005-11-07 2007-05-10 Kazantsev Aleksey G Compositions and methods for modulating poly(ADP-ribose) polymerase activity
WO2009124399A1 (en) * 2008-04-11 2009-10-15 Thallion Pharmaceuticals Inc. Inhibition of cell migration by a farnesylated dibenzodiazepinone
WO2012045194A1 (en) * 2010-10-09 2012-04-12 Abbott Laboratories Benzodiazepinones as fak inhibitors for treatment of cancer
JP2012511054A (ja) * 2008-12-08 2012-05-17 ブイエム ファーマ エルエルシー タンパク質受容体チロシンキナーゼ阻害薬の組成物
WO2014160430A1 (en) * 2013-03-13 2014-10-02 Georgetown University Small molecule lrrk2 and erk5 inhibitors
JP2015205911A (ja) * 2009-01-06 2015-11-19 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド ピリミド−ジアゼピノンキナーゼ骨格化合物及び疾患を治療する方法
WO2015196072A2 (en) * 2014-06-19 2015-12-23 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
WO2017024317A2 (en) * 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2017177092A1 (en) * 2016-04-07 2017-10-12 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating pi3k-mediated disorders
WO2017185023A1 (en) * 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 9 (cdk9) by conjugation of cdk9 inhibitors with e3 ligase ligand and methods of use
JP2021514399A (ja) * 2018-02-20 2021-06-10 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Ｅｇｆｒの阻害剤およびその使用法

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040254159A1 (en) * 2003-02-27 2004-12-16 Hasvold Lisa A. Heterocyclic kinase inhibitors
WO2006061126A2 (en) * 2004-12-09 2006-06-15 F. Hoffmann-La Roche Ag Dibenzoxazepinone derivatives
US20070105835A1 (en) * 2005-11-07 2007-05-10 Kazantsev Aleksey G Compositions and methods for modulating poly(ADP-ribose) polymerase activity
WO2009124399A1 (en) * 2008-04-11 2009-10-15 Thallion Pharmaceuticals Inc. Inhibition of cell migration by a farnesylated dibenzodiazepinone
JP2012511054A (ja) * 2008-12-08 2012-05-17 ブイエム ファーマ エルエルシー タンパク質受容体チロシンキナーゼ阻害薬の組成物
JP2015205911A (ja) * 2009-01-06 2015-11-19 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド ピリミド−ジアゼピノンキナーゼ骨格化合物及び疾患を治療する方法
WO2012045194A1 (en) * 2010-10-09 2012-04-12 Abbott Laboratories Benzodiazepinones as fak inhibitors for treatment of cancer
WO2014160430A1 (en) * 2013-03-13 2014-10-02 Georgetown University Small molecule lrrk2 and erk5 inhibitors
WO2015196072A2 (en) * 2014-06-19 2015-12-23 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
WO2017024317A2 (en) * 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2017177092A1 (en) * 2016-04-07 2017-10-12 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating pi3k-mediated disorders
WO2017185023A1 (en) * 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 9 (cdk9) by conjugation of cdk9 inhibitors with e3 ligase ligand and methods of use
JP2021514399A (ja) * 2018-02-20 2021-06-10 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Ｅｇｆｒの阻害剤およびその使用法

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MASTALERZ, HAROLD ET AL.: "Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. (2007), 17(10), 2828-2833, JPN6023003317, 2007, ISSN: 0004975939 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021514399A (ja) * 2018-02-20 2021-06-10 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Ｅｇｆｒの阻害剤およびその使用法
JP7335275B2 (ja) 2018-02-20 2023-08-29 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Ｅｇｆｒの阻害剤およびその使用法

Also Published As

Publication number Publication date
EP3755690A4 (en) 2021-10-27
CA3087288A1 (en) 2019-08-29
WO2019164948A1 (en) 2019-08-29
AU2019225806A1 (en) 2020-07-16
EP3755690A1 (en) 2020-12-30
US20200390783A1 (en) 2020-12-17

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