CN119343350A - Egfr抑制剂多晶型形式 - Google Patents

Egfr抑制剂多晶型形式 Download PDF

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Publication number
CN119343350A
CN119343350A CN202280077001.9A CN202280077001A CN119343350A CN 119343350 A CN119343350 A CN 119343350A CN 202280077001 A CN202280077001 A CN 202280077001A CN 119343350 A CN119343350 A CN 119343350A
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CN
China
Prior art keywords
compound
polymorph
cancer
polymorphic
suspension
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN202280077001.9A
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English (en)
Chinese (zh)
Inventor
F·布拉特
A·R·迈尔
N·图菲力
J-M·韦尼耶
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.)
Yirui Shikang Pharmaceutical Research And Development Co
Original Assignee
Yirui Shikang Pharmaceutical Research And Development Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Yirui Shikang Pharmaceutical Research And Development Co filed Critical Yirui Shikang Pharmaceutical Research And Development Co
Publication of CN119343350A publication Critical patent/CN119343350A/zh
Pending legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN202280077001.9A 2021-09-23 2022-09-23 Egfr抑制剂多晶型形式 Pending CN119343350A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163247774P 2021-09-23 2021-09-23
US63/247,774 2021-09-23
PCT/US2022/044475 WO2023049312A1 (en) 2021-09-23 2022-09-23 Egfr inhibitor polymorph forms

Publications (1)

Publication Number Publication Date
CN119343350A true CN119343350A (zh) 2025-01-21

Family

ID=85721153

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202280077001.9A Pending CN119343350A (zh) 2021-09-23 2022-09-23 Egfr抑制剂多晶型形式

Country Status (10)

Country Link
US (1) US12545686B2 (https=)
EP (1) EP4405360A4 (https=)
JP (1) JP2024535380A (https=)
KR (1) KR20250005041A (https=)
CN (1) CN119343350A (https=)
AU (1) AU2022350669A1 (https=)
CA (1) CA3233057A1 (https=)
IL (1) IL311616A (https=)
MX (1) MX2024003495A (https=)
WO (1) WO2023049312A1 (https=)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102809395B1 (ko) * 2019-03-15 2025-05-16 더 리전트 오브 더 유니버시티 오브 캘리포니아 암을 치료하기 위한 조성물 및 방법
EP4405360A4 (en) 2021-09-23 2025-08-20 Erasca Inc POLYMORPHIC FORMS OF EGFR INHIBITOR
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025255438A1 (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
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
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
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

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5538325A (en) 1978-09-11 1980-03-17 Sankyo Co Ltd 4-anilinoquinazoline derivative and its preparation
GB9323290D0 (en) 1992-12-10 1994-01-05 Zeneca Ltd Quinazoline derivatives
GB9510757D0 (en) 1994-09-19 1995-07-19 Wellcome Found Therapeuticaly active compounds
DE69536015D1 (de) 1995-03-30 2009-12-10 Pfizer Prod Inc Chinazolinone Derivate
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
GB9514265D0 (en) 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
CA2258548C (en) 1996-06-24 2005-07-26 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
US6706721B1 (en) 1998-04-29 2004-03-16 Osi Pharmaceuticals, Inc. N-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate anhydrate and monohydrate
KR100397792B1 (ko) 2001-06-28 2003-09-13 한국과학기술연구원 4-(페닐아미노)-[1,4]디옥사노[2,3-ｇ]퀴나졸린 유도체 및그의 제조방법
EP1491211A4 (en) 2002-03-29 2010-01-13 Astellas Pharma Inc DRUG AGAINST GLIOBLASTOMA
CN101219992B (zh) * 2003-02-12 2011-08-31 日产化学工业株式会社 匹伐他汀钙的晶形
EP1687308B1 (en) * 2003-11-17 2019-06-12 Merck & Cie Process for preparating (6R)-L-erythrotetrahydrobiopterin hydrochloride crystalline form B from other crystalline forms
CN1854130B (zh) 2005-04-15 2011-04-20 中国医学科学院药物研究所 喹唑啉衍生物、及其制法和药物组合物与用途
EP1960552A2 (en) 2005-12-16 2008-08-27 Genentech, Inc. Method for diagnosing, prognosing and treating glioma
JP2010501572A (ja) 2006-08-22 2010-01-21 コンサート ファーマシューティカルズ インコーポレイテッド ４−アミノキナゾリン誘導体およびその使用方法
WO2008046242A1 (fr) 2006-10-16 2008-04-24 Institute Of Mataria Medica, Chinese Academy Of Medical Sciences Nouveaux dérivés quinazolines, leurs procédés de préparation et leurs utilisations
JP2008308491A (ja) 2007-05-11 2008-12-25 Gunma Univ がん治療用の遊走阻害剤
TW201019961A (en) 2008-10-17 2010-06-01 Genentech Inc Combination therapy
WO2011035540A1 (zh) 2009-09-28 2011-03-31 齐鲁制药有限公司 作为酪氨酸激酶抑制剂的4-（取代苯胺基）喹唑啉衍生物
EA021439B1 (ru) 2009-11-03 2015-06-30 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Хиназолиновые соединения
BRPI1003128A2 (pt) 2010-08-06 2012-04-10 Unicamp processo de sìntese dos compostos meta e para-4-arilaminoquinazolìnicos para inibição da atividade tirosina-quinase do fator de crescimento epidérmico (egfrk)
ITPD20110091A1 (it) 2011-03-24 2012-09-25 Univ Padova Inibitori multitirosinchinasi utili per le patologie correlate: modelli farmacoforici, composti identificati tramite questi modelli, metodi per la loro preparazione, la loro formulazione e il loro impiego terapeutico.
WO2013013614A1 (zh) 2011-07-28 2013-01-31 南京英派药业有限公司 4-(3-杂芳基芳基氨基)喹唑啉和1-(3-杂芳基芳基氨基)异喹啉作为Hedgehog通路抑制剂及其应用
CN103965211A (zh) 2013-02-02 2014-08-06 江苏奥赛康药业股份有限公司 含喹唑啉结构的三环类衍生物及其制备方法和用途
CN103965213A (zh) 2013-02-02 2014-08-06 江苏奥赛康药业股份有限公司 7,8-二氢-6H-[1,4]噁嗪[3,2-g]喹唑啉类衍生物及其制备方法和用途
CN103965212A (zh) 2013-02-02 2014-08-06 江苏奥赛康药业股份有限公司 6,7,8,9-四氢-[1,4]氧氮杂卓[3,2-g]喹唑啉类衍生物及其制备方法和用途
MX367772B (es) 2013-04-04 2019-09-05 Janssen Pharmaceutica Nv Derivados de n-(2,3-dihidro-1h-pirrolo[2,3,b]piridin-5-il)-4-quina zolinamina y n-(2,3-dihidro-1h-indol-5-il)-4-quinazolinamina novedosos como inhibidores de perk.
NZ732511A (en) * 2014-12-15 2018-11-30 Univ Michigan Regents Small molecule inhibitors of egfr and pi3k
CA2974442A1 (en) 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Novel fluorinated derivatives as egfr inhibitors useful for treating cancers
HUE054065T2 (hu) 2015-08-04 2021-08-30 Dc Europa Ltd Szerek glióma kezelésében történõ alkalmazásra
CN105017163A (zh) 2015-08-25 2015-11-04 佛山市赛维斯医药科技有限公司 双乙氧基苯并喹唑啉类酪氨酸激酶抑制剂、制备方法及其用途
AU2017204973A1 (en) 2016-01-06 2018-07-12 Trillium Therapeutics Inc. Novel fluorinated quinazoline derivatives as EGFR inhibitors
CN106432202B (zh) 2016-09-22 2019-04-02 郑州大学第一附属医院 喹唑啉类衍生物及其应用
CN111868039A (zh) * 2017-09-26 2020-10-30 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
KR102809395B1 (ko) 2019-03-15 2025-05-16 더 리전트 오브 더 유니버시티 오브 캘리포니아 암을 치료하기 위한 조성물 및 방법
US20240058340A1 (en) 2020-09-21 2024-02-22 The Regents Of The University Of California Compositions and methods for treating cancer
WO2022061201A1 (en) 2020-09-21 2022-03-24 The Regents Of The University Of California Compositions and methods for treating cancer
WO2022061299A1 (en) 2020-09-21 2022-03-24 The Regents Of The University Of California Non-invasive functional companion assays for oncogene targeted therapy for brain cancer
EP4405360A4 (en) 2021-09-23 2025-08-20 Erasca Inc POLYMORPHIC FORMS OF EGFR INHIBITOR
WO2023244639A1 (en) 2022-06-14 2023-12-21 The Regents Of The University Of California Methods of predicting cns cancer response to treatment with egfr inhibitors
WO2024081447A1 (en) 2022-10-14 2024-04-18 The Regents Of The University Of California Egfr inhibitors for treating lung cancer
WO2024102177A1 (en) 2022-11-08 2024-05-16 The Regents Of The University Of California Combination therapies for the treatment of brain cancer

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Publication number Publication date
US12545686B2 (en) 2026-02-10
AU2022350669A1 (en) 2024-04-04
EP4405360A1 (en) 2024-07-31
CA3233057A1 (en) 2023-03-30
EP4405360A4 (en) 2025-08-20
IL311616A (en) 2024-05-01
MX2024003495A (es) 2025-01-09
JP2024535380A (ja) 2024-09-30
US20240287088A1 (en) 2024-08-29
WO2023049312A1 (en) 2023-03-30
KR20250005041A (ko) 2025-01-09

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