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CN109311852A - 作为egfr抑制剂的苯胺嘧啶化合物的结晶 - Google Patents

作为egfr抑制剂的苯胺嘧啶化合物的结晶 Download PDF

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Publication number
CN109311852A
CN109311852A CN201780037239.8A CN201780037239A CN109311852A CN 109311852 A CN109311852 A CN 109311852A CN 201780037239 A CN201780037239 A CN 201780037239A CN 109311852 A CN109311852 A CN 109311852A
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CN
China
Prior art keywords
crystal
anilidine
crystallization
compounds
egfr inhibitors
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Application number
CN201780037239.8A
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English (en)
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CN109311852B (zh
Inventor
朱益忠
汤剑秋
刘飞
张喜全
顾红梅
朱波
王路路
汤松
张艳阳
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.)
Centaurus Biopharma Co Ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
Original Assignee
Centaurus Biopharma Co Ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
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Publication of CN109311852A publication Critical patent/CN109311852A/zh
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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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

本申请属于医药化学领域，涉及作为EGFR抑制剂的苯胺嘧啶化合物的结晶，具体而言，本申请涉及N‑(2‑((2‑(二甲基氨基)乙基)(甲基)氨基)‑4‑甲氧基‑5‑(4‑(3‑甲基‑2‑氧代‑2，3‑二氢‑1H‑苯并[d]咪唑‑1‑基)嘧啶‑2‑基氨基)苯基)丙烯酰胺(式I)盐酸盐的结晶A、结晶B和结晶C，还涉及结晶A、结晶B和结晶C的制备方法、包含该结晶A、结晶B或结晶C的结晶组合物、包含该结晶A、结晶B和结晶C或其结晶组合物的药物组合物以及它们的医药用途。本申请的结晶A、结晶B和结晶C具有纯度高、结晶度高、稳定性好等优点。

Description

PCT国内申请，说明书已公开。

Claims (18)

  1. PCT国内申请，权利要求书已公开。
CN201780037239.8A 2016-06-24 2017-06-23 作为egfr抑制剂的苯胺嘧啶化合物的结晶 Active CN109311852B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610470835.2A CN107540661A (zh) 2016-06-24 2016-06-24 作为egfr抑制剂的苯胺嘧啶化合物的结晶
CN2016104708352 2016-06-24
PCT/CN2017/089693 WO2017220007A1 (zh) 2016-06-24 2017-06-23 作为egfr抑制剂的苯胺嘧啶化合物的结晶

Publications (2)

Publication Number Publication Date
CN109311852A true CN109311852A (zh) 2019-02-05
CN109311852B CN109311852B (zh) 2021-04-02

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CN201610470835.2A Pending CN107540661A (zh) 2016-06-24 2016-06-24 作为egfr抑制剂的苯胺嘧啶化合物的结晶
CN201780037239.8A Active CN109311852B (zh) 2016-06-24 2017-06-23 作为egfr抑制剂的苯胺嘧啶化合物的结晶

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CN201610470835.2A Pending CN107540661A (zh) 2016-06-24 2016-06-24 作为egfr抑制剂的苯胺嘧啶化合物的结晶

Country Status (9)

Country Link
US (2) US20190256497A1 (zh)
EP (1) EP3476841A4 (zh)
JP (1) JP2019518776A (zh)
KR (1) KR20190021345A (zh)
CN (2) CN107540661A (zh)
AU (1) AU2017282903B2 (zh)
CA (1) CA3028015A1 (zh)
RU (1) RU2019100065A (zh)
WO (1) WO2017220007A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119192184A (zh) * 2024-11-26 2024-12-27 江苏省中国科学院植物研究所 Egfr依赖型小分子偶联物-2及其制备方法和应用

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105085489B (zh) 2014-11-05 2019-03-01 益方生物科技（上海）有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
CN110698461B (zh) * 2018-07-09 2024-04-05 上海翰森生物医药科技有限公司 第三代egfr抑制剂的制备方法
KR20230002721A (ko) * 2020-04-14 2023-01-05 치루 파머수티컬 컴퍼니 리미티드 Egfr 억제제로서의 삼환계 화합물
CN113521074B (zh) * 2020-04-17 2024-12-03 南京圣和药业股份有限公司 一种包含喹啉类TGF-β1抑制剂的组合物及其用途
WO2023061433A1 (zh) * 2021-10-14 2023-04-20 齐鲁制药有限公司 一种egfr抑制剂的多晶型
KR20250164828A (ko) 2023-03-30 2025-11-25 레볼루션 메디슨즈, 인크. Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도
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
WO2025080946A2 (en) 2023-10-12 2025-04-17 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
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
WO2026015796A1 (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
WO2026015801A1 (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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103702990A (zh) * 2011-07-27 2014-04-02 阿斯利康(瑞典)有限公司 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症
CN105085489A (zh) * 2014-11-05 2015-11-25 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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5957460B2 (ja) * 2010-11-01 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド 複素環式化合物またはその使用
PT2880035T (pt) * 2012-08-06 2017-03-10 Acea Biosciences Inc Novos compostos de pirrolopirimidina como inibidores de proteína-cinases
RU2734849C2 (ru) * 2015-07-16 2020-10-23 Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд. Производные анилинпиримидина и их применения

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103702990A (zh) * 2011-07-27 2014-04-02 阿斯利康(瑞典)有限公司 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症
CN105085489A (zh) * 2014-11-05 2015-11-25 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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119192184A (zh) * 2024-11-26 2024-12-27 江苏省中国科学院植物研究所 Egfr依赖型小分子偶联物-2及其制备方法和应用
CN119192184B (zh) * 2024-11-26 2025-02-25 江苏省中国科学院植物研究所 Egfr依赖型小分子偶联物-2及其制备方法和应用

Also Published As

Publication number Publication date
WO2017220007A1 (zh) 2017-12-28
CN109311852B (zh) 2021-04-02
EP3476841A4 (en) 2020-01-22
AU2017282903A1 (en) 2019-02-07
EP3476841A1 (en) 2019-05-01
US20190256497A1 (en) 2019-08-22
KR20190021345A (ko) 2019-03-05
RU2019100065A3 (zh) 2020-09-25
JP2019518776A (ja) 2019-07-04
US20200361908A1 (en) 2020-11-19
CN107540661A (zh) 2018-01-05
CA3028015A1 (en) 2017-12-28
RU2019100065A (ru) 2020-07-24
AU2017282903B2 (en) 2021-03-25

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