CN115052881B - 作为HER2抑制剂的[1,3]二嗪并[5,4-d]嘧啶 - Google Patents

作为HER2抑制剂的[1,3]二嗪并[5,4-d]嘧啶 Download PDF

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Publication number
CN115052881B
CN115052881B CN202180012676.0A CN202180012676A CN115052881B CN 115052881 B CN115052881 B CN 115052881B CN 202180012676 A CN202180012676 A CN 202180012676A CN 115052881 B CN115052881 B CN 115052881B
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cancer
compound
her2
salt
compounds
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Chinese (zh)
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CN115052881A (zh
Inventor
B·维尔丁
D·布斯
H·恩格尔哈特
J·福克斯
R·纽穆勒
M·彼得罗茨基
D·沙恩
M·特罗伊
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Boehringer Ingelheim International GmbH
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Boehringer Ingelheim International GmbH
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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
    • A61K31/495—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202180012676.0A 2020-02-03 2021-02-01 作为HER2抑制剂的[1,3]二嗪并[5,4-d]嘧啶 Active CN115052881B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20155161 2020-02-03
EP20155161.1 2020-02-03
PCT/EP2021/052263 WO2021156180A1 (en) 2020-02-03 2021-02-01 [1,3]diazino[5,4-d]pyrimidines as her2 inhibitors

Publications (2)

Publication Number Publication Date
CN115052881A CN115052881A (zh) 2022-09-13
CN115052881B true CN115052881B (zh) 2024-07-09

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CN202180012676.0A Active CN115052881B (zh) 2020-02-03 2021-02-01 作为HER2抑制剂的[1,3]二嗪并[5,4-d]嘧啶

Country Status (5)

Country Link
US (1) US20230131720A1 (https=)
EP (1) EP4100412A1 (https=)
JP (1) JP7626774B2 (https=)
CN (1) CN115052881B (https=)
WO (1) WO2021156180A1 (https=)

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EP4323356A1 (en) 2021-04-13 2024-02-21 Nuvalent, Inc. Amino-substituted heterocycles for treating cancers with egfr mutations
PE20250118A1 (es) 2021-06-26 2025-01-16 Array Biopharma Inc Inhibidores de mutacion de her2
WO2023081637A1 (en) * 2021-11-02 2023-05-11 Enliven Therapeutics, Inc. Fused tetracyclic quinazoline derivatives as inhibitors of erbb2
CN114031619A (zh) * 2021-12-17 2022-02-11 山东汇海医药化工有限公司 一种图卡替尼中间体的制备方法
CN114621221B (zh) * 2022-03-12 2022-10-11 陕西海辰风扬医药科技有限公司 妥卡替尼关键中间体及其制备方法
JP2025509995A (ja) 2022-03-28 2025-04-11 江蘇恒瑞医薬股▲ふん▼有限公司 含窒素複素環系化合物、その調製方法及びその医薬的使用
CN117384162A (zh) * 2022-05-17 2024-01-12 浙江文达医药科技有限公司 选择性her2抑制剂
WO2024027695A1 (zh) * 2022-08-04 2024-02-08 微境生物医药科技(上海)有限公司 作为her2抑制剂的化合物
US20240132521A1 (en) 2022-08-22 2024-04-25 Iambic Therapeutics, Inc. Compounds and methods for modulating her2
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024229019A1 (en) * 2023-05-01 2024-11-07 Enliven Inc. Polymorphic forms of (e)-l-((10s)-4-((4-([l,2,4]triazolo[l,5-a]pyridin- 7-yloxy)-2-fluoro-5-methylphenyl)amino)-7,8,10,ll-tetrahydro- 9h-6,10-methanopyrimido[4',5':5,6]pyrido[3,2-b][l,4,7]oxadiazonin-9- yl)-4-(dimethylamino)but-2-en-l-one
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
CN116903615A (zh) * 2023-06-21 2023-10-20 江苏丽源医药有限公司 一种妥卡替尼及其中间体的制备方法
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
WO2025034912A2 (en) 2023-08-07 2025-02-13 Cogent Biosciences, Inc. Compounds for fgfr inhibition
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
WO2026007878A1 (zh) * 2024-07-01 2026-01-08 北京鞍石生物科技股份有限公司 稠环化合物及其制备方法和应用
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
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
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

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WO2003049740A1 (en) * 2001-12-12 2003-06-19 Pfizer Products Inc. Quinazoline derivatives for the treatment of abnormal cell growth
WO2005044302A1 (en) * 2003-11-06 2005-05-19 Pfizer Products Inc. Selective erbb2 inhibitor/anti-erbb antibody combinations in the treatment of cancer

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ES2364901T3 (es) 2005-11-15 2011-09-16 Array Biopharma, Inc. Procesos e intermedios para la preparación de derivados de n4-fenil-quinazolin-4-amina.
EP3143015B1 (en) * 2014-05-13 2019-02-20 ARIAD Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
CN110526912B (zh) 2014-06-19 2023-02-14 武田药品工业株式会社 用于激酶抑制的杂芳基化合物
JP6863901B2 (ja) * 2015-05-13 2021-04-28 アリアド ファーマシューティカルズ， インコーポレイテッド キナーゼ阻害のためのヘテロアリール化合物
JP6791979B2 (ja) * 2016-03-01 2020-11-25 シャンハイ ファーマシューティカルズ ホールディング カンパニー，リミティド 含窒素ヘテロ環化合物、製造方法、中間体、組成物及び応用
CN111032655B (zh) 2017-08-31 2022-09-02 达纳-法伯癌症研究所股份有限公司 Egfr和/或her2抑制剂和使用方法
EP3677583A4 (en) * 2017-09-01 2021-07-21 Shanghai Pharmaceuticals Holding Co., Ltd. NITROGENOUS HETEROCYCLIC COMPOUND, METHOD OF PREPARATION, INTERMEDIATE, COMPOSITION AND APPLICATION

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2003049740A1 (en) * 2001-12-12 2003-06-19 Pfizer Products Inc. Quinazoline derivatives for the treatment of abnormal cell growth
WO2005044302A1 (en) * 2003-11-06 2005-05-19 Pfizer Products Inc. Selective erbb2 inhibitor/anti-erbb antibody combinations in the treatment of cancer

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Publication number Publication date
JP7626774B2 (ja) 2025-02-04
WO2021156180A1 (en) 2021-08-12
EP4100412A1 (en) 2022-12-14
US20230131720A1 (en) 2023-04-27
JP2023512175A (ja) 2023-03-24
CN115052881A (zh) 2022-09-13

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