CN115052878B - 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
CN115052878B
CN115052878B CN202180012671.8A CN202180012671A CN115052878B CN 115052878 B CN115052878 B CN 115052878B CN 202180012671 A CN202180012671 A CN 202180012671A CN 115052878 B CN115052878 B CN 115052878B
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cancer
salt
compound
her2
compounds
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Chinese (zh)
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CN115052878A (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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202180012671.8A 2020-02-03 2021-02-01 作为HER2抑制剂的[1,3]二嗪并[5,4-d]嘧啶 Active CN115052878B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20155157.9 2020-02-03
EP20155157 2020-02-03
PCT/EP2021/052261 WO2021156178A1 (en) 2020-02-03 2021-02-01 [1,3]diazino[5,4-d]pyrimidines as her2 inhibitors

Publications (2)

Publication Number Publication Date
CN115052878A CN115052878A (zh) 2022-09-13
CN115052878B true CN115052878B (zh) 2024-07-09

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CN202180012671.8A Active CN115052878B (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) US20230126204A1 (https=)
EP (1) EP4100409B1 (https=)
JP (1) JP7626773B2 (https=)
CN (1) CN115052878B (https=)
WO (1) WO2021156178A1 (https=)

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TW202214641A (zh) 2020-06-30 2022-04-16 美商艾瑞生藥股份有限公司 Ｈｅｒ２突變抑制劑
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
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
WO2023195773A1 (ko) * 2022-04-05 2023-10-12 보로노이 주식회사 헤테로아릴 유도체 및 이의 용도
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
US20240132521A1 (en) 2022-08-22 2024-04-25 Iambic Therapeutics, Inc. Compounds and methods for modulating her2
EP4637773A1 (en) 2022-12-22 2025-10-29 Boehringer Ingelheim International GmbH Crystalline forms of a her2 inhibitor
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024215809A2 (en) * 2023-04-11 2024-10-17 Cogent Biosciences, Inc. Erbb2 inhibitors
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326016A (en) 2023-07-28 2026-03-01 Boehringer Ingelheim Int Process for manufacturing a HER2 inhibitor
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
CN119320383A (zh) * 2023-09-05 2025-01-17 北京鞍石生物科技股份有限公司 含氮杂芳基化合物及其制备方法和应用
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
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
WO2026015796A1 (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

Citations (2)

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WO2007059257A2 (en) * 2005-11-15 2007-05-24 Array Biopharma Inc. N4-phenyl-quinaz0line-4 -amine derivatives and related compounds as erbb type i receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases
WO2019042409A1 (zh) * 2017-09-01 2019-03-07 上海医药集团股份有限公司 一种含氮杂环化合物、制备方法、中间体、组合物和应用

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PL373848A1 (en) 2001-12-12 2005-09-19 Pfizer Products Inc. Quinazoline derivatives for the treatment of abnormal cell growth
MXPA06005024A (es) 2003-11-06 2006-07-06 Pfizer Prod Inc Combinaciones de inhibidor de erbb2 selectivo/anticuerpos anti-erbb en el tratamiento del cancer.
MX368464B (es) * 2013-12-05 2019-10-02 Pfizer Acrilamidas de pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinil o y pirrolo[2,3-d]piridinilo.
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
US11608343B2 (en) * 2020-04-24 2023-03-21 Boehringer Ingelheim International Gmbh Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors
EP4637773A1 (en) * 2022-12-22 2025-10-29 Boehringer Ingelheim International GmbH Crystalline forms of a her2 inhibitor
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Patent Citations (2)

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WO2007059257A2 (en) * 2005-11-15 2007-05-24 Array Biopharma Inc. N4-phenyl-quinaz0line-4 -amine derivatives and related compounds as erbb type i receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases
WO2019042409A1 (zh) * 2017-09-01 2019-03-07 上海医药集团股份有限公司 一种含氮杂环化合物、制备方法、中间体、组合物和应用

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Publication number Publication date
EP4100409A1 (en) 2022-12-14
JP2023512174A (ja) 2023-03-24
CN115052878A (zh) 2022-09-13
US20230126204A1 (en) 2023-04-27
JP7626773B2 (ja) 2025-02-04
EP4100409B1 (en) 2024-08-28
WO2021156178A1 (en) 2021-08-12

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