CN112105618A - 作为选择性HER2抑制剂的吡咯并[2,1-f][1,2,4]三嗪类衍生物及其应用 - Google Patents

作为选择性HER2抑制剂的吡咯并[2,1-f][1,2,4]三嗪类衍生物及其应用 Download PDF

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Publication number
CN112105618A
CN112105618A CN201980031008.5A CN201980031008A CN112105618A CN 112105618 A CN112105618 A CN 112105618A CN 201980031008 A CN201980031008 A CN 201980031008A CN 112105618 A CN112105618 A CN 112105618A
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compound
alkyl
reaction
isomer
pharmaceutically acceptable
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CN112105618B (zh
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陈新海
姜奋
陈鑫德
张丽
陈兆国
于衍新
周凯
胡伯羽
谢程
陈曙辉
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Medshine Discovery Inc
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Medshine Discovery Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

本发明涉及一类作为选择性HER2抑制剂的吡咯并[2,1‑f][1,2,4]三嗪类衍生物，以及在制备作为HER2抑制剂的药物中的应用。具体涉及式(Ⅰ)所示化合物、其异构体或其药学上可接受的盐。

Description

PCT国内申请，说明书已公开。

Claims (31)

  1. PCT国内申请，权利要求书已公开。
CN201980031008.5A 2018-05-08 2019-05-08 作为选择性HER2抑制剂的吡咯并[2,1-f][1,2,4]三嗪类衍生物及其应用 Active CN112105618B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201810434197 2018-05-08
CN2018104341978 2018-05-08
PCT/CN2019/086032 WO2019214651A1 (zh) 2018-05-08 2019-05-08 作为选择性HER2抑制剂的吡咯并[2,1-f][1,2,4]三嗪类衍生物及其应用

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CN112105618A true CN112105618A (zh) 2020-12-18
CN112105618B CN112105618B (zh) 2022-05-31

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US (1) US20210323979A1 (zh)
EP (1) EP3792263B1 (zh)
JP (1) JP7276719B2 (zh)
CN (1) CN112105618B (zh)
WO (1) WO2019214651A1 (zh)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019341273A1 (en) * 2018-09-18 2020-11-19 F. Hoffmann-La Roche Ag Quinazoline derivatives as antitumor agents
WO2021088987A1 (zh) * 2019-11-08 2021-05-14 南京明德新药研发有限公司 作为选择性her2抑制剂的盐型、晶型及其应用
CN114671867B (zh) * 2022-03-15 2023-09-19 上海法默生物科技有限公司 妥卡替尼中间体7-羟基-[1,2,4]三唑并[1,5-a]吡啶的制备方法
WO2024044570A1 (en) * 2022-08-22 2024-02-29 Iambic Therapeutics, Inc. Compounds and methods for modulating her2
WO2024048809A1 (ko) * 2022-08-31 2024-03-07 보로노이 주식회사 N을 포함하는 헤테로아릴 유도체, 이를 포함하는 약학적 조성물, 및 이의 용도

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005065266A2 (en) * 2003-12-29 2005-07-21 Bristol-Myers Squibb Company Di-substituted pyrrolotriazine compounds
CN1922182A (zh) * 2003-12-29 2007-02-28 布里斯托尔-迈尔斯·斯奎布公司 作为激酶抑制剂的吡咯并三嗪化合物
CN101356171A (zh) * 2005-11-15 2009-01-28 阿雷生物药品公司 作为erbbi型受体酪氨酸激酶抑制剂用于治疗增殖性疾病的n4-苯基-喹唑啉-4-胺衍生物和相关化合物
CN101611041A (zh) * 2006-12-12 2009-12-23 武田药品工业株式会社 稠合杂环化合物

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005065266A2 (en) * 2003-12-29 2005-07-21 Bristol-Myers Squibb Company Di-substituted pyrrolotriazine compounds
CN1922182A (zh) * 2003-12-29 2007-02-28 布里斯托尔-迈尔斯·斯奎布公司 作为激酶抑制剂的吡咯并三嗪化合物
CN101356171A (zh) * 2005-11-15 2009-01-28 阿雷生物药品公司 作为erbbi型受体酪氨酸激酶抑制剂用于治疗增殖性疾病的n4-苯基-喹唑啉-4-胺衍生物和相关化合物
CN101611041A (zh) * 2006-12-12 2009-12-23 武田药品工业株式会社 稠合杂环化合物

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BRIAN E. FINK 等: "Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *
HAROLD MASTALERZ 等: "5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *
HIBA ZALLOUM 等: "Discovery of New Human Epidermal Growth Factor Receptor-2 (HER2) Inhibitors for Potential Use as Anticancer Agents via Ligand-Based Pharmacophore Modeling", 《JOURNAL OF MOLECULAR GRAPHICS AND MODELLING》 *

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Publication number Publication date
EP3792263A4 (en) 2021-11-10
JP7276719B2 (ja) 2023-05-18
WO2019214651A1 (zh) 2019-11-14
CN112105618B (zh) 2022-05-31
US20210323979A1 (en) 2021-10-21
EP3792263A1 (en) 2021-03-17
EP3792263B1 (en) 2023-03-01
JP2021523165A (ja) 2021-09-02

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