[go: up one dir, main page]

CN115803325A - 一种egfr抑制剂及其制备方法和应用 - Google Patents

一种egfr抑制剂及其制备方法和应用 Download PDF

Info

Publication number
CN115803325A
CN115803325A CN202180047794.5A CN202180047794A CN115803325A CN 115803325 A CN115803325 A CN 115803325A CN 202180047794 A CN202180047794 A CN 202180047794A CN 115803325 A CN115803325 A CN 115803325A
Authority
CN
China
Prior art keywords
alkyl
radical
substituted
deuterium
cycloalkyl
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.)
Granted
Application number
CN202180047794.5A
Other languages
English (en)
Other versions
CN115803325B (zh
Inventor
杨飞
杨舒群
喻红平
陈椎
徐耀昌
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.)
Abbisko Therapeutics Co Ltd
Original Assignee
Abbisko Therapeutics Co Ltd
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 Abbisko Therapeutics Co Ltd filed Critical Abbisko Therapeutics Co Ltd
Publication of CN115803325A publication Critical patent/CN115803325A/zh
Application granted granted Critical
Publication of CN115803325B publication Critical patent/CN115803325B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

一种具有式(I)结构的EGFR抑制剂、其制备方法、含有其的药物组合物，以及其作为EGFR抑制剂的用途和其在制备治疗和/或预防至少部分与EGFR外显子20插入、缺失或其他突变相关的癌症、肿瘤或转移性疾病的药物中的用途，特别是在制备治疗和/或预防过度增殖性疾病和诱导细胞死亡障碍疾病的药物中的用途。其中式(I)的各取代基与说明书中的定义相同。

Description

PCT国内申请，说明书已公开。

Claims (22)

  1. PCT国内申请，权利要求书已公开。
CN202180047794.5A 2020-08-10 2021-08-09 一种egfr抑制剂及其制备方法和应用 Active CN115803325B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN2020107940668 2020-08-10
CN202010794066 2020-08-10
CN2020115460215 2020-12-24
CN202011546021 2020-12-24
CN202110676156 2021-06-18
CN2021106761561 2021-06-18
PCT/CN2021/111411 WO2022033410A1 (zh) 2020-08-10 2021-08-09 一种egfr抑制剂及其制备方法和应用

Publications (2)

Publication Number Publication Date
CN115803325A true CN115803325A (zh) 2023-03-14
CN115803325B CN115803325B (zh) 2024-04-26

Family

ID=80246896

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180047794.5A Active CN115803325B (zh) 2020-08-10 2021-08-09 一种egfr抑制剂及其制备方法和应用

Country Status (9)

Country Link
US (1) US20230271936A1 (zh)
EP (1) EP4194443A4 (zh)
JP (1) JP7449028B2 (zh)
KR (1) KR102887500B1 (zh)
CN (1) CN115803325B (zh)
AU (1) AU2021326209B2 (zh)
CA (1) CA3188077A1 (zh)
TW (1) TWI896726B (zh)
WO (1) WO2022033410A1 (zh)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112023021111A2 (pt) 2021-04-13 2023-12-19 Nuvalent Inc Composto, composição farmacêutica, método de tratamento de câncer, método para inibir seletivamente her2, método de regulação de um nível de her2, método para aumentar um nível de her2, método de diminuição da fosforilação de her2
TW202504611A (zh) 2023-03-30 2025-02-01 美商銳新醫藥公司 用於誘導ｒａｓ ｇｔｐ水解之組合物及其用途
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
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
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007082434A1 (en) * 2006-01-20 2007-07-26 Shanghai Allist Pharmaceutical., Inc. Quinazoline derivatives,preparation methods and uses thereof
CN101304978A (zh) * 2005-11-08 2008-11-12 韩美药品株式会社 作为多元抑制剂的喹唑啉衍生物及其制备方法
WO2020009156A1 (ja) * 2018-07-04 2020-01-09 第一三共株式会社 ビアリールエーテル型キナゾリン誘導体
WO2020068867A1 (en) * 2018-09-25 2020-04-02 Black Diamond Therapeutics, Inc. Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA73073C2 (uk) * 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
CN106892907B (zh) * 2016-08-09 2020-05-19 江西科技师范大学 含酰腙结构的喹唑啉类化合物及其应用
KR20220047810A (ko) * 2019-08-15 2022-04-19 블랙 다이아몬드 테라퓨틱스, 인코포레이티드 알키닐 퀴나졸린 화합물

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101304978A (zh) * 2005-11-08 2008-11-12 韩美药品株式会社 作为多元抑制剂的喹唑啉衍生物及其制备方法
WO2007082434A1 (en) * 2006-01-20 2007-07-26 Shanghai Allist Pharmaceutical., Inc. Quinazoline derivatives,preparation methods and uses thereof
WO2020009156A1 (ja) * 2018-07-04 2020-01-09 第一三共株式会社 ビアリールエーテル型キナゾリン誘導体
WO2020068867A1 (en) * 2018-09-25 2020-04-02 Black Diamond Therapeutics, Inc. Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use

Also Published As

Publication number Publication date
TW202214615A (zh) 2022-04-16
KR102887500B1 (ko) 2025-11-17
EP4194443A1 (en) 2023-06-14
EP4194443A4 (en) 2024-10-09
US20230271936A1 (en) 2023-08-31
JP2023536948A (ja) 2023-08-30
WO2022033410A1 (zh) 2022-02-17
KR20230049708A (ko) 2023-04-13
AU2021326209B2 (en) 2024-03-28
TWI896726B (zh) 2025-09-11
JP7449028B2 (ja) 2024-03-13
CN115803325B (zh) 2024-04-26
AU2021326209A1 (en) 2023-02-23
CA3188077A1 (en) 2022-02-17

Similar Documents

Publication Publication Date Title
CN115803325A (zh) 一种egfr抑制剂及其制备方法和应用
CN115803326A (zh) Egfr抑制剂及其制备方法与在药学上的应用
JP6524221B2 (ja) Ｅｇｆｒ変異型キナーゼ活性をモジュレートするための化合物および組成物
CN103153980B (zh) 吡唑并苯基苯磺酰胺化合物的衍生物及其作为抗肿瘤药的用途
AU2015360360B2 (en) Substituted 2-anilinopyrimidine derivatives as EGFR modulators
JP6487925B2 (ja) セリン／トレオニンキナーゼ阻害剤
CN105408334B (zh) 作为激酶抑制剂的取代的吡唑并嘧啶类化合物
AU2017335242C1 (en) Pyridine compound
JP5585892B2 (ja) キナーゼ阻害剤としての化合物
CN104203242B (zh) 取代的喹啉类作为布鲁顿酪氨酸激酶抑制剂
JP5855250B2 (ja) イミダゾオキサジン化合物による抗腫瘍効果増強剤
JP2017511311A5 (zh)
WO2013170770A1 (zh) 具有抗肿瘤活性的乙炔衍生物
BRPI0716224A2 (pt) Compostos inibidores de raf e métodos de uso dos mesmos.
WO2019233457A1 (zh) Erk抑制剂及其应用
US8791265B2 (en) Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors
CN103298805A (zh) 喹唑啉化合物及其使用方法
CN107501369A (zh) 一种胞苷衍生物的制备方法及其应用
CA2955872A1 (en) Glucose transport inhibitors
WO2023143135A1 (zh) 一种喹唑啉衍生物及其用途
CN117645616A (zh) 选择性her2抑制剂
CN119490450A (zh) 一种含肟化合物及其用途
CN107074814A (zh) 葡萄糖转运抑制剂
WO2016078397A1 (zh) 新型胞苷衍生物及其应用
CN116981662B (zh) 嘧啶-4,6-二胺衍生物及其制备方法和药学上的应用

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40081466

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant