CN114555588A - 作为axl抑制剂的喹唑啉类化合物 - Google Patents

作为axl抑制剂的喹唑啉类化合物 Download PDF

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Publication number
CN114555588A
CN114555588A CN202080067248.3A CN202080067248A CN114555588A CN 114555588 A CN114555588 A CN 114555588A CN 202080067248 A CN202080067248 A CN 202080067248A CN 114555588 A CN114555588 A CN 114555588A
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China
Prior art keywords
compound
methyl
phenyl
optionally substituted
formula
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CN202080067248.3A
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Inventor
李冬冬
马昌友
冯海威
吴舰
徐丹
朱春霞
田舟山
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Nanjing Chia Tai Tianqing Pharmaceutical Co Ltd
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Nanjing Chia Tai Tianqing Pharmaceutical Co Ltd
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Publication of CN114555588A publication Critical patent/CN114555588A/zh
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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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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

Abstract

本发明公开了作为AXL抑制剂的喹唑啉类化合物，该喹唑啉类化合物的结构如通式I所示，各取代基的定义如说明书所述，本发明还提供了其制备方法。本发明的喹唑啉类化合物具有显著的AXL抑制活性，能够用作AXL抑制剂。

Description

PCT国内申请，说明书已公开。

Claims (15)

  1. PCT国内申请，权利要求书已公开。
CN202080067248.3A 2019-11-07 2020-11-03 作为axl抑制剂的喹唑啉类化合物 Pending CN114555588A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201911081207 2019-11-07
CN2019110812075 2019-11-07
PCT/CN2020/126083 WO2021088787A1 (zh) 2019-11-07 2020-11-03 作为axl抑制剂的喹唑啉类化合物

Publications (1)

Publication Number Publication Date
CN114555588A true CN114555588A (zh) 2022-05-27

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CN202080067248.3A Pending CN114555588A (zh) 2019-11-07 2020-11-03 作为axl抑制剂的喹唑啉类化合物

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CN (1) CN114555588A (zh)
WO (1) WO2021088787A1 (zh)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116874503A (zh) * 2020-10-28 2023-10-13 杭州阿诺生物医药科技有限公司 一种高活性的hpk1激酶抑制剂
CN115504967A (zh) * 2021-06-23 2022-12-23 南京正大天晴制药有限公司 作为axl抑制剂的1,2,4-三唑化合物
CN115838383A (zh) * 2021-09-22 2023-03-24 南京正大天晴制药有限公司 作为axl抑制剂的苯并环庚烷类化合物
CN117003734A (zh) * 2022-04-27 2023-11-07 浙江海正药业股份有限公司 嘧啶并环类衍生物及其制备方法和用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170137426A1 (en) * 2014-03-28 2017-05-18 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as axl inhibitors
US20190276440A1 (en) * 2017-06-30 2019-09-12 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
CN110382490A (zh) * 2016-12-26 2019-10-25 中国医学科学院药物研究所 喹唑啉类化合物及其制备方法、用途和药物组合物

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201420285D0 (en) * 2014-11-14 2014-12-31 Bergenbio As Process
CN108250200A (zh) * 2016-12-28 2018-07-06 中国科学院上海药物研究所 一种具有Axl抑制活性的化合物及其制备和应用
CN109384774B (zh) * 2017-08-11 2023-02-17 中国科学院上海药物研究所 一类多取代的吡嗪/三嗪酰胺类化合物及其制备方法和应用

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170137426A1 (en) * 2014-03-28 2017-05-18 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as axl inhibitors
CN110382490A (zh) * 2016-12-26 2019-10-25 中国医学科学院药物研究所 喹唑啉类化合物及其制备方法、用途和药物组合物
US20190276440A1 (en) * 2017-06-30 2019-09-12 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof

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