CN114650826A - 一种多靶点蛋白激酶抑制剂的用途 - Google Patents

一种多靶点蛋白激酶抑制剂的用途 Download PDF

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CN114650826A
CN114650826A CN202080077604.XA CN202080077604A CN114650826A CN 114650826 A CN114650826 A CN 114650826A CN 202080077604 A CN202080077604 A CN 202080077604A CN 114650826 A CN114650826 A CN 114650826A
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acute myeloid
myeloid leukemia
compound
pharmaceutically acceptable
flt3
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CN114650826B (zh
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彭悦颖
詹国宁
李晓晶
郝春颜
赵学敏
胡炜
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CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co Ltd
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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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

本发明提供一种多靶点蛋白激酶抑制剂化合物A或其药学上可接受的盐在制备治疗白血病的药物中的用途，并提供了化合物A治疗急性髓系白血病，尤其是FLT3突变的急性髓系白血病的方法。化合物A在临床研究中对FLT3‑ITD突变和/或TKD突变的急性髓系白血病，以及DEK‑CAN阳性与FLT3‑ITD突变同时存在的急性髓系白血病均体现出一定的疗效。II型FLT3抑制剂(例如索拉非尼)治疗失败的复发和/或难治性急性髓系白血病患者经化合物A治疗仍能临床获益。
Figure DDA0003632169530000011

Description

PCT国内申请，说明书已公开。

Claims (24)

  1. PCT国内申请，权利要求书已公开。
CN202080077604.XA 2019-11-09 2020-11-09 一种多靶点蛋白激酶抑制剂的用途 Active CN114650826B (zh)

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CN2019110908222 2019-11-09
CN201911090822 2019-11-09
PCT/CN2020/127449 WO2021089038A1 (zh) 2019-11-09 2020-11-09 一种多靶点蛋白激酶抑制剂的用途

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CN114650826A true CN114650826A (zh) 2022-06-21
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US (1) US20220387435A1 (zh)
EP (1) EP4056184A1 (zh)
JP (1) JP2023502015A (zh)
KR (1) KR20220100006A (zh)
CN (1) CN114650826B (zh)
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JP2024501690A (ja) * 2020-12-31 2024-01-15 石薬集団中奇制薬技術（石家庄）有限公司 多標的タンパク質キナーゼ阻害剤の医薬組成物及びその使用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011147066A1 (zh) * 2010-05-26 2011-12-01 四川大学 芳胺基嘌呤衍生物及其制备方法和在医药上的用途
WO2019113345A1 (en) * 2017-12-06 2019-06-13 Spyro Mousses Combination of cancer therapeutics for treatment of cancer and hyperproliferative diseases

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011147066A1 (zh) * 2010-05-26 2011-12-01 四川大学 芳胺基嘌呤衍生物及其制备方法和在医药上的用途
WO2019113345A1 (en) * 2017-12-06 2019-06-13 Spyro Mousses Combination of cancer therapeutics for treatment of cancer and hyperproliferative diseases

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CAO，Z. X. 等: "SKLB1028, a novel oral multikinase inhibitor of EGFR, FLT3 and Abl, displays exceptional activity in models of FLT3-driven AML and considerable potency in models of CML harboring Abl mutants" *

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CN114650826B (zh) 2024-03-22
WO2021089038A1 (zh) 2021-05-14
US20220387435A1 (en) 2022-12-08
EP4056184A1 (en) 2022-09-14
JP2023502015A (ja) 2023-01-20
KR20220100006A (ko) 2022-07-14

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