CN111902405A - 靶向cdk4/6激酶抑制剂的晶型 - Google Patents

靶向cdk4/6激酶抑制剂的晶型 Download PDF

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CN111902405A
CN111902405A CN201880087850.6A CN201880087850A CN111902405A CN 111902405 A CN111902405 A CN 111902405A CN 201880087850 A CN201880087850 A CN 201880087850A CN 111902405 A CN111902405 A CN 111902405A
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compound
formula
cancer
solvent
ether
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CN201880087850.6A
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CN111902405B (zh
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冯玉真
房兰
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Xuanzhu Biopharmaceutical Co Ltd
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Xuanzhu Biopharmaceutical Co Ltd
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    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

本公开涉及5‑((4‑乙基哌嗪‑1‑基)甲基)‑N‑(5‑氟‑4‑(4‑氟‑1‑异丙基‑2‑甲基‑1H‑苯并[d]咪唑‑6‑基)吡啶‑2‑基)嘧啶‑2‑胺的晶型A，该晶型纯度高、残留溶剂少，溶解度较高，稳定性好；具有良好的性状、流动性、可压性，便于生产、检测、制剂制备、运输和储藏；制备方法操作简便，适合工业化生产，可用于治疗和/或预防CDK4/6激酶介导的癌症相关疾病。

Description

PCT国内申请，说明书已公开。

Claims (17)

  1. PCT国内申请，权利要求书已公开。
CN201880087850.6A 2018-01-29 2018-12-27 靶向cdk4/6激酶抑制剂的晶型 Active CN111902405B (zh)

Applications Claiming Priority (3)

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CN201810084351 2018-01-29
CN2018100843513 2018-01-29
PCT/CN2018/124418 WO2019144759A1 (zh) 2018-01-29 2018-12-27 靶向cdk4/6激酶抑制剂的晶型

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CN111902405A true CN111902405A (zh) 2020-11-06
CN111902405B CN111902405B (zh) 2021-09-10

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US (1) US11299474B2 (zh)
EP (1) EP3747880B1 (zh)
JP (1) JP6972390B2 (zh)
KR (1) KR102531772B1 (zh)
CN (1) CN111902405B (zh)
AU (1) AU2018404690B2 (zh)
CA (1) CA3089243C (zh)
EA (1) EA202091556A1 (zh)
WO (1) WO2019144759A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020224609A1 (zh) * 2019-05-08 2020-11-12 山东轩竹医药科技有限公司 激酶抑制剂的用途
US20240075032A1 (en) * 2020-12-31 2024-03-07 Xuanzhu Biopharmaceutical Co., Ltd. A Pharmaceutical Composition for Treating Cancer
CN118119610A (zh) * 2021-12-13 2024-05-31 轩竹生物科技股份有限公司 一种治疗癌症的药物组合物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102428086A (zh) * 2009-04-29 2012-04-25 内尔维阿诺医学科学有限公司 Cdk抑制剂的盐类
CN105916848A (zh) * 2013-12-31 2016-08-31 山东轩竹医药科技有限公司 激酶抑制剂及其用途
CN106795159A (zh) * 2015-04-22 2017-05-31 江苏恒瑞医药股份有限公司 一种周期素依赖性蛋白激酶抑制剂的结晶形式及其制备方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110092775B (zh) * 2018-01-29 2021-09-10 轩竹生物科技有限公司 靶向cdk4/6激酶抑制剂的晶型

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102428086A (zh) * 2009-04-29 2012-04-25 内尔维阿诺医学科学有限公司 Cdk抑制剂的盐类
CN105916848A (zh) * 2013-12-31 2016-08-31 山东轩竹医药科技有限公司 激酶抑制剂及其用途
CN106795159A (zh) * 2015-04-22 2017-05-31 江苏恒瑞医药股份有限公司 一种周期素依赖性蛋白激酶抑制剂的结晶形式及其制备方法

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US11299474B2 (en) 2022-04-12
EP3747880A1 (en) 2020-12-09
WO2019144759A1 (zh) 2019-08-01
KR20200116132A (ko) 2020-10-08
CN111902405B (zh) 2021-09-10
EA202091556A1 (ru) 2021-02-19
KR102531772B1 (ko) 2023-05-11
AU2018404690B2 (en) 2021-05-06
JP6972390B2 (ja) 2021-11-24
EP3747880A4 (en) 2021-03-24
EP3747880B1 (en) 2023-05-03
AU2018404690A1 (en) 2020-08-06
JP2021512170A (ja) 2021-05-13
CA3089243A1 (en) 2019-08-01
CA3089243C (en) 2023-03-14
US20210047292A1 (en) 2021-02-18

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