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WO2018145280A1 - Inhibiteur de kinase flt3 ou ses formes de sel cristallines et son procédé de préparation - Google Patents

Inhibiteur de kinase flt3 ou ses formes de sel cristallines et son procédé de préparation Download PDF

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Publication number
WO2018145280A1
WO2018145280A1 PCT/CN2017/073146 CN2017073146W WO2018145280A1 WO 2018145280 A1 WO2018145280 A1 WO 2018145280A1 CN 2017073146 W CN2017073146 W CN 2017073146W WO 2018145280 A1 WO2018145280 A1 WO 2018145280A1
Authority
WO
WIPO (PCT)
Prior art keywords
ethanone
dimethylamino
phenoxyphenyl
amino
pyrazolo
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.)
Ceased
Application number
PCT/CN2017/073146
Other languages
English (en)
Chinese (zh)
Inventor
张善春
方绪军
曹杰永
谢琼霞
程开生
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.)
Hefei Cosource Pharmaceuticals Inc
Original Assignee
Hefei Cosource Pharmaceuticals Inc
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 Hefei Cosource Pharmaceuticals Inc filed Critical Hefei Cosource Pharmaceuticals Inc
Priority to CN201780017991.6A priority Critical patent/CN109311883B/zh
Priority to PCT/CN2017/073146 priority patent/WO2018145280A1/fr
Publication of WO2018145280A1 publication Critical patent/WO2018145280A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • 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
    • 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

Definitions

  • the present inventors have found that the compound of the formula (I) has good crystallinity and is easy to purify, but has disadvantages in that it is poor in resistance to light and oxidation, and it is easy to form an oxide, thereby further degrading into other impurities.
  • the salt can be greatly improved in stability against oxidation, light, high temperature and high humidity after being formed into a salt. For this reason, the stability of the compound of the formula (I) and its hydrobromide salt (hereinafter collectively referred to as the sample to be tested) under light, oxidation, high temperature and high humidity conditions were examined.

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

Abstract

La présente invention concerne un inhibiteur de kinase FLT3, ses formes de sel cristallines et son procédé de préparation, et plus particulièrement, l'invention concerne des formes cristallines A, B, C, D et E de (R)-1-(3-(4-amino-(4-phénoxyphényl)-1H-pyrazolo[3, 4-d]pyrimidine-1-yl)pipéridin-1-yl)-2-(diméthylamino)éthanone ou de mono-halate ou de di-halate de celui-ci et son procédé de préparation. Les formes cristallines A et B du composé et les formes cristallines C et D du mono-halate ou du di-halate de la présente invention présentent une bonne stabilité à l'oxydation, aux conditions d'éclairement, à la température et à l'humidité élevées et ont une bonne solubilité dans l'eau.
PCT/CN2017/073146 2017-02-09 2017-02-09 Inhibiteur de kinase flt3 ou ses formes de sel cristallines et son procédé de préparation Ceased WO2018145280A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN201780017991.6A CN109311883B (zh) 2017-02-09 2017-02-09 Flt3激酶抑制剂或其盐的晶型及其制备方法
PCT/CN2017/073146 WO2018145280A1 (fr) 2017-02-09 2017-02-09 Inhibiteur de kinase flt3 ou ses formes de sel cristallines et son procédé de préparation

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CN2017/073146 WO2018145280A1 (fr) 2017-02-09 2017-02-09 Inhibiteur de kinase flt3 ou ses formes de sel cristallines et son procédé de préparation

Publications (1)

Publication Number Publication Date
WO2018145280A1 true WO2018145280A1 (fr) 2018-08-16

Family

ID=63107872

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2017/073146 Ceased WO2018145280A1 (fr) 2017-02-09 2017-02-09 Inhibiteur de kinase flt3 ou ses formes de sel cristallines et son procédé de préparation

Country Status (2)

Country Link
CN (1) CN109311883B (fr)
WO (1) WO2018145280A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111217816A (zh) * 2018-11-27 2020-06-02 中国科学院上海药物研究所 一类flt3激酶抑制剂及其制备和应用

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110531016B (zh) * 2019-09-05 2021-08-31 合肥诺明药物安全研究有限公司 一种hyml-122血药浓度定量分析方法
CN117903141B (zh) * 2023-12-19 2024-11-05 江苏长泰药业股份有限公司 一种化合物及其盐、在制备治疗癌症药物和激酶抑制剂中的用途、治疗癌症的药物

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011046964A2 (fr) * 2009-10-12 2011-04-21 Pharmacyclics, Inc. Inhibiteurs de tyrosine kinase de bruton
WO2012158843A2 (fr) * 2011-05-17 2012-11-22 The Regents Of The University Of California Inhibiteurs de kinase
WO2013003629A2 (fr) * 2011-06-28 2013-01-03 Pharmacyclics, Inc. Procédés et compositions visant à inhiber la résorption osseuse
WO2014139970A1 (fr) * 2013-03-15 2014-09-18 Janssen Pharmaceutica Nv Procédés et intermédiaires pour la préparation d'un médicament
WO2016115869A1 (fr) * 2015-01-21 2016-07-28 中国科学院合肥物质科学研究院 Nouvel inhibiteur de la kinase flt3 et utilisation de ce dernier

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105481862B (zh) * 2015-01-21 2018-08-21 中国科学院合肥物质科学研究院 Flt3激酶的新型抑制剂及其用途

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011046964A2 (fr) * 2009-10-12 2011-04-21 Pharmacyclics, Inc. Inhibiteurs de tyrosine kinase de bruton
WO2012158843A2 (fr) * 2011-05-17 2012-11-22 The Regents Of The University Of California Inhibiteurs de kinase
WO2013003629A2 (fr) * 2011-06-28 2013-01-03 Pharmacyclics, Inc. Procédés et compositions visant à inhiber la résorption osseuse
WO2014139970A1 (fr) * 2013-03-15 2014-09-18 Janssen Pharmaceutica Nv Procédés et intermédiaires pour la préparation d'un médicament
WO2016115869A1 (fr) * 2015-01-21 2016-07-28 中国科学院合肥物质科学研究院 Nouvel inhibiteur de la kinase flt3 et utilisation de ce dernier

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111217816A (zh) * 2018-11-27 2020-06-02 中国科学院上海药物研究所 一类flt3激酶抑制剂及其制备和应用
CN111217816B (zh) * 2018-11-27 2022-08-16 中国科学院上海药物研究所 一类flt3激酶抑制剂及其制备和应用

Also Published As

Publication number Publication date
CN109311883A (zh) 2019-02-05
CN109311883B (zh) 2021-03-19

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