WO2021143954A3 - 一种氟伐替尼或其甲磺酸盐的晶型及其制备方法 - Google Patents

一种氟伐替尼或其甲磺酸盐的晶型及其制备方法 Download PDF

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Publication number
WO2021143954A3
WO2021143954A3 PCT/CN2021/081023 CN2021081023W WO2021143954A3 WO 2021143954 A3 WO2021143954 A3 WO 2021143954A3 CN 2021081023 W CN2021081023 W CN 2021081023W WO 2021143954 A3 WO2021143954 A3 WO 2021143954A3
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WO
WIPO (PCT)
Prior art keywords
fluvatinib
crystalline form
methanesulfonate
preparation
method therefor
Prior art date
Application number
PCT/CN2021/081023
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English (en)
French (fr)
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WO2021143954A2 (zh
Inventor
贺帅
张杨
刘强
陈正霞
戴美碧
樊斌
谢佩钰
Original Assignee
重庆医药工业研究院有限责任公司
重庆药友制药有限责任公司
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Publication date
Application filed by 重庆医药工业研究院有限责任公司, 重庆药友制药有限责任公司 filed Critical 重庆医药工业研究院有限责任公司
Priority to JP2022543726A priority Critical patent/JP2023512621A/ja
Priority to US17/793,406 priority patent/US20230106064A1/en
Priority to EP21741704.7A priority patent/EP4092014A4/en
Publication of WO2021143954A2 publication Critical patent/WO2021143954A2/zh
Publication of WO2021143954A3 publication Critical patent/WO2021143954A3/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

一种氟伐替尼或其甲磺酸盐的晶型及其制备方法，所述氟伐替尼的晶型I具有图1所示的特征衍射峰，所述氟伐替尼甲磺酸盐的晶型为多晶现象，具有晶型I-VII七种晶型，其中晶型III具有图9所不的特征衍射峰，这些晶型适应氣伐替尼甲横酸盐的制剂的制造过程。
PCT/CN2021/081023 2020-01-19 2021-03-16 一种氟伐替尼或其甲磺酸盐的晶型及其制备方法 WO2021143954A2 (zh)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2022543726A JP2023512621A (ja) 2020-01-19 2021-03-16 フルバチニブ又はそのメタンスルホン酸塩の結晶形およびその製造方法
US17/793,406 US20230106064A1 (en) 2020-01-19 2021-03-16 Crystalline form of fluvatinib or fluvatinib methanesulfonate and preparation method therefor
EP21741704.7A EP4092014A4 (en) 2020-01-19 2021-03-16 CRYSTALLINE FORM OF FLUVATINIB OR FLUVATINIB METHANESULFONATE AND METHOD OF MANUFACTURE THEREOF

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN202010063033.6 2020-01-19
CN202010063033 2020-01-19

Publications (2)

Publication Number Publication Date
WO2021143954A2 WO2021143954A2 (zh) 2021-07-22
WO2021143954A3 true WO2021143954A3 (zh) 2021-08-26

Family

ID=76810909

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Application Number Title Priority Date Filing Date
PCT/CN2021/081023 WO2021143954A2 (zh) 2020-01-19 2021-03-16 一种氟伐替尼或其甲磺酸盐的晶型及其制备方法

Country Status (5)

Country Link
US (1) US20230106064A1 (zh)
EP (1) EP4092014A4 (zh)
JP (1) JP2023512621A (zh)
CN (2) CN113135853A (zh)
WO (1) WO2021143954A2 (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113480479B (zh) * 2021-08-12 2022-08-02 上海爱博医药科技有限公司 脲类多靶点酪氨酸激酶抑制剂及其医药应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018196687A1 (zh) * 2017-04-25 2018-11-01 苏州科睿思制药有限公司 乐伐替尼甲磺酸盐的新晶型及其制备方法
CN109134365A (zh) * 2017-09-28 2019-01-04 南京明德新药研发股份有限公司 喹啉衍生物及其作为酪氨酸激酶抑制剂的应用
US20190218184A1 (en) * 2016-06-08 2019-07-18 Crystal Pharmatech Co., Ltd Novel Crystalline Form of Lenvantinib Mesylate and Process of Preparation Thereof
WO2020187188A1 (zh) * 2019-03-15 2020-09-24 南京明德新药研发有限公司 喹啉衍生物及免疫调节剂联合在制备抗肿瘤药物中的应用

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10246418B2 (en) * 2015-05-21 2019-04-02 Crystal Pharmatech Co., Ltd. Crystal form of lenvatinib methanesulfonate salt and preparation method thereof
EP3299360A1 (en) * 2016-09-21 2018-03-28 INDENA S.p.A. Crystal forms of lenvatinib
JP6917448B2 (ja) * 2016-09-30 2021-08-11 広東衆生睿創生物科技有限公司Ｇｕａｎｇｄｏｎｇ Ｒａｙｎｏｖｅｎｔ Ｂｉｏｔｅｃｈ Ｃｏ．，Ｌｔｄ． チロシンキナーゼ阻害剤の結晶形、塩形態及び製造方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20190218184A1 (en) * 2016-06-08 2019-07-18 Crystal Pharmatech Co., Ltd Novel Crystalline Form of Lenvantinib Mesylate and Process of Preparation Thereof
WO2018196687A1 (zh) * 2017-04-25 2018-11-01 苏州科睿思制药有限公司 乐伐替尼甲磺酸盐的新晶型及其制备方法
CN109134365A (zh) * 2017-09-28 2019-01-04 南京明德新药研发股份有限公司 喹啉衍生物及其作为酪氨酸激酶抑制剂的应用
WO2020187188A1 (zh) * 2019-03-15 2020-09-24 南京明德新药研发有限公司 喹啉衍生物及免疫调节剂联合在制备抗肿瘤药物中的应用

Also Published As

Publication number Publication date
US20230106064A1 (en) 2023-04-06
WO2021143954A2 (zh) 2021-07-22
EP4092014A4 (en) 2023-08-16
CN113135853A (zh) 2021-07-20
CN117945999A (zh) 2024-04-30
JP2023512621A (ja) 2023-03-28
EP4092014A2 (en) 2022-11-23

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