TWI647224B - 激酶抑制劑化合物的多晶型、含其的藥物組合物及其製備方法和應用 - Google Patents

激酶抑制劑化合物的多晶型、含其的藥物組合物及其製備方法和應用 Download PDF

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Publication number
TWI647224B
TWI647224B TW106133830A TW106133830A TWI647224B TW I647224 B TWI647224 B TW I647224B TW 106133830 A TW106133830 A TW 106133830A TW 106133830 A TW106133830 A TW 106133830A TW I647224 B TWI647224 B TW I647224B
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Taiwan
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methanol
solvent
compound
crystal form
preparation
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TW106133830A
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English (en)
Chinese (zh)
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TW201815785A (zh
Inventor
從新 梁
Cong-Xin Liang
謝利華
Li-hua XIE
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大陸商貝達藥業股份有限公司
Betta Pharmaceuticals Co.,Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW106133830A 2016-09-29 2017-09-29 激酶抑制劑化合物的多晶型、含其的藥物組合物及其製備方法和應用 TWI647224B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610866253.6 2016-09-29
??201610866253.6 2016-09-29
CN201610866253 2016-09-29

Publications (2)

Publication Number Publication Date
TW201815785A TW201815785A (zh) 2018-05-01
TWI647224B true TWI647224B (zh) 2019-01-11

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US (3) US11053224B2 (enExample)
EP (1) EP3502105B8 (enExample)
JP (2) JP7253491B2 (enExample)
KR (1) KR102289684B1 (enExample)
CN (1) CN108884080B (enExample)
AU (1) AU2017336889B2 (enExample)
CA (2) CA3035124C (enExample)
EA (1) EA201990688A1 (enExample)
ES (1) ES2914294T3 (enExample)
IL (2) IL265266B2 (enExample)
MY (1) MY194364A (enExample)
PH (1) PH12019500681A1 (enExample)
PL (1) PL3502105T3 (enExample)
SG (1) SG11201901962QA (enExample)
TW (1) TWI647224B (enExample)
WO (1) WO2018059556A1 (enExample)
ZA (1) ZA201901717B (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201901962QA (en) * 2016-09-29 2019-04-29 Equinox Sciences Llc Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereof
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
CA3171563A1 (en) 2020-03-25 2021-09-30 Charles D. Blizzard Ocular implant containing a tyrosine kinase inhibitor
SI4210682T1 (sl) 2020-09-14 2026-07-31 EyePoint, Inc. Bioerozibilni očesni vložek za dovajanje zdravil in terapevtska metoda
CN117157294A (zh) * 2021-03-16 2023-12-01 怡诺安有限公司 作为蛋白激酶抑制剂的杂环化合物的结晶形式
JP7138982B1 (ja) 2021-09-24 2022-09-20 東海物産株式会社 アンセリンの結晶及びその製造方法
IL315331A (en) 2022-03-11 2024-10-01 Eyepoint Pharmaceuticals Inc A method of preventing age-related ocular degeneration by providing a drug entry mechanism into the eye
US20250186398A1 (en) 2022-03-11 2025-06-12 EyePoint Pharmaceuticals, Inc. Continuous dosing regimen for treatment of a condition of the eye
TW202345804A (zh) 2022-03-11 2023-12-01 美商視點製藥有限公司 治療濕性老年黃斑部病變(Wet Age-related Macular Degeneration)之方法
JP2026520094A (ja) 2023-04-11 2026-06-22 オキュラ セラピューティクス,インコーポレイテッド アキシチニブ多形ivを含む眼科インプラント
CN117143083B (zh) * 2023-08-30 2026-02-27 沈阳药科大学 VEGFR抑制剂Vorolanib的合成方法

Citations (3)

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WO2003031438A1 (en) * 2001-10-10 2003-04-17 Sugen, Inc. 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives as kinase inhibitors
CN101553482A (zh) * 2006-09-15 2009-10-07 艾科睿制药公司 激酶抑制剂化合物
CN102272124A (zh) * 2008-11-13 2011-12-07 力奇制药公司 舒尼替尼苹果酸盐的新晶形

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US20110026367A1 (en) * 2007-05-07 2011-02-03 Baumer Electric Ag Acoustic Transducer
US20100256392A1 (en) * 2007-11-21 2010-10-07 Teva Pharmaceutical Industries Ltd. Polymorphs of sunitinib base and processes for preparation thereof
WO2009128083A1 (en) * 2008-04-16 2009-10-22 Natco Pharma Limited Novel polymorphic forms of sunitinib base
CN102066362B (zh) 2008-05-23 2014-07-30 上海医药工业研究院 二氢吲哚酮衍生物
EP2264027A1 (en) 2009-05-27 2010-12-22 Ratiopharm GmbH Process for the preparation of N-[2-(Diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene) methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
CN106928114B (zh) * 2015-12-31 2020-07-28 韶远科技(上海)有限公司 含有脲基的环状手性氨基类化合物及其可放大工艺和用途
SG11201901962QA (en) * 2016-09-29 2019-04-29 Equinox Sciences Llc Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003031438A1 (en) * 2001-10-10 2003-04-17 Sugen, Inc. 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives as kinase inhibitors
CN101553482A (zh) * 2006-09-15 2009-10-07 艾科睿制药公司 激酶抑制剂化合物
CN102272124A (zh) * 2008-11-13 2011-12-07 力奇制药公司 舒尼替尼苹果酸盐的新晶形

Also Published As

Publication number Publication date
CA3253105A1 (en) 2025-07-08
IL265266A (en) 2019-05-30
WO2018059556A1 (zh) 2018-04-05
JP7763203B2 (ja) 2025-10-31
CA3035124C (en) 2025-11-18
JP2019529568A (ja) 2019-10-17
JP7253491B2 (ja) 2023-04-06
NZ751911A (en) 2024-07-26
HK1257194A1 (zh) 2019-10-18
EP3502105B8 (en) 2022-06-01
KR20190039823A (ko) 2019-04-15
ES2914294T3 (es) 2022-06-08
SG11201901962QA (en) 2019-04-29
IL311631B2 (en) 2026-07-01
PL3502105T3 (pl) 2022-07-11
CN108884080A (zh) 2018-11-23
AU2017336889A1 (en) 2019-04-11
ZA201901717B (en) 2019-11-27
IL311631B1 (en) 2026-03-01
CN108884080B (zh) 2020-10-27
IL311631A (en) 2024-05-01
US20250188063A1 (en) 2025-06-12
AU2017336889B2 (en) 2021-11-25
US20220356173A1 (en) 2022-11-10
EP3502105B1 (en) 2022-03-30
IL265266B2 (en) 2024-08-01
MY194364A (en) 2022-11-29
US11053224B2 (en) 2021-07-06
TW201815785A (zh) 2018-05-01
US12209080B2 (en) 2025-01-28
PH12019500681A1 (en) 2019-11-25
EA201990688A1 (ru) 2019-08-30
EP3502105A1 (en) 2019-06-26
IL265266B1 (en) 2024-04-01
US20190233403A1 (en) 2019-08-01
KR102289684B1 (ko) 2021-08-12
CA3035124A1 (en) 2018-04-05
BR112019006023A2 (pt) 2019-06-18
EP3502105A4 (en) 2020-04-15
JP2023082086A (ja) 2023-06-13

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