AU2017336889B2 - Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereof - Google Patents

Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereof Download PDF

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Publication number
AU2017336889B2
AU2017336889B2 AU2017336889A AU2017336889A AU2017336889B2 AU 2017336889 B2 AU2017336889 B2 AU 2017336889B2 AU 2017336889 A AU2017336889 A AU 2017336889A AU 2017336889 A AU2017336889 A AU 2017336889A AU 2017336889 B2 AU2017336889 B2 AU 2017336889B2
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crystalline form
preparation
compound
formula
solvent
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AU2017336889A1 (en
Inventor
Congxin Liang
Lihua Xie
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Equinox Sciences LLC
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Equinox Sciences LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/4025Heterocyclic 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/485Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2017336889A 2016-09-29 2017-09-29 Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereof Active AU2017336889B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610866253 2016-09-29
CN201610866253.6 2016-09-29
PCT/CN2017/104506 WO2018059556A1 (zh) 2016-09-29 2017-09-29 激酶抑制剂化合物的多晶型、含其的药物组合物及其制备方法和应用

Publications (2)

Publication Number Publication Date
AU2017336889A1 AU2017336889A1 (en) 2019-04-11
AU2017336889B2 true AU2017336889B2 (en) 2021-11-25

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AU2017336889A Active AU2017336889B2 (en) 2016-09-29 2017-09-29 Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereof

Country Status (17)

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

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018059556A1 (zh) * 2016-09-29 2018-04-05 贝达药业股份有限公司 激酶抑制剂化合物的多晶型、含其的药物组合物及其制备方法和应用
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
CN115531352B (zh) 2020-09-14 2025-04-25 视点制药公司 可生物蚀解的眼部药物递送插入剂及治疗方法
BR112023018649A2 (pt) * 2021-03-16 2023-10-10 Hk Inno N Corp Forma cristalina e método para preparar uma forma cristalina
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
CA3245205A1 (en) 2022-03-11 2023-09-14 EyePoint Pharmaceuticals, Inc. METHOD FOR PREVENTING AGE-RELATED MACULAR DEGENERATION BY ADMINISTRATION OF A DRUG-DELIVERING OPHTHALMIC INSERT
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
TW202400143A (zh) 2022-03-11 2024-01-01 美商視點製藥有限公司 用於治療眼睛病況之持續給藥方案
TW202448436A (zh) 2023-04-11 2024-12-16 美商視爾普斯眼科公司 含有酪胺酸激酶抑制劑之眼部植入物
CN117143083A (zh) * 2023-08-30 2023-12-01 沈阳药科大学 VEGFR抑制剂Vorolanib的合成方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008033562A2 (en) * 2006-09-15 2008-03-20 Xcovery, Inc. Kinase inhibitor compounds

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BR0213185A (pt) 2001-10-10 2004-09-14 Sugen Inc Derivados de 3-[4-(heterociclila substituìda)-pirrol-2-ilmetilideno]2-indolinona como inibidores de cinase
EP2145505A1 (de) * 2007-05-07 2010-01-20 Baumer Electric AG Akustischer wandler
US20100256392A1 (en) * 2007-11-21 2010-10-07 Teva Pharmaceutical Industries Ltd. Polymorphs of sunitinib base and processes for preparation thereof
CA2720943A1 (en) * 2008-04-16 2009-10-22 Natco Pharma Limited Novel polymorphic forms of sunitinib base
RU2468022C2 (ru) 2008-05-23 2012-11-27 Шанхай Инститьют Оф Фармасьютикал Индастри Производные дигидроиндолона
EP2186809A1 (en) * 2008-11-13 2010-05-19 LEK Pharmaceuticals D.D. New crystal form of sunitinib malate
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
WO2018059556A1 (zh) 2016-09-29 2018-04-05 贝达药业股份有限公司 激酶抑制剂化合物的多晶型、含其的药物组合物及其制备方法和应用

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008033562A2 (en) * 2006-09-15 2008-03-20 Xcovery, Inc. Kinase inhibitor compounds

Also Published As

Publication number Publication date
ES2914294T3 (es) 2022-06-08
MY194364A (en) 2022-11-29
CA3253105A1 (en) 2025-07-08
KR102289684B1 (ko) 2021-08-12
CA3035124C (en) 2025-11-18
TW201815785A (zh) 2018-05-01
CN108884080B (zh) 2020-10-27
NZ751911A (en) 2024-07-26
US11053224B2 (en) 2021-07-06
JP2019529568A (ja) 2019-10-17
CN108884080A (zh) 2018-11-23
JP2023082086A (ja) 2023-06-13
BR112019006023A2 (pt) 2019-06-18
CA3035124A1 (en) 2018-04-05
JP7763203B2 (ja) 2025-10-31
TWI647224B (zh) 2019-01-11
HK1257194A1 (zh) 2019-10-18
EP3502105A1 (en) 2019-06-26
US20190233403A1 (en) 2019-08-01
IL311631A (en) 2024-05-01
WO2018059556A1 (zh) 2018-04-05
SG11201901962QA (en) 2019-04-29
IL265266B2 (en) 2024-08-01
EA201990688A1 (ru) 2019-08-30
EP3502105B8 (en) 2022-06-01
EP3502105A4 (en) 2020-04-15
PH12019500681A1 (en) 2019-11-25
ZA201901717B (en) 2019-11-27
EP3502105B1 (en) 2022-03-30
US12209080B2 (en) 2025-01-28
US20250188063A1 (en) 2025-06-12
PL3502105T3 (pl) 2022-07-11
US20220356173A1 (en) 2022-11-10
KR20190039823A (ko) 2019-04-15
AU2017336889A1 (en) 2019-04-11
IL265266A (en) 2019-05-30
JP7253491B2 (ja) 2023-04-06
IL265266B1 (en) 2024-04-01

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