CN108884080B - 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 - Google Patents

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 Download PDF

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CN108884080B
CN108884080B CN201780008042.1A CN201780008042A CN108884080B CN 108884080 B CN108884080 B CN 108884080B CN 201780008042 A CN201780008042 A CN 201780008042A CN 108884080 B CN108884080 B CN 108884080B
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crystal form
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methanol
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compound
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CN108884080A (zh
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梁从新
谢利华
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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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201780008042.1A 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 Active CN108884080B (zh)

Applications Claiming Priority (3)

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

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CN108884080A CN108884080A (zh) 2018-11-23
CN108884080B true CN108884080B (zh) 2020-10-27

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US (3) US11053224B2 (https=)
EP (1) EP3502105B8 (https=)
JP (2) JP7253491B2 (https=)
KR (1) KR102289684B1 (https=)
CN (1) CN108884080B (https=)
AU (1) AU2017336889B2 (https=)
CA (2) CA3253105A1 (https=)
EA (1) EA201990688A1 (https=)
ES (1) ES2914294T3 (https=)
IL (2) IL265266B2 (https=)
MY (1) MY194364A (https=)
PH (1) PH12019500681A1 (https=)
PL (1) PL3502105T3 (https=)
SG (1) SG11201901962QA (https=)
TW (1) TWI647224B (https=)
WO (1) WO2018059556A1 (https=)
ZA (1) ZA201901717B (https=)

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Publication number Priority date Publication date Assignee Title
IL265266B2 (en) * 2016-09-29 2024-08-01 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
EP3884929B1 (en) 2020-03-25 2023-06-14 Ocular Therapeutix, Inc. Ocular implant containing a tyrosine kinase inhibitor
EP4210682B1 (en) 2020-09-14 2026-03-25 EyePoint, Inc. Bioerodible ocular drug delivery insert and therapeutic method
WO2022197104A1 (ko) * 2021-03-16 2022-09-22 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물의 결정형
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
WO2023173088A1 (en) 2022-03-11 2023-09-14 EyePoint Pharmaceuticals, Inc. Method of preventing age-related macular degeneration by administering an ocular drug delivery insert
CA3245209A1 (en) 2022-03-11 2023-09-14 EyePoint Pharmaceuticals, Inc. CONTINUOUS DOSAGE REGIMEN FOR THE TREATMENT OF AN EYE CONDITION
CA3245207A1 (en) 2022-03-11 2023-09-14 EyePoint Pharmaceuticals, Inc. TREATMENT METHOD FOR MOISTURE-RELATED MACULAR DEGENERATION
CN120897764A (zh) 2023-04-11 2025-11-04 视尔普斯眼科公司 包含阿西替尼多晶型物iv的眼部植入物
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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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
CN106928114A (zh) * 2015-12-31 2017-07-07 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

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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
KR20100135910A (ko) * 2008-04-16 2010-12-27 낫코 파마 리미티드 수니티닙 염기의 신규한 다형 형태
EP2292613B1 (en) * 2008-05-23 2015-09-30 Shanghai Institute of Pharmaceutical Industry Dihydroindolinone derivatives
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
IL265266B2 (en) * 2016-09-29 2024-08-01 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
CN106928114A (zh) * 2015-12-31 2017-07-07 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

Also Published As

Publication number Publication date
TWI647224B (zh) 2019-01-11
IL265266B2 (en) 2024-08-01
MY194364A (en) 2022-11-29
AU2017336889A1 (en) 2019-04-11
SG11201901962QA (en) 2019-04-29
TW201815785A (zh) 2018-05-01
KR102289684B1 (ko) 2021-08-12
IL311631B1 (en) 2026-03-01
US20220356173A1 (en) 2022-11-10
US11053224B2 (en) 2021-07-06
JP2023082086A (ja) 2023-06-13
EP3502105B8 (en) 2022-06-01
PL3502105T3 (pl) 2022-07-11
IL265266A (en) 2019-05-30
EA201990688A1 (ru) 2019-08-30
US20190233403A1 (en) 2019-08-01
IL311631A (en) 2024-05-01
CN108884080A (zh) 2018-11-23
ES2914294T3 (es) 2022-06-08
HK1257194A1 (zh) 2019-10-18
EP3502105B1 (en) 2022-03-30
US20250188063A1 (en) 2025-06-12
JP7763203B2 (ja) 2025-10-31
WO2018059556A1 (zh) 2018-04-05
EP3502105A4 (en) 2020-04-15
CA3035124A1 (en) 2018-04-05
NZ751911A (en) 2024-07-26
AU2017336889B2 (en) 2021-11-25
JP7253491B2 (ja) 2023-04-06
US12209080B2 (en) 2025-01-28
JP2019529568A (ja) 2019-10-17
IL265266B1 (en) 2024-04-01
KR20190039823A (ko) 2019-04-15
CA3253105A1 (en) 2025-07-08
EP3502105A1 (en) 2019-06-26
PH12019500681A1 (en) 2019-11-25
BR112019006023A2 (pt) 2019-06-18
CA3035124C (en) 2025-11-18
ZA201901717B (en) 2019-11-27

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