KR102289684B1 - 키나아제 억제제 화합물의 다결정형(polymorphic form), 이를 함유한 약물 조성물 및 그의 제조방법과 응용 - Google Patents

키나아제 억제제 화합물의 다결정형(polymorphic form), 이를 함유한 약물 조성물 및 그의 제조방법과 응용 Download PDF

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KR102289684B1
KR102289684B1 KR1020197008752A KR20197008752A KR102289684B1 KR 102289684 B1 KR102289684 B1 KR 102289684B1 KR 1020197008752 A KR1020197008752 A KR 1020197008752A KR 20197008752 A KR20197008752 A KR 20197008752A KR 102289684 B1 KR102289684 B1 KR 102289684B1
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crystalline form
methanol
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충신 량
리화 셰
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이쿼녹스 사이언시스, 엘엘씨
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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
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    • 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
    • A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
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    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • 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
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
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    • 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)
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  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020197008752A 2016-09-29 2017-09-29 키나아제 억제제 화합물의 다결정형(polymorphic form), 이를 함유한 약물 조성물 및 그의 제조방법과 응용 Active KR102289684B1 (ko)

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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KR20190039823A KR20190039823A (ko) 2019-04-15
KR102289684B1 true KR102289684B1 (ko) 2021-08-12

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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)
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IL (2) IL265266B2 (enExample)
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EA201990688A1 (ru) * 2016-09-29 2019-08-30 Эквинокс Сайенсиз, Ллк. Полиморфные формы соединения, представляющего собой ингибитор киназ, содержащая их фармацевтическая композиция, способ их получения и их применение
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
CA3191463A1 (en) 2020-09-14 2022-03-17 Said Saim Bioerodible ocular drug delivery insert and therapeutic method
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
US20250205152A1 (en) 2022-03-11 2025-06-26 EyePoint Pharmaceuticals, Inc. Method of preventing age-related macular degeneration by administering an ocular drug delivery insert
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
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
IL322360A (en) 2023-04-11 2025-09-01 Ocular Therapeutix Inc Intraocular implant containing axitinib iv polymorph
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)

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WO2008033562A2 (en) * 2006-09-15 2008-03-20 Xcovery, Inc. Kinase inhibitor compounds

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EP1434774A1 (en) 2001-10-10 2004-07-07 Sugen, Inc. 3-(4-substituted heterocyclyl)-pyrrol-2-ylmethylidene)-2-indolinone derivatives as protein kinase inhibitors
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
CA2720943A1 (en) * 2008-04-16 2009-10-22 Natco Pharma Limited Novel polymorphic forms of sunitinib base
KR101375156B1 (ko) 2008-05-23 2014-03-18 쟝수 치아타이 티안큉 파마수티컬 주식회사 디하이드로인돌리논 유도체들
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
EA201990688A1 (ru) * 2016-09-29 2019-08-30 Эквинокс Сайенсиз, Ллк. Полиморфные формы соединения, представляющего собой ингибитор киназ, содержащая их фармацевтическая композиция, способ их получения и их применение

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WO2008033562A2 (en) * 2006-09-15 2008-03-20 Xcovery, Inc. Kinase inhibitor compounds

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MY194364A (en) 2022-11-29
AU2017336889B2 (en) 2021-11-25
AU2017336889A1 (en) 2019-04-11
EP3502105A4 (en) 2020-04-15
KR20190039823A (ko) 2019-04-15
ES2914294T3 (es) 2022-06-08
CA3035124A1 (en) 2018-04-05
SG11201901962QA (en) 2019-04-29
IL265266B1 (en) 2024-04-01
PL3502105T3 (pl) 2022-07-11
CA3035124C (en) 2025-11-18
EP3502105B1 (en) 2022-03-30
JP2023082086A (ja) 2023-06-13
US20250188063A1 (en) 2025-06-12
JP7763203B2 (ja) 2025-10-31
CA3253105A1 (en) 2025-07-08
US12209080B2 (en) 2025-01-28
BR112019006023A2 (pt) 2019-06-18
IL265266B2 (en) 2024-08-01
JP2019529568A (ja) 2019-10-17
US11053224B2 (en) 2021-07-06
HK1257194A1 (zh) 2019-10-18
TWI647224B (zh) 2019-01-11
CN108884080A (zh) 2018-11-23
US20190233403A1 (en) 2019-08-01
WO2018059556A1 (zh) 2018-04-05
JP7253491B2 (ja) 2023-04-06
TW201815785A (zh) 2018-05-01
PH12019500681A1 (en) 2019-11-25
EP3502105B8 (en) 2022-06-01
US20220356173A1 (en) 2022-11-10
CN108884080B (zh) 2020-10-27
NZ751911A (en) 2024-07-26
IL265266A (en) 2019-05-30
ZA201901717B (en) 2019-11-27
EP3502105A1 (en) 2019-06-26
EA201990688A1 (ru) 2019-08-30
IL311631A (en) 2024-05-01

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