CA3035124C - POLYMORPHIC FORM OF A KINASE INHIBITOR COMPOUND, PHARMACEUTICAL COMPOSITION, CONTAINER, PROCESS OF PREPARATION AND USE - Google Patents

POLYMORPHIC FORM OF A KINASE INHIBITOR COMPOUND, PHARMACEUTICAL COMPOSITION, CONTAINER, PROCESS OF PREPARATION AND USE

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Publication number
CA3035124C
CA3035124C CA3035124A CA3035124A CA3035124C CA 3035124 C CA3035124 C CA 3035124C CA 3035124 A CA3035124 A CA 3035124A CA 3035124 A CA3035124 A CA 3035124A CA 3035124 C CA3035124 C CA 3035124C
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CA
Canada
Prior art keywords
crystalline form
preparation
ray powder
methanol
solvent
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Application number
CA3035124A
Other languages
English (en)
French (fr)
Other versions
CA3035124A1 (en
Inventor
Congxin Liang
Lihua Xie
Original Assignee
Equinox Sciences LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Equinox Sciences LLC filed Critical Equinox Sciences LLC
Priority to CA3253105A priority Critical patent/CA3253105A1/en
Publication of CA3035124A1 publication Critical patent/CA3035124A1/en
Application granted granted Critical
Publication of CA3035124C publication Critical patent/CA3035124C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • 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
    • 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

Landscapes

  • 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)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA3035124A 2016-09-29 2017-09-29 POLYMORPHIC FORM OF A KINASE INHIBITOR COMPOUND, PHARMACEUTICAL COMPOSITION, CONTAINER, PROCESS OF PREPARATION AND USE Active CA3035124C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA3253105A CA3253105A1 (en) 2016-09-29 2017-09-29 POLYMORPHIC FORM OF A KINASE INHIBITOR COMPOUND, PHARMACEUTICAL COMPOSITION, CONTAINER, PREPARATION PROCESS AND USE

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA3253105A Division CA3253105A1 (en) 2016-09-29 2017-09-29 POLYMORPHIC FORM OF A KINASE INHIBITOR COMPOUND, PHARMACEUTICAL COMPOSITION, CONTAINER, PREPARATION PROCESS AND USE

Publications (2)

Publication Number Publication Date
CA3035124A1 CA3035124A1 (en) 2018-04-05
CA3035124C true CA3035124C (en) 2025-11-18

Family

ID=61763329

Family Applications (2)

Application Number Title Priority Date Filing Date
CA3035124A Active CA3035124C (en) 2016-09-29 2017-09-29 POLYMORPHIC FORM OF A KINASE INHIBITOR COMPOUND, PHARMACEUTICAL COMPOSITION, CONTAINER, PROCESS OF PREPARATION AND USE
CA3253105A Pending CA3253105A1 (en) 2016-09-29 2017-09-29 POLYMORPHIC FORM OF A KINASE INHIBITOR COMPOUND, PHARMACEUTICAL COMPOSITION, CONTAINER, PREPARATION PROCESS AND USE

Family Applications After (1)

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CA3253105A Pending CA3253105A1 (en) 2016-09-29 2017-09-29 POLYMORPHIC FORM OF A KINASE INHIBITOR COMPOUND, PHARMACEUTICAL COMPOSITION, CONTAINER, PREPARATION PROCESS AND USE

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
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

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1434774A1 (en) 2001-10-10 2004-07-07 Sugen, Inc. 3-(4-substituted heterocyclyl)-pyrrol-2-ylmethylidene)-2-indolinone derivatives as protein kinase inhibitors
JP5568304B2 (ja) * 2006-09-15 2014-08-06 タイロジェネクス,インコーポレイテッド キナーゼ阻害剤化合物
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

Also Published As

Publication number Publication date
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
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
KR102289684B1 (ko) 2021-08-12
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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