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
Authority
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.)
Active
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.)
Filing date
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

Links

Classifications

    • 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
    • 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
    • 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

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)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (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)

Application Number Title Priority Date Filing Date
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 (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

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005508953A (ja) * 2001-10-10 2005-04-07 スージェン・インコーポレーテッド キナーゼ阻害剤としての３−［４−（置換ヘテロサイクリル）−ピロール−２−イルメチリデン］−２−インドリノン誘導体
WO2008033562A2 (en) * 2006-09-15 2008-03-20 Xcovery, Inc. Kinase inhibitor compounds
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
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
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

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
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
TWI647224B (zh) 2019-01-11
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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