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

Info

Publication number
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
Authority
CN
China
Prior art keywords
crystal form
preparation
methanol
solvent
compound
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
CN201780008042.1A
Other languages
English (en)
Chinese (zh)
Other versions
CN108884080A (zh
Inventor
梁从新
谢利华
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Betta Pharmaceuticals Co Ltd
Original Assignee
Betta Pharmaceuticals Co Ltd
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 Betta Pharmaceuticals Co Ltd filed Critical Betta Pharmaceuticals Co Ltd
Publication of CN108884080A publication Critical patent/CN108884080A/zh
Application granted granted Critical
Publication of CN108884080B publication Critical patent/CN108884080B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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

Landscapes

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

Family

ID=61763329

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780008042.1A Active CN108884080B (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

Country Status (17)

Country Link
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=)

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
PT3884929T (pt) 2020-03-25 2023-08-09 Ocular Therapeutix Inc Implante ocular contendo um inibidor da tirosina cinase
AU2021340733A1 (en) 2020-09-14 2023-05-18 EyePoint Pharmaceuticals, Inc. Bioerodible ocular drug delivery insert and therapeutic method
CA3212253A1 (en) * 2021-03-16 2022-09-22 Young Ju Kim Crystalline form of heterocyclic compound as protein kinase inhibitor
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
WO2023173093A1 (en) 2022-03-11 2023-09-14 EyePoint Pharmaceuticals, Inc. Continuous dosing regimen for treatment of a condition of the eye
CA3245207A1 (en) 2022-03-11 2023-09-14 EyePoint Pharmaceuticals, Inc. TREATMENT METHOD FOR MOISTURE-RELATED MACULAR DEGENERATION
KR20250002220A (ko) 2022-03-11 2025-01-07 아이포인트 파마슈티컬스, 인코포레이티드 안구 약물 전달 삽입물을 투여하여 연령 관련 황반 변성을 예방하는 방법
PE20260040A1 (es) 2023-04-11 2026-01-09 Ocular Therapeutix Inc Implante ocular que contiene un inhibidor de la tirosina cinasa
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)

* 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

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008134909A1 (de) * 2007-05-07 2008-11-13 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
WO2009128083A1 (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
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 (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
JP7763203B2 (ja) 2025-10-31
EP3502105A4 (en) 2020-04-15
PL3502105T3 (pl) 2022-07-11
US12209080B2 (en) 2025-01-28
US11053224B2 (en) 2021-07-06
JP2023082086A (ja) 2023-06-13
IL265266B1 (en) 2024-04-01
US20190233403A1 (en) 2019-08-01
TW201815785A (zh) 2018-05-01
IL265266A (en) 2019-05-30
KR20190039823A (ko) 2019-04-15
BR112019006023A2 (pt) 2019-06-18
CA3035124A1 (en) 2018-04-05
KR102289684B1 (ko) 2021-08-12
CN108884080A (zh) 2018-11-23
ES2914294T3 (es) 2022-06-08
MY194364A (en) 2022-11-29
AU2017336889A1 (en) 2019-04-11
EP3502105A1 (en) 2019-06-26
TWI647224B (zh) 2019-01-11
EP3502105B1 (en) 2022-03-30
AU2017336889B2 (en) 2021-11-25
PH12019500681A1 (en) 2019-11-25
JP2019529568A (ja) 2019-10-17
EP3502105B8 (en) 2022-06-01
IL311631A (en) 2024-05-01
WO2018059556A1 (zh) 2018-04-05
NZ751911A (en) 2024-07-26
JP7253491B2 (ja) 2023-04-06
CA3035124C (en) 2025-11-18
EA201990688A1 (ru) 2019-08-30
US20250188063A1 (en) 2025-06-12
CA3253105A1 (en) 2025-07-08
IL311631B1 (en) 2026-03-01
SG11201901962QA (en) 2019-04-29
US20220356173A1 (en) 2022-11-10
HK1257194A1 (zh) 2019-10-18
IL265266B2 (en) 2024-08-01
ZA201901717B (en) 2019-11-27

Similar Documents

Publication Publication Date Title
CN108884080B (zh) 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
JP6756617B2 (ja) Ｎ−｛４−［（６，７−ジメトキシキノリン−４−イル）オキシ］フェニル｝−ｎ’−（４−フルオロフェニル）シクロプロパン−１，１−ジカルボキサミドの結晶性固体形態、製造プロセス、及び使用方法
US10519176B2 (en) Crystalline forms
CN110621662B (zh) 一种盐的结晶性固体形式、制备工艺和使用方法
JP2017505796A5 (https=)
EP3279201B1 (en) Cdk inhibitor, eutectic crystal of mek inhibitor, and preparation method therefor
CN105753869B (zh) 一种cdk抑制剂和mek抑制剂的共晶及其制备方法
CN105732642B (zh) 一种cdk抑制剂和mek抑制剂的共晶及其制备方法
HK1257194B (en) Polymorphic form of kinase inhibitor compound, pharmaceutical composition containing same, and preparation method therefor and use thereof
CN102770416A (zh) 美他沙酮共晶体
BR112019006023B1 (pt) Forma cristalina, método de preparação da forma cristalina, e, composição farmacêutica
WO2021176216A1 (en) Salts and polymorphic forms of 6-chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1h-pyrazol-4-yl)-3h-imidazo[4,5-b]pyridine
HK40020497B (en) Crystalline solid forms of salts, processes for making, and methods of use

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1257194

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant