CA3026142C - Crystalline form of compound suppressing protein kinase activity, and application thereof - Google Patents

Crystalline form of compound suppressing protein kinase activity, and application thereof Download PDF

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Publication number
CA3026142C
CA3026142C CA3026142A CA3026142A CA3026142C CA 3026142 C CA3026142 C CA 3026142C CA 3026142 A CA3026142 A CA 3026142A CA 3026142 A CA3026142 A CA 3026142A CA 3026142 C CA3026142 C CA 3026142C
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Prior art keywords
crystalline form
disease
compound
pharmaceutical composition
cancer
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CA3026142A
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English (en)
French (fr)
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CA3026142A1 (en
Inventor
Congxin Liang
Yongbin MA
Wei He
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Xcovery Holdings Inc
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Xcovery Holdings Inc
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    • 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
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C403/00Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone
    • C07C403/06Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms
    • C07C403/10Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms by etherified hydroxy groups
    • 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
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Enzymes And Modification Thereof (AREA)
CA3026142A 2016-06-01 2017-06-01 Crystalline form of compound suppressing protein kinase activity, and application thereof Active CA3026142C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2016/084300 2016-06-01
CNPCT/CN2016/084300 2016-06-01
PCT/CN2017/086760 WO2017206924A1 (zh) 2016-06-01 2017-06-01 抑制蛋白激酶活性化合物的晶型及其应用

Publications (2)

Publication Number Publication Date
CA3026142A1 CA3026142A1 (en) 2017-12-07
CA3026142C true CA3026142C (en) 2024-02-13

Family

ID=60477983

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3026142A Active CA3026142C (en) 2016-06-01 2017-06-01 Crystalline form of compound suppressing protein kinase activity, and application thereof

Country Status (17)

Country Link
US (1) US10899744B2 (https=)
EP (1) EP3470410B1 (https=)
JP (1) JP7054528B2 (https=)
KR (1) KR102466958B1 (https=)
CN (1) CN109195964B (https=)
AU (1) AU2017274110B2 (https=)
CA (1) CA3026142C (https=)
EA (1) EA201892687A1 (https=)
ES (1) ES2981015T3 (https=)
IL (1) IL263356B (https=)
MY (1) MY188379A (https=)
PH (1) PH12018502529A1 (https=)
PL (1) PL3470410T3 (https=)
RU (1) RU2744264C2 (https=)
SG (1) SG11201810800VA (https=)
TW (1) TWI646094B (https=)
WO (1) WO2017206924A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL279579B2 (en) 2018-06-21 2023-02-01 Betta Pharmaceuticals Co Ltd Crystalline form of a compound to inhibit the activity of cdk4/6 and its use
EP4188922A1 (en) 2020-08-03 2023-06-07 Teva Pharmaceuticals International GmbH Solid state forms of ensartinib and ensartinib salts
EP4385510A4 (en) * 2021-08-10 2025-08-20 Betta Pharmaceuticals Co Ltd USE OF ENSARTINIB OR A CORRESPONDING SALT IN THE TREATMENT OF A DISEASE CARRYING A MET EXON 14 SKIPPING MUTATION
KR102851417B1 (ko) * 2022-08-16 2025-08-28 제이투에이치바이오텍 (주) 피리미딘-4-카복사마이드 화합물의 결정형 및 이를 포함하는 경구용 약학 제제

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL358271A1 (pl) * 2000-03-06 2004-08-09 Warner-Lambert Company 5-alkilopirydo[2,3-D]pirymidyny jako inhibitory kinazy tyrozyny
CA2517256C (en) * 2003-02-26 2013-04-30 Sugen, Inc. Aminoheteroaryl compounds as protein kinase inhibitors
US8414489B2 (en) 2003-11-13 2013-04-09 Medtronic Minimed, Inc. Fabrication of multi-sensor arrays
ME01309B (me) * 2004-08-26 2013-12-20 Pfizer Pirazolom supstituirani heteroarilni spojevi kao inhibitori proteinskih kinaza
BRPI0514687A (pt) 2004-08-26 2008-06-17 Pfizer compostos amino heteroarila como inibidores de proteìna tirosina cinase
KR101146852B1 (ko) * 2005-12-05 2012-05-16 화이자 프로덕츠 인크. C?met/hgfr 억제제의 다형체
CN101652068A (zh) * 2007-01-19 2010-02-17 艾科睿制药公司 激酶抑制物化合物
ES2670665T3 (es) * 2008-06-19 2018-05-31 Xcovery Holding Company Llc Compuestos de piridazina carboxamida sustituidos como compuestos inhibidores de quinasa
EA024809B1 (ru) * 2010-10-08 2016-10-31 Икскавери Холдинг Кампани, Ллс Замещенные соединения пиридазинкарбоксамида
WO2012048258A2 (en) * 2010-10-08 2012-04-12 Xcovery Holding Company, Llc Substituted pyridazine carboxamide compounds as kinase inhibitor compounds

Also Published As

Publication number Publication date
HK1259249A1 (zh) 2019-11-29
TWI646094B (zh) 2019-01-01
ES2981015T3 (es) 2024-10-04
AU2017274110B2 (en) 2021-05-06
MY188379A (en) 2021-12-07
JP2019518026A (ja) 2019-06-27
JP7054528B2 (ja) 2022-04-14
NZ750921A (en) 2024-12-20
EP3470410B1 (en) 2024-04-17
PH12018502529A1 (en) 2019-04-08
BR112018074612A2 (pt) 2019-03-19
CA3026142A1 (en) 2017-12-07
EP3470410A4 (en) 2019-12-04
TW201742865A (zh) 2017-12-16
RU2018145183A3 (https=) 2020-07-16
EA201892687A1 (ru) 2019-06-28
RU2744264C2 (ru) 2021-03-04
IL263356B (en) 2022-08-01
RU2018145183A (ru) 2020-07-14
SG11201810800VA (en) 2019-01-30
CN109195964B (zh) 2021-08-10
CN109195964A (zh) 2019-01-11
US20190135792A1 (en) 2019-05-09
AU2017274110A1 (en) 2019-01-24
IL263356A (en) 2018-12-31
PL3470410T3 (pl) 2024-09-16
EP3470410A1 (en) 2019-04-17
KR102466958B1 (ko) 2022-11-14
US10899744B2 (en) 2021-01-26
KR20190012231A (ko) 2019-02-08
WO2017206924A1 (zh) 2017-12-07

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