RU2744264C2 - Кристаллическая форма соединения, подавляющего активность протеинкиназы, и её применение - Google Patents

Кристаллическая форма соединения, подавляющего активность протеинкиназы, и её применение Download PDF

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RU2744264C2
RU2744264C2 RU2018145183A RU2018145183A RU2744264C2 RU 2744264 C2 RU2744264 C2 RU 2744264C2 RU 2018145183 A RU2018145183 A RU 2018145183A RU 2018145183 A RU2018145183 A RU 2018145183A RU 2744264 C2 RU2744264 C2 RU 2744264C2
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crystalline form
cancer
disorder
compound
pharmaceutical composition
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RU2018145183A
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RU2018145183A3 (https=
RU2018145183A (ru
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Цунсинь Лян
Юнбинь Ма
Вэй ХЭ
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ЭксКАВЕРИ ХОЛДИНГЗ, ИНК.
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    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C403/00—Derivatives 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
    • C07C403/06—Derivatives 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
    • C07C403/10—Derivatives 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
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/10—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 two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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)
  • 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)
RU2018145183A 2016-06-01 2017-06-01 Кристаллическая форма соединения, подавляющего активность протеинкиназы, и её применение RU2744264C2 (ru)

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

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RU2018145183A RU2018145183A (ru) 2020-07-14
RU2018145183A3 RU2018145183A3 (https=) 2020-07-16
RU2744264C2 true RU2744264C2 (ru) 2021-03-04

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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=)

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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

Citations (2)

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WO2012048259A2 (en) * 2010-10-08 2012-04-12 Xcovery Holding Company, Llc Substituted pyridazine carboxamide compounds
RU2526618C2 (ru) * 2008-06-19 2014-08-27 Икскавери Холдинг Кампани Ллс Замещенные пиридазин-карбоксамидные соединения в качестве соединений, ингибирующих киназы

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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
WO2012048258A2 (en) * 2010-10-08 2012-04-12 Xcovery Holding Company, Llc Substituted pyridazine carboxamide compounds as kinase inhibitor compounds

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RU2526618C2 (ru) * 2008-06-19 2014-08-27 Икскавери Холдинг Кампани Ллс Замещенные пиридазин-карбоксамидные соединения в качестве соединений, ингибирующих киназы
WO2012048259A2 (en) * 2010-10-08 2012-04-12 Xcovery Holding Company, Llc Substituted pyridazine carboxamide compounds

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Clinical pharmacokinetics: theoretical, applied and analytical aspects: manual / Ed. V.G. Kukesa. (Chapter 11.2. RELATIONSHIP OF THE CRYSTALLINE STRUCTURE OF SUBSTANCE OF SUBSTANCE, PHARMACOKINETICS AND EFFICIENCY OF A DRUG, IG Smirnova, V.V. Chistyakov, pp. 235-249), 2009. *
Mino R. Caira, Crystalline Polymorphism of Organic Compounds, Topics in Current Chemistry, vol. 198, section 3.1, p. 188, 2nd paragraph, 1998. *
Mino R. Caira, Crystalline Polymorphism of Organic Compounds, Topics in Current Chemistry, т. 198, разд.3.1, стр.188, 2-й абзац, 1998. Клиническая фармакокинетика: теоретические, прикладные и аналитические аспекты: руководство / Под ред. В.Г. Кукеса. (Глава 11.2. ВЗАИМОСВЯЗЬ КРИСТАЛЛИЧЕСКОЙ СТРУКТУРЫ СУБСТАНЦИИ ВЕЩЕСТВА, ФАРМАКОКИНЕТИКИ И ЭФФЕКТИВНОСТИ ЛЕКАРСТВЕННОГО СРЕДСТВА, И.Г. Смирнова, В.В. Чистяков, стр. 235-249), 2009. Sherry L.Morissette et al.: "High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids", ADVANCED DRUG DELIVERY REVIEWS, 2004, v.56, pp.275-300 (section 3.1), DOI: 10.1016/J.ADDR.2003.10.020. STEPHEN M.BERGE et al., Pharmaceuticals Salts, JOURNAL of PHARMACEUTICAL SCIENCES, 1977, v.66 (1), p.1-19 (стр.1-5, 9 "Stability"). *
Sherry L. Morissette et al crystallization : polymorphs, salts, co-crystals and solvates of pharmaceutical solids ", ADVANCED DRUG DELIVERY REVIEWS, 2004, v. 56, pp. 275-300 (section 3.1), DOI: 10.1016 / J. ADDR.2003.10.020. *
STEPHEN M.BERGE et al., Pharmaceuticals Salts, JOURNAL of PHARMACEUTICAL SCIENCES, 1977, v.66 (1), p.1-19 (стр.1-5, 9 "Stability"). *

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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
CA3026142C (en) 2024-02-13
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
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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