BR112018074612A2 - forma cristalina de composto que suprimir a atividade de proteína quinase e aplicação da mesma - Google Patents

forma cristalina de composto que suprimir a atividade de proteína quinase e aplicação da mesma

Info

Publication number
BR112018074612A2
BR112018074612A2 BR112018074612-6A BR112018074612A BR112018074612A2 BR 112018074612 A2 BR112018074612 A2 BR 112018074612A2 BR 112018074612 A BR112018074612 A BR 112018074612A BR 112018074612 A2 BR112018074612 A2 BR 112018074612A2
Authority
BR
Brazil
Prior art keywords
compound
crystalline form
application
protein kinase
kinase activity
Prior art date
Application number
BR112018074612-6A
Other languages
English (en)
Inventor
Liang Congxin
Ma Yongbin
He Wei
Original Assignee
Xcovery Holdings, Inc.
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 Xcovery Holdings, Inc. filed Critical Xcovery Holdings, Inc.
Publication of BR112018074612A2 publication Critical patent/BR112018074612A2/pt

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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
    • C07D403/02—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
    • 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
    • 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)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

a presente invenção refere-se a um composto conforme representado pela fórmula (i) ({5-[(1r)-1-(2,6- dicloro-3- fluorofenil)etóxi]-6-aminopiridazin-3-il}-n-{4-[((3s,5r)-3,5-dimetilpiperazinil)carbonil]fenil}carboxamida) e um nova forma cristalina de um hidrato ou solvato do composto. além disso, são fornecidos um método fabricação do composto e da forma cristalina, um intermediário relacionado, uma composição farmacêutica que compreende o composto, uma aplicação que usa o composto ou a forma cristalina para preparar um produto farmacêutico para tratar uma doença, sintoma ou transtorno e um método terapêutico para tratar uma doença, sintoma ou transtorno.
BR112018074612-6A 2016-06-01 2017-06-01 forma cristalina de composto que suprimir a atividade de proteína quinase e aplicação da mesma BR112018074612A2 (pt)

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 (1)

Publication Number Publication Date
BR112018074612A2 true BR112018074612A2 (pt) 2019-03-19

Family

ID=60477983

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018074612-6A BR112018074612A2 (pt) 2016-06-01 2017-06-01 forma cristalina de composto que suprimir a atividade de proteína quinase e aplicação da mesma

Country Status (17)

Country Link
US (1) US10899744B2 (pt)
EP (1) EP3470410B1 (pt)
JP (1) JP7054528B2 (pt)
KR (1) KR102466958B1 (pt)
CN (1) CN109195964B (pt)
AU (1) AU2017274110B2 (pt)
BR (1) BR112018074612A2 (pt)
CA (1) CA3026142C (pt)
EA (1) EA201892687A1 (pt)
HK (1) HK1259249A1 (pt)
IL (1) IL263356B (pt)
MY (1) MY188379A (pt)
PH (1) PH12018502529A1 (pt)
RU (1) RU2744264C2 (pt)
SG (1) SG11201810800VA (pt)
TW (1) TWI646094B (pt)
WO (1) WO2017206924A1 (pt)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI786303B (zh) * 2018-06-21 2022-12-11 大陸商貝達藥業股份有限公司 抑制ｃｄｋ4/6活性化合物的晶型及其應用
WO2022031636A1 (en) 2020-08-03 2022-02-10 Teva Pharmaceuticals International Gmbh Solid state forms of ensartinib and ensartinib salts
CN117897156A (zh) * 2021-08-10 2024-04-16 贝达药业股份有限公司 恩沙替尼或其盐在治疗携带met 14外显子跳跃突变的疾病中的用途

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001233028A1 (en) * 2000-03-06 2001-10-03 Warner-Lambert Company 5-alkylpyrido(2,3-D)pyrimidines tyrosine kinase inhibitors
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
WO2006021881A2 (en) * 2004-08-26 2006-03-02 Pfizer Inc. Pyrazole-substituted aminoheteroaryl compounds as protein kinase inhibitors
EP1786777A1 (en) 2004-08-26 2007-05-23 Pfizer, Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
WO2007066185A2 (en) * 2005-12-05 2007-06-14 Pfizer Products Inc. Polymorphs of a c-met/hgfr inhibitor
CN101652068A (zh) * 2007-01-19 2010-02-17 艾科睿制药公司 激酶抑制物化合物
US8697866B2 (en) 2008-06-19 2014-04-15 Xcovery Holding Company Llc Substituted pyridazine carboxamide compounds as kinase inhibitor compounds
ES2610226T3 (es) * 2010-10-08 2017-04-26 Xcovery Holding Company Llc Compuestos de 6-amino-piridazin-3-il-carboxamida sustituidos como moduladores de proteínas cinasas
JP5909236B2 (ja) * 2010-10-08 2016-04-26 エックスカバリー ホールディング カンパニー エルエルシー キナーゼ阻害剤化合物としての置換ピリダジンカルボキサミド化合物

Also Published As

Publication number Publication date
WO2017206924A1 (zh) 2017-12-07
RU2744264C2 (ru) 2021-03-04
CA3026142C (en) 2024-02-13
RU2018145183A3 (pt) 2020-07-16
CN109195964B (zh) 2021-08-10
IL263356A (en) 2018-12-31
JP2019518026A (ja) 2019-06-27
CN109195964A (zh) 2019-01-11
CA3026142A1 (en) 2017-12-07
AU2017274110A1 (en) 2019-01-24
SG11201810800VA (en) 2019-01-30
KR102466958B1 (ko) 2022-11-14
EP3470410A1 (en) 2019-04-17
RU2018145183A (ru) 2020-07-14
AU2017274110B2 (en) 2021-05-06
EP3470410B1 (en) 2024-04-17
US20190135792A1 (en) 2019-05-09
EA201892687A1 (ru) 2019-06-28
IL263356B (en) 2022-08-01
TWI646094B (zh) 2019-01-01
PH12018502529A1 (en) 2019-04-08
JP7054528B2 (ja) 2022-04-14
EP3470410A4 (en) 2019-12-04
HK1259249A1 (zh) 2019-11-29
TW201742865A (zh) 2017-12-16
KR20190012231A (ko) 2019-02-08
US10899744B2 (en) 2021-01-26
MY188379A (en) 2021-12-07

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Legal Events

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B350 Update of information on the portal [chapter 15.35 patent gazette]
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]