KR102466958B1 - 단백질 키나제 활성을 억제하는 화합물의 결정 형태 및 이의 응용 - Google Patents

단백질 키나제 활성을 억제하는 화합물의 결정 형태 및 이의 응용 Download PDF

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KR102466958B1
KR102466958B1 KR1020187038142A KR20187038142A KR102466958B1 KR 102466958 B1 KR102466958 B1 KR 102466958B1 KR 1020187038142 A KR1020187038142 A KR 1020187038142A KR 20187038142 A KR20187038142 A KR 20187038142A KR 102466958 B1 KR102466958 B1 KR 102466958B1
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crystalline form
compound
formula
cancer
water
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KR20190012231A (ko
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콩신 리앙
용빈 마
웨이 헤
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타이로제넥스, 인코포레이티드
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    • 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
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    • 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
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    • 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
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    • 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

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  • 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)
KR1020187038142A 2016-06-01 2017-06-01 단백질 키나제 활성을 억제하는 화합물의 결정 형태 및 이의 응용 Active KR102466958B1 (ko)

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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KR20190012231A KR20190012231A (ko) 2019-02-08
KR102466958B1 true KR102466958B1 (ko) 2022-11-14

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KR1020187038142A Active KR102466958B1 (ko) 2016-06-01 2017-06-01 단백질 키나제 활성을 억제하는 화합물의 결정 형태 및 이의 응용

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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=)

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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006021886A1 (en) 2004-08-26 2006-03-02 Pfizer Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
WO2006076412A1 (en) 2005-01-12 2006-07-20 Medtronic Minimed, Inc. Fabrication of multi-sensor arrays
WO2009154769A1 (en) 2008-06-19 2009-12-23 Xcovery, Inc. Substituted pyridazine carboxamide compounds as kinase inhibitor compounds
CN103298806A (zh) 2010-10-08 2013-09-11 艾科睿控股公司 取代的哒嗪羧酰胺化合物

Family Cites Families (6)

* 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
ME01309B (me) * 2004-08-26 2013-12-20 Pfizer Pirazolom supstituirani heteroarilni spojevi kao inhibitori proteinskih kinaza
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

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006021886A1 (en) 2004-08-26 2006-03-02 Pfizer Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
WO2006076412A1 (en) 2005-01-12 2006-07-20 Medtronic Minimed, Inc. Fabrication of multi-sensor arrays
WO2009154769A1 (en) 2008-06-19 2009-12-23 Xcovery, Inc. Substituted pyridazine carboxamide compounds as kinase inhibitor compounds
CN102098917A (zh) 2008-06-19 2011-06-15 艾科睿控股公司 作为激酶抑制剂化合物的取代的哒嗪羧酰胺化合物
CN103298806A (zh) 2010-10-08 2013-09-11 艾科睿控股公司 取代的哒嗪羧酰胺化合物

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
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
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
US10899744B2 (en) 2021-01-26
KR20190012231A (ko) 2019-02-08
WO2017206924A1 (zh) 2017-12-07

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