TWI646094B - Crystal form of inhibitory protein kinase active compound and application thereof - Google Patents

Crystal form of inhibitory protein kinase active compound and application thereof Download PDF

Info

Publication number
TWI646094B
TWI646094B TW106117900A TW106117900A TWI646094B TW I646094 B TWI646094 B TW I646094B TW 106117900 A TW106117900 A TW 106117900A TW 106117900 A TW106117900 A TW 106117900A TW I646094 B TWI646094 B TW I646094B
Authority
TW
Taiwan
Prior art keywords
compound
formula
crystal form
added
water
Prior art date
Application number
TW106117900A
Other languages
English (en)
Chinese (zh)
Other versions
TW201742865A (zh
Inventor
從新 梁
馬勇斌
何偉
Original Assignee
大陸商貝達藥業股份有限公司
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 大陸商貝達藥業股份有限公司 filed Critical 大陸商貝達藥業股份有限公司
Publication of TW201742865A publication Critical patent/TW201742865A/zh
Application granted granted Critical
Publication of TWI646094B publication Critical patent/TWI646094B/zh

Links

Classifications

    • 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

Landscapes

  • 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)
TW106117900A 2016-06-01 2017-05-31 Crystal form of inhibitory protein kinase active compound and application thereof TWI646094B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CNPCT/CN2016/084300 2016-06-01
??PCT/CN2016/084300 2016-06-01

Publications (2)

Publication Number Publication Date
TW201742865A TW201742865A (zh) 2017-12-16
TWI646094B true TWI646094B (zh) 2019-01-01

Family

ID=60477983

Family Applications (1)

Application Number Title Priority Date Filing Date
TW106117900A TWI646094B (zh) 2016-06-01 2017-05-31 Crystal form of inhibitory protein kinase active compound 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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (8)

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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
KR102466958B1 (ko) 2022-11-14
US10899744B2 (en) 2021-01-26
KR20190012231A (ko) 2019-02-08
WO2017206924A1 (zh) 2017-12-07

Similar Documents

Publication Publication Date Title
CN102510855B (zh) N-[3-氟-4-({6-(甲基氧基)-7-[(3-吗啉-4-基丙基)氧基]-喹啉-4-基}氧基)苯基]-n′-(4-氟苯基)环丙烷-1,1-二甲酰胺的晶形
CN102408411B (zh) 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
CN101998951B (zh) 酰基硫脲化合物或其盐及其用途
TWI646094B (zh) Crystal form of inhibitory protein kinase active compound and application thereof
CN111788197B (zh) 取代的二氨基杂环甲酰胺化合物及包含该化合物的组合物及其用途
EP3865487A1 (en) Aromatic ring-linked dioxane-quinazoline or -quinoline compounds, compositions and use thereof
CN104557870B (zh) 一种吡啶胺化合物的富马酸盐
CN103373986A (zh) 克里唑替尼前药及其制备方法与用途
JP7391226B2 (ja) ピリミジン化合物の結晶
HK1259249B (zh) 抑制蛋白激酶活性化合物的晶型及其应用
TW202104216A (zh) Plk4抑制劑之結晶型
CN110023298B (zh) 异柠檬酸脱氢酶(idh)抑制剂
BR112018074612B1 (pt) Compostos intermediários, composto que suprime a atividade de proteína quinase, sua forma cristalina, método de produção, composição farmacêutica e aplicação da forma cristalina
EP4696689A1 (en) Salt form and crystal form of chiral heterocyclic compound having hedgehog pathway antagonist activity
Alwan et al. In Silico Molecular Docking, Synthesis and Preliminary Evaluation of Antibacterial Activity of Levofloxacin Carboxamides with Certain Amino Acids
TW201829398A (zh) 酪胺酸蛋白激酶調節劑、晶型及其用途
EA041596B1 (ru) Кристаллическая форма соединения, подавляющего активность протеинкиназы, и её применение
WO2018099451A1 (zh) 化合物的晶型
NZ788961A (en) Crystalline form of compound suppressing protein kinase activity, and application thereof
TW202527935A (zh) 吲唑巨環多晶型物
WO2022247772A1 (zh) 一种含氧杂环化合物的晶型、其制备方法及应用
TW202120511A (zh) 雜環化合物
HK40057704A (en) Aromatic ring-linked dioxane-quinazoline or -quinoline compounds, compositions and use thereof
HK1171009B (en) Preparation method, drug component and application of a hydroximic acid compound which has quinolyl