KR102945602B1 - N-[4-(클로로디플루오로메톡시)페닐]-6-[(3r)-3-히드록시피롤리딘-1-일]-5-(1h-피라졸-5-일)피리딘-3-카복사미드의 결정질 형태 - Google Patents

N-[4-(클로로디플루오로메톡시)페닐]-6-[(3r)-3-히드록시피롤리딘-1-일]-5-(1h-피라졸-5-일)피리딘-3-카복사미드의 결정질 형태

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Publication number
KR102945602B1
KR102945602B1 KR1020217040723A KR20217040723A KR102945602B1 KR 102945602 B1 KR102945602 B1 KR 102945602B1 KR 1020217040723 A KR1020217040723 A KR 1020217040723A KR 20217040723 A KR20217040723 A KR 20217040723A KR 102945602 B1 KR102945602 B1 KR 102945602B1
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Prior art keywords
crystalline form
hydrochloride
asciminib
phase
granule
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KR1020217040723A
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English (en)
Korean (ko)
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KR20220009414A (ko
Inventor
스테파니 카이 도드
아르노 그란도이리
에프게니아 로우자키
엠마누엘 주페르트
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노파르티스 아게
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/2095—Tabletting processes
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
KR1020217040723A 2019-05-16 2020-05-15 N-[4-(클로로디플루오로메톡시)페닐]-6-[(3r)-3-히드록시피롤리딘-1-일]-5-(1h-피라졸-5-일)피리딘-3-카복사미드의 결정질 형태 Active KR102945602B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962848857P 2019-05-16 2019-05-16
US62/848,857 2019-05-16
US201962949599P 2019-12-18 2019-12-18
US62/949,599 2019-12-18
PCT/IB2020/054628 WO2020230099A1 (en) 2019-05-16 2020-05-15 Crystalline forms of n-[4-(chlorodifluoromethoxy)phenyl]-6-[(3r)-3-hydroxypyrrolidin-1-yl]-5-(1h-pyrazol-5-yl)pyridine-3-carboxamide

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020267009222A Division KR20260055492A (ko) 2019-05-16 2020-05-15 N-[4-(클로로디플루오로메톡시)페닐]-6-[(3r)-3-히드록시피롤리딘-1-일]-5-(1h-피라졸-5-일)피리딘-3-카복사미드의결정질 형태

Publications (2)

Publication Number Publication Date
KR20220009414A KR20220009414A (ko) 2022-01-24
KR102945602B1 true KR102945602B1 (ko) 2026-03-31

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KR1020217040723A Active KR102945602B1 (ko) 2019-05-16 2020-05-15 N-[4-(클로로디플루오로메톡시)페닐]-6-[(3r)-3-히드록시피롤리딘-1-일]-5-(1h-피라졸-5-일)피리딘-3-카복사미드의 결정질 형태

Country Status (13)

Country Link
US (3) US11407735B2 (https=)
EP (1) EP3969117B1 (https=)
JP (2) JP2022532404A (https=)
KR (1) KR102945602B1 (https=)
CN (1) CN114144232A (https=)
AU (1) AU2020276701B2 (https=)
BR (1) BR112021022712A2 (https=)
CA (1) CA3139812A1 (https=)
CL (1) CL2021003011A1 (https=)
IL (1) IL287995A (https=)
MX (1) MX2021013970A (https=)
TW (2) TWI853027B (https=)
WO (1) WO2020230099A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI853027B (zh) 2019-05-16 2024-08-21 瑞士商諾華公司 N-[4-(氯二氟甲氧基)苯基]-6-[(3r)-3-羥基吡咯啶-1-基]-5-(1h-吡唑-5-基)吡啶-3-甲醯胺之結晶形狀
ES3057399T3 (en) 2020-01-28 2026-03-02 Tapi Czech Ind S R O Solid state forms of asciminib and processes for the preparation thereof
WO2022206937A1 (zh) * 2021-04-01 2022-10-06 苏州晶云药物科技股份有限公司 一种吡唑取代的烟酰胺类化合物的盐酸盐新晶型及其制备方法
CN114369085B (zh) * 2021-12-27 2023-01-03 武汉九州钰民医药科技有限公司 盐酸Asciminib的制备方法
WO2024100212A1 (en) 2022-11-10 2024-05-16 Synthon B.V. Crystalline form of asciminib hydrochloride
WO2024257116A1 (en) * 2023-06-13 2024-12-19 Natco Pharma Limited Novel polymorphic forms of asciminib and its pharmaceutical salts thereof
WO2025032514A1 (en) * 2023-08-07 2025-02-13 Biophore India Pharmaceuticals Pvt. Ltd A process for the preparation of solid forms of n-[4(chlorodifluoromethoxy)phenyl]-6-[(3r)-3-hydroxypyrrolidin-1-yl]-5-(1h-pyrazol-3-yl) pyridine-3-carboxamide hydrogen chloride

Citations (2)

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WO2004005281A1 (en) 2002-07-05 2004-01-15 Novartis Ag Inhibitors of tyrosine kinases
WO2013171639A1 (en) * 2012-05-15 2013-11-21 Novartis Ag Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1

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CO4920215A1 (es) 1997-02-14 2000-05-29 Novartis Ag Tabletas de oxacarbazepina recubiertas de una pelicula y metodo para la produccion de estas formulaciones
WO2001051919A2 (en) 2000-01-07 2001-07-19 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
KR20150008406A (ko) 2012-05-15 2015-01-22 노파르티스 아게 Abl1, abl2 및 bcr-abl1의 활성을 억제하기 위한 벤즈아미드 유도체
HUE031227T2 (en) 2012-12-27 2017-07-28 Zentiva Saglik Ueruenleri San Ve Tic A S Dry granulation process for preparing metformin tablet compositions and compositions thereof
US10085993B2 (en) 2014-07-25 2018-10-02 Novartis Ag Tablet formulation of 2-fluoro-N-methyl-4-[ 7-( quinolin-6-ylmethyl) imidazo [1,2-B] [1,2,4] triazin-2-yl] benzamide
WO2016100882A1 (en) 2014-12-19 2016-06-23 Novartis Ag Combination therapies
EP3120851A1 (en) 2015-07-21 2017-01-25 Pangaea Biotech S.L. 4-amino-6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)-pyrido[2,3-d]pyrimidin-7(8h)-one for treatment of solid cancers
US9931342B2 (en) 2016-02-02 2018-04-03 Duke University Compositions and methods for the treatment of cancer
EP3292870A1 (en) 2016-09-08 2018-03-14 Chemotherapeutisches Forschungsinstitut Georg-Speyer-Haus Fibronectin for use in the treatment of leukemia
EP3519400A1 (en) 2016-09-27 2019-08-07 Novartis AG Surfactant systems for crystallization of organic compounds
EP3700516B1 (en) 2017-10-27 2024-01-24 Sonic Master Limited Inhibitors of dux4 induction for regulation of muscle function
US20210214459A1 (en) 2018-05-31 2021-07-15 Novartis Ag Antibody molecules to cd73 and uses thereof
TWI853027B (zh) 2019-05-16 2024-08-21 瑞士商諾華公司 N-[4-(氯二氟甲氧基)苯基]-6-[(3r)-3-羥基吡咯啶-1-基]-5-(1h-吡唑-5-基)吡啶-3-甲醯胺之結晶形狀

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004005281A1 (en) 2002-07-05 2004-01-15 Novartis Ag Inhibitors of tyrosine kinases
WO2013171639A1 (en) * 2012-05-15 2013-11-21 Novartis Ag Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1

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Publication number Publication date
US12252478B2 (en) 2025-03-18
CA3139812A1 (en) 2020-11-19
IL287995A (en) 2022-01-01
EP3969117A1 (en) 2022-03-23
CL2021003011A1 (es) 2022-09-09
WO2020230099A1 (en) 2020-11-19
JP2022532404A (ja) 2022-07-14
KR20220009414A (ko) 2022-01-24
US20230089503A1 (en) 2023-03-23
US20230074064A1 (en) 2023-03-09
BR112021022712A2 (pt) 2022-03-29
US11407735B2 (en) 2022-08-09
MX2021013970A (es) 2022-01-04
US12252479B2 (en) 2025-03-18
AU2020276701A8 (en) 2022-05-12
TWI853027B (zh) 2024-08-21
EP3969117B1 (en) 2026-03-25
AU2020276701A1 (en) 2022-01-06
US20200361904A1 (en) 2020-11-19
TW202110823A (zh) 2021-03-16
JP2024095697A (ja) 2024-07-10
AU2020276701B2 (en) 2023-11-23
TW202444706A (zh) 2024-11-16
CN114144232A (zh) 2022-03-04

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