CN114144232A - N-[4-(氯二氟甲氧基)苯基]-6-[(3r)-3-羟基吡咯烷-1-基]-5-(1h-吡唑-5-基)吡啶-3-甲酰胺的结晶形式 - Google Patents

N-[4-(氯二氟甲氧基)苯基]-6-[(3r)-3-羟基吡咯烷-1-基]-5-(1h-吡唑-5-基)吡啶-3-甲酰胺的结晶形式 Download PDF

Info

Publication number
CN114144232A
CN114144232A CN202080051576.4A CN202080051576A CN114144232A CN 114144232 A CN114144232 A CN 114144232A CN 202080051576 A CN202080051576 A CN 202080051576A CN 114144232 A CN114144232 A CN 114144232A
Authority
CN
China
Prior art keywords
crystalline form
pyridine
phenyl
chlorodifluoromethoxy
pyrazol
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN202080051576.4A
Other languages
English (en)
Chinese (zh)
Inventor
S·K·都德
A·格朗德里
E·鲁萨基
E·萨弗特
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of CN114144232A publication Critical patent/CN114144232A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • 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
    • 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)
  • 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)
CN202080051576.4A 2019-05-16 2020-05-15 N-[4-(氯二氟甲氧基)苯基]-6-[(3r)-3-羟基吡咯烷-1-基]-5-(1h-吡唑-5-基)吡啶-3-甲酰胺的结晶形式 Pending CN114144232A (zh)

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

Publications (1)

Publication Number Publication Date
CN114144232A true CN114144232A (zh) 2022-03-04

Family

ID=70775449

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080051576.4A Pending CN114144232A (zh) 2019-05-16 2020-05-15 N-[4-(氯二氟甲氧基)苯基]-6-[(3r)-3-羟基吡咯烷-1-基]-5-(1h-吡唑-5-基)吡啶-3-甲酰胺的结晶形式

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

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
KR20150008406A (ko) 2012-05-15 2015-01-22 노파르티스 아게 Abl1, abl2 및 bcr-abl1의 활성을 억제하기 위한 벤즈아미드 유도체
PT2861579T (pt) * 2012-05-15 2018-04-27 Novartis Ag Derivados de benzamida para inibir a atividade de abl1, abl2 e bcr-abl
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

Also Published As

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
KR102945602B1 (ko) 2026-03-31
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

Similar Documents

Publication Publication Date Title
TWI853027B (zh) 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
EP3969449B1 (en) New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
JP7659097B2 (ja) Ｎ－｛４－［（６，７－ジメトキシキノリン－４－イル）オキシ］フェニル｝－ｎ’－（４－フルオロフェニル）シクロプロパン－１，１－ジカルボキサミドの塩の結晶性固体形態、製造プロセス、及び使用方法
JP6621761B2 (ja) 薬学的に活性な化合物の固体形態
HRP20000328A2 (en) Novel polymorph v of torasemide
RU2836337C2 (ru) Кристаллические формы n-[4-(хлордифторметокси)фенил]-6-[(3r)-3-гидроксипирролидин-1-ил]-5-(1h-пиразол-5-ил)пиридин-3-карбоксамида
US20240293420A1 (en) Pharmaceutical composition, preparation, and preparation method therefor and use thereof
KR20260055492A (ko) N-[4-(클로로디플루오로메톡시)페닐]-6-[(3r)-3-히드록시피롤리딘-1-일]-5-(1h-피라졸-5-일)피리딘-3-카복사미드의결정질 형태
JP4684545B2 (ja) 溶出性の良好なイソキサゾール誘導体経口製剤
HK40127061A (en) New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl) isonicotinamide as raf inhibitors for the treatment of cancer
HK40065390B (en) New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
HK40065390A (en) New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
HK40026069A (en) Crystalline solid forms of salts of n-{4-[(6,7-dimethoxyquinolin-4-yl) oxy]phenyl}-n'-(4-fluorphenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination