JP2022532404A - N-[4-(クロロジフルオロメトキシ)フェニル]-6-[(3r)-3-ヒドロキシピロリジン-1-イル]-5-(1h-ピラゾール-5-イル)ピリジン-3-カルボキサミドの結晶性形態 - Google Patents
N-[4-(クロロジフルオロメトキシ)フェニル]-6-[(3r)-3-ヒドロキシピロリジン-1-イル]-5-(1h-ピラゾール-5-イル)ピリジン-3-カルボキサミドの結晶性形態 Download PDFInfo
- Publication number
- JP2022532404A JP2022532404A JP2021568319A JP2021568319A JP2022532404A JP 2022532404 A JP2022532404 A JP 2022532404A JP 2021568319 A JP2021568319 A JP 2021568319A JP 2021568319 A JP2021568319 A JP 2021568319A JP 2022532404 A JP2022532404 A JP 2022532404A
- Authority
- JP
- Japan
- Prior art keywords
- chlorodifluoromethoxy
- pyridine
- phenyl
- pyrazole
- crystalline form
- 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.)
- Withdrawn
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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)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024045596A JP2024095697A (ja) | 2019-05-16 | 2024-03-21 | N-[4-(クロロジフルオロメトキシ)フェニル]-6-[(3r)-3-ヒドロキシピロリジン-1-イル]-5-(1h-ピラゾール-5-イル)ピリジン-3-カルボキサミドの結晶性形態 |
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 |
|---|---|---|---|
| JP2024045596A Division JP2024095697A (ja) | 2019-05-16 | 2024-03-21 | N-[4-(クロロジフルオロメトキシ)フェニル]-6-[(3r)-3-ヒドロキシピロリジン-1-イル]-5-(1h-ピラゾール-5-イル)ピリジン-3-カルボキサミドの結晶性形態 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022532404A true JP2022532404A (ja) | 2022-07-14 |
| JP2022532404A5 JP2022532404A5 (https=) | 2022-08-25 |
| JPWO2020230099A5 JPWO2020230099A5 (https=) | 2022-08-25 |
Family
ID=70775449
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021568319A Withdrawn JP2022532404A (ja) | 2019-05-16 | 2020-05-15 | N-[4-(クロロジフルオロメトキシ)フェニル]-6-[(3r)-3-ヒドロキシピロリジン-1-イル]-5-(1h-ピラゾール-5-イル)ピリジン-3-カルボキサミドの結晶性形態 |
| JP2024045596A Pending JP2024095697A (ja) | 2019-05-16 | 2024-03-21 | N-[4-(クロロジフルオロメトキシ)フェニル]-6-[(3r)-3-ヒドロキシピロリジン-1-イル]-5-(1h-ピラゾール-5-イル)ピリジン-3-カルボキサミドの結晶性形態 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024045596A Pending JP2024095697A (ja) | 2019-05-16 | 2024-03-21 | N-[4-(クロロジフルオロメトキシ)フェニル]-6-[(3r)-3-ヒドロキシピロリジン-1-イル]-5-(1h-ピラゾール-5-イル)ピリジン-3-カルボキサミドの結晶性形態 |
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=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2025536048A (ja) * | 2022-11-10 | 2025-10-30 | シントン・ビー.ブイ. | アシミニブ塩酸塩の結晶形態 |
Families Citing this family (6)
| 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 |
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003519698A (ja) * | 2000-01-07 | 2003-06-24 | トランスフォーム ファーマスーティカルズ,インコーポレイテッド | 多様な固体形態のハイスループットでの形成、同定および分析 |
| JP2015521185A (ja) * | 2012-05-15 | 2015-07-27 | ノバルティス アーゲー | Abl1、abl2およびbcr−abl1の活性を阻害するためのベンズアミド誘導体 |
Family Cites Families (13)
| 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 |
| 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 |
| 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 |
-
2020
- 2020-05-14 TW TW109116067A patent/TWI853027B/zh active
- 2020-05-14 TW TW113128176A patent/TW202444706A/zh unknown
- 2020-05-14 US US16/874,622 patent/US11407735B2/en active Active
- 2020-05-15 BR BR112021022712A patent/BR112021022712A2/pt unknown
- 2020-05-15 MX MX2021013970A patent/MX2021013970A/es unknown
- 2020-05-15 CA CA3139812A patent/CA3139812A1/en active Pending
- 2020-05-15 AU AU2020276701A patent/AU2020276701B2/en active Active
- 2020-05-15 EP EP20726959.8A patent/EP3969117B1/en active Active
- 2020-05-15 KR KR1020217040723A patent/KR102945602B1/ko active Active
- 2020-05-15 WO PCT/IB2020/054628 patent/WO2020230099A1/en not_active Ceased
- 2020-05-15 CN CN202080051576.4A patent/CN114144232A/zh active Pending
- 2020-05-15 JP JP2021568319A patent/JP2022532404A/ja not_active Withdrawn
-
2021
- 2021-11-10 IL IL287995A patent/IL287995A/en unknown
- 2021-11-15 CL CL2021003011A patent/CL2021003011A1/es unknown
-
2022
- 2022-07-06 US US17/858,701 patent/US12252478B2/en active Active
- 2022-07-06 US US17/858,713 patent/US12252479B2/en active Active
-
2024
- 2024-03-21 JP JP2024045596A patent/JP2024095697A/ja active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003519698A (ja) * | 2000-01-07 | 2003-06-24 | トランスフォーム ファーマスーティカルズ,インコーポレイテッド | 多様な固体形態のハイスループットでの形成、同定および分析 |
| JP2015521185A (ja) * | 2012-05-15 | 2015-07-27 | ノバルティス アーゲー | Abl1、abl2およびbcr−abl1の活性を阻害するためのベンズアミド誘導体 |
Non-Patent Citations (4)
| Title |
|---|
| ""新医薬品の規格及び試験方法の設定について"", 医薬審発第568号, JPN6010021254, 1 May 2001 (2001-05-01), ISSN: 0005301604 * |
| 山野光久: "医薬品のプロセス研究における結晶多形現象への取り組み", 有機合成化学協会誌, JPN6010003277, 2007, ISSN: 0005301606 * |
| 川口洋子ら: "医薬品と結晶多形", 生活工学研究, JPN6014015069, 2002, ISSN: 0005301603 * |
| 高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0005301605 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2025536048A (ja) * | 2022-11-10 | 2025-10-30 | シントン・ビー.ブイ. | アシミニブ塩酸塩の結晶形態 |
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 |
| 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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