BR112021014563A2 - Dispersão sólida amorfa, complexo da fórmula (i), formas cristalina de composto 1, cristal isolado, métodos de preparação da dispersão sólida amorfa, de tratamento ou prevenção de doenças, de preparação de compostos da fórmula i, composto da fórmula ia - Google Patents
Dispersão sólida amorfa, complexo da fórmula (i), formas cristalina de composto 1, cristal isolado, métodos de preparação da dispersão sólida amorfa, de tratamento ou prevenção de doenças, de preparação de compostos da fórmula i, composto da fórmula ia Download PDFInfo
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- BR112021014563A2 BR112021014563A2 BR112021014563-0A BR112021014563A BR112021014563A2 BR 112021014563 A2 BR112021014563 A2 BR 112021014563A2 BR 112021014563 A BR112021014563 A BR 112021014563A BR 112021014563 A2 BR112021014563 A2 BR 112021014563A2
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- hpmcas
- free base
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
-
- 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
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/61—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- 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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Inorganic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Dispersion Chemistry (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2019/073254 | 2019-01-25 | ||
| CN2019073254 | 2019-01-25 | ||
| CN2019095227 | 2019-07-09 | ||
| CNPCT/CN2019/095227 | 2019-07-09 | ||
| PCT/CN2020/073944 WO2020151756A1 (en) | 2019-01-25 | 2020-01-23 | Stable solid dispersions of b-raf kinase dimer inhibitor, methods of preparation, and uses therefor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112021014563A2 true BR112021014563A2 (pt) | 2021-10-05 |
Family
ID=71735582
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112021014563-0A BR112021014563A2 (pt) | 2019-01-25 | 2020-01-23 | Dispersão sólida amorfa, complexo da fórmula (i), formas cristalina de composto 1, cristal isolado, métodos de preparação da dispersão sólida amorfa, de tratamento ou prevenção de doenças, de preparação de compostos da fórmula i, composto da fórmula ia |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US12582604B2 (https=) |
| EP (1) | EP3914591A4 (https=) |
| JP (2) | JP7591504B2 (https=) |
| KR (1) | KR20210120039A (https=) |
| CN (1) | CN113330011A (https=) |
| AU (1) | AU2020211000B2 (https=) |
| BR (1) | BR112021014563A2 (https=) |
| CA (1) | CA3123476A1 (https=) |
| IL (1) | IL284636A (https=) |
| MX (1) | MX2021008884A (https=) |
| SG (1) | SG11202107849RA (https=) |
| TW (2) | TWI849043B (https=) |
| WO (1) | WO2020151756A1 (https=) |
| ZA (1) | ZA202104032B (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111484490B (zh) * | 2019-01-25 | 2024-07-09 | 百济神州有限公司 | 适合大规模生产b-raf激酶二聚体抑制剂的方法 |
| TWI849043B (zh) | 2019-01-25 | 2024-07-21 | 英屬開曼群島商百濟神州有限公司 | B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途 |
| JP2024504285A (ja) * | 2020-12-29 | 2024-01-31 | ティーエックスイノ バイオサイエンス インコーポレイテッド | エクトヌクレオチドピロホスファターゼ－ホスホジエステラーゼの阻害活性を有する新規のナフチリジノン誘導体及びこれらの用途 |
| KR102889693B1 (ko) | 2021-09-08 | 2025-11-20 | 주식회사 엘지에너지솔루션 | 배터리 진단 장치, 배터리 관리 시스템, 배터리 팩, 전기 차량 및 배터리 진단 방법 |
| CN114366717B (zh) * | 2022-01-11 | 2023-06-09 | 四川农业大学 | 一种基于egcg纳米粒的肠溶固体分散体颗粒、制备方法及其应用 |
| WO2023240178A1 (en) * | 2022-06-08 | 2023-12-14 | Mapkure, Llc | Methods of treating cancer with a b-raf inhibitor |
| EP4593831A1 (en) * | 2022-09-26 | 2025-08-06 | Mapkure, LLC | Combinations of a b-raf inhibitor, and an anti-egfr antibody for the treatment of cancer |
| JP2026507361A (ja) * | 2023-03-10 | 2026-03-02 | エスティー ファーム カンパニー リミテッド | 新規固体分散体およびその製造方法 |
| TW202515875A (zh) | 2023-10-12 | 2025-04-16 | 瑞士商百濟神州瑞士有限責任公司 | 包含b-raf激酶二聚體抑制劑之固體形式、其製備方法及用途 |
| WO2025252204A1 (en) * | 2024-06-07 | 2025-12-11 | Beigene (Suzhou) Co., Ltd. | Amorphous solid dispersions of a braf inhibitor |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6350786B1 (en) | 1998-09-22 | 2002-02-26 | Hoffmann-La Roche Inc. | Stable complexes of poorly soluble compounds in ionic polymers |
| ATE400251T1 (de) | 1999-02-09 | 2008-07-15 | Pfizer Prod Inc | Zusammensetzungen basischer arzneistoffe mit verbesserter bioverfügbarkeit |
| SE0100733D0 (sv) | 2001-03-05 | 2001-03-05 | Medivir Ab | Non-nucleoside reverse transcriptase inhibitors |
| EP1534276B1 (en) | 2002-09-05 | 2008-11-05 | Medivir AB | Non-nucleoside reverse transcriptase inhibitors |
| CN1925855B (zh) | 2003-12-19 | 2010-06-16 | 普莱希科公司 | 开发Ret调节剂的化合物和方法 |
| JP2008525355A (ja) | 2004-12-23 | 2008-07-17 | エフ．ホフマン−ラ ロシュ アーゲー | ベンズアミド誘導体、これらの製造及び医薬剤としての使用。 |
| WO2007067444A1 (en) | 2005-12-08 | 2007-06-14 | Millennium Pharmaceuticals, Inc. | Bicyclic compounds with kinase inhibitory activity |
| EP2021327B1 (en) | 2006-05-15 | 2012-04-04 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| KR101104666B1 (ko) | 2006-09-06 | 2012-01-13 | 에프. 호프만-라 로슈 아게 | 단백질 키나제 억제제로서의 헤테로아릴 유도체 |
| WO2008079909A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
| PE20121126A1 (es) | 2006-12-21 | 2012-08-24 | Plexxikon Inc | Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa |
| JP2010526848A (ja) | 2007-05-11 | 2010-08-05 | エフ．ホフマン−ラ ロシュ アーゲー | 難溶性薬物用の医薬組成物 |
| WO2009012283A1 (en) | 2007-07-17 | 2009-01-22 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| EP3147281A1 (en) * | 2008-03-17 | 2017-03-29 | Ambit Biosciences Corporation | Quinazoline derivatives as raf kinase modulators and methods of use thereof |
| JO3101B1 (ar) | 2008-12-02 | 2017-09-20 | Takeda Pharmaceuticals Co | مشتقات بنزوثيازول كعوامل مضادة للسرطان |
| US20100197924A1 (en) | 2008-12-22 | 2010-08-05 | Millennium Pharmaceuticals, Inc. | Preparation of aminotetralin compounds |
| MY172424A (en) * | 2009-04-03 | 2019-11-25 | Hoffmann La Roche | Propane- i-sulfonic acid {3- (4-chloro-phenyl)-1h-pyrrolo [2, 3-b] pyridine-3-carconyl] -2, 4-difluoro-phenyl} -amide compositions and uses thereof |
| JP2013503189A (ja) * | 2009-08-28 | 2013-01-31 | アレイ バイオファーマ、インコーポレイテッド | Ｒａｆ阻害化合物およびその使用方法 |
| CN104958294A (zh) | 2010-01-27 | 2015-10-07 | 内尔维安诺医学科学有限公司 | 作为蛋白激酶抑制剂的3,4-二芳基吡唑的亚磺酰氨基衍生物 |
| WO2011115069A1 (ja) | 2010-03-19 | 2011-09-22 | 第一三共株式会社 | 結晶の網羅的探索 |
| US9624213B2 (en) * | 2011-02-07 | 2017-04-18 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| PL2797888T3 (pl) | 2011-12-31 | 2016-12-30 | Połączone związki tricykliczne jako inhibitory kinazy raf | |
| JP6342396B2 (ja) * | 2012-08-07 | 2018-06-13 | ノバルティス アーゲー | Ｂ−Ｒａｆ阻害薬、ＥＧＦＲ阻害薬及び場合によってはＰＩ３Ｋ−α阻害薬を含む組合せ医薬 |
| WO2014114575A1 (en) | 2013-01-22 | 2014-07-31 | F. Hoffmann-La Roche Ag | Pharmaceutical composition with improved bioavailability |
| JP2014189462A (ja) | 2013-03-27 | 2014-10-06 | Osaka Univ | 結晶製造方法、準安定形結晶、医薬の製造方法および医薬 |
| EP3013797B1 (en) * | 2013-06-28 | 2018-01-03 | BeiGene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
| EA029412B1 (ru) * | 2013-06-28 | 2018-03-30 | Бейджин, Лтд. | Конденсированные трициклические соединения мочевины в качестве ингибиторов киназы raf и/или димера киназы raf |
| WO2015152433A1 (en) * | 2014-03-31 | 2015-10-08 | Hanmi Pharm. Co., Ltd. | Amorphous solid dispersion comprising paclitaxel, tablet comprising the same, and method for preparing the same |
| TWI849043B (zh) | 2019-01-25 | 2024-07-21 | 英屬開曼群島商百濟神州有限公司 | B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途 |
-
2020
- 2020-01-22 TW TW109102401A patent/TWI849043B/zh active
- 2020-01-22 TW TW113123511A patent/TWI909513B/zh active
- 2020-01-23 AU AU2020211000A patent/AU2020211000B2/en active Active
- 2020-01-23 MX MX2021008884A patent/MX2021008884A/es unknown
- 2020-01-23 KR KR1020217026908A patent/KR20210120039A/ko active Pending
- 2020-01-23 BR BR112021014563-0A patent/BR112021014563A2/pt unknown
- 2020-01-23 US US17/423,600 patent/US12582604B2/en active Active
- 2020-01-23 EP EP20744694.9A patent/EP3914591A4/en active Pending
- 2020-01-23 CA CA3123476A patent/CA3123476A1/en active Pending
- 2020-01-23 SG SG11202107849RA patent/SG11202107849RA/en unknown
- 2020-01-23 WO PCT/CN2020/073944 patent/WO2020151756A1/en not_active Ceased
- 2020-01-23 CN CN202080010548.8A patent/CN113330011A/zh active Pending
- 2020-01-23 JP JP2021542104A patent/JP7591504B2/ja active Active
-
2021
- 2021-06-11 ZA ZA2021/04032A patent/ZA202104032B/en unknown
- 2021-07-06 IL IL284636A patent/IL284636A/en unknown
-
2024
- 2024-11-18 JP JP2024200421A patent/JP2025017374A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| AU2020211000A1 (en) | 2021-08-12 |
| US12582604B2 (en) | 2026-03-24 |
| IL284636A (en) | 2021-08-31 |
| AU2020211000B2 (en) | 2025-11-06 |
| SG11202107849RA (en) | 2021-08-30 |
| US20220105033A1 (en) | 2022-04-07 |
| TW202444718A (zh) | 2024-11-16 |
| MX2021008884A (es) | 2021-08-19 |
| CA3123476A1 (en) | 2020-07-30 |
| JP2025017374A (ja) | 2025-02-05 |
| TW202043225A (zh) | 2020-12-01 |
| CN113330011A (zh) | 2021-08-31 |
| JP7591504B2 (ja) | 2024-11-28 |
| EP3914591A4 (en) | 2022-11-09 |
| JP2022517675A (ja) | 2022-03-09 |
| WO2020151756A1 (en) | 2020-07-30 |
| KR20210120039A (ko) | 2021-10-06 |
| ZA202104032B (en) | 2022-08-31 |
| EP3914591A1 (en) | 2021-12-01 |
| TWI849043B (zh) | 2024-07-21 |
| TWI909513B (zh) | 2025-12-21 |
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