TWI909513B - 作為ｂ-ｒａｆ激酶二聚體抑制劑之化合物及其製備方法 - Google Patents
作為ｂ-ｒａｆ激酶二聚體抑制劑之化合物及其製備方法Info
- Publication number
- TWI909513B TWI909513B TW113123511A TW113123511A TWI909513B TW I909513 B TWI909513 B TW I909513B TW 113123511 A TW113123511 A TW 113123511A TW 113123511 A TW113123511 A TW 113123511A TW I909513 B TWI909513 B TW I909513B
- Authority
- TW
- Taiwan
- Prior art keywords
- compound
- hpmcas
- mixture
- volumes
- amorphous
- Prior art date
Links
Classifications
-
- 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
- A61K47/30—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
- 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
- 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
- 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
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (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 (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019073254 | 2019-01-25 | ||
| WOPCT/CN2019/073254 | 2019-01-25 | ||
| CN2019095227 | 2019-07-09 | ||
| WOPCT/CN2019/095227 | 2019-07-09 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202444718A TW202444718A (zh) | 2024-11-16 |
| TWI909513B true TWI909513B (zh) | 2025-12-21 |
Family
ID=71735582
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW113123511A TWI909513B (zh) | 2019-01-25 | 2020-01-22 | 作為ｂ-ｒａｆ激酶二聚體抑制劑之化合物及其製備方法 |
| TW109102401A TWI849043B (zh) | 2019-01-25 | 2020-01-22 | 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 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW109102401A TWI849043B (zh) | 2019-01-25 | 2020-01-22 | 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 |
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) | TWI909513B (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 |
| TWI909513B (zh) | 2019-01-25 | 2025-12-21 | 英屬開曼群島商百濟神州有限公司 | 作為ｂ-ｒａｆ激酶二聚體抑制劑之化合物及其製備方法 |
| WO2022146022A1 (ko) * | 2020-12-29 | 2022-07-07 | 주식회사 티씨노바이오사이언스 | 엑토뉴클레오티드 피로포스파타아제-포스포디에스터라아제의 저해 활성을 갖는 신규한 나프티리딘온 유도체 및 이들의 용도 |
| 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 |
| KR20250069903A (ko) * | 2022-09-26 | 2025-05-20 | 맵큐어, 엘엘씨 | 암 치료를 위한 B-Raf 저해제와 항-EGFR 항체의 조합물 |
| 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014206343A1 (en) * | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors |
| WO2014206344A1 (en) * | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US6350786B1 (en) | 1998-09-22 | 2002-02-26 | Hoffmann-La Roche Inc. | Stable complexes of poorly soluble compounds in ionic polymers |
| ES2306646T3 (es) | 1999-02-09 | 2008-11-16 | Pfizer Products Inc. | Composiciones de farmacos basicos con biodisponibilidad incrementada. |
| 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 |
| CA2550361C (en) | 2003-12-19 | 2014-04-29 | Prabha Ibrahim | Compounds and methods for development of ret modulators |
| US7618964B2 (en) | 2004-12-23 | 2009-11-17 | Hoffmann-La Roche Inc. | Benzamide derivatives, their manufacture and use as pharmaceutical agents |
| CN101365682A (zh) | 2005-12-08 | 2009-02-11 | 千禧药品公司 | 具有激酶抑制活性的双环化合物 |
| ATE552245T1 (de) | 2006-05-15 | 2012-04-15 | Merck Sharp & Dohme | Antidiabetische bicyclische verbindungen |
| JP2010502660A (ja) | 2006-09-06 | 2010-01-28 | エフ．ホフマン−ラ ロシュ アーゲー | プロテインキナーゼインヒビターとしてのヘテロアリール誘導体 |
| PE20081581A1 (es) | 2006-12-21 | 2008-11-12 | Plexxikon Inc | COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA |
| WO2008079909A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
| CN101702878B (zh) | 2007-05-11 | 2012-11-28 | 弗·哈夫曼-拉罗切有限公司 | 可溶性差的药物的药物组合物 |
| JP2010533729A (ja) | 2007-07-17 | 2010-10-28 | プレキシコン，インコーポレーテッド | キナーゼ調節のための化合物と方法、及びそのための適応 |
| SI2947072T1 (sl) * | 2008-03-17 | 2017-03-31 | Ambit Biosciences Corporation | 1-(3-(6,7-dimetoksikinazolin-4-iloksi)fenil)-3-(5-1,1,1-trifluoro-2- metilpropan-2-il)izoksazol-3-il)urea kot modulator raf kinaze pri zdravljenju rakavih bolezni |
| 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 |
| KR101739994B1 (ko) * | 2009-04-03 | 2017-05-25 | 에프. 호프만-라 로슈 아게 | 프로판-１-술폰산 ｛３-［５-（４-클로로-페닐）-１Ｈ-피롤로［２，３-ｂ］피리딘-３-카르보닐］-２，４-디플루오로-페닐｝-아미드 조성물 및 그의 용도 |
| US20120157453A1 (en) * | 2009-08-28 | 2012-06-21 | Genentech, Inc. | Raf inhibitor compounds and methods of use thereof |
| WO2011092088A1 (en) | 2010-01-27 | 2011-08-04 | Nerviano Medical Sciences S.R.L. | Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors |
| WO2011115069A1 (ja) | 2010-03-19 | 2011-09-22 | 第一三共株式会社 | 結晶の網羅的探索 |
| KR101911972B1 (ko) * | 2011-02-07 | 2018-10-25 | 플렉시콘 인코퍼레이티드 | 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증 |
| US9273046B2 (en) | 2011-12-31 | 2016-03-01 | Beigene, Ltd. | Fused tricyclic compounds as Raf kinase inhibitors |
| TR201904980T4 (tr) * | 2012-08-07 | 2019-05-21 | Novartis Ag | Bir B-Raf inhibitörü, bir EGFR inhibitörü ve isteğe bağlı olarak bir PI3K-alfa inhibitörü içeren farmasötik kombinasyonlar. |
| CN112353762A (zh) * | 2013-01-22 | 2021-02-12 | 霍夫曼-拉罗奇有限公司 | 具有改善的生物利用度的药物组合物 |
| 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 |
| 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 |
| TWI909513B (zh) | 2019-01-25 | 2025-12-21 | 英屬開曼群島商百濟神州有限公司 | 作為ｂ-ｒａｆ激酶二聚體抑制劑之化合物及其製備方法 |
-
2020
- 2020-01-22 TW TW113123511A patent/TWI909513B/zh active
- 2020-01-22 TW TW109102401A patent/TWI849043B/zh active
- 2020-01-23 SG SG11202107849RA patent/SG11202107849RA/en unknown
- 2020-01-23 MX MX2021008884A patent/MX2021008884A/es unknown
- 2020-01-23 JP JP2021542104A patent/JP7591504B2/ja active Active
- 2020-01-23 EP EP20744694.9A patent/EP3914591A4/en active Pending
- 2020-01-23 US US17/423,600 patent/US12582604B2/en active Active
- 2020-01-23 KR KR1020217026908A patent/KR20210120039A/ko active Pending
- 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 CA CA3123476A patent/CA3123476A1/en active Pending
- 2020-01-23 AU AU2020211000A patent/AU2020211000B2/en active Active
- 2020-01-23 BR BR112021014563-0A patent/BR112021014563A2/pt unknown
-
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
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014206343A1 (en) * | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors |
| WO2014206344A1 (en) * | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| US12582604B2 (en) | 2026-03-24 |
| BR112021014563A2 (pt) | 2021-10-05 |
| JP7591504B2 (ja) | 2024-11-28 |
| ZA202104032B (en) | 2022-08-31 |
| EP3914591A1 (en) | 2021-12-01 |
| IL284636A (en) | 2021-08-31 |
| SG11202107849RA (en) | 2021-08-30 |
| CA3123476A1 (en) | 2020-07-30 |
| EP3914591A4 (en) | 2022-11-09 |
| TWI849043B (zh) | 2024-07-21 |
| CN113330011A (zh) | 2021-08-31 |
| WO2020151756A1 (en) | 2020-07-30 |
| MX2021008884A (es) | 2021-08-19 |
| US20220105033A1 (en) | 2022-04-07 |
| TW202444718A (zh) | 2024-11-16 |
| KR20210120039A (ko) | 2021-10-06 |
| AU2020211000A1 (en) | 2021-08-12 |
| JP2025017374A (ja) | 2025-02-05 |
| TW202043225A (zh) | 2020-12-01 |
| JP2022517675A (ja) | 2022-03-09 |
| AU2020211000B2 (en) | 2025-11-06 |
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