JPWO2020151756A5 - - Google Patents
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- Publication number
- JPWO2020151756A5 JPWO2020151756A5 JP2021542104A JP2021542104A JPWO2020151756A5 JP WO2020151756 A5 JPWO2020151756 A5 JP WO2020151756A5 JP 2021542104 A JP2021542104 A JP 2021542104A JP 2021542104 A JP2021542104 A JP 2021542104A JP WO2020151756 A5 JPWO2020151756 A5 JP WO2020151756A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- hpmcas
- cancer
- aryl
- heterocyclyl
- 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.)
- Granted
Links
- 229940125904 compound 1 Drugs 0.000 claims 33
- 125000003118 aryl group Chemical group 0.000 claims 19
- 239000012458 free base Substances 0.000 claims 19
- 125000000623 heterocyclic group Chemical group 0.000 claims 19
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims 12
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 125000000304 alkynyl group Chemical group 0.000 claims 10
- 239000007962 solid dispersion Substances 0.000 claims 9
- 229920000642 polymer Polymers 0.000 claims 7
- 238000000634 powder X-ray diffraction Methods 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 239000013078 crystal Substances 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 239000007787 solid Substances 0.000 claims 5
- 230000000087 stabilizing effect Effects 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 239000006185 dispersion Substances 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 201000005188 adrenal gland cancer Diseases 0.000 claims 2
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000009477 glass transition Effects 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 239000011159 matrix material Substances 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 201000008968 osteosarcoma Diseases 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 208000013076 thyroid tumor Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 102100039788 GTPase NRas Human genes 0.000 claims 1
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 claims 1
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims 1
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 239000007864 aqueous solution Substances 0.000 claims 1
- -1 carbamoyl compound Chemical class 0.000 claims 1
- 239000002131 composite material Substances 0.000 claims 1
- 238000006482 condensation reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 239000002244 precipitate Substances 0.000 claims 1
- 238000001556 precipitation Methods 0.000 claims 1
- 108010077182 raf Kinases Proteins 0.000 claims 1
- 102000009929 raf Kinases Human genes 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 238000005406 washing Methods 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024200421A JP2025017374A (ja) | 2019-01-25 | 2024-11-18 | Ｂ－ｒａｆキナーゼ二量体阻害剤の安定な固体分散体、その調製方法及び使用 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019073254 | 2019-01-25 | ||
| CNPCT/CN2019/073254 | 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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024200421A Division JP2025017374A (ja) | 2019-01-25 | 2024-11-18 | Ｂ－ｒａｆキナーゼ二量体阻害剤の安定な固体分散体、その調製方法及び使用 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022517675A JP2022517675A (ja) | 2022-03-09 |
| JPWO2020151756A5 true JPWO2020151756A5 (https=) | 2023-01-27 |
| JP2022517675A5 JP2022517675A5 (https=) | 2023-01-27 |
| JP7591504B2 JP7591504B2 (ja) | 2024-11-28 |
Family
ID=71735582
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021542104A Active JP7591504B2 (ja) | 2019-01-25 | 2020-01-23 | Ｂ－ｒａｆキナーゼ二量体阻害剤の安定な固体分散体、その調製方法及び使用 |
| JP2024200421A Pending JP2025017374A (ja) | 2019-01-25 | 2024-11-18 | Ｂ－ｒａｆキナーゼ二量体阻害剤の安定な固体分散体、その調製方法及び使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024200421A Pending JP2025017374A (ja) | 2019-01-25 | 2024-11-18 | Ｂ－ｒａｆキナーゼ二量体阻害剤の安定な固体分散体、その調製方法及び使用 |
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 |
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 |
| 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 |
| US9670231B2 (en) * | 2013-06-28 | 2017-06-06 | Beigene, Ltd. | Fused tricyclic amide compounds as multiple kinase inhibitors |
| US9670203B2 (en) | 2013-06-28 | 2017-06-06 | Beigene, Ltd. | Fused tricyclic urea compounds as Raf kinase and/or Raf kinase dimer inhibitors |
| 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
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