TWI792406B - B-raf激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途 - Google Patents
B-raf激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途 Download PDFInfo
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- TWI792406B TWI792406B TW110125410A TW110125410A TWI792406B TW I792406 B TWI792406 B TW I792406B TW 110125410 A TW110125410 A TW 110125410A TW 110125410 A TW110125410 A TW 110125410A TW I792406 B TWI792406 B TW I792406B
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- sesquimaleate
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- 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
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
- A61K31/558—Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes
- A61K31/5585—Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes having five-membered rings containing oxygen as the only ring hetero atom, e.g. prostacyclin
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/42—Separation; Purification; Stabilisation; Use of additives
- C07C51/43—Separation; Purification; Stabilisation; Use of additives by change of the physical state, e.g. crystallisation
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/145—Maleic acid
-
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| WOPCT/CN2015/076639 | 2015-04-15 | ||
| CN2015076639 | 2015-04-15 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202138370A TW202138370A (zh) | 2021-10-16 |
| TWI792406B true TWI792406B (zh) | 2023-02-11 |
Family
ID=57125563
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW110125410A TWI792406B (zh) | 2015-04-15 | 2016-04-14 | B-raf激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途 |
| TW105111715A TWI736531B (zh) | 2015-04-15 | 2016-04-14 | B-raf 激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途 |
| TW113101605A TWI876835B (zh) | 2015-04-15 | 2016-04-14 | B-raf激酶抑制劑的馬來酸鹽、其結晶形式及用途 |
| TW112101259A TWI832668B (zh) | 2015-04-15 | 2016-04-14 | Ｂ-ｒａｆ激酶抑制劑的無定形形式、鹽酸鹽、甲磺酸鹽、２-羥基乙磺酸鹽、ｌ-酒石酸鹽或草酸鹽及其用途 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW105111715A TWI736531B (zh) | 2015-04-15 | 2016-04-14 | B-raf 激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途 |
| TW113101605A TWI876835B (zh) | 2015-04-15 | 2016-04-14 | B-raf激酶抑制劑的馬來酸鹽、其結晶形式及用途 |
| TW112101259A TWI832668B (zh) | 2015-04-15 | 2016-04-14 | Ｂ-ｒａｆ激酶抑制劑的無定形形式、鹽酸鹽、甲磺酸鹽、２-羥基乙磺酸鹽、ｌ-酒石酸鹽或草酸鹽及其用途 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10351559B2 (https=) |
| EP (2) | EP3283486B1 (https=) |
| JP (3) | JP7320741B2 (https=) |
| KR (2) | KR102643609B1 (https=) |
| CN (2) | CN113307805A (https=) |
| AU (1) | AU2016248376B2 (https=) |
| CA (1) | CA2981746C (https=) |
| EA (1) | EA035680B1 (https=) |
| IL (2) | IL287740B2 (https=) |
| MX (1) | MX381053B (https=) |
| NZ (1) | NZ735715A (https=) |
| SG (1) | SG11201707984TA (https=) |
| TW (4) | TWI792406B (https=) |
| WO (1) | WO2016165626A1 (https=) |
| ZA (1) | ZA201706392B (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1888548E (pt) | 2005-05-26 | 2012-10-30 | Neuron Systems Inc | Derivado de quinolina para o tratamento de doenças da retina |
| WO2011072141A1 (en) | 2009-12-11 | 2011-06-16 | Neuron Systems, Inc. | Compositions and methods for the treatment of macular degeneration |
| US9273046B2 (en) | 2011-12-31 | 2016-03-01 | Beigene, Ltd. | Fused tricyclic compounds as Raf kinase inhibitors |
| CA2898631C (en) | 2013-01-23 | 2023-06-13 | Aldeyra Therapeutics, Inc. | Toxic aldehyde related diseases and treatment |
| NZ735715A (en) * | 2015-04-15 | 2022-09-30 | Beigene Ltd | Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore |
| CN118724806A (zh) | 2015-08-21 | 2024-10-01 | 奥尔德拉医疗公司 | 氘化化合物和其用途 |
| US10864203B2 (en) | 2016-07-05 | 2020-12-15 | Beigene, Ltd. | Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer |
| ES2952265T3 (es) | 2017-05-02 | 2023-10-30 | Novartis Ag | Terapia combinada que comprende un inhibidor de Raf y trametinib |
| JP7311162B2 (ja) | 2017-10-10 | 2023-07-19 | アルデイラ セラピューティクス， インコーポレイテッド | 炎症性障害の処置 |
| WO2020033344A1 (en) * | 2018-08-06 | 2020-02-13 | Aldeyra Therapeutics, Inc. | Polymorphic compounds and uses thereof |
| HUE062000T2 (hu) * | 2018-10-31 | 2023-09-28 | Servier Lab | BCL-2 inhibitor új sója, vonatkozó kristályforma, ezek elõállítási eljárása és ezeket tartalmazó gyógyszerkészítmények |
| CN111484488A (zh) * | 2019-01-25 | 2020-08-04 | 百济神州(北京)生物科技有限公司 | 一种b-raf激酶二聚体抑制剂的稳定结晶形式a |
| CN111484489B (zh) * | 2019-01-25 | 2023-05-23 | 百济神州(北京)生物科技有限公司 | 无定形的b-raf激酶二聚体抑制剂 |
| EP3937936A4 (en) * | 2019-03-15 | 2022-12-28 | Forma Therapeutics, Inc. | INHIBITION OF CYCLIC AMP-RESPONSIVE ELEMENT-BINDING PROTEIN (CREB) |
| US12098132B2 (en) | 2019-05-02 | 2024-09-24 | Aldeyra Therapeutics, Inc. | Process for preparation of aldehyde scavenger and intermediates |
| CN113784954A (zh) | 2019-05-02 | 2021-12-10 | 奥尔德拉医疗公司 | 多晶型化合物和其用途 |
| ES3025633T3 (en) | 2019-05-13 | 2025-06-09 | Novartis Ag | 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 |
| CN111184693B (zh) * | 2019-05-29 | 2023-07-21 | 百济神州(苏州)生物科技有限公司 | 一种raf激酶抑制剂制剂及其制备方法 |
| US20230128315A1 (en) * | 2020-04-03 | 2023-04-27 | Beigene, Ltd. | Co-administration of mirdametinib and lifirafenib for use in treating cancers |
| CA3175856A1 (en) | 2020-05-13 | 2021-11-18 | Todd Brady | Pharmaceutical formulations and uses thereof |
| WO2023240178A1 (en) * | 2022-06-08 | 2023-12-14 | Mapkure, Llc | Methods of treating cancer with a b-raf inhibitor |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103596926A (zh) * | 2011-12-31 | 2014-02-19 | 百济神州有限公司 | 作为raf激酶抑制剂的稠合三环化合物 |
| TWI736531B (zh) * | 2015-04-15 | 2021-08-21 | 英屬開曼群島商百濟神州有限公司 | B-raf 激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005316668B2 (en) | 2004-12-13 | 2012-09-06 | Millennium Pharmaceuticals, Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors |
| TW200639163A (en) | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
| 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 |
| US20100292205A1 (en) | 2006-08-23 | 2010-11-18 | Pfizer Inc. | Pyrimidone Compounds As GSK-3 Inhibitors |
| EP2061761A1 (en) | 2006-09-07 | 2009-05-27 | Millennium Pharmaceuticals, Inc. | Phenethylamide derivatives with kinase inhibitory activity |
| EA016329B1 (ru) | 2007-05-04 | 2012-04-30 | Айрм Ллк | СОЕДИНЕНИЯ И КОМПОЗИЦИИ, КАК ИНГИБИТОРЫ КИНАЗЫ c-KIT И PDGFR |
| US20100197924A1 (en) | 2008-12-22 | 2010-08-05 | Millennium Pharmaceuticals, Inc. | Preparation of aminotetralin compounds |
| CN103476770B (zh) * | 2010-11-25 | 2017-02-15 | 拉蒂欧制药有限责任公司 | 阿法替尼盐和多晶型物 |
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2016
- 2016-04-14 NZ NZ735715A patent/NZ735715A/en unknown
- 2016-04-14 IL IL287740A patent/IL287740B2/en unknown
- 2016-04-14 TW TW110125410A patent/TWI792406B/zh active
- 2016-04-14 MX MX2017013219A patent/MX381053B/es unknown
- 2016-04-14 WO PCT/CN2016/079251 patent/WO2016165626A1/en not_active Ceased
- 2016-04-14 EP EP16779601.0A patent/EP3283486B1/en active Active
- 2016-04-14 KR KR1020177033101A patent/KR102643609B1/ko active Active
- 2016-04-14 CN CN202110419671.1A patent/CN113307805A/zh active Pending
- 2016-04-14 JP JP2017553956A patent/JP7320741B2/ja active Active
- 2016-04-14 US US15/565,807 patent/US10351559B2/en active Active
- 2016-04-14 TW TW105111715A patent/TWI736531B/zh active
- 2016-04-14 CN CN201680021109.0A patent/CN107531682B/zh active Active
- 2016-04-14 KR KR1020247006890A patent/KR20240049684A/ko active Pending
- 2016-04-14 EA EA201792254A patent/EA035680B1/ru unknown
- 2016-04-14 AU AU2016248376A patent/AU2016248376B2/en active Active
- 2016-04-14 EP EP22179294.8A patent/EP4119559A1/en active Pending
- 2016-04-14 TW TW113101605A patent/TWI876835B/zh active
- 2016-04-14 CA CA2981746A patent/CA2981746C/en active Active
- 2016-04-14 TW TW112101259A patent/TWI832668B/zh active
- 2016-04-14 SG SG11201707984TA patent/SG11201707984TA/en unknown
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2017
- 2017-09-21 ZA ZA2017/06392A patent/ZA201706392B/en unknown
- 2017-11-09 IL IL255555A patent/IL255555B/en unknown
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2021
- 2021-01-22 JP JP2021009106A patent/JP7383652B2/ja active Active
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2023
- 2023-11-08 JP JP2023190552A patent/JP2024012540A/ja not_active Withdrawn
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103596926A (zh) * | 2011-12-31 | 2014-02-19 | 百济神州有限公司 | 作为raf激酶抑制剂的稠合三环化合物 |
| TWI736531B (zh) * | 2015-04-15 | 2021-08-21 | 英屬開曼群島商百濟神州有限公司 | B-raf 激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途 |
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