CA2981746C - Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore - Google Patents
Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore Download PDFInfo
- Publication number
- CA2981746C CA2981746C CA2981746A CA2981746A CA2981746C CA 2981746 C CA2981746 C CA 2981746C CA 2981746 A CA2981746 A CA 2981746A CA 2981746 A CA2981746 A CA 2981746A CA 2981746 C CA2981746 C CA 2981746C
- Authority
- CA
- Canada
- Prior art keywords
- crystalline form
- compound
- dihydro
- maleate
- cancer
- 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.)
- Active
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
- A61K31/41—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
-
- 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
- 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
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2015076639 | 2015-04-15 | ||
| CNPCT/CN2015/076639 | 2015-04-15 | ||
| PCT/CN2016/079251 WO2016165626A1 (en) | 2015-04-15 | 2016-04-14 | Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2981746A1 CA2981746A1 (en) | 2016-10-20 |
| CA2981746C true CA2981746C (en) | 2023-08-01 |
Family
ID=57125563
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2981746A Active CA2981746C (en) | 2015-04-15 | 2016-04-14 | Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10351559B2 (enExample) |
| EP (2) | EP3283486B1 (enExample) |
| JP (3) | JP7320741B2 (enExample) |
| KR (2) | KR20240049684A (enExample) |
| CN (2) | CN107531682B (enExample) |
| AU (1) | AU2016248376B2 (enExample) |
| CA (1) | CA2981746C (enExample) |
| EA (1) | EA035680B1 (enExample) |
| IL (2) | IL255555B (enExample) |
| MX (1) | MX381053B (enExample) |
| NZ (1) | NZ735715A (enExample) |
| SG (1) | SG11201707984TA (enExample) |
| TW (4) | TWI792406B (enExample) |
| WO (1) | WO2016165626A1 (enExample) |
| ZA (1) | ZA201706392B (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2609659C (en) | 2005-05-26 | 2014-01-28 | Neuron Systems, Inc. | Azanaphthalenes, compositions and methods for treating retinal disease |
| CA2782015C (en) | 2009-12-11 | 2020-08-25 | Neuron Systems, Inc. | Topical ophthalmic compositions and methods for the treatment of macular degeneration |
| CN103596926B (zh) | 2011-12-31 | 2015-11-25 | 百济神州有限公司 | 作为raf激酶抑制剂的稠合三环化合物 |
| AU2014209387B2 (en) | 2013-01-23 | 2018-11-01 | Aldeyra Therapeutics, Inc. | Toxic aldehyde related diseases and treatment |
| EP3283486B1 (en) | 2015-04-15 | 2022-07-27 | BeiGene, Ltd. | Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore |
| EP4400106A1 (en) | 2015-08-21 | 2024-07-17 | Aldeyra Therapeutics, Inc. | Deuterated compounds and uses thereof |
| AU2017293423B2 (en) | 2016-07-05 | 2023-05-25 | Beone Medicines I Gmbh | Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer |
| DK3618875T3 (da) | 2017-05-02 | 2023-07-10 | Novartis Ag | Kombinationsterapi omfattende en raf-inhibitor og trametinib |
| WO2019075136A1 (en) | 2017-10-10 | 2019-04-18 | Aldeyra Therapeutics, Inc. | TREATMENT OF INFLAMMATORY DISORDERS |
| US12006298B2 (en) | 2018-08-06 | 2024-06-11 | Aldeyra Therapeutics, Inc. | Polymorphic compounds and uses thereof |
| MY202547A (en) * | 2018-10-31 | 2024-05-07 | Servier Lab | Novel salt of a bcl-2 inhibitor, related crystalline form, method for preparing the same and pharmaceutical compositions containing the same |
| CN116715662A (zh) * | 2019-01-25 | 2023-09-08 | 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 |
| 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 |
| MX2021010829A (es) * | 2019-03-15 | 2021-12-10 | Forma Therapeutics Inc | Inhibición de la proteína de unión al elemento de respuesta a adenosín monofosfato (amp) cíclica (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 |
| KR102881316B1 (ko) | 2019-05-13 | 2025-11-05 | 노파르티스 아게 | 암 치료를 위한 raf 억제제로서의 n-(3-(2-(2-하이드록시에톡시)-6-모르폴리노피리딘-4-일)-4-메틸페닐)-2 (트리플루오로메틸)이소니코틴아미드의 새로운 결정질 형태 |
| 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 |
| PE20231211A1 (es) * | 2020-04-03 | 2023-08-17 | Springworks Therapeutics Inc | Administracion conjunta de mirdametinib y lifirafenib para uso en el tratamiento de canceres |
| CA3175856A1 (en) | 2020-05-13 | 2021-11-18 | Todd Brady | Pharmaceutical formulations and uses thereof |
| JP2025519981A (ja) * | 2022-06-08 | 2025-06-30 | マップキュア，エルエルシー | Ｂ－ｒａｆ阻害剤によるがんの治療方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006065703A1 (en) | 2004-12-13 | 2006-06-22 | Sunesis 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 |
| EP2021327B1 (en) | 2006-05-15 | 2012-04-04 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| WO2008023239A1 (en) | 2006-08-23 | 2008-02-28 | Pfizer Products Inc. | Pyrimidone compounds as gsk-3 inhibitors |
| WO2008030448A1 (en) | 2006-09-07 | 2008-03-13 | Millennium Pharmaceuticals, Inc. | Phenethylamide derivatives with kinase inhibitory activity |
| AU2008247500A1 (en) | 2007-05-04 | 2008-11-13 | Irm Llc | Compounds and compositions as c-kit and PDGFR kinase inhibitors |
| US20100197924A1 (en) | 2008-12-22 | 2010-08-05 | Millennium Pharmaceuticals, Inc. | Preparation of aminotetralin compounds |
| JP5808818B2 (ja) * | 2010-11-25 | 2015-11-10 | ラツィオファーム・ゲーエムベーハー | アファチニブの新規塩及び多形形態 |
| CN103596926B (zh) | 2011-12-31 | 2015-11-25 | 百济神州有限公司 | 作为raf激酶抑制剂的稠合三环化合物 |
| EP3283486B1 (en) | 2015-04-15 | 2022-07-27 | BeiGene, Ltd. | Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore |
-
2016
- 2016-04-14 EP EP16779601.0A patent/EP3283486B1/en active Active
- 2016-04-14 TW TW110125410A patent/TWI792406B/zh active
- 2016-04-14 US US15/565,807 patent/US10351559B2/en active Active
- 2016-04-14 MX MX2017013219A patent/MX381053B/es unknown
- 2016-04-14 SG SG11201707984TA patent/SG11201707984TA/en unknown
- 2016-04-14 NZ NZ735715A patent/NZ735715A/en unknown
- 2016-04-14 AU AU2016248376A patent/AU2016248376B2/en active Active
- 2016-04-14 CA CA2981746A patent/CA2981746C/en active Active
- 2016-04-14 CN CN201680021109.0A patent/CN107531682B/zh active Active
- 2016-04-14 CN CN202110419671.1A patent/CN113307805A/zh active Pending
- 2016-04-14 TW TW105111715A patent/TWI736531B/zh active
- 2016-04-14 KR KR1020247006890A patent/KR20240049684A/ko active Pending
- 2016-04-14 TW TW112101259A patent/TWI832668B/zh active
- 2016-04-14 EA EA201792254A patent/EA035680B1/ru unknown
- 2016-04-14 KR KR1020177033101A patent/KR102643609B1/ko active Active
- 2016-04-14 EP EP22179294.8A patent/EP4119559A1/en active Pending
- 2016-04-14 JP JP2017553956A patent/JP7320741B2/ja active Active
- 2016-04-14 WO PCT/CN2016/079251 patent/WO2016165626A1/en not_active Ceased
- 2016-04-14 TW TW113101605A patent/TWI876835B/zh active
-
2017
- 2017-09-21 ZA ZA2017/06392A patent/ZA201706392B/en unknown
- 2017-11-09 IL IL255555A patent/IL255555B/en unknown
-
2021
- 2021-01-22 JP JP2021009106A patent/JP7383652B2/ja active Active
- 2021-10-31 IL IL287740A patent/IL287740B2/en unknown
-
2023
- 2023-11-08 JP JP2023190552A patent/JP2024012540A/ja not_active Withdrawn
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20210225 |
|
| EEER | Examination request |
Effective date: 20210225 |
|
| EEER | Examination request |
Effective date: 20210225 |
|
| EEER | Examination request |
Effective date: 20210225 |
|
| EEER | Examination request |
Effective date: 20210225 |
|
| EEER | Examination request |
Effective date: 20210225 |