IL252323B - Solid dispersions of 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-n-methylbenzamide (arn-509) and hydroxypropyl methylcellulose acetate succinate (hpmcas) - Google Patents
Solid dispersions of 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-n-methylbenzamide (arn-509) and hydroxypropyl methylcellulose acetate succinate (hpmcas)Info
- Publication number
- IL252323B IL252323B IL252323A IL25232317A IL252323B IL 252323 B IL252323 B IL 252323B IL 252323 A IL252323 A IL 252323A IL 25232317 A IL25232317 A IL 25232317A IL 252323 B IL252323 B IL 252323B
- Authority
- IL
- Israel
- Prior art keywords
- trifluoromethylpyridin
- hpmcas
- diazaspiro
- arn
- methylbenzamide
- Prior art date
Links
- HJBWBFZLDZWPHF-UHFFFAOYSA-N apalutamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1N1C2(CCC2)C(=O)N(C=2C=C(C(C#N)=NC=2)C(F)(F)F)C1=S HJBWBFZLDZWPHF-UHFFFAOYSA-N 0.000 title 2
- 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 title 1
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 title 1
- 239000007962 solid dispersion Substances 0.000 title 1
Classifications
-
- 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
- A61K31/41—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
-
- 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
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
-
- 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
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- 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
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14196594 | 2014-12-05 | ||
| PCT/US2015/063661 WO2016090098A1 (en) | 2014-12-05 | 2015-12-03 | Anticancer compositions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL252323A0 IL252323A0 (en) | 2017-07-31 |
| IL252323B true IL252323B (en) | 2021-04-29 |
Family
ID=52006906
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL252323A IL252323B (en) | 2014-12-05 | 2017-05-16 | Solid dispersions of 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-n-methylbenzamide (arn-509) and hydroxypropyl methylcellulose acetate succinate (hpmcas) |
| IL279833A IL279833B (en) | 2014-12-05 | 2020-12-29 | cyano 5-trifluoromethylpyridine -3- yl(- -8 oxo- (-7[) A combination of a solid dispersion containing -4 methylbenzamide -n - -6 thioxo- -5,7 diazespiro[ 3.4 [oct- -5 yl] 2- Fluoro and hydroxypropyl methylcellulose acetate succinate |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL279833A IL279833B (en) | 2014-12-05 | 2020-12-29 | cyano 5-trifluoromethylpyridine -3- yl(- -8 oxo- (-7[) A combination of a solid dispersion containing -4 methylbenzamide -n - -6 thioxo- -5,7 diazespiro[ 3.4 [oct- -5 yl] 2- Fluoro and hydroxypropyl methylcellulose acetate succinate |
Country Status (29)
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|---|---|
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| EP (2) | EP4494636A3 (enExample) |
| JP (2) | JP6937692B2 (enExample) |
| KR (2) | KR102348320B1 (enExample) |
| CN (2) | CN114886852A (enExample) |
| AR (1) | AR102926A1 (enExample) |
| AU (3) | AU2015358490B2 (enExample) |
| BR (1) | BR112017011788A2 (enExample) |
| CA (1) | CA2969656A1 (enExample) |
| CL (1) | CL2017001371A1 (enExample) |
| CO (1) | CO2017005572A2 (enExample) |
| CR (1) | CR20170216A (enExample) |
| EA (1) | EA201791222A1 (enExample) |
| ES (1) | ES2996833T3 (enExample) |
| HR (1) | HRP20241719T1 (enExample) |
| HU (1) | HUE069689T2 (enExample) |
| IL (2) | IL252323B (enExample) |
| MA (1) | MA41107B1 (enExample) |
| MD (1) | MD3226841T2 (enExample) |
| MX (2) | MX387933B (enExample) |
| NZ (1) | NZ770528A (enExample) |
| PH (1) | PH12017500964A1 (enExample) |
| PL (1) | PL3226841T3 (enExample) |
| RS (1) | RS66323B1 (enExample) |
| SG (1) | SG11201704267VA (enExample) |
| SM (1) | SMT202400518T1 (enExample) |
| TW (2) | TWI702966B (enExample) |
| UA (1) | UA120950C2 (enExample) |
| WO (1) | WO2016090098A1 (enExample) |
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| CN115737643A (zh) | 2012-09-26 | 2023-03-07 | 阿拉贡药品公司 | 用于治疗非转移性去势抵抗性前列腺癌的抗雄激素 |
| US10285948B2 (en) | 2014-12-05 | 2019-05-14 | Janssen Pharmaceutica Nv | Anticancer compositions |
| EA201791222A1 (ru) | 2014-12-05 | 2017-09-29 | Арагон Фармасьютикалз, Инк. | Противораковые композиции |
| MX2020003845A (es) | 2017-10-16 | 2020-11-06 | Aragon Pharmaceuticals Inc | Antiandrógenos para el tratamiento de cáncer de próstata no metastásico resistente a la castración. |
| WO2020144647A1 (en) | 2019-01-10 | 2020-07-16 | Aragon Pharmaceuticals, Inc. | Pharmaceutical composition comprising apalutamide dispersed in apple sauce |
| JP2022523094A (ja) | 2019-01-30 | 2022-04-21 | アラゴン ファーマシューティカルズ，インコーポレイテッド | 転移性去勢感受性前立腺癌の治療のための抗アンドロゲン剤 |
| CN113711316A (zh) | 2019-01-30 | 2021-11-26 | 詹森药业有限公司 | 基于分子亚型治疗前列腺癌的方法 |
| WO2020239478A1 (en) | 2019-05-28 | 2020-12-03 | Pharma Mar, S.A. | Trabectedin for treating sarcomas based on genomic markers |
| EP3811932A1 (en) | 2019-10-22 | 2021-04-28 | Zentiva K.S. | Dosage form of apalutamide |
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| WO2021245285A1 (en) | 2020-06-05 | 2021-12-09 | Janssen Pharmaceutica Nv | Methods of treating prostate cancer based on molecular subtypes |
| TW202228794A (zh) | 2020-09-04 | 2022-08-01 | 美商艾瑞岡醫藥公司 | 用於治療前列腺癌之方法 |
| WO2022195407A1 (en) | 2021-03-19 | 2022-09-22 | Aragon Pharmaceuticals, Inc. | Methods for treating prostate cancer |
| WO2023122842A1 (es) * | 2021-12-31 | 2023-07-06 | Gador Limitada | Proceso para la preparación de apalutamida, intermediarios de sintesis y la dispersion solida amorfa que la contiene |
| WO2023152611A1 (en) | 2022-02-11 | 2023-08-17 | Aragon Pharmaceuticals, Inc. | Apalutamide and relugolix for the treatment of prostate cancer |
| WO2023209555A1 (en) | 2022-04-26 | 2023-11-02 | Aragon Pharmaceuticals, Inc. | Approved drug products and methods for treating prostate cancer |
| CN116183787A (zh) * | 2022-12-26 | 2023-05-30 | 郑州德迈药业有限公司 | 醋酸羟丙甲纤维素琥珀酸酯在阿帕他胺溶出检测中的应用以及检测方法 |
| KR20250157532A (ko) | 2023-03-16 | 2025-11-04 | 바이엘 컨수머 케어 악티엔게젤샤프트 | 호르몬 감수성 전립선암의 생화학적 재발이 있는 환자의 치료를 위한 안드로겐 수용체 길항제 |
| WO2025153768A1 (en) * | 2024-01-18 | 2025-07-24 | Nanoform Finland Oyj | Composition comprising crystalline nanosized apalutamide |
| WO2025174375A1 (en) * | 2024-02-15 | 2025-08-21 | Aragon Pharmaceuticals, Inc. | Anticancer compositions |
| WO2026052846A1 (en) | 2024-09-09 | 2026-03-12 | Synthon B.V. | Pharmaceutical formulation comprising apalutamide |
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| ATE307571T1 (de) | 2001-02-27 | 2005-11-15 | Pharmazeutische formulierung enthaltend bicalutamid | |
| CA2443040A1 (en) | 2001-04-02 | 2002-10-17 | Nicola Frances Bateman | Solid pharmaceutical composition comprising 4 -cyano-trifluoro-3-(4-fluorophenyl-sulphonyl) -2-hydroxy-2-methylpropiono- m toluidide and pvp |
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| EP3811932A1 (en) | 2019-10-22 | 2021-04-28 | Zentiva K.S. | Dosage form of apalutamide |
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2015
- 2015-12-03 EA EA201791222A patent/EA201791222A1/ru unknown
- 2015-12-03 MA MA41107A patent/MA41107B1/fr unknown
- 2015-12-03 KR KR1020177018239A patent/KR102348320B1/ko active Active
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