EA201691568A1 - Твердые фармацевтические композиции антагонистов рецепторов андрогенов - Google Patents

Твердые фармацевтические композиции антагонистов рецепторов андрогенов

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Publication number
EA201691568A1
EA201691568A1 EA201691568A EA201691568A EA201691568A1 EA 201691568 A1 EA201691568 A1 EA 201691568A1 EA 201691568 A EA201691568 A EA 201691568A EA 201691568 A EA201691568 A EA 201691568A EA 201691568 A1 EA201691568 A1 EA 201691568A1
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EA
Eurasian Patent Office
Prior art keywords
pharmaceutical compositions
solid pharmaceutical
antagonists
androgen receptors
present
Prior art date
Application number
EA201691568A
Other languages
English (en)
Other versions
EA037895B1 (ru
Inventor
Рок Грахек
Андрия Лебар
Петра Дракслер
Бостьян Петек
Йернея Опара
Клемен Наверсник
Петра Божич
Original Assignee
Лек Фармасьютикалз Д.Д.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Лек Фармасьютикалз Д.Д. filed Critical Лек Фармасьютикалз Д.Д.
Publication of EA201691568A1 publication Critical patent/EA201691568A1/ru
Publication of EA037895B1 publication Critical patent/EA037895B1/ru

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    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
    • 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
    • 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
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • 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
    • A61K9/10—Dispersions; Emulsions
    • 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
    • A61K9/143—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 inorganic compounds
    • 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
    • A61K9/1611—Inorganic compounds
    • 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
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • A61K9/4825—Proteins, e.g. gelatin
    • 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
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (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)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Dispersion Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Настоящее изобретение принадлежит к области фармацевтической промышленности и относится к твердым фармацевтическим композициям, включающим антагонисты рецепторов андрогена, например энзалутамид или ARN-509, а также к способам получения этих композиций. Твердые фармацевтические композиции по настоящему изобретению применимы в лечении рака простаты.
EA201691568A 2014-02-05 2015-02-04 Твердые фармацевтические композиции антагонистов рецепторов андрогенов EA037895B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14154047 2014-02-05
PCT/EP2015/052311 WO2015118015A1 (en) 2014-02-05 2015-02-04 Solid pharmaceutical compositions of androgen receptor antagonists

Publications (2)

Publication Number Publication Date
EA201691568A1 true EA201691568A1 (ru) 2017-01-30
EA037895B1 EA037895B1 (ru) 2021-06-02

Family

ID=50031275

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201891397A EA201891397A1 (ru) 2014-02-05 2015-02-04 Твердые фармацевтические композиции антагонистов рецепторов андрогенов
EA201691568A EA037895B1 (ru) 2014-02-05 2015-02-04 Твердые фармацевтические композиции антагонистов рецепторов андрогенов

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Country Status (10)

Country Link
US (2) US20160346207A1 (ru)
EP (1) EP3102183A1 (ru)
JP (2) JP6666254B2 (ru)
KR (2) KR20160113294A (ru)
CN (2) CN112402360A (ru)
AU (1) AU2015215000B2 (ru)
CA (1) CA2940984A1 (ru)
EA (2) EA201891397A1 (ru)
MX (1) MX2016010216A (ru)
WO (1) WO2015118015A1 (ru)

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EA201791251A1 (ru) * 2014-12-05 2017-11-30 Арагон Фармасьютикалз, Инк. Противораковые композиции
EP3226842B1 (en) * 2014-12-05 2020-11-25 Aragon Pharmaceuticals, Inc. Anticancer compositions
MA41107A (fr) * 2014-12-05 2017-10-10 Aragon Pharmaceuticals Inc Compositions anti-cancéreuses
AU2017275396A1 (en) * 2016-06-03 2018-11-22 Aragon Pharmaceuticals, Inc. Anticancer compositions
WO2017221144A1 (en) * 2016-06-20 2017-12-28 Dr. Reddy's Laboratories Limited Process for the preparation of elagolix sodium and its polymorph
WO2018009678A1 (en) * 2016-07-08 2018-01-11 Janssen Pharmaceutica Nv Substituted hydantoin and thiohydantoin derivatives as androgen receptor antagonists
US20190209469A1 (en) * 2016-08-20 2019-07-11 Ftf Pharma Private Limited Pharmaceutical composition comprising an androgen receptor inhibitor
RU2019138248A (ru) * 2017-04-28 2021-05-28 Астеллас Фарма Инк. Фармацевтическая композиция для перорального введения, содержащая энзалутамид
RU2020105102A (ru) * 2017-07-04 2021-08-04 Бдр Фармасьютикалз Интернэшнл Прайвит Лимитед Новая композиция пероральной лекарственной формы энзалутамида и способ ее получения
WO2019016747A1 (en) * 2017-07-20 2019-01-24 Dr. Reddy's Laboratories Limited AMORPHOUS SOLID DISPERSIONS OF APALUTAMIDE AND PROCESS FOR THEIR PREPARATION
RU2020109948A (ru) * 2017-08-08 2021-09-10 Др. Редди'З Лабораториз Лимитед Экструдированные композиции энзалутамида
CZ2018234A3 (cs) 2018-05-21 2019-12-04 Zentiva Ks Zvýšení rozpustnosti a biodostupnosti enzalutamidu
CN108815129A (zh) * 2018-07-12 2018-11-16 天津双硕医药科技有限公司 一种恩杂鲁胺纳米晶体口服固体药物组合物
LT3886820T (lt) 2018-11-30 2023-06-12 Chemocentryx, Inc. Kapsulės vaisto formos
US20220249388A1 (en) * 2019-05-23 2022-08-11 Helm Ag Nanoparticles comprising enzalutamide
EP4037659A1 (en) 2019-10-03 2022-08-10 Synthon BV Pharmaceutical composition comprising enzalutamide
EP3811932A1 (en) 2019-10-22 2021-04-28 Zentiva K.S. Dosage form of apalutamide
US20240207239A1 (en) * 2021-02-06 2024-06-27 Sunshine Lake Pharma Co., Ltd. Composition and preparation method therefor
WO2024127361A1 (en) * 2022-12-16 2024-06-20 Ferring B.V. Enzalutamide nanocrystals, methods and compositions

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Publication number Priority date Publication date Assignee Title
OA12625A (en) * 2001-06-22 2006-06-12 Pfizer Prod Inc Pharmaceutical compositions of adsorbates of amorphous drug.
MX2008012492A (es) * 2006-03-29 2008-12-12 Univ California Compuestos de diariltiohidantoina.
DK3124481T3 (en) * 2010-02-16 2018-05-07 Aragon Pharmaceuticals Inc ANDROGEN RECEPTOR MODULATORS AND APPLICATIONS THEREOF
JP6297556B2 (ja) * 2012-07-27 2018-03-20 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 アンドロゲン受容体治療に対する抵抗性を判定する方法及び組成物
LT3725778T (lt) * 2012-09-11 2021-12-27 Medivation Prostate Therapeutics Llc Enzalutamido kompozicijos

Also Published As

Publication number Publication date
US20200163882A1 (en) 2020-05-28
EA201891397A1 (ru) 2019-03-29
AU2015215000A1 (en) 2016-09-15
EA037895B1 (ru) 2021-06-02
US20160346207A1 (en) 2016-12-01
AU2015215000B2 (en) 2017-10-19
CN106102716A (zh) 2016-11-09
WO2015118015A1 (en) 2015-08-13
JP6666254B2 (ja) 2020-03-13
EP3102183A1 (en) 2016-12-14
KR20160113294A (ko) 2016-09-28
JP6934932B2 (ja) 2021-09-15
KR20200015830A (ko) 2020-02-12
CN112402360A (zh) 2021-02-26
CA2940984A1 (en) 2015-08-13
MX2016010216A (es) 2016-11-15
JP2017507928A (ja) 2017-03-23
JP2020090505A (ja) 2020-06-11

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