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EA201591276A1 - Фармацевтическая композиция с улучшенной биодоступностью - Google Patents

Фармацевтическая композиция с улучшенной биодоступностью

Info

Publication number
EA201591276A1
EA201591276A1 EA201591276A EA201591276A EA201591276A1 EA 201591276 A1 EA201591276 A1 EA 201591276A1 EA 201591276 A EA201591276 A EA 201591276A EA 201591276 A EA201591276 A EA 201591276A EA 201591276 A1 EA201591276 A1 EA 201591276A1
Authority
EA
Eurasian Patent Office
Prior art keywords
improved bioavailability
pharmaceutical composition
fluorophenyl
chloro
compounds
Prior art date
Application number
EA201591276A
Other languages
English (en)
Other versions
EA028009B1 (ru
Inventor
Стив Ломуссио
Хуа Ма
Майкл Аллен Мэтчетт
Харпреет К. Сэндху
Навнит Харговиндас Шах
Ю-Э Чжан
Original Assignee
Ф. Хоффманн-Ля Рош Аг
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50023547&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201591276(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Publication of EA201591276A1 publication Critical patent/EA201591276A1/ru
Publication of EA028009B1 publication Critical patent/EA028009B1/ru

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate 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
    • A61K9/146Intimate 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/284Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2813Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/282Organic compounds, e.g. fats

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dispersion Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Изобретение относится к твердым дисперсиям слаборастворимых в воде соединений, в частности 4-{[(2R,3S,4R,5S)-4-(4-хлор-2-фторфенил)-3-(3-хлор-2-фторфенил)-4-циано-5-(2,2-диметилпропил)пирролидин-2-карбонил]амино}-3-метоксибензойной кислоты, образуемым совместным осаждением с растворителем или сушкой распылением, что дает в результате улучшенные биодоступность, безопасность и переносимость указанных соединений.
EA201591276A 2013-01-22 2014-01-20 Фармацевтическая композиция с улучшенной биодоступностью EA028009B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361755074P 2013-01-22 2013-01-22
PCT/EP2014/050974 WO2014114575A1 (en) 2013-01-22 2014-01-20 Pharmaceutical composition with improved bioavailability

Publications (2)

Publication Number Publication Date
EA201591276A1 true EA201591276A1 (ru) 2016-01-29
EA028009B1 EA028009B1 (ru) 2017-09-29

Family

ID=50023547

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201591276A EA028009B1 (ru) 2013-01-22 2014-01-20 Фармацевтическая композиция с улучшенной биодоступностью

Country Status (24)

Country Link
US (2) US9427427B2 (ru)
EP (1) EP2948141B1 (ru)
JP (1) JP6192244B2 (ru)
KR (1) KR101737250B1 (ru)
CN (3) CN104936589A (ru)
AR (1) AR094548A1 (ru)
AU (1) AU2014210103B2 (ru)
BR (1) BR112015015758B1 (ru)
CA (1) CA2892025C (ru)
CL (1) CL2015001649A1 (ru)
CR (1) CR20150287A (ru)
EA (1) EA028009B1 (ru)
HK (1) HK1211217A1 (ru)
IL (1) IL239657B (ru)
MA (1) MA38289A1 (ru)
MX (1) MX372668B (ru)
MY (1) MY192032A (ru)
NZ (1) NZ708272A (ru)
PE (1) PE20151335A1 (ru)
PH (1) PH12015501620B1 (ru)
SG (1) SG11201504499VA (ru)
UA (1) UA116004C2 (ru)
WO (1) WO2014114575A1 (ru)
ZA (1) ZA201504187B (ru)

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RU2767872C2 (ru) * 2017-07-04 2022-03-22 Цзянсу Хэнжуй Медсин Ко., Лтд. Фармацевтическая композиция и способ ее получения

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TW202444718A (zh) * 2019-01-25 2024-11-16 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
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MX2021014402A (es) * 2019-05-31 2022-02-14 Jiangsu Hengrui Medicine Co Dispersion de solidos y metodo de preparacion de los mismos.
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CN112022812B (zh) * 2020-11-03 2021-01-29 上海亚盛医药科技有限公司 一种包含杂环类化合物的组合物、其制备方法和应用
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US12031128B2 (en) 2021-04-07 2024-07-09 Battelle Memorial Institute Rapid design, build, test, and learn technologies for identifying and using non-viral carriers
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* Cited by examiner, † Cited by third party
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RU2767872C2 (ru) * 2017-07-04 2022-03-22 Цзянсу Хэнжуй Медсин Ко., Лтд. Фармацевтическая композиция и способ ее получения

Also Published As

Publication number Publication date
KR101737250B1 (ko) 2017-05-17
IL239657B (en) 2019-05-30
CN112370427A (zh) 2021-02-19
BR112015015758A2 (pt) 2018-06-19
ZA201504187B (en) 2018-11-28
US9427427B2 (en) 2016-08-30
EP2948141A1 (en) 2015-12-02
CA2892025A1 (en) 2014-07-31
CN104936589A (zh) 2015-09-23
AU2014210103B2 (en) 2018-09-06
EP2948141B1 (en) 2025-05-14
US10034854B2 (en) 2018-07-31
MY192032A (en) 2022-07-24
PH12015501620B1 (en) 2018-08-24
MA38289A1 (fr) 2017-01-31
NZ708272A (en) 2020-07-31
MX2015008911A (es) 2015-10-22
SG11201504499VA (en) 2015-08-28
JP2016505029A (ja) 2016-02-18
PH12015501620A1 (en) 2015-09-28
BR112015015758B1 (pt) 2022-01-04
CN112353762A (zh) 2021-02-12
MX372668B (es) 2020-04-23
PE20151335A1 (es) 2015-09-18
EA028009B1 (ru) 2017-09-29
IL239657A0 (en) 2015-08-31
KR20150097792A (ko) 2015-08-26
US20140206742A1 (en) 2014-07-24
EP2948141C0 (en) 2025-05-14
UA116004C2 (uk) 2018-01-25
BR112015015758B8 (pt) 2021-10-13
HK1211217A1 (en) 2016-05-20
AR094548A1 (es) 2015-08-12
AU2014210103A1 (en) 2015-06-11
CR20150287A (es) 2015-09-01
JP6192244B2 (ja) 2017-09-06
CL2015001649A1 (es) 2015-10-23
CA2892025C (en) 2022-02-15
US20170000764A1 (en) 2017-01-05
WO2014114575A1 (en) 2014-07-31

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