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RU2018114447A - Введение дейтерированных усилителей cftr - Google Patents

Введение дейтерированных усилителей cftr Download PDF

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RU2018114447A
RU2018114447A RU2018114447A RU2018114447A RU2018114447A RU 2018114447 A RU2018114447 A RU 2018114447A RU 2018114447 A RU2018114447 A RU 2018114447A RU 2018114447 A RU2018114447 A RU 2018114447A RU 2018114447 A RU2018114447 A RU 2018114447A
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pharmaceutical composition
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pharmaceutically acceptable
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RU2018114447A
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RU2761344C2 (ru
RU2018114447A3 (ru
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Вирджиния БРАМАН
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Вертекс Фармасьютикалз (Юроп) Лимитед
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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/145Intimate 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 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
    • A61K9/141Intimate 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
    • 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
    • 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
    • A61K9/2009Inorganic 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/12Mucolytics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth 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)
  • Organic Chemistry (AREA)
  • Pulmonology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (18)

1. Способ лечения состояния, которое опосредовано CFTR, у пациента, включающий введение пациенту соединения, представленного следующей структурной формулой
Figure 00000001
или его фармацевтически приемлемой соли
в количестве от 50 мг до 200 мг, один раз в сутки.
2. Способ по п. 1, где состоянием является муковисцидоз.
3. Способ по любому из пп. 1-2, включающий введение пациенту 100 мг Соединения (I) или его фармацевтически приемлемой соли в сутки.
4. Способ по любому из пп. 1-3, где соединение вводят перорально.
5. Способ по п. 4, где соединение вводят в составе фармацевтической композиции, которая является таблеткой.
6. Способ по п. 4, где соединение вводят в составе фармацевтической композиции, которая является гранулами.
7. Способ по любому из пп. 1-6, где любой атом, не обозначенный как дейтерий в любом из вариантов осуществления изобретения, указанных выше, присутствует в его натуральной изотопной обогащенности.
8. Фармацевтическая композиция, включающая фармацевтически приемлемый носитель или разбавитель и от 50 мг до 200 мг соединения представленного следующей структурной формулой
Figure 00000001
или его фармацевтически приемлемой соли.
9. Фармацевтическая композиция по п. 8, включающая 100 мг соединения (I).
10. Фармацевтическая композиция по п. 8 или 9, где фармацевтическая композиция подходит для перорального введения.
11. Фармацевтическая композиция по п. 8 или 9, где композицией является таблетка.
12. Фармацевтическая композиция по п. 8 или 9, где композицией является гранула.
13. Фармацевтическая композиция по любому из пп. 8-12, где композицию вводят один раз в сутки.
RU2018114447A 2015-09-21 2016-09-21 Введение дейтерированных усилителей cftr RU2761344C2 (ru)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201562221531P 2015-09-21 2015-09-21
US62/221,531 2015-09-21
US201562238511P 2015-10-07 2015-10-07
US62/238,511 2015-10-07
US201662348855P 2016-06-10 2016-06-10
US62/348,855 2016-06-10
PCT/US2016/052922 WO2017053455A1 (en) 2015-09-21 2016-09-21 Administration of deuterated cftr potentiators

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RU2018114447A true RU2018114447A (ru) 2019-10-23
RU2018114447A3 RU2018114447A3 (ru) 2020-02-21
RU2761344C2 RU2761344C2 (ru) 2021-12-07

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EP (2) EP3352757B1 (ru)
JP (2) JP6849686B2 (ru)
KR (1) KR102828163B1 (ru)
CN (1) CN108367002A (ru)
AU (2) AU2016326441B2 (ru)
BR (1) BR112018005454A2 (ru)
CA (1) CA2998911C (ru)
HK (1) HK1258472A1 (ru)
IL (2) IL257993A (ru)
MA (1) MA42950A (ru)
MX (1) MX388470B (ru)
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SG (1) SG10201913588YA (ru)
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WO (1) WO2017053455A1 (ru)

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AU2020328568A1 (en) 2019-08-14 2022-03-03 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
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EP3352757B1 (en) 2023-08-16
IL291517A (en) 2022-05-01
CA2998911A1 (en) 2017-03-30
RU2761344C2 (ru) 2021-12-07
JP2021091723A (ja) 2021-06-17
US20180353500A1 (en) 2018-12-13
CA2998911C (en) 2023-05-23
CN108367002A (zh) 2018-08-03
KR102828163B1 (ko) 2025-07-02
JP6849686B2 (ja) 2021-03-24
AU2022201135A1 (en) 2022-03-17
AU2016326441B2 (en) 2021-11-25
MX388470B (es) 2025-03-20
BR112018005454A2 (pt) 2018-10-09
EP3352757A4 (en) 2018-08-01
EP3352757C0 (en) 2023-08-16
AU2016326441A1 (en) 2018-04-19
US20200375973A1 (en) 2020-12-03
NZ741069A (en) 2024-12-20
WO2017053455A1 (en) 2017-03-30
KR20180058745A (ko) 2018-06-01
MX2018003331A (es) 2018-08-16
JP2018534348A (ja) 2018-11-22
EP4292588A3 (en) 2024-02-28
AU2022201135B2 (en) 2024-03-28
JP7196217B2 (ja) 2022-12-26
IL257993A (en) 2018-05-31
EP4292588A2 (en) 2023-12-20
RU2018114447A3 (ru) 2020-02-21
UA124619C2 (uk) 2021-10-20
EP3352757A1 (en) 2018-08-01
HK1258472A1 (zh) 2019-11-15
MA42950A (fr) 2018-08-01
SG10201913588YA (en) 2020-02-27

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