RU2761344C2 - Введение дейтерированных усилителей cftr - Google Patents

Введение дейтерированных усилителей cftr Download PDF

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RU2761344C2
RU2761344C2 RU2018114447A RU2018114447A RU2761344C2 RU 2761344 C2 RU2761344 C2 RU 2761344C2 RU 2018114447 A RU2018114447 A RU 2018114447A RU 2018114447 A RU2018114447 A RU 2018114447A RU 2761344 C2 RU2761344 C2 RU 2761344C2
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compound
pharmaceutically acceptable
ivacaftor
ctp
acceptable salt
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RU2018114447A
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English (en)
Russian (ru)
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RU2018114447A3 (enExample
RU2018114447A (ru
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Вирджиния БРАМАН
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Вертекс Фармасьютикалз (Юроп) Лимитед
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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K9/145—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 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
    • A61K9/141—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
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • 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
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/12—Mucolytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon 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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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

Publications (3)

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

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RU2018114447A RU2761344C2 (ru) 2015-09-21 2016-09-21 Введение дейтерированных усилителей cftr

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US (2) US20180353500A1 (enExample)
EP (2) EP4292588A3 (enExample)
JP (2) JP6849686B2 (enExample)
KR (1) KR102828163B1 (enExample)
CN (1) CN108367002A (enExample)
AU (2) AU2016326441B2 (enExample)
BR (1) BR112018005454A2 (enExample)
CA (1) CA2998911C (enExample)
HK (1) HK1258472A1 (enExample)
IL (2) IL257993A (enExample)
MA (1) MA42950A (enExample)
MX (1) MX388470B (enExample)
RU (1) RU2761344C2 (enExample)
SG (1) SG10201913588YA (enExample)
UA (1) UA124619C2 (enExample)
WO (1) WO2017053455A1 (enExample)

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US12458635B2 (en) 2008-08-13 2025-11-04 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
HUE047354T2 (hu) 2011-05-18 2020-04-28 Vertex Pharmaceuticals Europe Ltd Ivacaftor deuterizált származékai
RU2692779C2 (ru) 2012-02-27 2019-06-27 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтическая композиция и ее введения
TW202140422A (zh) 2014-10-06 2021-11-01 美商維泰克斯製藥公司 囊腫纖維化症跨膜傳導調節蛋白之調節劑
EP3277647A1 (en) 2015-03-31 2018-02-07 Vertex Pharmaceuticals (Europe) Limited Deuterated vx-661
RU2761344C2 (ru) 2015-09-21 2021-12-07 Вертекс Фармасьютикалз (Юроп) Лимитед Введение дейтерированных усилителей cftr
EP3352758A4 (en) 2015-09-25 2018-08-01 Vertex Pharmaceuticals (Europe) Limited Deuterated cftr potentiators
EP3436446B1 (en) 2016-03-31 2023-06-07 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
JOP20190042B1 (ar) 2016-09-30 2021-08-17 Vertex Pharma مُعدِّل‏ لمنظم موصلية التليف الكيسي عبر الغشاء، وتركيبات صيدلانية، وطرق للعلاج، وعملية لتصنيع المُعدِّل
HRP20201946T1 (hr) 2016-12-09 2021-01-22 Vertex Pharmaceuticals Incorporated Modulator regulatora transmembranske provodljivosti cistične fibroze, farmaceutski sastavi, postupci liječenja, i postupak za dobivanje modulatora
MA54105A (fr) 2017-06-08 2021-09-15 Vertex Pharma Méthodes de traitement de la fibrose kystique
CA3069225A1 (en) * 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
BR112020000941A2 (pt) 2017-07-17 2020-07-21 Vertex Pharmaceuticals Incorporated métodos de tratamento para fibrose cística
WO2019028228A1 (en) 2017-08-02 2019-02-07 Vertex Pharmaceuticals Incorporated PROCESSES FOR THE PREPARATION OF PYRROLIDINE COMPOUNDS
WO2019079760A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS
SG11202004264VA (en) 2017-12-01 2020-06-29 Vertex Pharma Processes for making modulators of cystic fibrosis transmembrane conductance regulator
AU2018380426B2 (en) 2017-12-08 2023-05-18 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
TWI810243B (zh) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
IL276662B (en) 2018-02-15 2022-08-01 Vertex Pharma Macrocycles as modulators of the cystic fibrosis transmembrane conductance regulator, their pharmaceutical compounds, their use in the treatment of cystic fibrosis, and a process for their preparation.
WO2019200246A1 (en) 2018-04-13 2019-10-17 Alexander Russell Abela Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
EP3880197B9 (en) 2018-11-14 2025-07-02 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
TWI848092B (zh) 2019-04-03 2024-07-11 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白調節劑
WO2020214921A1 (en) 2019-04-17 2020-10-22 Vertex Pharmaceuticals Incorporated Solid forms of modulators of cftr
FR3096890B1 (fr) 2019-06-07 2021-05-14 H4 Orphan Pharma Utilisation d’une molécule opioïde pour traiter l’œil sec et l’œil allergique.
TWI899097B (zh) 2019-08-14 2025-10-01 美商維泰克斯製藥公司 製備cftr調節劑之方法
TWI867024B (zh) 2019-08-14 2024-12-21 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白之調節劑
KR20220064366A (ko) 2019-08-14 2022-05-18 버텍스 파마슈티칼스 인코포레이티드 Cftr 조절제의 결정질 형태
WO2021030556A1 (en) 2019-08-14 2021-02-18 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
FR3109524B1 (fr) 2020-04-22 2022-04-08 H4 Orphan Pharma Utilisation d’un ligand multifonctionnel pour traiter l’œil sec et les dysfonctionnements des glandes de Meibomius et des glandes lacrymales.
FR3111071B1 (fr) 2020-06-04 2023-01-13 H4 Orphan Pharma Utilisation de ligands multifonctionnels pour traiter les syndromes de détresse respiratoire et le choc cytokinique liés aux infections virales à coronavirus.
CR20230120A (es) 2020-08-07 2023-09-01 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
JP2023537944A (ja) 2020-08-13 2023-09-06 バーテックス ファーマシューティカルズ インコーポレイテッド Ｃｆｔｒモジュレーターの結晶形態
EP4225762A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022076621A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225447A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225750A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20230373939A1 (en) 2020-10-07 2023-11-23 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022076626A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225764A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225748A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022076622A2 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US12324802B2 (en) 2020-11-18 2025-06-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022125826A1 (en) 2020-12-10 2022-06-16 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
US20250221971A1 (en) 2022-02-03 2025-07-10 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
WO2023154291A1 (en) 2022-02-08 2023-08-17 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
CA3258118A1 (en) 2022-04-06 2023-10-12 Vertex Pharmaceuticals Incorporated MODULATORS OF THE TRANSMEMBRANE CONDUCTANCE REGULATOR IN CYSTIC FIBROSIS
EP4525858A1 (en) 2022-05-16 2025-03-26 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
WO2025076240A1 (en) 2023-10-04 2025-04-10 Vertex Pharmaceuticals Incorporated Solid forms of modulators of cystic fibrosis transmembrane conductance regulator
WO2025076235A1 (en) 2023-10-04 2025-04-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2025166342A1 (en) 2024-02-04 2025-08-07 Vertex Pharmaceuticals Incorporated Combination of vanzacaftor, tezacaftor, deutivacaftor for use in treating cystic fibrosis
WO2025171098A1 (en) 2024-02-07 2025-08-14 Vertex Pharmaceuticals Incorporated Compositions for the treatment of cftr-mediated diseases

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WO2014078842A1 (en) * 2012-11-19 2014-05-22 Concert Pharmaceuticals, Inc. Deuterated cftr potentiators

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NZ741069A (en) 2024-12-20
EP4292588A3 (en) 2024-02-28
US20180353500A1 (en) 2018-12-13
JP2021091723A (ja) 2021-06-17
MX2018003331A (es) 2018-08-16
EP3352757B1 (en) 2023-08-16
IL291517A (en) 2022-05-01
UA124619C2 (uk) 2021-10-20
EP4292588A2 (en) 2023-12-20
IL257993A (en) 2018-05-31
BR112018005454A2 (pt) 2018-10-09
RU2018114447A3 (enExample) 2020-02-21
KR20180058745A (ko) 2018-06-01
CA2998911A1 (en) 2017-03-30
US20200375973A1 (en) 2020-12-03
JP7196217B2 (ja) 2022-12-26
EP3352757A1 (en) 2018-08-01
MA42950A (fr) 2018-08-01
EP3352757C0 (en) 2023-08-16
RU2018114447A (ru) 2019-10-23
JP6849686B2 (ja) 2021-03-24
CN108367002A (zh) 2018-08-03
AU2022201135A1 (en) 2022-03-17
HK1258472A1 (zh) 2019-11-15
MX388470B (es) 2025-03-20
CA2998911C (en) 2023-05-23
SG10201913588YA (en) 2020-02-27
AU2016326441B2 (en) 2021-11-25
AU2022201135B2 (en) 2024-03-28
WO2017053455A1 (en) 2017-03-30
EP3352757A4 (en) 2018-08-01
KR102828163B1 (ko) 2025-07-02
JP2018534348A (ja) 2018-11-22
AU2016326441A1 (en) 2018-04-19

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