CN108367002A - 氘化cftr增强剂的给予 - Google Patents

氘化cftr增强剂的给予 Download PDF

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Publication number
CN108367002A
CN108367002A CN201680067707.1A CN201680067707A CN108367002A CN 108367002 A CN108367002 A CN 108367002A CN 201680067707 A CN201680067707 A CN 201680067707A CN 108367002 A CN108367002 A CN 108367002A
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CN
China
Prior art keywords
compound
ivacaftor
pharmaceutically acceptable
ctp
acceptable salt
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201680067707.1A
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English (en)
Chinese (zh)
Inventor
V.布拉曼
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Concert Pharmaceuticals Inc
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Concert Pharmaceuticals Inc
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=58387264&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN108367002(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Concert Pharmaceuticals Inc filed Critical Concert Pharmaceuticals Inc
Publication of CN108367002A publication Critical patent/CN108367002A/zh
Pending legal-status Critical Current

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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)
  • 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)
CN201680067707.1A 2015-09-21 2016-09-21 氘化cftr增强剂的给予 Pending CN108367002A (zh)

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 (1)

Publication Number Publication Date
CN108367002A true CN108367002A (zh) 2018-08-03

Family

ID=58387264

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680067707.1A Pending CN108367002A (zh) 2015-09-21 2016-09-21 氘化cftr增强剂的给予

Country Status (16)

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

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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
EP2819670A1 (en) 2012-02-27 2015-01-07 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administration thereof
TWI735416B (zh) 2014-10-06 2021-08-11 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
HK1249893A1 (zh) 2015-03-31 2018-11-16 Vertex Pharmaceuticals (Europe) Limited 氘代vx-661
UA124619C2 (uk) 2015-09-21 2021-10-20 Вертекс Фармасьютікалз (Юроп) Лімітед Введення дейтерованих підсилювачів cftr
HK1258473A1 (zh) 2015-09-25 2019-11-15 Vertex Pharmaceuticals (Europe) Limited 氘代cftr增效剂
ES2946970T3 (es) 2016-03-31 2023-07-28 Vertex Pharma Regulador de conductancia transmembrana de moduladores de fibrosis quística
SI3519401T1 (sl) 2016-09-30 2022-01-31 Vertex Pharmaceuticals Incorporated Modulator regulatorja transmembranske prevodnosti pri cistični fibrozi, farmacevtski sestavki, postopki zdravljenja in proces za izdelavo modulatorja
CN110267948B (zh) 2016-12-09 2023-12-08 弗特克斯药品有限公司 囊性纤维化跨膜传导调控剂的调节剂、药物组合物、治疗方法和制备所述调节剂的方法
AU2018279646B2 (en) 2017-06-08 2023-04-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
MA49631A (fr) 2017-07-17 2020-05-27 Vertex Pharma Méthodes de traitement de la fibrose kystique
US20200171015A1 (en) * 2017-07-17 2020-06-04 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
TWI799435B (zh) 2017-08-02 2023-04-21 美商維泰克斯製藥公司 製備化合物之製程
US10654829B2 (en) 2017-10-19 2020-05-19 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of CFTR modulators
CA3082444A1 (en) 2017-12-01 2019-06-06 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
KR102716244B1 (ko) 2017-12-08 2024-10-14 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유증 막횡단 전도 조절자의 조정제의 제조 방법
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
AU2019222758B2 (en) 2018-02-15 2022-07-07 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cystic fibrosis, and process for making them
EP3774825A1 (en) 2018-04-13 2021-02-17 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
PT3880197T (pt) 2018-11-14 2023-05-09 Vertex Pharma Métodos de tratamento para a fibrose quística
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
CA3150162A1 (en) 2019-08-14 2021-02-18 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
CN114585628B (zh) 2019-08-14 2024-03-26 弗特克斯药品有限公司 囊性纤维化跨膜传导调节因子的调节剂
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
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
IL300413A (en) 2020-08-13 2023-04-01 Vertex Pharma Crystal forms of CFTR modulators
US20230373935A1 (en) 2020-10-07 2023-11-23 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225765A2 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022076628A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225762A1 (en) 2020-10-07 2023-08-16 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
EP4225447A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
MX2023004074A (es) 2020-10-07 2023-07-05 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica.
WO2022076629A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225446A1 (en) 2020-10-07 2023-08-16 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
AU2021397294A1 (en) 2020-12-10 2023-07-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
IL314449A (en) 2022-02-03 2024-09-01 Vertex Pharma Methods of treatment for cystic fibrosis
WO2023154291A1 (en) 2022-02-08 2023-08-17 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
IL315715A (en) 2022-04-06 2024-11-01 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulation
EP4525858A1 (en) 2022-05-16 2025-03-26 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
WO2025076235A1 (en) 2023-10-04 2025-04-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2025076240A1 (en) 2023-10-04 2025-04-10 Vertex Pharmaceuticals Incorporated Solid forms of 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
US20250248981A1 (en) 2024-02-07 2025-08-07 Vertex Pharmaceuticals Incorporated Compositions for the treatment of cftr-mediated diseases

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EP2819670A1 (en) 2012-02-27 2015-01-07 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administration thereof
MY183582A (en) * 2012-11-19 2021-02-26 Vertex Pharmaceuticals Europe Ltd Deuterated cftr potentiators
UA124619C2 (uk) 2015-09-21 2021-10-20 Вертекс Фармасьютікалз (Юроп) Лімітед Введення дейтерованих підсилювачів cftr

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CN103833630A (zh) * 2012-11-21 2014-06-04 康塞特医药品有限公司 氘化cftr增效剂
US20140221424A1 (en) * 2013-01-30 2014-08-07 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for use in the treatment of cystic fibrosis

Also Published As

Publication number Publication date
JP2018534348A (ja) 2018-11-22
EP3352757B1 (en) 2023-08-16
IL291517A (en) 2022-05-01
MX2018003331A (es) 2018-08-16
EP3352757A4 (en) 2018-08-01
BR112018005454A2 (pt) 2018-10-09
RU2018114447A (ru) 2019-10-23
KR20180058745A (ko) 2018-06-01
AU2016326441B2 (en) 2021-11-25
SG10201913588YA (en) 2020-02-27
RU2018114447A3 (https=) 2020-02-21
EP3352757A1 (en) 2018-08-01
JP2021091723A (ja) 2021-06-17
EP4292588A2 (en) 2023-12-20
CA2998911C (en) 2023-05-23
MA42950A (fr) 2018-08-01
WO2017053455A1 (en) 2017-03-30
IL257993A (en) 2018-05-31
KR102828163B1 (ko) 2025-07-02
CA2998911A1 (en) 2017-03-30
JP7196217B2 (ja) 2022-12-26
RU2761344C2 (ru) 2021-12-07
MX388470B (es) 2025-03-20
UA124619C2 (uk) 2021-10-20
AU2016326441A1 (en) 2018-04-19
EP4292588A3 (en) 2024-02-28
US20200375973A1 (en) 2020-12-03
EP3352757C0 (en) 2023-08-16
AU2022201135B2 (en) 2024-03-28
JP6849686B2 (ja) 2021-03-24
AU2022201135A1 (en) 2022-03-17
NZ741069A (en) 2024-12-20
US20180353500A1 (en) 2018-12-13
HK1258472A1 (zh) 2019-11-15

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