NZ741069B2 - Administration of deuterated cftr potentiators - Google Patents

Administration of deuterated cftr potentiators Download PDF

Info

Publication number
NZ741069B2
NZ741069B2 NZ741069A NZ74106916A NZ741069B2 NZ 741069 B2 NZ741069 B2 NZ 741069B2 NZ 741069 A NZ741069 A NZ 741069A NZ 74106916 A NZ74106916 A NZ 74106916A NZ 741069 B2 NZ741069 B2 NZ 741069B2
Authority
NZ
New Zealand
Prior art keywords
pharmaceutical composition
compound
medicament
ctp
composition
Prior art date
Application number
NZ741069A
Other versions
NZ741069A (en
Inventor
Virginia Braman
Original Assignee
Vertex Pharmaceuticals (Europe) Limited
Filing date
Publication date
Application filed by Vertex Pharmaceuticals (Europe) Limited filed Critical Vertex Pharmaceuticals (Europe) Limited
Priority claimed from PCT/US2016/052922 external-priority patent/WO2017053455A1/en
Publication of NZ741069A publication Critical patent/NZ741069A/en
Publication of NZ741069B2 publication Critical patent/NZ741069B2/en

Links

Classifications

    • 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

Abstract

Disclosed is a method of treating in a subject of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator The method comprises administering to the subject an amount in the range of about 50 mg to about 200 mg once a day of Compound (I) or (II) or pharmaceutically acceptable salts thereof, This invention also provides compositions comprising Compound (I) or (II) and the use of such compositions in methods.

Claims (21)

We claim:
1. Use of Compound (I): or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment of cystic fibrosis, wherein the medicament is to be administered in an amount equivalent to 90-200 mg of Compound (I), once per day.
2. The use of any one of claim 1, wherein the medicament is to be administered in an amount equivalent to 100 mg of Compound (I), once per day.
3. The use of claim 1, wherein the medicament is to be administered in an amount equivalent to 150 mg of Compound (I), once per day.
4. The use of any one of claims 1-3, wherein the medicament is to be administered orally.
5. The use of any one of claims 1-4, wherein the medicament is a tablet.
6. The use of any one of claims 1-4, wherein the medicament is a granule.
7. The use of any one of claims 1-6, wherein any atom not designated as deuterium in Compound (I) is present at its natural isotopic abundance.
8. The use of any one of claims 1-7, wherein the medicament is to be administered orally concurrently with, prior to, or subsequent to one or more second therapeutic agents.
9. The use of claim 8, wherein the second therapeutic agent is an agent useful in the treatment of cystic fibrosis.
10. The use of claim 8 or 9, wherein the second therapeutic agent is VX-809 (lumacaftor) or VX-661 (tezacaftor).
11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and 90 mg to 200 mg of Compound (I): or a pharmaceutically acceptable salt thereof.
12. The pharmaceutical composition of claim 11, comprising 100 mg of Compound (I).
13. The pharmaceutical composition of claim 11, comprising 150 mg of Compound (I).
14. The pharmaceutical composition of any one of claims 11-13, wherein the pharmaceutical composition is suitable for oral administration.
15. The pharmaceutical composition of any one of claims 11-14, wherein the composition is a tablet.
16. The pharmaceutical composition of any one of claims 11-14, wherein the composition is a granule.
17. The pharmaceutical composition of any one of claims 11-16, wherein the composition is suitable for oral administration concurrently with, prior to, or subsequent to one or more second therapeutic agents.
18. The pharmaceutical composition of claim 17, wherein the second therapeutic agent is an agent useful in the treatment of cystic fibrosis.
19. The pharmaceutical composition of claim 17 or 18, wherein the second therapeutic agent is VX-809 (lumacaftor) or VX-661 (tezacaftor).
20. Use of any one of claims 1-10, substantially as herein described with reference to any example thereof and with or without reference to the accompanying drawings.
21. A pharmaceutical composition of any one of claims 11-19, substantially as herein described with reference to any example thereof and with or without reference to the accompanying drawings. IvacaftarJ 50 mg ¦ CTP-656„75 mg — CTP-656J50mg CTP-656„300 mg Time (hr) Figure ] A O' 10000-1 «* IvacaftoMSOmg t*~ CTP-656„75 mg CTP-656J50 mg CTP-656„300 mg 4| wjl 0 8 16 24 Time (hr)
NZ741069A 2016-09-21 Administration of deuterated cftr potentiators NZ741069B2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562221531P 2015-09-21 2015-09-21
US201562238511P 2015-10-07 2015-10-07
US201662348855P 2016-06-10 2016-06-10
PCT/US2016/052922 WO2017053455A1 (en) 2015-09-21 2016-09-21 Administration of deuterated cftr potentiators

Publications (2)

Publication Number Publication Date
NZ741069A NZ741069A (en) 2024-12-20
NZ741069B2 true NZ741069B2 (en) 2025-03-21

Family

ID=

Similar Documents

Publication Publication Date Title
JP2018520189A5 (en)
AU2012284627A8 (en) Method for manufacturing a pharmaceutical composition in the form of extended-release tablets containing Pirfenidone and use thereof in the regression of chronic renal insufficiency, breast capsular contracture and hepatic fibrosis in humans
RU2018114447A (en) INTRODUCTION OF CFTER DUTERED AMPLIFIERS
JP2018534348A5 (en)
JP2018507243A5 (en)
IL314873A (en) Compositions and methods for the treatment of diseases improved by the activation of muscarinic receptors
JP2018090566A5 (en)
CA3019769C (en) Methods of treating parkinson's disease by administration of apomorphine to an oral mucosa
JP2012502047A5 (en)
WO2015034678A3 (en) Corticosteroid containing orally disintegrating tablet compositions for eosinophilic esophagitis
HRP20192189T1 (en) Dosage forms and therapeutic uses l-4-chlorokynurenine
NZ591204A (en) Pharmaceutical compositions and methods for stabilizing the same
MX2018000084A (en) Pharmaceutical composition containing amlodipine, valsartan, and rosuvastatin.
ZA202000028B (en) Use of vibegron to treat overactive bladder
JP2016505050A5 (en)
WO2012042197A3 (en) Low dose pharmaceutical composition comprising zanamivir
RU2018146504A (en) Treatment of intrahepatic cholestatic diseases
JP2016512247A5 (en)
NZ751972A (en) Treatment of prurigo nodularis
WO2007038428A3 (en) Prevention and treatment of gastrointestinal and bladder disorders using active vitamin d compounds
JP2019509309A5 (en)
MX2022012693A (en) Composition comprising methylfolate.
RU2017112748A (en) ONAPRISTON COMPOSITIONS OF LONG-TERM ACTIONS AND METHODS
CA2595363A1 (en) Methods and materials with trans-clomiphene for the treatment of male infertility
JP2019535830A5 (en)