HRP20201946T1 - Modulator regulatora transmembranske provodljivosti cistične fibroze, farmaceutski sastavi, postupci liječenja, i postupak za dobivanje modulatora - Google Patents

Modulator regulatora transmembranske provodljivosti cistične fibroze, farmaceutski sastavi, postupci liječenja, i postupak za dobivanje modulatora Download PDF

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Publication number
HRP20201946T1
HRP20201946T1 HRP20201946TT HRP20201946T HRP20201946T1 HR P20201946 T1 HRP20201946 T1 HR P20201946T1 HR P20201946T T HRP20201946T T HR P20201946TT HR P20201946 T HRP20201946 T HR P20201946T HR P20201946 T1 HRP20201946 T1 HR P20201946T1
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Croatia
Prior art keywords
modulator
pharmaceutically acceptable
cystic fibrosis
pharmaceutical composition
acceptable salt
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Application number
HRP20201946TT
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English (en)
Inventor
Alexander Russell Abela
Timothy ALCACIO
Corey Anderson
Paul Timothy Angell
Minson BAEK
Jeremy J. Clemens
Thomas Cleveland
Lori Ann Ferris
Peter Diederik Jan Grootenhuis
Raymond Stanley GROSS
Anton GULEVICH
Sara Sabina Hadida Ruah
Clara Kuang-Ju Hsia
Robert M. Hughes
Pramod Virupax Joshi
Ping KANG
Ali Keshavarz-Shokri
Haripada Khatuya
Paul John Krenitsky
Jason Mccartney
Mark Thomas Miller
Prasuna PARASELLI
Fabrice Jean Denis Pierre
Yi Shi
Muna SHRESTHA
David Andrew Siesel
Kathy Stavropoulos
Andreas P. Termin
Johnny Uy
Fredrick F. Van Goor
Tomothy John Young
Jinglan Zhou
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Vertex Pharmaceuticals Incorporated
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Application filed by Vertex Pharmaceuticals Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of HRP20201946T1 publication Critical patent/HRP20201946T1/hr

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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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/18—One oxygen or sulfur atom
    • C07D231/20—One oxygen atom attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (10)

1. Spoj koji ima sljedeću formulu: [image] njegova farmaceutski prihvatljiva sol, ili deuterirani derivat bilo kojeg od prethodno spomenutih.
2. Spoj prema zahtjevu 1 koji ima sljedeću formulu: [image] ili njegova farmaceutski prihvatljiva sol.
3. Farmaceutski sastav koji sadrži bar jedan spoj izabran od spoja prema zahtjevu 1 ili zahtjevu 2, njegove farmaceutski prihvatljive soli, ili deuteriranog derivata bilo kojeg od prethodno spomenutih.
4. Spoj prema zahtjevu 1 ili zahtjevu 2, ili njegova farmaceutski prihvatljiva sol, ili deuterirani derivat bilo kojeg od prethodno spomenutih, ili farmaceutski sastav prema zahtjevu 3 za upotrebu u postupku liječenja cistične fibroze.
5. Spoj prema zahtjevu 1 koji ima sljedeću formulu: [image]
6. Farmaceutski sastav prema zahtjevu 3 koji sadrži spoj prema zahtjevu 5 i farmaceutski prihvatljiv nosač.
7. Spoj ili farmaceutski sastav za upotrebu prema zahtjevu 4 pri čemu je spoj prema zahtjevu 5, ili farmaceutski sastav prema zahtjevu 6, za upotrebu u postupku liječenja cistične fibroze.
8. Farmaceutski prihvatljiva sol prema zahtjevu 1 spoja koji ima sljedeću formulu: [image]
9. Farmaceutski sastav prema zahtjevu 3 koji sadrži farmaceutski prihvatljivu sol prema zahtjevu 8 i farmaceutski prihvatljiv nosač.
10. Farmaceutski prihvatljiva sol ili farmaceutski sastav za upotrebu prema zahtjevu 4 pri čemu je farmaceutski prihvatljiva sol prema zahtjevu 8, ili farmaceutski sastav prema zahtjevu 9, za upotrebu u postupku liječenja cistične fibroze.
HRP20201946TT 2016-12-09 2020-12-04 Modulator regulatora transmembranske provodljivosti cistične fibroze, farmaceutski sastavi, postupci liječenja, i postupak za dobivanje modulatora HRP20201946T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662432537P 2016-12-09 2016-12-09
EP17826629.2A EP3551622B1 (en) 2016-12-09 2017-12-08 Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
PCT/US2017/065425 WO2018107100A1 (en) 2016-12-09 2017-12-08 Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator

Publications (1)

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HRP20201946T1 true HRP20201946T1 (hr) 2021-01-22

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HRP20201946TT HRP20201946T1 (hr) 2016-12-09 2020-12-04 Modulator regulatora transmembranske provodljivosti cistične fibroze, farmaceutski sastavi, postupci liječenja, i postupak za dobivanje modulatora

Country Status (34)

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US (3) US10793547B2 (hr)
EP (2) EP3551622B1 (hr)
JP (3) JP6916285B2 (hr)
KR (1) KR102269492B1 (hr)
CN (2) CN110267948B (hr)
AR (1) AR110346A1 (hr)
AU (3) AU2017371200B2 (hr)
BR (1) BR112019011626A2 (hr)
CA (1) CA3046086A1 (hr)
CL (1) CL2019001553A1 (hr)
CO (1) CO2019007129A2 (hr)
CY (1) CY1123736T1 (hr)
DK (1) DK3551622T3 (hr)
EA (2) EA039280B1 (hr)
EC (1) ECSP19048759A (hr)
ES (1) ES2837431T3 (hr)
HR (1) HRP20201946T1 (hr)
HU (1) HUE052205T2 (hr)
IL (3) IL277491B (hr)
JO (1) JOP20190125B1 (hr)
LT (1) LT3551622T (hr)
MA (2) MA49235B1 (hr)
MD (1) MD3551622T2 (hr)
MX (2) MX2019006637A (hr)
PE (1) PE20191304A1 (hr)
PT (1) PT3551622T (hr)
RS (1) RS61150B1 (hr)
SA (1) SA519401947B1 (hr)
SG (1) SG10201913606VA (hr)
SI (1) SI3551622T1 (hr)
TW (1) TWI774712B (hr)
UY (2) UY37513A (hr)
WO (1) WO2018107100A1 (hr)
ZA (1) ZA201904062B (hr)

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WO2023224924A1 (en) 2022-05-16 2023-11-23 Vertex Pharmaceuticals Incorporated Solid forms of a macrocyclic compounds as cftr modulators and their preparation
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