DK3000466T3 - Inhibitor til retinochoroidale sygdomme - Google Patents

Inhibitor til retinochoroidale sygdomme Download PDF

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Publication number
DK3000466T3
DK3000466T3 DK14800477.3T DK14800477T DK3000466T3 DK 3000466 T3 DK3000466 T3 DK 3000466T3 DK 14800477 T DK14800477 T DK 14800477T DK 3000466 T3 DK3000466 T3 DK 3000466T3
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Prior art keywords
inhibitor
use according
salt
benzoic acid
retinochoroidal
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DK14800477.3T
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English (en)
Inventor
Kazuhiro Kimura
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Univ Yamaguchi
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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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61JCONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J9/00Feeding-bottles in general
    • A61J9/08Protective covers for bottles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • 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
    • 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
    • A61K9/2013Organic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (15)

1. Inhibitor til anvendelse i en fremgangsmåde til behandling afen retinochoroidal sygdom omfattende (E)-4-(2-{3-[(lH-pyrazol-l-yl)methyl]-5,5,8,8-tetramethyl- 5,6,7,8-tetrahydronaphthalen-2-yl}vinyl)benzoesyre, en ester deraf, eller et salt deraf som en effektiv bestanddel, hvor behandlingen omfatter inhibering af ardannelse eller atrofi.
2. Inhibitoren til anvendelse ifølge krav 1, hvor behandlingen omfatter inhibering af ardannelse.
3. Inhibitoren til anvendelse ifølge krav 1 eller 2, hvor arret er et fibrøst bindevæv der forekommer på et epiretinalt-, intraretinalt-, og/eller subretinalt skadested med progressionen afen ophthalmisk inflammation.
4. Inhibitoren til anvendelse ifølge et hvilket som helst af kravene 1 til 3, hvor arret omfatter en retinal pigmentepitelcelle med ekstracellulær matrix omfattende kollagen.
5. Inhibitoren til anvendelse ifølge krav 1, hvor behandlingen omfatter forebyggende deformation eller disintegration af en vævsstruktur.
6. Inhibitoren til anvendelse ifølge krav 1, hvor behandlingen omfatter inhibering af dannelsen og atrofi af et retinochoroidalt ar i epiretinalt-, intraretinalt-, og/eller subretinalt væv.
7. Inhibitoren til anvendelse ifølge krav 1, hvor behandlingen omfatter inhibering af kollagenatrofi, og hvor kollagenatrofi er en retinal pigmentepitelcelle, en fibroblast, og/eller en glialcelle.
8. Inhibitoren til anvendelse ifølge et hvilket som helst af kravene 1-7, hvor den retinochoroidale sygdom er en vitreoretinal sygdom, fortrinsvis, hvor den vitreoretinale sygdom er diabetisk retinopati, alders-relateret makulær degeneration, retinal adskillelse, proliferative vitreoretinopati, uveitis, okulær infektion, retinopati af prematuritet, neovaskulær maculopati, eller retinochoroiditis.
9. Inhibitoren til anvendelse ifølge krav 1, hvor behandlingen omfatter inhibering af vævsgenopbygning der sker efter inflammation, blødning, infektion, kirurgi, eller skade i ophthalmisk væv.
10. Inhibitoren til anvendelse ifølge et hvilket som helst af kravene 1-9, hvor inhibitoren er formuleret til administration oralt, intravenøst, intramuskulært, intraperitolealt, perkutant, intratrachealt, intrakutant, subkutant, eller ved inddrypning.
11. Inhibitoren til anvendelse ifølge et hvilket som helst af kravene 1-10, hvor (E)-4-(2-{3-[(lH-pyrazol-l-yl)methyl]-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl}vinyl)benzoesyren, en ester deraf, eller et salt deraf er formuleret som en salve, injektion, tablet, granulat, fint granulat, pulver, kapsel, inhalationsmiddel, sirup, pille, flydende formulering, suspension, emulsion, perkutant absorptionsmiddel, stikpille, lotion, eller inddrypning.
12. Inhibitoren til anvendelse ifølge krav 11, hvor salven er en opthalmisk salve, fortrinsvis, hvor koncentrationen af(E)-4-(2-{3-[(lH-pyrazol-l-yl)methyl]- 5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl}vinyl)benzoesyre, en ester deraf, eller et salt deraf i den ophthalmiske salve administreret til et individ er fra 0,00001 til 10% (vægt/vægt), fra 0,0001 til 3% (vægt/vægt), eller fra 0,001 til 1% (vægt/vægt).
13. Inhibitoren til anvendelse ifølge krav 10, hvor inhibitoren formuleres til administration ved inddrypning, fortrinsvis, hvor koncentrationen af (E)-4-(2-{3-[(lH-pyrazol-l-yl)methyl]-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl}vinyl)benzoesyre, en ester deraf, eller et salt deraf i inddrypningen administreret til et individ er fra 0,000001 til 10% (vægt/volumen), from 0,00001 til 3% (vægt/volumen), eller fra 0,0001% til 1% (vægt/volumen).
14. Inhibitoren til anvendelse ifølge krav 10, hvor inhibitoren er formuleret til administration oralt, fortrinsvis, hvor mængden af (E)-4-(2-{3-[(lH-pyrazol-l- yl)methyl]-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2- yl}vinyl)benzoesyre, en ester deraf, eller et salt deraf administreret oralt til et individ er fra 0,01 til 5000 mg, fra 0,1 til 2500 mg, eller fra 0,5 til 1000 mg.
15. Inhibitoren til anvendelse ifølge et hvilket som helst af kravene 1-14, hvor (E)-4-(2-{3-[( 1 H-pyrazol-l-yl)methyl]-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl}vinyl)benzoesyren, en ester deraf, eller et salt deraf formuleres til administration i én eller flere daglige doser.
DK14800477.3T 2013-05-22 2014-05-21 Inhibitor til retinochoroidale sygdomme DK3000466T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2013107706 2013-05-22
PCT/JP2014/002667 WO2014188716A1 (ja) 2013-05-22 2014-05-21 網脈絡膜障害の抑制剤

Publications (1)

Publication Number Publication Date
DK3000466T3 true DK3000466T3 (da) 2018-11-26

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US (3) US10702502B2 (da)
EP (2) EP3446690B1 (da)
JP (2) JP6407145B2 (da)
KR (1) KR102303316B1 (da)
CN (1) CN105377258B (da)
AU (1) AU2014269762B2 (da)
BR (1) BR112015029114B1 (da)
CA (1) CA2913005C (da)
CY (1) CY1121036T1 (da)
DK (1) DK3000466T3 (da)
ES (2) ES2694831T3 (da)
HR (1) HRP20181876T1 (da)
LT (1) LT3000466T (da)
MX (1) MX362239B (da)
PL (1) PL3000466T3 (da)
PT (1) PT3000466T (da)
RS (1) RS58045B1 (da)
RU (1) RU2672057C2 (da)
SI (1) SI3000466T1 (da)
SM (1) SMT201800593T1 (da)
WO (1) WO2014188716A1 (da)
ZA (1) ZA201508940B (da)

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PL3000466T3 (pl) * 2013-05-22 2019-04-30 Univ Yamaguchi Inhibitor dla zaburzeń siatkówkowo-naczyniówkowych
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PL3000466T3 (pl) 2013-05-22 2019-04-30 Univ Yamaguchi Inhibitor dla zaburzeń siatkówkowo-naczyniówkowych

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Publication number Publication date
NZ715245A (en) 2021-04-30
MX362239B (es) 2019-01-09
EP3000466A4 (en) 2017-01-25
JP2018115221A (ja) 2018-07-26
CY1121036T1 (el) 2019-12-11
SI3000466T1 (sl) 2019-02-28
RU2672057C2 (ru) 2018-11-09
ZA201508940B (en) 2017-11-29
JP6749962B2 (ja) 2020-09-02
HK1221909A1 (zh) 2017-06-16
EP3446690B1 (en) 2024-09-11
CA2913005A1 (en) 2014-11-27
PL3000466T3 (pl) 2019-04-30
KR102303316B1 (ko) 2021-09-23
BR112015029114A2 (pt) 2017-07-25
RS58045B1 (sr) 2019-02-28
HRP20181876T1 (hr) 2019-03-08
EP3446690C0 (en) 2024-09-11
CN105377258B (zh) 2020-08-28
US10702502B2 (en) 2020-07-07
ES2694831T3 (es) 2018-12-27
KR20160013075A (ko) 2016-02-03
CA2913005C (en) 2021-08-10
SMT201800593T1 (it) 2019-02-28
EP3446690A1 (en) 2019-02-27
AU2014269762B2 (en) 2019-09-12
BR112015029114A8 (pt) 2020-03-17
AU2014269762A1 (en) 2016-01-07
LT3000466T (lt) 2019-02-11
US20160120843A1 (en) 2016-05-05
US20240180873A1 (en) 2024-06-06
US12357613B2 (en) 2025-07-15
RU2015154741A (ru) 2017-06-28
PT3000466T (pt) 2018-11-27
US11730718B2 (en) 2023-08-22
JPWO2014188716A1 (ja) 2017-02-23
US20210121442A1 (en) 2021-04-29
EP3000466B1 (en) 2018-08-15
CN105377258A (zh) 2016-03-02
BR112015029114B1 (pt) 2020-11-24
MX2015016083A (es) 2016-03-21
JP6407145B2 (ja) 2018-10-17
ES2989991T3 (es) 2024-11-28
EP3000466A1 (en) 2016-03-30
WO2014188716A1 (ja) 2014-11-27

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