DK2729147T3 - Nk-1-receptorantagonister til behandling af hornhindeneovaskularisering - Google Patents

Nk-1-receptorantagonister til behandling af hornhindeneovaskularisering Download PDF

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Publication number
DK2729147T3
DK2729147T3 DK12741268.2T DK12741268T DK2729147T3 DK 2729147 T3 DK2729147 T3 DK 2729147T3 DK 12741268 T DK12741268 T DK 12741268T DK 2729147 T3 DK2729147 T3 DK 2729147T3
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Prior art keywords
methyl
phenyl
fluoro
trifluoromethyl
compound
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DK12741268.2T
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English (en)
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Giulio Ferrari
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Irbm - Science Park S P A
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Publication of DK2729147T3 publication Critical patent/DK2729147T3/da

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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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (13)

1. Forbindelse, der er en NK-1-receptorantagonist til anvendelse i behandling eller forebyggelse af hornhindeneovaskularisering (CNV), hvor NK-1-receptorantagonisten administreres topisk til hornhinden, og hvor forbindelsen er udvalgt fra aprepitant, fosaprepitant, befetupitant og lanepitant og farmaceutisk acceptable salte af en hvilken som helst deraf.
2. Forbindelse til anvendelse ifølge krav 1, hvor CNV er samtidig med eller følger efter en inflammatorisk tilstand.
3. Forbindelse til anvendelse ifølge krav 1 eller 2, hvor CNV er forårsaget af én af følgende tilstande: bakterieinfektion, virusinfektion, Chlamydia trachomatis-infektion, infektiøs keratitis, herunder herpes simplex keratitis, viral interstitiel keratitis, infektioner forårsaget af stafylokokker, streptokokker, Pseudomonas eller mikrobiel keratoconjunctivitis, Pseudomonas aeruginosa-infektion, kemisk eller fysisk øjenlæsion, degenerative og traumatiske forstyrrelser, tørre øjne, progressiv hornhindevaskularisering forårsaget af graft-versus-host-sygdom, limbal stamcelledeficiens (herunder idiopatisk, traumatisk, aniridi, autoimmun polyendokrinopati), Stevens-Johnson-syndrom, okulær pemphigoid, tilbagevendende pterygium efter operativt indgreb, længevarende bæring af hydrogelkontaktlinser.
4. Forbindelse, der er en NK-1 -antagonist, til anvendelse i behandlingen af kemiske forbrændinger af øjet, hvor NK-1-receptorantagonisten administreres topisk til hornhinden, og hvor forbindelsen er udvalgt fra aprepitant, fosaprepitant, befetupitant og lanepitant og farmaceutisk acceptable salte af en hvilken som helst deraf.
5. Forbindelse til anvendelse ifølge krav 4, hvor de kemiske forbrændinger af øjet er alkaliforbrændinger af øjet.
6. Forbindelse til anvendelse ifølge krav 4 eller krav 5, hvor NK-1-antagonistbehandlingen fører til én eller flere af følgende specifikke fordele efter eller i forbindelse med kemiske forbrændinger af øjet, navnlig alkaliforbrændinger af øjet: reduceret ardannelse i øjet, reduceret øjenbetændelse, reduceret hornhindeperforation og bevaring eller forbedring af anatomisk integritet af øjets adnexa efter kemiske forbrændinger, navnlig alkaliforbrændinger.
7. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 6, hvor NK-1-antagonisten er aprepitant eller et farmaceutisk acceptabelt salt deraf.
8. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 6, hvor NK-1-antagonisten er fosaprepitant eller et farmaceutisk acceptabelt salt deraf.
9. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 6, hvor NK-1-antagonisten er befetupitant eller et farmaceutisk acceptabelt salt deraf.
10. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 6, hvor NK-1-antagonisten er lanepitant eller et farmaceutisk acceptabelt salt deraf.
11. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 10, hvor NK-1-antagonisten administreres i kombination, ad samme eller anden vej, med ét eller flere yderligere terapeutisk aktive midler.
12. Forbindelse til anvendelse ifølge krav 11, hvor det ene eller flere yderligere terapeutisk aktive midler indbefatter et antibakterielt middel, såsom et antibiotikum.
13. Forbindelse til anvendelse ifølge krav 11, hvor det ene eller flere yderligere terapeutisk aktive midler indbefatter et antiviralt middel.
DK12741268.2T 2011-07-04 2012-07-04 Nk-1-receptorantagonister til behandling af hornhindeneovaskularisering DK2729147T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161504265P 2011-07-04 2011-07-04
PCT/EP2012/063067 WO2013004766A1 (en) 2011-07-04 2012-07-04 Nk-1 receptor antagonists for treating corneal neovascularisation

Publications (1)

Publication Number Publication Date
DK2729147T3 true DK2729147T3 (da) 2017-12-18

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DK12741268.2T DK2729147T3 (da) 2011-07-04 2012-07-04 Nk-1-receptorantagonister til behandling af hornhindeneovaskularisering

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US (2) US9782397B2 (da)
EP (1) EP2729147B1 (da)
DK (1) DK2729147T3 (da)
ES (1) ES2672099T3 (da)
NO (1) NO2729147T3 (da)
WO (1) WO2013004766A1 (da)

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WO2019023175A1 (en) * 2017-07-25 2019-01-31 Gt Biopharma, Inc. PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE AND NEOSTIGMINE AND AN ANTAGONIST NK-1 FOR THE TREATMENT OF SEVERE MYASTHENIA
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Publication number Publication date
NO2729147T3 (da) 2018-02-03
US9782397B2 (en) 2017-10-10
EP2729147B1 (en) 2017-09-06
ES2672099T3 (es) 2018-06-12
US20180021327A1 (en) 2018-01-25
US20140128395A1 (en) 2014-05-08
WO2013004766A1 (en) 2013-01-10
EP2729147A1 (en) 2014-05-14

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