HRP20192010T1 - Muskarinski antagonisti i njihove kombinacije za liječenje bolesti dišnih puteva kod konja - Google Patents

Muskarinski antagonisti i njihove kombinacije za liječenje bolesti dišnih puteva kod konja Download PDF

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HRP20192010T1
HRP20192010T1 HRP20192010TT HRP20192010T HRP20192010T1 HR P20192010 T1 HRP20192010 T1 HR P20192010T1 HR P20192010T T HRP20192010T T HR P20192010TT HR P20192010 T HRP20192010 T HR P20192010T HR P20192010 T1 HRP20192010 T1 HR P20192010T1
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lama
halogen
alkyl
pharmaceutically acceptable
alkyloxy
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HRP20192010TT
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Balazs Albrecht
Michael Aven
Janine LAMAR
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Boehringer Ingelheim Vetmedica Gmbh
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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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/02—Medicinal preparations containing materials or reaction products thereof with undetermined constitution from inanimate materials
    • A61K35/04—Tars; Bitumens; Mineral oils; Ammonium bituminosulfonate
    • A61K35/06—Mineral oils, e.g. paraffinic oils or aromatic oils based on aromatic hydrocarbons
    • 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
    • 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
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • 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
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M15/00—Inhalators
    • A61M15/009—Inhalators using medicine packages with incorporated spraying means, e.g. aerosol cans
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M2250/00—Specially adapted for animals

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
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  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (12)

1. Dugodjelujući muskarinski antagonist (LAMA – engl. long-acting muscarinic antagonist) ili njegova farmaceutski prihvatljiva sol od kationa, naznačen time, da se upotrebljava u postupku liječenja bolesti dišnih puteva kod jednokopitara, poželjno konja, pri čemu je LAMA spoj opće formule: u kojoj A označava dvostruko vezanu skupinu odabranu između sljedećih: X- označava anion s jednostrukim negativnim nabojem; R1 i R2 označavaju C1-C4-alkil koji može biti opcionalno supstituiran s hidroksi ili halogenom; R3, R4, R5 i R6, koji mogu biti isti ili različiti, označavaju vodik, C1-C4-alkil, C1-C4-alkiloksi, hidroksi, CF3, CN, NO2 ili halogen; R7 označava vodik, C1-C4-alkil, C1-C4-alkiloksi, C1-C4-alkilen-halogen, halogen-C1-C4-alkiloksi, C1-C4-alkilen-OH, CF3, -C1-C4-alkilen-C1-C4-alkiloksi, -O-COC1-C4-alkil, OCOC1-C4-alkil-halogen, -O-COCF3 ili halogen, opcionalno u obliku njihovih pojedinačnih optičkih izomera, mješavina njihovih pojedinačnih enantiomera ili racemata, dok, u slučaju da A označava tada R1 i R2 označavaju metil i R3, R4, R5 i R6 označavaju vodik, a R7 ne može biti također vodik, poželjno, LAMA je spoj formule (LAMA 1):
2. Dugodjelujući muskarinski antagonist (LAMA) ili njegova farmaceutski prihvatljiva sol od kationa, ili farmaceutski pripravak koji sadrži LAMA ili njegovu farmaceutski prihvatljivu sol od kationa, naznačen time, da se u kombinaciji s glukokortikoidom kao što je ciklesonid ili budesonid ili s farmaceutskim pripravkom koji sadrži ciklesonid ili njegovu farmaceutski prihvatljivu sol, upotrebljava kao lijek kod jednokopitara kao što je konj, pri čemu je LAMA spoj opće formule: u kojoj A označava dvostruko vezanu skupinu odabranu od sljedećih: X- označava anion s jednostrukim negativnim nabojem; R1 i R2 označavaju C1-C4-alkil koji može biti opcionalno supstituiran s hidroksi ili halogenom; R3, R4, R5 i R6, koji mogu biti isti ili različiti, označavaju vodik, C1-C4-alkil, C1-C4-alkiloksi, hidroksi, CF3, CN, NO2 ili halogen; R7 označava vodik, C1-C4-alkil, C1-C4-alkiloksi, C1-C4-alkilen-halogen, halogen-C1-C4-alkiloksi, C1-C4-alkilen-OH, CF3, C1-C4-alkilen-C1-C4-alkiloksi, -O-COC1-C4-alkil, OCOC1-C4-alkil-halogen, -O-COCF3 ili halogen, opcionalno u obliku njihovih pojedinačnih optičkih izomera, mješavina od njihovih pojedinačnih enantiomera ili racemata, dok, u slučaju da A označava tada R1 i R2 označavaju metil i R3, R4, R5 i R6 označavaju vodik, a R7 ne može biti također vodik, poželjno, LAMA je spoj formule (LAMA 1):
3. Dugodjelujući muskarinski antagonist (LAMA) ili njegova farmaceutski prihvatljiva sol od kationa, ili farmaceutski pripravak koji sadrži LAMA ili njegovu farmaceutski prihvatljivu sol od kationa, naznačen time, da se u kombinaciji s glukokortikoidom kao što je ciklesonid ili s farmaceutskim pripravkom koji sadrži ciklesonid ili njegovu farmaceutski prihvatljivu sol, upotrebljava u postupku liječenja bolesti dišnih puteva kod jednokopitara, poželjno konja, pri čemu je LAMA spoj opće formule: u kojoj A označava a dvostruko vezanu skupinu odabranu od sljedećih: X- označava anion s jednostrukim negativnim nabojem; R1 i R2 označavaju C1-C4-alkil koji može biti opcionalno supstituiran s hidroksi ili halogenom; R3, R4, R5 i R6, koji mogu biti isti ili različiti, označavaju vodik, C1-C4-alkil, C1-C4-alkiloksi, hidroksi, CF3, CN, NO2 ili halogen; R7 označava vodik, C1-C4-alkil, C1-C4-alkiloksi, C1-C4-alkilen-halogen, halogen-C1-C4-alkiloksi, C1-C4-alkilen-OH, CF3, C1-C4-alkilen-C1-C4-alkiloksi, -O-COC1-C4-alkil, OCOC1-C4-alkil-halogen, -O-COCF3 ili halogen, opcionalno u obliku njihovih pojedinačnih optičkih izomera, mješavina od njihovih pojedinačnih enantiomera ili racemata, dok, u slučaju da A označava tada R1 i R2 označavaju metil i R3, R4, R5 i R6 označavaju vodik, a R7 ne može biti također vodik, poželjno, LAMA je spoj formule (LAMA 1):
4. LAMA za uporabu u skladu s patentnim zahtjevom 2 ili 3, naznačen time, da farmaceutski pripravak je farmaceutski pripravak koji sadrži LAMA ili njegove farmaceutski prihvatljive soli i glukokortikoid kao što je ciklesonid ili budesonid ili njihove farmaceutski prihvatljive soli i opcionalno beta-2-adrenoreceptor-agonist kao što je dugodjelujući beta-2-adrenergijski agonist (LABA – engl. long-acting beta agonist) ili njegove farmaceutski prihvatljive soli te opcionalno jedno farmaceutski prihvatljivo pomoćno sredstvo.
5. LAMA za uporabu u skladu s bilo kojim od patentnih zahtjeva 2 do 4, naznačen time, da su LAMA i glukokortikoid nadalje kombinirani s beta-2-adrenoreceptor-agonistom kao što je dugodjelujući beta-2-adrenergijski agonist (LABA) ili njegove farmaceutski prihvatljive soli.
6. LAMA za uporabu u skladu s bilo kojim od patentnih zahtjeva 1 i 3 do 5, naznačen time, da se kod bolesti dišnih puteva radi o plućnoj bolesti, prvenstveno je bolest dišnih puteva odabrana iz skupine koja se sastoji od sljedećih: periodična opstrukcija dišnih puteva (RAO – engl. recurrent airway obstruction), opstrukcijska plućna bolest povezana s ljetnom ispašom (SPAOPD – engl. summer pasture associated obstructive pulmonary disease) i upalna bolest dišnih puteva (IAD – engl. inflammatory airway disease).
7. LAMA za uporabu u skladu s bilo kojim od patentnih zahtjeva 1 do 6, naznačen time, da se navedeni LAMA ili farmaceutski pripravak koji sadrži LAMA, nalazi u tekućoj formulaciji koja je poželjno djelomično etanolska formulacija, dok navedena tekuća formulacija prvenstveno služi za inhalaciju.
8. LAMA za uporabu u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time, da se navedeni LAMA ili farmaceutski pripravak koji sadrži LAMA, primjenjuje preko inhalacijskog uređaja (za kopitare), pri čemu navedeni inhalacijski uređaj poželjno obuhvaća: a. inhalator s odmjerenom dozom pod tlakom ili vodeni/etanolski kapljični inhalator kao što je primjerice Respimat®-inhalator ili neki drugi inhalacijski uređaj koji koristi Respimat®-tehnologiju proizvodnje aerosola, i b. prilagodnu napravu za primjenu na kopitaru.
9. LAMA za uporabu u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da se LAMA 1 ili njegova farmaceutski prihvatljiva sol od kationa primjenjuje u iznosu jedne doze od 100 µg do 3000 µg izbačene iz inhalatora, od 200 µg do 2000 µg izbačene doze iz inhalatora, od 200 µg do 800 µg izbačene doze iz inhalatora, poželjno u iznosu jedne doze od 200 µg do 800 µg izbačene iz inhalatora.
10. LAMA za uporabu u skladu s bilo kojim od patentnih zahtjeva 2 do 8, naznačen time, da se ciklesonid ili farmaceutski pripravak koji sadrži ciklesonid ili njegovu farmaceutski prihvatljivu sol primjenjuje u iznosu jedne doze od 100 µg do 5000 µg izbačene iz inhalatora, od 450 µg do 3712,5 µg izbačene doze iz inhalatora, od 900 µg do 3712,5 µg izbačene doze iz inhalatora, poželjno u iznosu jedne doze od 900 µg do 3712,5 µg izbačene iz inhalatora.
11. LAMA za uporabu u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačen time, da se LAMA ili farmaceutski pripravak koji sadrži LAMA primjenjuje jednom ili dva puta dnevno, poželjno jednom dnevno.
12. LAMA za uporabu u skladu s bilo kojim od patentnih zahtjeva 1 do 11, naznačen time, da se koncentracija LAMA 1 nalazi u rasponu od 0,2 do 7% m/V, još poželjnije od 0,3 do 6,0% m/V ili od 0,4 do 5% m/V od ukupnog sastava pripravka.
HRP20192010TT 2014-06-18 2015-06-15 Muskarinski antagonisti i njihove kombinacije za liječenje bolesti dišnih puteva kod konja HRP20192010T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14172925 2014-06-18
EP15728025.6A EP3157522B1 (en) 2014-06-18 2015-06-15 Muscarinic antagonists and combinations thereof for the treatment of airway disease in horses
PCT/EP2015/063265 WO2015193213A1 (en) 2014-06-18 2015-06-15 Muscarinic antagonists and combinations thereof for the treatment of airway disease in horses

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US (3) US9474747B2 (hr)
EP (2) EP3157522B1 (hr)
KR (1) KR102618119B1 (hr)
AU (2) AU2015276310B2 (hr)
CA (1) CA2952701C (hr)
CY (1) CY1122335T1 (hr)
DK (1) DK3157522T3 (hr)
ES (1) ES2759247T3 (hr)
HR (1) HRP20192010T1 (hr)
HU (1) HUE051527T2 (hr)
LT (1) LT3157522T (hr)
MX (2) MX370430B (hr)
PL (1) PL3157522T3 (hr)
PT (1) PT3157522T (hr)
RS (1) RS59613B1 (hr)
SI (1) SI3157522T1 (hr)
WO (1) WO2015193213A1 (hr)

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CA2952701A1 (en) 2015-12-23
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MX2016016720A (es) 2017-04-13
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RS59613B1 (sr) 2020-01-31
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