HRP20201435T1 - Spojevi koji imaju aktivnost kao antagonist muskarinskog receptora i kao agonist beta2 adrenergijskog receptora - Google Patents

Spojevi koji imaju aktivnost kao antagonist muskarinskog receptora i kao agonist beta2 adrenergijskog receptora Download PDF

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Publication number
HRP20201435T1
HRP20201435T1 HRP20201435TT HRP20201435T HRP20201435T1 HR P20201435 T1 HRP20201435 T1 HR P20201435T1 HR P20201435T T HRP20201435T T HR P20201435TT HR P20201435 T HRP20201435 T HR P20201435T HR P20201435 T1 HRP20201435 T1 HR P20201435T1
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Croatia
Prior art keywords
inhibitors
formula
image
compound
group
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HRP20201435TT
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English (en)
Inventor
Fabio Rancati
Ian Linney
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Chiesi Farmaceutici S.P.A.
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Publication of HRP20201435T1 publication Critical patent/HRP20201435T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/12Aerosols; Foams
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES 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
    • A61M11/00Sprayers or atomisers specially adapted for therapeutic purposes
    • A61M11/005Sprayers or atomisers specially adapted for therapeutic purposes using ultrasonics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES 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
    • A61M15/00Inhalators
    • A61M15/0028Inhalators using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up
    • A61M15/003Inhalators using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up using capsules, e.g. to be perforated or broken-up
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES 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
    • A61M15/00Inhalators
    • A61M15/0028Inhalators using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up
    • A61M15/0045Inhalators using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up using multiple prepacked dosages on a same carrier, e.g. blisters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES 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
    • A61M15/00Inhalators
    • A61M15/0065Inhalators with dosage or measuring devices
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES 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
    • A61M15/00Inhalators
    • A61M15/009Inhalators using medicine packages with incorporated spraying means, e.g. aerosol cans
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES 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
    • A61M16/00Devices for influencing the respiratory system of patients by gas treatment, e.g. mouth-to-mouth respiration; Tracheal tubes
    • A61M16/10Preparation of respiratory gases or vapours
    • A61M16/14Preparation of respiratory gases or vapours by mixing different fluids, one of them being in a liquid phase
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES 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
    • A61M2202/00Special media to be introduced, removed or treated
    • A61M2202/06Solids
    • A61M2202/064Powder
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Pulmonology (AREA)
  • Organic Chemistry (AREA)
  • Anesthesiology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Dispersion Chemistry (AREA)
  • Biophysics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Hydrogenated Pyridines (AREA)

Claims (7)

1. Spoj opće formule I [image] pri čemu Q je skupina formule Q1 [image] Z je H ili OH; Y je odabran od Y’ i Y1 koje su dvovalentne skupine formule [image] ili [image] pri čemu A1 je butilen; A2 nedostaje ili je (C1-C6)alkilen; B je odabran iz skupine koju čine pirazoldiil i tiofendiil, opcionalno supstituiran jednom ili više skupina odabranih od metilne; C je -OC(O)- ili je C1 [image] pri čemu R4 jest H; D nedostaje; n’ je 1; E je -O-; G je fenilen; R1 i R2 neovisno jesu H ili aril; R3 je skupina formule J1 ili J2 [image] gdje je R5 skupina formule K [image] pri čemu p’ jest 0 ili 1, P nedostaje ili je CO, q nedostaje ili je 1 i W jest heteroaril, te farmaceutski prihvatljive soli ili njihovi solvati.
2. Farmaceutski pripravak koji sadrži spoj formule I kao što je definiran u patentnom zahtjevu 1, s jednim ili više farmaceutski prihvatljivih nosača i/ili ekscipijensa.
3. Spoj formule I prema patentnom zahtjevu I za upotrebu u prevenciji i/ili liječenju bronhoopstruktivnih ili upalnih bolesti.
4. Spoj za upotrebu prema patentnom zahtjevu 3, naznačeno time da bronhoopstruktivne ili upalne bolesti jesu astma ili kronični bronhitis ili kronična opstruktivna plućna bolest (COPD).
5. Kombinacija spoja formule I kao što je definirano u patentnom zahtjevu 1 s jednim ili više aktivnih sastojaka odabranih iz klasa koje čine beta2 agonisti, antimuskarinska sredstva, inhibitori mitogenom aktiviranih proteinskih kinaza (P38 MAP kinaza), inihibitori beta-podjedinice kapa-B kinaze (IKK2) nuklearnog faktora, inhibitori humane neutrofilne elastaze (HNE), inhibitori fosfodiesteraze 4 (PDE4), modulatori leukotriena, nesteroidna protuupalna sredstva (NSAIDs), antitusivna sredstva, regulatori mukusa, mukolitici, ekspektoranski/mukokinetički modulatori, peptidni mukolitici, antibiotici, inhibitori JAK, inhibitori SYK, inhibitori PI3Kdelta ili PI3Kgama, kortikosteroidi i M3-antagonisti/PDE4-inhibitori (MAPI).
6. Farmaceutski pripravak prema patentnom zahtjevu 2 koji se daje inhalacijom, kao što su prašci za inhalaciju, mjerni aerosoli koji sadrže propelant ili formulacije za inhalaciju bez propelanta.
7. Uređaj koji sadrži farmaceutski pripravak prema patentnom zahtjevu 6, koji može biti inhalator jedinične doze ili višestruke doze suhog praška, inhalator s odmjerenom dozom i nebulizer magličastog raspršenja.
HRP20201435TT 2012-12-06 2020-09-09 Spojevi koji imaju aktivnost kao antagonist muskarinskog receptora i kao agonist beta2 adrenergijskog receptora HRP20201435T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12195891 2012-12-06
EP18156043.4A EP3345904B1 (en) 2012-12-06 2013-12-05 Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity

Publications (1)

Publication Number Publication Date
HRP20201435T1 true HRP20201435T1 (hr) 2020-11-27

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Family Applications (2)

Application Number Title Priority Date Filing Date
HRP20180915TT HRP20180915T1 (hr) 2012-12-06 2018-06-13 Spojevi koji imaju aktivnost kao antagonist muskarinskog receptora i kao agonist beta2 adrenergijskog receptora
HRP20201435TT HRP20201435T1 (hr) 2012-12-06 2020-09-09 Spojevi koji imaju aktivnost kao antagonist muskarinskog receptora i kao agonist beta2 adrenergijskog receptora

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HRP20180915TT HRP20180915T1 (hr) 2012-12-06 2018-06-13 Spojevi koji imaju aktivnost kao antagonist muskarinskog receptora i kao agonist beta2 adrenergijskog receptora

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US (2) US8987299B2 (hr)
EP (2) EP2928889B1 (hr)
JP (1) JP6421989B2 (hr)
KR (2) KR102156443B1 (hr)
CN (1) CN104822678B (hr)
AR (1) AR093825A1 (hr)
AU (1) AU2013354043C1 (hr)
BR (1) BR112015012730B1 (hr)
CA (1) CA2893626C (hr)
CL (1) CL2015001483A1 (hr)
CO (1) CO7400870A2 (hr)
CY (2) CY1120159T1 (hr)
DK (2) DK2928889T3 (hr)
EA (1) EA030552B1 (hr)
ES (2) ES2670686T3 (hr)
GE (1) GEP20186839B (hr)
HK (1) HK1212989A1 (hr)
HR (2) HRP20180915T1 (hr)
HU (2) HUE051394T2 (hr)
IL (1) IL239182B (hr)
LT (2) LT3345904T (hr)
MA (1) MA38147B1 (hr)
MX (1) MX369311B (hr)
NZ (1) NZ708738A (hr)
PE (1) PE20151216A1 (hr)
PH (1) PH12015501247A1 (hr)
PL (2) PL2928889T3 (hr)
PT (2) PT2928889T (hr)
RS (2) RS57232B1 (hr)
SA (1) SA515360514B1 (hr)
SG (2) SG10201704032RA (hr)
SI (2) SI2928889T1 (hr)
TN (1) TN2015000244A1 (hr)
TR (1) TR201808698T4 (hr)
TW (1) TWI637954B (hr)
UA (1) UA118181C2 (hr)
WO (1) WO2014086924A1 (hr)
ZA (1) ZA201503965B (hr)

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GEP20186839B (en) 2018-04-10
WO2014086924A1 (en) 2014-06-12
KR20200027049A (ko) 2020-03-11
JP2016502557A (ja) 2016-01-28
CO7400870A2 (es) 2015-09-30
CY1123365T1 (el) 2021-12-31
PT2928889T (pt) 2018-05-29
ZA201503965B (en) 2016-09-28
AR093825A1 (es) 2015-06-24
MA38147A1 (fr) 2018-03-30
CA2893626C (en) 2021-08-24
SI3345904T1 (sl) 2020-09-30
NZ708738A (en) 2019-02-22
JP6421989B2 (ja) 2018-11-14
KR102156443B1 (ko) 2020-09-17
HRP20180915T1 (hr) 2018-07-27
ES2670686T3 (es) 2018-05-31
HK1212989A1 (zh) 2016-06-24
CL2015001483A1 (es) 2015-10-23
PT3345904T (pt) 2020-09-07
PL3345904T3 (pl) 2020-12-14
EA030552B1 (ru) 2018-08-31
AU2013354043C1 (en) 2017-08-31
RS60864B1 (sr) 2020-11-30
US20150133491A1 (en) 2015-05-14
MX2015006788A (es) 2015-08-05
PH12015501247B1 (en) 2015-08-17
IL239182A0 (en) 2015-07-30
TW201427976A (zh) 2014-07-16
EP2928889A1 (en) 2015-10-14
SG10201704032RA (en) 2017-06-29
TN2015000244A1 (en) 2016-10-03
KR20150090108A (ko) 2015-08-05
PH12015501247A1 (en) 2015-08-17
AU2013354043B2 (en) 2017-06-15
MA38147B1 (fr) 2018-09-28
PE20151216A1 (es) 2015-09-08
EP3345904A1 (en) 2018-07-11
SI2928889T1 (en) 2018-05-31
EP2928889B1 (en) 2018-03-21
KR102240459B1 (ko) 2021-04-16
EA201590873A1 (ru) 2015-09-30
CY1120159T1 (el) 2018-12-12
RS57232B1 (sr) 2018-07-31
US8987299B2 (en) 2015-03-24
ES2816210T3 (es) 2021-03-31
SG11201504318UA (en) 2015-07-30
BR112015012730B1 (pt) 2022-07-05
US9371318B2 (en) 2016-06-21
LT3345904T (lt) 2020-09-25
MX369311B (es) 2019-11-05
CN104822678B (zh) 2017-03-08
US20140161736A1 (en) 2014-06-12
CA2893626A1 (en) 2014-06-12
TR201808698T4 (tr) 2018-07-23
UA118181C2 (uk) 2018-12-10
EP3345904B1 (en) 2020-07-29
BR112015012730A2 (pt) 2017-07-11
DK3345904T3 (da) 2020-08-31
IL239182B (en) 2018-12-31
HUE051394T2 (hu) 2021-03-01
TWI637954B (zh) 2018-10-11
DK2928889T3 (en) 2018-05-22
SA515360514B1 (ar) 2016-08-30
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LT2928889T (lt) 2018-06-11
CN104822678A (zh) 2015-08-05

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