EA201791579A1 - Соединения, обладающие активностью антагонистов мускариновых рецепторов и агонистов бета-2 адренергических рецепторов - Google Patents

Соединения, обладающие активностью антагонистов мускариновых рецепторов и агонистов бета-2 адренергических рецепторов

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Publication number
EA201791579A1
EA201791579A1 EA201791579A EA201791579A EA201791579A1 EA 201791579 A1 EA201791579 A1 EA 201791579A1 EA 201791579 A EA201791579 A EA 201791579A EA 201791579 A EA201791579 A EA 201791579A EA 201791579 A1 EA201791579 A1 EA 201791579A1
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Eurasian Patent Office
Prior art keywords
receptors
agonists
antagonists
beta
activity
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EA201791579A
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EA032937B1 (ru
EA032937B9 (ru
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Фабио РАНКАТИ
Андреа Рицци
Лаура КАРЦАНИГА
Йен Линней
Крис Найт
Вольфганг Шмидт
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КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А.
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Application filed by КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. filed Critical КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А.
Publication of EA201791579A1 publication Critical patent/EA201791579A1/ru
Publication of EA032937B1 publication Critical patent/EA032937B1/ru
Publication of EA032937B9 publication Critical patent/EA032937B9/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/20—Oxygen atoms
    • C07D215/24—Oxygen atoms attached in position 8
    • C07D215/26—Alcohols; Ethers thereof
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
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    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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    • 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
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
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    • C07—ORGANIC CHEMISTRY
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    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C07D453/04—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems having a quinolyl-4, a substituted quinolyl-4 or a alkylenedioxy-quinolyl-4 radical linked through only one carbon atom, attached in position 2, e.g. quinine
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    • C07D498/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Otolaryngology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Quinoline Compounds (AREA)

Abstract

Настоящее изобретение относится к соединениям, действующим как в качестве антагонистов мускариновых рецепторов, так и в качестве агонистов бета-2 адренергических рецепторов, к способам их получения, к композициям, содержащим их, к терапевтическим применениям и комбинациям с другими фармацевтическими активными ингредиентами.
EA201791579A 2015-02-12 2016-02-10 Соединения, обладающие активностью антагонистов мускариновых рецепторов и агонистов бета-2 адренергических рецепторов EA032937B9 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15154917 2015-02-12
PCT/EP2016/052812 WO2016128456A1 (en) 2015-02-12 2016-02-10 Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity

Publications (3)

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EA201791579A1 true EA201791579A1 (ru) 2018-02-28
EA032937B1 EA032937B1 (ru) 2019-08-30
EA032937B9 EA032937B9 (ru) 2019-11-27

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EA201791579A EA032937B9 (ru) 2015-02-12 2016-02-10 Соединения, обладающие активностью антагонистов мускариновых рецепторов и агонистов бета-2 адренергических рецепторов

Country Status (26)

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US (2) US9579314B2 (ru)
EP (1) EP3256464B1 (ru)
JP (1) JP6905466B2 (ru)
KR (1) KR20170115069A (ru)
CN (1) CN107207473B (ru)
AR (1) AR103666A1 (ru)
AU (1) AU2016217955B2 (ru)
BR (1) BR112017017296A2 (ru)
CA (1) CA2976150A1 (ru)
CL (1) CL2017002017A1 (ru)
CO (1) CO2017008031A2 (ru)
EA (1) EA032937B9 (ru)
ES (1) ES2916924T3 (ru)
GE (1) GEP20207098B (ru)
IL (1) IL253922B (ru)
MA (1) MA41492A (ru)
MX (1) MX369348B (ru)
PE (1) PE20171347A1 (ru)
PH (1) PH12017501424A1 (ru)
PL (1) PL3256464T3 (ru)
SG (1) SG11201706455QA (ru)
TN (1) TN2017000346A1 (ru)
TW (1) TWI703138B (ru)
UA (1) UA124138C2 (ru)
WO (1) WO2016128456A1 (ru)
ZA (1) ZA201705376B (ru)

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SG11202010115RA (en) 2018-05-15 2020-11-27 Alkahest Inc Treatment of aging-associated disease with modulators of leukotriene a4 hydrolase
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JP6905466B2 (ja) 2021-07-21
JP2018510137A (ja) 2018-04-12
MX2017010366A (es) 2018-01-23
CO2017008031A2 (es) 2017-11-10
WO2016128456A1 (en) 2016-08-18
SG11201706455QA (en) 2017-09-28
AR103666A1 (es) 2017-05-24
MA41492A (fr) 2021-04-28
US10004728B2 (en) 2018-06-26
CN107207473A (zh) 2017-09-26
PL3256464T3 (pl) 2022-07-18
US20170119753A1 (en) 2017-05-04
PH12017501424B1 (en) 2018-01-15
TWI703138B (zh) 2020-09-01
AU2016217955A1 (en) 2017-08-31
CN107207473B (zh) 2020-07-07
ZA201705376B (en) 2018-12-19
US9579314B2 (en) 2017-02-28
EA032937B1 (ru) 2019-08-30
UA124138C2 (uk) 2021-07-28
CA2976150A1 (en) 2016-08-18
ES2916924T3 (es) 2022-07-06
US20160235734A1 (en) 2016-08-18
IL253922B (en) 2019-11-28
MX369348B (es) 2019-11-06
PH12017501424A1 (en) 2018-01-15
GEP20207098B (en) 2020-04-10
CL2017002017A1 (es) 2018-04-13
EA032937B9 (ru) 2019-11-27
EP3256464B1 (en) 2022-05-11
AU2016217955B2 (en) 2020-03-05
EP3256464A1 (en) 2017-12-20
PE20171347A1 (es) 2017-09-13
KR20170115069A (ko) 2017-10-16
BR112017017296A2 (pt) 2018-04-10
IL253922A0 (en) 2017-10-31
TN2017000346A1 (en) 2019-01-16
TW201636338A (zh) 2016-10-16

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