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HK1198120A1 - Combinations comprising antimuscarininc agents and beta-adrenergic agonists - Google Patents

Combinations comprising antimuscarininc agents and beta-adrenergic agonists Download PDF

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Publication number
HK1198120A1
HK1198120A1 HK14110614.9A HK14110614A HK1198120A1 HK 1198120 A1 HK1198120 A1 HK 1198120A1 HK 14110614 A HK14110614 A HK 14110614A HK 1198120 A1 HK1198120 A1 HK 1198120A1
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HK
Hong Kong
Prior art keywords
agonist
antagonist
combination
muscarinic receptors
formoterol
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HK14110614.9A
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English (en)
French (fr)
Chinese (zh)
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HK1198120B (en
Inventor
Jordi Gras Escardo
Jesus Llenas Calvo
Hamish Ryder
Pio Orviz Diaz
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Almirall S.A.
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Application filed by Almirall S.A. filed Critical Almirall S.A.
Publication of HK1198120A1 publication Critical patent/HK1198120A1/en
Publication of HK1198120B publication Critical patent/HK1198120B/en

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    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
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    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
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    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
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    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
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    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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    • A61K31/655—Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Claims (23)

  1. Kombination, die umfasst: (a) einen β2-Agonisten und (b) einen Antagonisten von muskarinischen M3-Rezeptoren, der 3(R)-(2-Hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octan ist, in der Form eines Salzes, das ein Anion X, welches ein pharmazeutisch verträgliches Anion einer ein- oder mehrwertigen Säure ist, aufweist.
  2. Kombination nach Anspruch 1, wobei der Antagonist von muskarinischen M3-Rezeptoren (b) 3(R)-(2-Hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octan-bromid ist.
  3. Kombination nach Anspruch 1 oder 2, wobei der β2-Agonist ein lange wirkender β2-Agonist ist.
  4. Kombination nach einem der Ansprüche 1 bis 3, wobei der β2-Agonist ausgewählt ist aus der Gruppe, umfassend Arformoterol, Bambuterol, Bitolterol, Broxaterol, Carbuterol, Clenbuterol, Dopexamin, Fenoterol, Formoterol, Hexoprenalin, Ibuterol, Isoprenalin, Levosalbutamol, Mabuterol, Meluadrin, Nolomirol, Orciprenalin, Pirbuterol, Procaterol, (R,R)-Formoterol, Reproterol, Ritodrin, Rimoterol, Salbutamol, Salmeterol, Sibenadet, Sulfonterol, Terbutalin, Tulobuterol, GSK-597901, GSK-159797, KUL-1248, TA-2005 und QAB-149, gegebenenfalls in der Form von ihren Racematen, ihren Enantiomeren, ihren Diastereomeren und Gemischen davon und gegebenenfalls ihrer pharmakologisch verträglichen Säureadditionssalze.
  5. Kombination nach Anspruch 3 oder 4, wobei der β2-Agonist ausgewählt ist aus der Gruppe, umfassend Formoterol, Salmeterol und QAB-149, gegebenenfalls in der Form von ihren Racematen, ihren Enantiomeren, ihren Diastereomeren und Gemischen davon, und gegebenenfalls ihrer pharmakologisch verträglichen Säureadditionssalze.
  6. Kombination nach Anspruch 5, wobei der β2-Agonist Formoterolfumarat ist.
  7. Kombination nach Anspruch 5, wobei der β2-Agonist Salmeterolxinafoat ist.
  8. Kombination nach einem der vorstehenden Ansprüche, dadurch gekennzeichnet, dass die aktiven Ingredienzien (a) und (b) einen Teil einer einzigen pharmazeutischen Zusammensetzung bilden.
  9. Kombination nach einem der vorstehenden Ansprüche, die des Weiteren umfasst: (c) eine weitere aktive Verbindung, ausgewählt aus: (i) PDE-IV-Inhibitoren, (ii) Corticosteroiden, (iii) Leukotrien-D4-Antagonisten, (iv) Inhibitoren von egfr-Kinase, (v) p38-Kinase-Inhibitoren und (vi) NK1-Rezeptor-Agonisten.
  10. Kombination nach Anspruch 9, wobei die aktive Verbindung (c) ausgewählt ist aus der Gruppe, bestehend aus (i) PDE-IV-Inhibitoren und (b) Corticosteroiden.
  11. Verwendung von (a) einem β2-Agonisten, wie in einem der Ansprüche 1 und 3 bis 7 definiert, und (b) einem Antagonisten von muskarinischen M3-Rezeptoren, wie in Anspruch 1 oder 2 definiert, für die Herstellung eines Medikaments zur simultanen, gleichzeitigen bzw. gleichlaufenden, getrennten oder sequentiellen Verwendung bei der Behandlung einer Atemwegserkrankung, die Asthma, akute oder chronische Bronchitis, Emphysem, chronisch-obstruktive Lungenerkrankung (COPD), Bronchialhyperreaktivität oder Rhinitis ist, bei einem Patienten.
  12. Verwendung nach Anspruch 11, wobei die Atemwegserkrankung Asthma oder chronisch-obstruktive Lungenerkrankung (COPD) ist.
  13. Verwendung nach Anspruch 11 oder 12, wobei der Patient an einer vorher existierenden Herzerkrankung oder einer Erkrankung, die durch Tachykardie verschlimmert würde, leidet.
  14. Produkt, umfassend: (a) einen β2-Agonisten, wie in einem der Ansprüche 1 und 3 bis 7 definiert, und (b) einen Antagonisten von muskarinischen M3-Rezeptoren, wie in Anspruch 1 oder 2 definiert, als Kombinationspräparat für die simultane, gleichzeitige bzw. gleichlaufende, getrennte oder sequentielle Verwendung bei der Behandlung eines Patienten, der an einer Atemwegserkrankung, wie in Anspruch 11 oder 12 definiert, leidet oder dafür anfällig ist.
  15. Produkt zur Verwendung nach Anspruch 14, das außerdem eine aktive Verbindung (c), wie in Anspruch 9 oder 10 definiert, umfasst.
  16. Kit von Komponenten, umfassend: (b) einen Antagonisten von muskarinischen M3-Rezeptoren, wie in Anspruch 1 oder 2 definiert, zusammen mit Anweisungen für die simultane, gleichzeitige bzw. gleichlaufende, getrennte oder sequentielle Verwendung in Kombination mit (a) einem β2-Agonisten, wie in einem der Ansprüche 1 und 3 bis 7 definiert, für die Behandlung eines Patienten, der an einer Atemwegserkrankung, wie in Anspruch 11 oder 12 definiert, leidet oder dafür anfällig ist.
  17. Kit zur Verwendung nach Anspruch 17, der außerdem eine aktive Verbindung (c), wie in Anspruch 9 oder 10 definiert, umfasst.
  18. Packung, umfassend: (b) einen Antagonisten von muskarinischen M3-Rezeptoren, wie in Anspruch 1 oder 2 definiert, und (a) einen β2-Agonisten, wie in einem der Ansprüche 1 und 3 bis 7 definiert, für die simultane, gleichzeitige bzw. gleichlaufende, getrennte oder sequentielle Verwendung bei der Behandlung einer Atemwegserkrankung, wie in Anspruch 11 oder 12 definiert.
  19. Packung zur Verwendung nach Anspruch 18, die außerdem eine aktive Verbindung (c), wie in Anspruch 9 oder 10 definiert, umfasst.
  20. Antagonist von muskarinischen M3-Rezeptoren, wie in Anspruch 1 oder 2 definiert, für die simultane, gleichzeitige bzw. gleichlaufende, getrennte oder sequentielle Verwendung in Kombination mit einem β2-Agonisten, wie in einem der Ansprüche 1 und 3 bis 7 definiert, für die Behandlung einer Atemwegserkrankung, wie in Anspruch 11 oder 12 definiert.
  21. Antagonist von muskarinischen M3-Rezeptoren zur Verwendung nach Anspruch 20, wobei der Patient an einer vorher existierenden Herzerkrankung oder einer Erkrankung, die durch Tachykardie verschlimmert würde, leidet.
  22. β2-Agonist, wie in einem der Ansprüche 1 und 3 bis 7 definiert, zur simultanen, gleichzeitigen bzw. gleichlaufenden, getrennten oder sequentiellen Verwendung in Kombination mit einem Antagonisten von muskarinischen M3-Rezeptoren, wie in Anspruch 1 oder 2 definiert, für die Behandlung einer Atemwegserkrankung, wie in Anspruch 11 oder 12 definiert.
  23. β2-Agonist für eine Verwendung nach Anspruch 22, wobei der Patient an einer vorher existierenden Herzerkrankung oder einer Erkrankung, die durch Tachykardie verschlimmert würde, leidet.
HK14110614.9A 2004-05-31 2014-10-23 Combinations comprising antimuscarininc agents and beta-adrenergic agonists HK1198120B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ES200401312A ES2257152B1 (es) 2004-05-31 2004-05-31 Combinaciones que comprenden agentes antimuscarinicos y agonistas beta-adrenergicos.
ES200401312 2004-05-31

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HK1198120A1 true HK1198120A1 (en) 2015-03-13
HK1198120B HK1198120B (en) 2015-09-11

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