Quinuclidine derivatives and medicinal compositions containing the same

• US 9,687,478 B2
• Filed: 04/09/2016
• Issued: 06/27/2017
• Est. Priority Date: 07/14/1999
• Status: Expired due to Fees

• Current Assignee: Almirall, S.A. (Grupo Corporativo Landon SL)
• Original Assignee: Almirall, S.A. (Grupo Corporativo Landon SL)
• Inventors: Prat Quinones, Maria, Fernandez Forner, Maria Dolors, Buil Albero, Maria Antonia
• Primary Examiner(s): Aulakh, Charanjit
• Application Number:
  US15/095,036
• Publication Number:
  US 20160296503A1
• Time in Patent Office: 444 Days
• Field of Search: 514305, 514826
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/439 the ring forming part of a bridged ring system, e.g. quinuclidine 8-azabicyclo [3.2.1] octanes A61K31/46
• CPC Class Codes: A61K 31/4745 condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/26 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
• CPC Class Codes: A61K 9/0073 Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M
• CPC Class Codes: A61K 9/0075 for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 1/06 Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
• CPC Class Codes: A61P 1/12 Antidiarrhoeals
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 11/08 Bronchodilators
• CPC Class Codes: A61P 11/14 Antitussive agents
• CPC Class Codes: A61P 13/00 Drugs for disorders of the urinary system
• CPC Class Codes: A61P 13/02 of urine or of the urinary tract, e.g. urine acidifiers
• CPC Class Codes: A61P 13/06 Anti-spasmodics
• CPC Class Codes: A61P 13/10 : of the bladder
• CPC Class Codes: A61P 27/16 : Otologicals
• CPC Class Codes: A61P 43/00 : Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 453/02 : containing not further condensed quinuclidine ring systems

Abstract

Provided is an aerosol container comprising a powder inhalant comprising 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane wherein an anion X⁻ is associated with the positive charge of the nitrogen atom and wherein X⁻ is a pharmaceutically acceptable anion of a mono- or polyvalent acid.

Claims

1. An aerosol container comprising a powder inhalant comprising 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane wherein an anion X⁻

is associated with the positive charge of the nitrogen atom and wherein X⁻

is a pharmaceutically acceptable anion of a mono- or polyvalent acid.

2. The aerosol container of claim 1, wherein the powder inhalant further comprises a pharmaceutically acceptable carrier or diluent.

3. The aerosol container of claim 2, wherein the pharmaceutically acceptable carrier or diluent of the powder inhalant is lactose.

4. The aerosol container of claim 1, wherein the powder inhalant further comprises a β

₂ agonist.

5. The aerosol container of claim 4, wherein the powder inhalant further comprises a steroid or a phosphodiesterase IV inhibitor.

6. The aerosol container of claim 1, wherein the powder inhalant further comprises a steroid.

7. The aerosol container of claim 6, wherein the powder inhalant further comprises a phosphodiesterase IV inhibitor.

8. The aerosol container of claim 1, wherein the powder inhalant further comprises a phosphodiesterase IV inhibitor.

9. A method for treating chronic obstructive pulmonary disease, chronic bronchitis, bronchial hyperreactivity, asthma, or rhinitis which method comprises use of an aerosol container of claim 1 to administer to a human or animal patient in need of such treatment an effective amount of the powder inhalant of claim 1.

10. The method of claim 9 further comprising administering an effective amount of a β

₂ agonist.

11. The method of claim 10 further comprising administering an effective amount of a steroid or a phosphodiesterase IV inhibitor.

12. The method of claim 9 further comprising administering an effective amount of a steroid.

13. The method of claim 12 further comprising administering an effective amount of a phosphodiesterase IV inhibitor.

14. The method of claim 9 further comprising administering an effective amount of a phosphodiesterase IV inhibitor.