M3 Muscarinic Acetylcholine Receptor Antagonists
AssigneeGlaxo Group Limited
InventorsZEHONG WAN, HONGXING YAN, MICHAEL R. PALOVICH, DRAMANE I. LAINE
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Abstract
Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
Claims19
A method of inhibiting the binding of acetylcholine to a acetylcholine receptor in the respiratory tract of a mammal in need thereof, which comprises contacting the acetylcholine receptor with an effective amount of a compound of formula (I)
- wherein:
- R1− represents an anion associated with the positive charge of the N atom;
- R2 is aryl;
- R3 is (C1-C6)alkyl-O-(C1-C6)aryl,
- via inhalation by the mouth or nose of the mammal.
A method of inhibiting the binding of acetylcholine to an M3 muscarinic acetylcholine receptor in the respiratory tract of a mammal in need thereof, which comprises contacting the M3 muscarinic acetylcholine receptor with an effective amount of a compound of formula (I)
- wherein:
- R1− represents an anion associated with the positive charge of the N atom;
- R2 is aryl;
- R3 is (C1-C6)alkyl-O-(C1-C6)aryl, via inhalation by the mouth or nose of the mammal:
The method according to claim 13 wherein the binding of the M3 muscarinic acetylcholine receptor is useful in the treatment of chronic obstructive lung disease, chronic bronchitis, asthma, chronic respiratory obstruction, pulmonary fibrosis, pulmonary emphysema or allergic rhinitis.
The method according to claim 13 wherein the compound of formula (I) is N-(Endo)-(3-endo)-(2-cyano-2,2-diphenylethyl)-(8-endo)-methyl-8-{2-[(phenylmethyl)oxy]ethyl}-8-azoniabicyclo[3.2.1]octane and a pharmaceutically acceptable anion thereof.
The method according claim 13 wherein the compound of formula (I) is N-(Endo)-(3-endo)-(2-cyano-2,2-diphenylethyl)-(8-endo)-methyl-8-{2-[(phenylmethyl)oxy]ethyl}-8-azoniabicyclo[3.2.1]octane bromide.
A method of treating chronic obstructive lung disease, chronic bronchitis, asthma, chronic respiratory obstruction, pulmonary fibrosis, pulmonary emphysema or allergic rhinitis in a human in need thereof, comprising administering to said human by inhalation via the mouth or nose, an effective amount of a compound of formula (I)
- wherein:
- R1− represents an anion associated with the positive charge of the N atom;
- R2 is aryl;
- R3 is (C1-C6)alkyl-O-(C1-C6)aryl.
Dependencies are inferred from the claim text.