Substituted pyrimidines for treatment of acute cough, chronic cough and urge to cough
AssigneeAfferent Pharmaceuticals, Inc.
InventorsAnthony P. Ford, Bruce G. McCarthy
Life of this patent
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Abstract
Methods for treating cough, chronic cough and urges to cough associated with respiratory diseases with a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are as defined herein.
Claims20
A method for treating chronic cough in a patient in need thereof, the method comprising administering to said patient an effective amount of a compound of Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is hydrogen or C1-C6 alkyl optionally substituted with cycloalkyl, halo, nitro, cyano, hydroxy, alkoxy, amino, acylamino, mono-alkylamino, di-alkylamino, haloalkoxy, heteroalkyl, —COR wherein R is hydrogen, alkyl, phenyl or phenylalkyl, —(CR′R″)n—COOR wherein n is 0, 1, 2, 3, 4 or 5, R′ and R″ are independently hydrogen or alkyl, and R is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenyl or phenylalkyl, or —(CR′R″)n—CONRaRb wherein n is 0, 1, 2, 3, 4 or 5, R′ and R″ are independently hydrogen or alkyl, and Ra and Rb are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenyl or phenylalkyl;
- and
- R2 is alkyl, alkenyl, alkynyl, amino, aminosulfonyl, halo, amido, alkoxy, hydroxy, haloalkoxy, nitro, hydroxyalkyl, alkoxyalkyl, hydroxyalkoxy, alkynylalkoxy, alkylsulfonyl, arylsulfonyl, carboxyalkyl, cyano or alkylcarbonyl.
The method of claim h wherein the compound of Formula (I) is administered at about 600 mg twice daily.
A method for treating neuronal hypersensitivity underlying acute, sub-acute, or chronic cough in a patient in need thereof, the method comprising administering to said patient an effective amount of a compound of Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is hydrogen or C1-C6 alkyl optionally substituted with cycloalkyl, halo, nitro, cyano, hydroxy, alkoxy, amino, acylamino, mono-alkylamino, di-alkylamino, haloalkoxy, heteroalkyl, —COR wherein R is hydrogen, alkyl, phenyl or phenylalkyl, —(CR′R″)n—COOR wherein n is 0, 1, 2, 3, 4 or 5, R′ and R″ are independently hydrogen or alkyl, and R is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenyl or phenylalkyl, —(CR′R″)n—CONRaRb wherein n is 0, 1, 2, 3, 4 or 5, R′ and R″ are independently hydrogen or alkyl, and Ra and Rb are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenyl or phenylalkyl;
- and
- R2 is alkyla alkenyl, alkynyl, amino, aminosulfonyl, halo, amido, haloalkyl, alkoxy, hydroxy, haloalkoxy, nitro, hydroxyalkyl, alkoxyalkyl, hydroxyalkoxy, alkynylalkoxy, alkylsulfonyl, arylsulfonyl, carboxyalkyl, cyano or alkylcarbonyl.
A method for treating chronic cough in a patient in need thereof, the method comprising administering to said patient an effective amount of a compound is selected from:
Dependencies are inferred from the claim text.