Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the ß2 adrenergic receptor

摘要

The present invention provides a compound of formula (I):
wherein:
€¢ R 1 is a group selected from -CH 2 OH, -NHC(O)H and
€¢ R 2 is a hydrogen atom; or
€¢ R 1 together with R 2 form the group -NH-C(O)-CH=CH- wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R 1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R 2
€¢ R 3 is selected from hydrogen and halogen atoms or groups selected from -SO-R 5 , -SO 2 -R 5 , -NH-CO-NH 2 , -CO-NH 2 , hydantoino, C 1-4 alkyl, C 1-4 alkoxy and -SO 2 NR 5 R 6
€¢ R 4 is selected from hydrogen atoms, halogen atoms and C 1-4 alkyl groups
€¢ R 5 is a C 1-4 alkyl group or C 3-8 cycloalkyl
€¢ R 6 is independently selected from hydrogen atoms and C 1-4 alkyl groups
€¢ n, p and q are independently 0, 1, 2, 3 or 4
€¢ m and s are independently 0, 1, 2 or 3
€¢ r is 0, 1 or 2
with the provisos that:
€¢ at least one of m and r is not 0
€¢ the sum n+m+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13
€¢ the sum q+r+s is 2, 3, 4, 5 or 6
or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof.