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US 8,420,669 B2Granted
Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the BETA2 adrenergic receptor
AssigneeLaboratories Almirall, S.A.
InventorsCarlos Puig Duran, Maria Isabel Crespo Crespo, Julio Cesar Castro Palomino Laria, Silvia Gual Roig, Eloisa Navarro Romero
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Abstract
The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the BETA2 adrenergic receptor.
Claims6
A method of treating a pulmonary disease in a mammal comprising administering to the mammal a therapeutically effective amount of a pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I):
- wherein:
- R1 together with R2 form the group —NH—C(O)—CH═CH—, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2;
- R3 is chosen from a hydrogen atom, halogen atoms, —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoin, C1-4alkyl, C1-4alkoxy and —SO2NR5R6;
- R4 is chosen from a hydrogen atom, halogen atoms and C1-4 alkyl groups;
- R5 is chosen from C1-4 alkyl groups and C3-8 cycloalkyl groups;
- R6 is chosen from a hydrogen atom and C1-4 alkyl groups;
- n, p and q are each independently 0, 1, 2, 3 or 4;
- m and s are each independently 0, 1, 2 or 3;
- and
- 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 or stereoisomer thereof.
12 more elements
Dependencies are inferred from the claim text.