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US 6,747,043 B2Granted
Alkoxy aryl β2 adrenergic receptor agonists
AssigneeTheravance, Inc.
InventorsEdmund J. Moran, Eric Fournier
Life of this patent
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Abstract
The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
Claims30
A compound of formula (I):
- wherein:
- R1 is —CH2OH or —NHCHO, and R2is hydrogen;
- or R1 and R2 taken together are —NHC(═O)CH═CH—;
- R3, R4, and R5 are each independently hydrogen, halo, alkyl, alkoxy, or aryl, wherein each alkyl and alkoxy is optionally substituted with one or more halo;
- or R3 and R4 together form a fused benzo ring;
- or R4 and R5 together form a fused benzo ring;
- and
- R6 is hydrogen or hydroxy;
- or a pharmaceutically-acceptable salt or solvate or stereoisomer thereof.
6 more elements
A compound selected from the group consisting of:
- 4-((R)-1-Hydroxy-2-{2-[4-((R)-2-hydroxy-2-phenyl-ethoxy)-phenyl]-ethylamino}-ethyl)-2-hydroxymethyl-phenol;
- 4-[(R)-1-Hydroxy-2-(2-{4-[(R)-2-hydroxy-2-(2-methoxy-phenyl)-ethoxy]-phenyl}-ethylamino)-ethyl]-2-hydroxymethyl-phenol;
- N-[2-Hydroxy-5-((R)-1-hydroxy-2-{2-[4-((R)-2-hydroxy-2-phenyl-ethoxy)-phenyl]-ethylamino}-ethyl)-phenyl]-formamide;
- N-{2-Hydroxy-5-[(R)-1-hydroxy-2-(2-{4-[(R)-2-hydroxy-2-(2-methoxy-phenyl)-ethoxy]-phenyl}-ethylamino)-ethyl]phenyl}-formamide;
- 8-Hydroxy-5-((R)-1-hydroxy-2-{2-[4-((R)-2-hydroxy-2-phenyl-ethoxy)-phenyl]-ethylamino}-ethyl)-1H-quinolin-2-one;
- 8-Hydroxy-5-[(R)-1-hydroxy-2-(2-{4-[(R)-2-hydroxy-2-(2-methoxy-phenyl)-ethoxy]-phenyl}-ethylamino)-ethyl]-1H-quinolin-2-one;
- and
- pharmaceutically-acceptable salts and solvates and stereoisomers thereof.
5 more elements
Dependencies are inferred from the claim text.