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US 7,009,060 B2Granted
2-oxo-benzimidazolyl substituted ethanolamine derivatives and their use as β3 agonists
AssigneeEli Lilly and Company
InventorsCynthia Darshini Jesudason, Don Richard Finley
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Abstract
The present invention relates to a β3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.
Claims1
A compound of formula IV:
- wherein:
- R is C3–C8 alkyl or (C3–C7 cycloalkyl)C1–C5 alk-di-yl;
- R1 is H, CN, halo, C1–C6 alkyl, C1–C4 haloalkyl, CO2R6, CONR6R6, NR6COR7, NR6R6, OR6, SR6, SOR7, SO2R7 or SO2NR6R6;
- R1a is H, halo or C1–C6 alkyl;
- R2 is H or C1–C6 alkyl;
- R3 and R4 are independently H or C1–C6 alkyl
- R5 is hydrogen, optionally substituted phenyl or optionally substituted heterocycle;
- X is absent or is OCH2 or SCH2;
- X1 is absent or C1–C5 alk-di-yl;
- and
- X2 is absent or is O, S, NH, NHSO2, SO2NH or CH2;
- Y is nitro or amino;
- R6 is independently at each occurrence H, C1–C6 alkyl or phenyl;
- or when two R6 moieties are connected to the same nitrogen atom, then said R6 moieties may combine with the nitrogen to which they are attached to form a pyrollidinyl, piperidinyl or hexamethyleneimino ring;
- and
- R7 is C1–C6 alkyl or phenyl;
- or a salt thereof.
14 more elements
Dependencies are inferred from the claim text.