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US 7,071,208 B2Granted
β3 Adrenergic agonists
AssigneeEli Lilly and Company
InventorsJolie Anne Bastian, Gerd Ruehter, Daniel Jon Sall, Theo Schotten
Life of this patent
Estimating the term…
Abstract
The present invention relates to a β3 adrenergic receptor agonist of formula (I) or a pharmaceutical salt thereof; useful for treating Type II diabetes and/or obesity.
Claims5
A compound of the formula:
- wherein:
- m is 1,2,3,4 or 5;
- n is 0, 1 or 2;
- A1, A2 and A3 are carbon;
- Het is thien-2-yl optionally substituted with COCH3;
- R1 and R2 are H;
- R3 is H or C1–C6 alkyl;
- R4 and R5 are independently at each occurrence H or C1–C6 alkyl;
- or R4 and R5 combine with the carbon to which they are both attached to form a C3–C7 carbocyclic ring;
- R6 is independently at each occurrence halo, hydroxyl, cyano, C1–C6 alkyl, C1–C4 haloalkyl or C1–C6 alkoxy;
- R7 is H, CO2R8, CONR8R8, CH═CHR9, CH2CH2R9, NR8R8, NR8SO2R8, O(CR10R11)pR12, O(CR10R11)qR13, SO2R8, SO2NR8R8, optionally substituted phenyl where when substituted has one to three groups independently selected from halo, hydroxy, oxo, cyano, nitro, phenyl, benzyl, C1–C6 alkyl, C1–C4 haloalkyl, C1–C6 alkoxy, COR17, CONR17R17, CO2R17, NR17R17, NR17COR18, NR17SO2R18, OCOR18, OCO2R17, OCONR17R17, SR17, SOR18, SO2R18 and SO2(NR17R17), where R17 is independently at each occurrence H, C1–C6 alkyl, phenyl or benzyl and R18 is independently at each occurrence C1–C6 alkyl, phenyl or benzyl;
- X is OCH2;
- p is 0, 1, 2 or 3;
- q is 1, 2 or 3;
- R8 is independently at each occurrence H, C1–C6 alkyl or phenyl;
- R9 is cyano, CO2R14, CONR14R14, CONR14SO2R14, SO2R14 or optionally substituted phenyl where when substituted has one to three groups independently selected from halo, hydroxy, oxo, cyano, nitro, phenyl, benzyl, C1–C6 alkyl, C1–C4 haloalkyl, C1–C6 alkoxy, COR17, CONR17R17, CO2R17, NR17R17, NR17COR18, NR17SO2R18, OCOR18, OCO2R17, OCONR17R17, SR17, SOR18, SO2R18 and SO2(NR17R17), where R17 is independently at each occurrence H, C1–C6 alkyl, phenyl or benzyl and R18 is independently at each occurrence C1–C6 alkyl, phenyl or benzyl;
- R10 and R11 are independently at each occurrence H or C1–C6 alkyl;
- R12 is hydrogen, CO2R15, CONR15R15, SO2R15, SO2NR16R16, pyridyl or optionally substituted phenyl where when substituted has one to three groups independently selected from halo, hydroxy, oxo, cyano, nitro, phenyl, benzyl, C1–C6 alkyl, C1–C4 haloalkyl, C1–C6 alkoxy, COR17, CONR17R17, CO2R17, NR17R17, NR17COR18, NR17SO2R18, OCOR18, OCO2R17, OCONR17R17, SR17, SOR18, SO2R18 and SO2(NR17R17), where R17 is independently at each occurrence H, C1–C6 alkyl, phenyl or benzyl and R18 is independently at each occurrence C1–C6 alkyl, phenyl or benzyl;
- R13 is cyano, NR16R16, NR16SO2R16 or OR16;
- R14, R15 and R16 are independently at each occurrence H, C1–C6 alkyl or phenyl;
- or a pharmaceutical salt thereof.
18 more elements
Dependencies are inferred from the claim text.