Back to results
US 2006/0142329 A1Published application
Beta 3 adrenergic agonists
AssigneeEli Lilly and Company
InventorsJolie Bastian, Gerd Ruehter, Daniel 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.
Claims18
(canceled)
(canceled)
(canceled)
(canceled)
The compound of claim 18 wherein:
- m is 2;
- n is 0 or 1;
- A1, A2 and A3 are carbon;
- Het is at the ortho-position relative to X and is pyrrol-1-yl;
- R1, R2 and R3 are H;
- R4 and R5 are independently H or methyl at each occurrence;
- the 6,5 ring system is connected to the (CR4R5)2 moiety at the 3-position of the 6,5 ring system;
- R6 is independently at each occurrence methyl;
- R7 is at the 6- or 7-position of the 6,5 ring system to which it is attached and is selected from H, O(CH2)pR12 or thienyl;
- X is OCH2;
- p is 0 or 1;
- and
- R12 is CO2R15CONH2, phenyl or pyridyl substituted once with CONH2 where R15 is H or C1-C6 alkyl;
- or a pharmaceutical salt thereof.
11 more elements
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
The compound of claim which is the hydrochloride salt.
(canceled)
(canceled)
(canceled)
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;
- each D is either carbon or nitrogen provided that at least one D must be nitrogen;
- Het is pyrrol-1-yl optionally substituted with CN;
- 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;
- 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, OCOR2R17, OCONR17R17, SR17, SOR18, SO2R18 and SO2(NR17R17), where R17 is independently a 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.