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US 2008/0176912 A1Published application
Gpr40 agonists
AssigneeJanssen Pharmaceutica NV
InventorsGee-Hong Kuo, Fengbin Song, Joseph Gunnet, Keith Demarest
Life of this patent
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Abstract
The invention is directed to compounds of Formula (I) useful as GPR40 agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, insulin resistance, hyperglycemia, obesity, diabetes such as NIDDM, and other disorders related to lipid metabolism, energy homeostasis, and complications thereof, using compounds of the invention are also described.
Claims21
A compound of Formula (I)
- wherein
- R1 is —O—R4, or when R2 is —O5, R1 is H;
- R2 is selected from H, halo, cyano, acetyl, C1-3alkyl optionally substituted with halo, C1-3alkoxy optionally substituted with halo, and —O—R5;
- R3 is selected from H, halo, cyano, acetyl, C1-3alkyl optionally substituted with halo, and C1-3alkoxy optionally substituted with halo;
- R4 and R5 are each independently selected from C3-8alkyl optionally substituted with halo or cyano, C3-8alkenyl optionally substituted with halo, C3-8alkynyl optionally substituted with halo, C3-8cycloalkyl optionally substituted with C1-3alkyl, C1-4alkoxy-C3-5alkyl;
- Q is selected from phenyl,
- said Q being substituted with 0-2 groups independently selected from halo, C1-3alkyl, halo substituted C1-3alkyl, C1-3alkoxy, halo substituted C1-3alkoxy, cyano, acetyl or hydroxy;
- and
- n is 1, 2 or 3;
- or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt or solvate thereof.
7 more elements
A compound selected from the group consisting of
- 3-Phenyl-3-(4-propoxy-phenyl)-propionic acid;
- 3-(4-Butoxy-phenyl)-3-phenyl-propionic acid;
- 3-(4-Pentyloxy-phenyl)-3-phenyl-propionic acid;
- 3-(4-Hexyloxy-phenyl)-3-phenyl-propionic acid;
- 3-(4-Heptyloxy-phenyl)-3-phenyl-propionic acid;
- 3-Phenyl-3-[4-(4,4,4-trifluoro-butoxy)-phenyl]-propionic acid;
- 3-[4-(3-Methyl-but-3-enyloxy)-phenyl]-3-phenyl-propionic acid;
- 3-[4-(3-Methyl-butoxy)-phenyl]-3-phenyl-propionic acid;
- 3-(4-But-2-enyloxy-phenyl)-3-phenyl-propionic acid;
- 3-[4-(3-methoxy-propoxy)-phenyl]-3-phenyl-propionic acid;
- 3-(3-Pentyloxy-phenyl)-3-phenyl-propionic acid;
- 5-(4-Butoxy-phenyl)-5-phenyl-pentanoic acid;
- 3-[4-(4-Methyl-cyclohexyloxy)-phenyl]-3-phenyl-propionic acid;
- 3-[4-(2-Ethyl-butoxy)-phenyl]-3-phenyl-propionic acid;
- 3-[4-(2-Methyl-butoxy)-phenyl]-3-phenyl-propionic acid;
- 3-(4-Butoxy-phenyl)-3-(3-fluoro-phenyl)-propionic acid;
- 3-(4-Butoxy-phenyl)-3-(3-trifluoromethyl-phenyl)-propionic acid;
- 3-(4-Butoxy-phenyl)-3-(2-hydroxy-phenyl)-propionic acid;
- 3-(4-Butoxy-phenyl)-3-thiophen-2-yl-propionic acid;
- 3-[4-(2-Methoxy-ethoxy)-phenyl]-3-phenyl-propionic acid;
- 3-[4-(1-Ethyl-propoxy)-phenyl]-3-phenyl-propionic acid;
- 3-(4-Butoxy-phenyl)-3-(4-trifluoromethoxy-phenyl)-propionic acid;
- 3-(4-Butoxy-phenyl)-3-(4-trifluoromethyl-phenyl)-propionic acid;
- 3-[4-(3,3-Dimethyl-butoxy)-phenyl]-3-phenyl-propionic acid;
- and
- an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt or solvate thereof.
23 more elements
Dependencies are inferred from the claim text.