Heterocycle-aryl compounds for inflammation and immune-related uses
The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
1. A compound selected from the group consisting of:
2,6-difluoro-N-(4-(5-(isoxazol-5-yl)-3-methylthiophen-2-yl)phenyl)benzamide;
2,6-difluoro-N-(4-(3-methyl-5-(thiazol-2-yl)thiophen-2-yl)phenyl)benzamide;
2,6-difluoro-N-(4-(3-methyl-5-(1-methyl-1H-imidazol-5-yl)thiophen-2-yl)phenyl)benzamide;
2,6-difluoro-N-(5-(2-methyl-5-(oxazol-5-yl)thiophen-3-yl)pyrazin-2-yl)benzamide;
2,6-difluoro-N-(5-(2-methyl-5-(oxazol-5-yl)thiophen-3-yl)pyridin-2-yl)benzamide;
2,6-difluoro-N-(4-(3-methyl-5-(pyridin-3-yl)thiophen-2-yl)phenyl)benzamide;
2,6-difluoro-N-(4-(2-methyl-5-(pyridin-3-yl)thiophen-3-yl)phenyl)benzamide;
2,6-difluoro-N-(4-(2-methyl-5-(thiazol-2-yl)thiophen-3-yl)phenyl)benzamide;
2,6-difluoro-N-(4-(2-methyl-5-(1,3,4-oxadiazol-2-yl)thiophen-3-yl)phenyl)benzamide;
2,6-difluoro-N-(6-(2-methyl-5-(oxazol-5-yl)thiophen-3-yl)pyridin-3-yl)benzamide;
N-(4-(5-(1H-imidazol-5-yl)-2-methylthiophen-3-yl)phenyl)-2,6-difluorobenzamide;
2,6-difluoro-N-(4-(2-methyl-5-(4-methylpyridin-3-yl)thiophen-3-yl)phenyl)benzamide;
N-(4-(5-(5-chloro-2-methoxypyridin-3-yl)-2-methylthiophen-3-yl)phenyl)-2,6-difluorobenzamide;
2,6-difluoro-N-(5-(2-methyl-5-(thiazol-2-yl)thiophen-3-yl)pyridin-2-yl)benzamide;
2,6-difluoro-N-(5-(2-methyl-5-(thiazol-2-yl)thiophen-3-yl)pyrazin-2-yl)benzamide;
N-(5-(5-(1H-imidazol-5-yl)-2-methylthiophen-3-yl)pyridin-2-yl)-2,6-difluorobenzamide;
2,6-difluoro-N-(5-(2-methyl-5-(1-methyl-1H-imidazol-5-yl)thiophen-3-yl)pyridin-2-yl)benzamide;
3-methyl-N-(5-(2-methyl-5-(oxazol-5-yl)thiophen-3-yl)pyridin-2-yl)isonicotinamide;
N-(4-(5-(4-chloropyridin-3-yl)-2-methylthiophen-3-yl)phenyl)-2,6-difluorobenzamide;
2,6-difluoro-N-(4-(5-(4-methoxypyridin-3-yl)-2-methylthiophen-3-yl)phenyl)benzamide;
2,6-difluoro-N-(5-(2-methyl-5-(1-methyl-1H-imidazol-5-yl)thiophen-3-yl)pyrazin-2-yl)benzamide;
N-(5-(5-(1H-imidazol-5-yl)-2-methylthiophen-3-yl)pyrazin-2-yl)-2,6-difluorobenzamide;
2,6-difluoro-N-(4-(2-methyl-5-(1-methyl-1H-imidazol-5-yl)thiophen-3-yl)phenyl)benzamide;
2,6-difluoro-N-(4-(2-methyl-5-(1-methyl-1H-imidazol-5-yl)thiophen-3-yl)phenyl)benzamide hydrochloride; and
N-(4-(5-(1-ethyl-1H-imidazol-5-yl)-2-methylthiophen-3-yl)phenyl)-2,6-difluorobenzamide; or
a pharmaceutically acceptable salt thereof.
2. A pharmaceutical composition, comprising a compound of claim 1 , and:
(i) a pharmaceutically acceptable carrier; and/or
(ii) one or more additional therapeutic agents.
3. The pharmaceutical composition according to claim 2 , wherein the one or more additional therapeutic agents is selected from
the group consisting of immunosuppressive agents, anti-inflammatory agents and mixtures thereof; or is selected from
the group consisting of steroids, non-steroidal anti-inflammatory agents, antihistamines, analgesics, and suitable mixtures thereof.