Oxamides as impdh inhibitors

Details Oxamides as impdh inhibitors Oxamides as impdh inhibitors

C - Chemistry, Metallurgy

07

D

C07D 263/32 (2006.01) A61K 31/00 (2006.01) A61K 31/42 (2006.01) A61K 31/427 (2006.01) A61K 31/433 (2006.01) A61K 31/4439 (2006.01) A61K 31/454 (2006.01) A61K 31/4709 (2006.01) A61K 31/4725 (2006.01) A61K 31/496 (2006.01) A61K 31/506 (2006.01) A61K 31/5377 (2006.01) A61K 38/21 (2006.01) A61K 45/06 (2006.01) A61P 9/10 (2006.01) A61P 11/06 (2006.01) A61P 31/00 (2006.01) A61P 33/00 (2006.01) A61P 35/00 (2006.01) C07D 249/08 (2006.01) C07D 263/48 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2337588

Disclosed are compounds of the general formula Image wherein R1 represents heterocyclyl; R2 represents hydrogen, unsubstituted lower alkyl, lower alkoxy, halo, hydroxy or cyano; R3 represents hydrogen, unsubstituted lower alkyl, lower alkoxy, halo, or cyano; R4 represents hydrogen, lower alkyl, lower cycloalkyl, aryl, or heterocyclyl; R5 represents hydrogen, unsubstituted lower alkyl, lower alkoxy, halo, or cyano; R6 represents hydrogen, unsubstituted lower alkyl, lower alkoxy, halo, or cyano; R7 represents hydrogen, or unsubstituted lower alkyl; R8 represents hydrogen, or unsubstituted lower alkyl; or R4 and R8 together with the nitrogen atom to which they are attached represent heterocyclyl; and pharmaceutically acceptable salts thereof. The disclosed oxamide derivatives are inhibitors of the enzyme inosine monophosphate dehydrogenase (IMPDH). They can be used as medicaments, especially for treating immune mediated conditions or diseases, viral diseases, bacterial diseases, parasitic diseases, inflammation, inflammatory diseases, hyperproliferative vascular diseases, tumours, and cancer. They can be used alone, or in combination with other therapeutically active agents, for example, an immunosuppressant, a chemotherapeutic agent, an anti-viral agent, an antibiotic, an anti- parasitic agent, an anti-inflammatory agent, an anti-fungal agent and/or an anti-vascular hyperproliferation agent.

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