Synthesis and potential antiallergic activity of new pteridinones and related compounds
The synthesis and pharmacological profile of a series of 2-alkoxy and 2-phenoxymethyl-3H-pteridin-4-ones and related compounds are described. These compounds displayed antiallergic activity in the passive cutaneous anaphylaxis test in rats. In contrast to both sodium cromoglycate and nedocromil sodium, many of our compounds were active when administered orally. The most potent in this series, 2-ethoxymethyl-3H-pteridin-4-one 2b (LCB 2183) was investigated in other models of allergy and inflammation. The antiallergic activity was confirmed and interesting antiinflammatory properties were observed. It was therefore selected for further development as a human therapeutic agent.
4(3H)-pteridinones, preparation processes and drugs containing them
The present invention relates to 4(3H)-pteridinones represented by the formula: STR1 in which X is an oxygen atom or a sulphur atom, Y is a hydrogen atom, a lower alkyl radical, especially a methyl radical, at the 6-position or a hydroxyl group at the 7-p
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(2008/06/13)
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