Patent Evaluation : WO9302080-: British Bio-technology Ltd: lmidazo[4,5-c]pyridine derivatives as PAF antagonists

Abstract

AbstractNovelty: Novel imidazo[4,5-c]pyridine derivatives are claimed to be PAF antagonists. They are potentially useful for the treatment of inflammatory and allergic disorders, asthma, endotoxin shock, respiratory distress syndrome and transplant rejection.Biology: Inhibition of [3H]-PAF receptor binding was determined using washed human platelets. IC50 values are reported for seven compounds and are in the range 2-22 nM.Chemistry: A total of twenty-three compounds are disclosed. Detailed, stepwise syntheses are given for all compounds. Yields, physical appearance of products, elemental analyses, IR and 1H nmr data are given. All twenty-three compounds are specifically claimed including N-methyl-N-4-(5H-2-methylimidazo[4,5-c]pyridinylmethyl)-3-chlorophenylsulphonyl-L-leucine ethyl ester.