Thiadiazole compounds useful as inhibitors of cysteine...

Details Thiadiazole compounds useful as inhibitors of cysteine... Thiadiazole compounds useful as inhibitors of cysteine...

C - Chemistry, Metallurgy

07

K

C07K 5/062 (2006.01) A61K 31/425 (2006.01) A61K 38/05 (2006.01) C07D 285/08 (2006.01) C07K 5/06 (2006.01) C07K 5/065 (2006.01)

Patent

CA 2322838

Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in treating acne by inhibition of transglutaminase, common cold by inhibition of human rhinovirus 3C protease and inflammatory joint disease by inhibition of cathepsins. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadazole of general formula (I), where Z is a nitrogen containing group with recognition sequence for the enzyme and Y is a substituent that tunes the reactivity of the inhibitor towards the thiol group of the cysteine activity-dependent enzyme. The Y group may also serve in recognition.

L'invention concerne de nouveaux composés à base de 1,2,4-thiadiazole qui s'avèrent efficaces en tant qu'inhibiteurs des enzymes dépendant de l'activité de la cystéine, en particulier des protéases de la cystéine. Les composés peuvent servir à traiter l'acné par l'inhibition de la transglutaminase, les refroidissements par l'inhibition de la protéase 3C du rhinovirus humain et la maladie inflammatoire des articulations par l'inhibition des cathépsines. Les composés de la présente invention se présentent comme 1,2,4-thiadiazole 3,5 substitué qui correspond à la formule générale (I) dans laquelle Z est un groupe contenant l'azote avec une séquence de reconnaissance pour l'enzyme et Y est un substituant qui régule la réactivité de l'inhibiteur par rapport au groupe thiol de l'enzyme dépendant de l'activité de la cystéine. Le groupe Y peut aussi servir pour la reconnaissance.

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