Adenosine deaminase inhibitors

Details Adenosine deaminase inhibitors Adenosine deaminase inhibitors

C - Chemistry, Metallurgy

07

D

C07D 473/34 (2006.01) A61K 31/52 (2006.01) C07D 473/00 (2006.01)

Patent

CA 2261591

This invention disclosed (2S,3R)-3(6-aminopurin-9-yl)aralkan-2-ols, a novel class of adenine derivatives (also called 9-aralkyladenines, ARADS), which have been shown to inhibit the enzyme adenosine deaminase at therapeutically useful levels. The relevant inhibitory constant (Ki) values are in the range of 10-7 - 10-10 M. These compounds with potencies in this range can reversibly inhibit ADA in an effective manner, without permanently deactivating the enzyme. ADA inhibitors that have similar biological profiles have been shown to be of therapeutic value when used to protect heart muscle against ischemic damage.

L'invention concerne des (2S, 3R)-3(6-aminopurine-9-yl) aralcan-2-ols, une nouvelle classe de dérivés d'adénine (également appelée 9-aralkyladénines, ARADS) démontrant une capacité d'inhibition de l'ADA à des niveaux thérapeutiquement utiles. Les valeurs de la constante d'inhibition appropriée (K¿i?) sont comprises entre 10?-7¿ et 10?-10¿ M, et les composés dont le potentiel se situe dans cette fourchette peuvent inhiber l'ADA de manière réversible et efficace, sans désactivation permanente de l'enzyme. Les inhibiteurs de l'ADA ayant des profils biologiques similaires démontrent leur valeur thérapeutique dans les applications qui visent à protéger le myocarde contre une détérioration ischémique.

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